Quarterlytics / Healthcare / Biotechnology / Milestone Pharmaceuticals Inc.

Milestone Pharmaceuticals Inc.

mist · NASDAQ Healthcare
Claim this profile
Ticker mist
Exchange NASDAQ
Sector Healthcare
Industry Biotechnology
Employees 33
← All annual reports
FY2021 Annual Report · Milestone Pharmaceuticals Inc.
Sign in to download
Loading PDF…
Table of Contents

UNITED STATES
SECURITIES AND EXCHANGE COMMISSION
Washington, D.C. 20549
FORM 10-K

(Mark One)

☒    ANNUAL REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934

For the fiscal year ended December 31, 2021

OR

☐    TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934

For the transition period from                    to

Commission file number 001-38899
Milestone Pharmaceuticals Inc.
(Exact name of registrant as specified in its charter)

Québec
(State or Other Jurisdiction of Incorporation or Organization)

Not applicable
(I.R.S. Employer Identification No.)

1111 Dr. Frederik-Phillips Boulevard, Suite 420
Montréal, Québec CA
(Address of Principal Executive Offices)

H4M 2X6
(Zip Code)

Registrant’s telephone number, including area code (514)-336-0444

Securities registered pursuant to Section 12(b) of the Act:

Title of each class
Common Shares

Trading Symbol(s)
MIST

Name of each exchange on which registered
The Nasdaq Stock Market LLC

Indicate by check mark if the registrant is a well-known seasoned issuer, as defined in Rule 405 of the Securities Act. Yes  ☐ No ☒

Indicate by check mark if the registrant is not required to file reports pursuant to Section 13 or Section 15(d) of the Act. Yes ☐ No ☒

Indicate by check mark whether the registrant (1) has filed all reports required to be filed by Section 13 or 15(d) of the Securities Exchange Act of

1934 during the preceding 12 months (or for such shorter period that the registrant was required to file such reports), and (2) has been subject to such
filing requirements for the past 90 days. Yes ☒ No ☐

Indicate by check mark whether the registrant has submitted electronically, if any, every Interactive Data File required to be submitted pursuant to
Rule 405 of Regulation S-T during the preceding 12 months (or for such shorter period that the registrant was required to submit and post such files). Yes
☒ No ☐

Indicate by check mark whether the registrant is a large accelerated filer, an accelerated filer, a non-accelerated filer, a smaller reporting company,
or an emerging growth company. See the definitions of “large accelerated filer,” “accelerated filer”, “smaller reporting company” and “emerging growth
company” in Rule 12b-2 of the Exchange Act.

Large accelerated filer ☐

Accelerated filer ☐

Non-accelerated filer ☒

Smaller reporting company ☒

Emerging growth company ☒

If an emerging growth company, indicate by check mark if the registrant has elected not to use the extended transition period for complying with

any new or revised financial accounting standards provided pursuant to Section 13(a) of the Exchange Act. ☒

Indicate by check mark whether the registrant has filed a report on and attestation to its management's assessment of the effectiveness of its

internal control over financial reporting under Section 404(b) of the Sarbanes-Oxley Act (15 U.S.C 7262(b)) by the registered public accounting firm that
prepared or issued its audit report. Yes ☐ No ☒

Indicate by check mark whether the registrant is a shell company (as defined in Rule 12b-2 of the Exchange Act). Yes ☐ No ☒

The aggregate market value (approximate) of the registrant’s common equity held by non-affiliates based on the closing price of a share of the

registrant’s common share for The Nasdaq Stock Market on June 30, 2021 (the last business day of the registrant’s most recently completed second fiscal
quarter) was $ 164.2 million.

As of March 21st, 2022, the total number of shares outstanding of the registrant’s Common Shares was 29,917,326 shares, net of treasury shares.

Portions of the registrant’s definitive proxy statement for the registrant’s 2022 annual meeting of stockholders, to be filed within 120 days after the
close of the registrant’s fiscal year, are incorporated by reference into Part III of this Annual Report.

DOCUMENTS INCORPORATED BY REFERENCE:

Table of Contents

TABLE OF CONTENTS

Special Note Regarding Forward-Looking Statements

Summary of Risk Factors

PART I

Item 1. Business

Item 1A. Risk Factors

Item 1B. Unresolved Staff Comments

Item 2. Properties

Item 3. Legal Proceedings

Item 4. Mine Safety Disclosures

PART II

Item  5.  Market  for  Registrant’s  Common  Equity,  Related  Stockholder  Matters  and  Issuer  Purchases  of  Equity
Securities

Item 6. Selected Financial Data

Item 7. Management’s Discussion and Analysis of Financial Condition and Results of Operations

Item 7A. Quantitative and Qualitative Disclosures About Market Risk

Item 8. Financial Statements

Item 9. Changes in and Disagreements with Accountants on Accounting and Financial Disclosure

Item 9A. Controls and Procedures

Item 9B. Other Information

Item 9C. Disclosure Regarding Foreign Jurisdictions that Prevent Inspections

PART III

Item 10. Directors, Executive Officers and Corporate Governance

Item 11. Executive Compensation

Item 12. Security Ownership of Certain Beneficial Owners and Management and Related Stockholder Matters

Item 13. Certain Relationships and Related Transactions, and Director Independence

Item 14. Principal Accountant Fees and Services

PART IV

Item 15. Exhibits and Financial Statement Schedules

Item 16. Form 10-K Summary

2

    3

5

6

45

88

88

89

89

90

90

91

103

104

127

127

128

128

128

128

128

129

129

130

132

Table of Contents

“Milestone  Pharmaceuticals”  and  the  Milestone  logo  appearing  in  this  Annual  Report  on  Form  10-K  are  unregistered
trademarks  of  Milestone  Pharmaceuticals  Inc.  All  other  trademarks,  trade  names  and  service  marks  appearing  in  this
Annual Report on Form 10-K are the property of their respective owners. Solely for convenience, the trademarks and trade
names in this Annual Report on Form 10-K may be referred to without the ® and ™ symbols, but such references should
not be construed as any indicator that their respective owners will not assert their rights thereto.

This Annual Report on Form 10-K contains references to United States dollars and Canadian dollars. All dollar amounts
referenced, unless otherwise indicated, are expressed in United States dollars. References to “$” are to United States dollars
and references to “C$” are to Canadian dollars.

SPECIAL NOTE REGARDING FORWARD-LOOKING STATEMENTS

This Annual Report on Form 10-K contains forward-looking statements about us and our industry that involve substantial
risks and uncertainties. All statements other than statements of historical facts contained in this Annual Report on Form 10-
K,  including  statements  regarding  our  strategy,  future  financial  condition,  future  operations,  projected  costs,  prospects,
plans,  objectives  of  management  and  expected  market  growth,  are  forward-looking  statements.  In  some  cases,  you  can
identify  forward-looking  statements  by  terminology  such  as  "aim,"  "anticipate,"  "assume,"  "believe,"  "contemplate,"
"continue,"  "could,"  "design,"  "due,"  "estimate,"  "expect,"  "goal,"  "intend,"  "may,"  "objective,"  "plan,"  "predict,"
"positioned," "potential," "seek," "should," "target," "will," "would" and other similar expressions that are predictions of or
indicate future events and future trends, or the negative of these terms or other comparable terminology.

We have based these forward-looking statements largely on our current expectations and projections about future events
and financial trends that we believe may affect our financial condition, results of operations, business strategy and financial
needs.  These  forward-looking  statements  are  subject  to  a  number  of  known  and  unknown  risks,  uncertainties  and
assumptions, including risks described in the section titled "Risk Factors" and elsewhere in this Annual Report on Form 10-
K, regarding, among other things:

● the  initiation,  timing,  progress  and  results  of  our  current  and  future  clinical  trials  of  etripamil,  including  our
Phase  3  clinical  trials  of  etripamil  for  the  treatment  of  paroxysmal  supraventricular  tachycardia,  our  Phase  2
clinical trial of etripamil for the treatment of atrial fibrillation and rapid ventricular rate, and of our research and
development programs;

● uncertain  impacts  that  the  COVID-19  pandemic  may  have  on  our  business,  strategy,  clinical  trial  progress  and

research and development efforts;

● macroeconomic  conditions  and  periods  of  volatility,  which  may  be  exacerbated  by  the  effects  of  the  pandemic

and general inflationary trends;

● our plans to develop and commercialize etripamil and any future product candidates;

● our estimates regarding expenses, future revenue, capital requirements and needs for additional financing;

● our ability to successfully acquire or in-license additional product candidates on reasonable terms;

● our ability to establish collaborations or obtain additional funding;

● our ability to obtain regulatory approval of our current and future product candidates;

● our expectations regarding the potential market size and the rate and degree of market acceptance of etripamil and

any future product candidates;

3

Table of Contents

● our  ability  to  fund  our  working  capital  requirements  and  expectations  regarding  the  sufficiency  of  our  capital

resources;

● the implementation of our business model and strategic plans for our business, etripamil and any future product

candidates;

● our intellectual property position and the duration of our patent rights;

● developments or disputes concerning our intellectual property or other proprietary rights;

● our expectations regarding government and third-party payor coverage and reimbursement;

● our ability to compete in the markets we serve;

● the impact of government laws and regulations;

● developments relating to our competitors and our industry; and

● the factors that may impact our financial results.

The foregoing list of risks is not exhaustive. Other sections of this Annual Report on Form 10-K may include additional
factors that could harm our business and financial performance. Moreover, we operate in a very competitive and rapidly
changing environment. New risk factors emerge from time to time, and it is not possible for our management to predict all
risk factors nor can we assess the impact of all factors on our business or the extent to which any factor, or combination of
factors,  may  cause  actual  results  to  differ  materially  from  those  contained  in,  or  implied  by,  any  forward-looking
statements.

In  light  of  the  significant  uncertainties  in  these  forward-looking  statements,  you  should  not  rely  upon  forward-looking
statements as predictions of future events. Although we believe that we have a reasonable basis for each forward-looking
statement  contained  in  this  Annual  Report  on  Form  10-K,  we  cannot  guarantee  that  the  future  results,  levels  of  activity,
performance or events and circumstances reflected in the forward-looking statements will be achieved or occur at all. You
should refer to the section titled "Risk Factors" for a discussion of important factors that may cause our actual results to
differ materially from those expressed or implied by our forward-looking statements. Furthermore, if our forward-looking
statements prove to be inaccurate, the inaccuracy may be material. Except as required by law, we undertake no obligation
to publicly update any forward-looking statements, whether as a result of new information, future events or otherwise. The
Private Securities Litigation Reform Act of 1995 and Section 27A of the Securities Act of 1933, as amended, do not protect
any forward-looking statements that we make in connection with this Annual Report on Form 10-K.

4

Table of Contents

SUMMARY OF RISK FACTORS

Our business is subject to numerous risks and uncertainties, including those described in Item 1A “Risk Factors”. These
risks include, but are not limited to the following:

● We  have  incurred  significant  operating  losses  since  inception  and  anticipate  that  we  will  continue  to  incur

substantial operating losses for the foreseeable future and may never achieve or maintain profitability.

● We will require substantial additional funding to finance our operations. If we are unable to raise capital when

needed, we could be forced to delay, reduce or terminate our development of etripamil or other operations.

● Raising  additional  capital  may  cause  dilution  to  our  shareholders,  restrict  our  operations  or  require  us  to

relinquish rights to our product candidates.

● Economic uncertainty, including related to inflation, may adversely affect our results of operations.
● We have only one product candidate, etripamil, for which we are currently pursuing clinical development. Our
future  success  is  substantially  dependent  on  the  successful  clinical  development  and  regulatory  approval  of
etripamil. If we are not able to obtain required regulatory approvals for etripamil or any future product candidates,
we  will  not  be  able  to  commercialize  etripamil  or  any  future  product  candidates  and  our  ability  to  generate
revenue will be adversely affected.

● We  may  not  be  successful  in  our  efforts  to  expand  our  pipeline  of  product  candidates  beyond  etripamil  for

paroxysmal supraventricular tachycardia, or PSVT.

● The development of additional product candidates is risky and uncertain.
● Success in preclinical studies or earlier clinical trials may not be indicative of results in future clinical trials and
we  cannot  assure  you  that  any  ongoing,  planned  or  future  clinical  trials  will  lead  to  results  sufficient  for  the
necessary regulatory approvals.

● Our business, operations and clinical development timelines and plans have been adversely affected by the effects

of health epidemics, including the COVID-19 pandemic, and could be affected by future health epidemics.

● We may encounter substantial delays or difficulties in our clinical trials.
● Enrollment and retention of patients in clinical trials is an expensive and time-consuming process and could be

delayed, made more difficult or rendered impossible by multiple factors outside our control.

● If we are unable to establish sales and marketing capabilities or enter into agreements with third parties to market
and sell etripamil or any future product candidates, we may not be successful in commercializing etripamil or any
future product candidates, if and when they are approved.

● Even if etripamil or any future product candidates receive marketing approval, they may fail to achieve market
acceptance  by  physicians,  patients,  third-party  payors  or  others  in  the  medical  community  necessary  for
commercial success.

● Even if we successfully obtain approval for etripamil, its success will be dependent on its use in accordance with

labeled instructions for use.

● If  the  market  opportunities  for  etripamil  and  any  future  product  candidates  are  smaller  than  we  estimate,  our

business may suffer.

● Coverage and adequate reimbursement may not be available for etripamil or any future product candidates, which

could make it difficult for us to gain market acceptance.

● Even if we obtain and maintain approval for etripamil or any future product candidates from the Food and Drug
Administration, or FDA, we may never obtain approval of etripamil or any future product candidates outside of
the United States, which would limit our market opportunities and could harm our business.

● Even if we obtain regulatory approval for etripamil or any future product candidates, they will remain subject to

ongoing regulatory oversight.

● We  will  rely  on  third  parties  to  produce  clinical  and  commercial  supplies  of  etripamil  and  any  future  product

candidates.

● We rely on third parties to conduct, supervise and monitor our preclinical studies and clinical trials, and if those

third parties perform in an unsatisfactory manner, it may harm our business.

● Etripamil is intended to be used with a nasal-spray device, which may result in additional regulatory and supply

risks.

5

Table of Contents

● If we are unable to obtain and maintain patent protection for etripamil or any future product candidates, or if the
scope  of  the  patent  protection  obtained  is  not  sufficiently  broad,  our  competitors  could  develop  and
commercialize  drugs  similar  or  identical  to  ours,  and  our  ability  to  commercialize  successfully  our  product
candidates may be impaired.

● Our  future  success  depends  on  our  ability  to  retain  key  executives  and  to  attract,  retain  and  motivate  qualified

personnel.

● The market price of our common shares has been and may continue to be volatile and fluctuate substantially, and

you could lose all or part of your investment.

● Our common shares are thinly traded and our shareholders may be unable to sell their shares quickly or at market

price.

● Concentration of ownership of our common shares among our existing executive officers, directors and principal

shareholders may prevent new investors from influencing significant corporate decisions.

PART I

ITEM 1.      BUSINESS

Company Overview

We  are  a  biopharmaceutical  company  focused  on  the  development  and  commercialization  of  innovative  cardiovascular
medicines.  Our  lead  product  candidate  etripamil  is  a  novel,  potent  and  short-acting  calcium  channel  blocker  that  we
designed as a rapid-onset nasal spray to be self-administered by patients. We are developing etripamil for the treatment of
specific arrhythmias with a lead indication to treat PSVT, with subsequent indications to treat atrial fibrillation and rapid
ventricular rate, or AFib-RVR, and other cardiovascular indications.

PSVT is a rapid heart rate condition characterized by episodes of supraventricular tachycardia, or SVT, that start and stop
without warning. Episodes of SVT are often experienced by patients with symptoms including palpitations, sweating, chest
pressure or pain, shortness of brea
th, sudden onset of fatigue, lightheadedness or dizziness, fainting and anxiety. Calcium channel blockers have long been
approved for the treatment of PSVT as well as other cardiac conditions. Calcium channel blockers available in oral form
are  frequently  used  prophylactically  to  control  the  frequency  and  duration  of  future  episodes  of  SVT.  For  treatment  of
episodes of SVT, approved calcium channel blockers are administered intravenously under medical supervision, usually in
the emergency department. The combination of convenient nasal-spray delivery, rapid-onset and short duration of action of
etripamil  has  the  potential  to  shift  the  current  treatment  paradigm  for  episodes  of  SVT  away  from  the  burdensome  and
costly emergency department setting. If approved, we believe that etripamil will be the first self-administered therapy for
the rapid termination of episodes of SVT wherever and whenever they occur.

While PSVT is characterized by a faster than normal heart rate where the heart beats at regular intervals, with AFib-RVR
the  heart  often  beats  faster  than  normal  and  always  with  a  random,  irregular  rhythm.  Pharmacologic  treatment  of  PSVT
focuses on terminating the arrhythmia using an agent to slow conduction over the AV node. With AFib-RVR, there are two
approaches to treatment: rate control to reduce the heart rate and rhythm control to restore sinus rhythm and prevent AFib
recurrences.  Either  of  these  pharmacological  management  approaches  may  be  administered  chronically  or  acutely,
depending on patient preference and episode frequency and/or severity. Several rhythm control strategies exist, including
electrical cardioversion, catheter ablation and anti-arrhythmic drug therapy. For rate control, the rapid heart rate of atrial
fibrillation is typically treated with AV nodal blocking drugs (for example, calcium channel blockers, beta blockers, or less
commonly  digoxin)  to  control  symptoms  and  improve  cardiac  function/hemodynamic  stability.  Similar  to  PSVT,  we
believe that etripamil could be the first patient self-administered therapy to provide rapid rate control of episodes of AFib-
RVR wherever and whenever they occur.

We  believe  that  PSVT  is  a  large  and  under-recognized  market  that  we  estimate  affects  approximately  two  million
Americans and results in over 600,000 healthcare claims in the United States alone per year, including more than 150,000

6

Table of Contents

emergency  department  visits  and  hospital  admissions  and  up  to  80,000  ablations.  Furthermore,  we  estimate  that
approximately 300,000 people are diagnosed with PSVT each year in the United States. Finally, our research with patients
shows  that  the  average  patient  takes  two  or  more  years  to  obtain  a  diagnosis  of  PSVT  once  they  start  to  experience
symptoms, which suggests that many more patients with PSVT are currently undiagnosed.  

For  our  planned  second  indication,  AFib-RVR,  the  American  Heart  Association  (AHA)  estimates  that  in  2016
approximately five million people suffered from AFib in the United States. This estimate is projected to increase over the
next  ten  years;  the  AHA  suggests  a  prevalence  of  seven  million  by  2030,  while  the  Centers  for  Disease  Control  (CDC)
reports this prevalence as increasing to 12 million over the same time period.  Our quantitative market research indicates
that the target addressable market for etripamil in patients with atrial fibrillation and rapid ventricular rate is approximately
30% to 40% of the five to six million patients diagnosed with atrial fibrillation.

Our late-stage etripamil clinical program for the treatment of PSVT is currently executing on two ongoing Phase 3 trials,
RAPID and NODE-303. The RAPID study is our ongoing pivotal Phase 3 safety and efficacy trial. This study enrolled its
first patient in November 2020 and topline data is expected in mid-second half 2022. NODE-303 is an open-label global
safety trial enrolling patients to collect safety data that when combined with the safety data from the rest of the program
will  form  the  safety  dataset  to  be  evaluated  by  the  FDA  and  other  regulatory  agencies  to  form  the  basis  for  marketing
approval. We have also completed our first Phase 3 safety and efficacy trial of etripamil, NODE-301, and its open-label
safety extension trial, NODE-302. In addition to our PSVT clinical program, we began enrollment of patients in a Phase 2
proof-of-concept clinical trial titled ReVeRA in the first quarter of 2021 to evaluate the potential effectiveness of etripamil
to reduce ventricular rate during AFib-RVR episodes.

Our Pipeline

The following table sets forth the status and initial focus of etripamil.

In March 2020, we reported topline results of the first part of the NODE-301 pivotal trial of etripamil for the treatment of
PSVT, which is a placebo-controlled Phase 3 safety and efficacy trial. The first part of NODE-301, which enrolled a total
of 431 patients across 65 sites in the United States and Canada, did not meet its primary endpoint of time to conversion of
SVT to sinus rhythm compared to placebo over the five-hour period after study drug administration. The median time to
conversion for etripamil was 25 minutes (95% CI: 16, 43) compared to 50 minutes (95% CI: 31,101) for placebo (p=0.12).
Despite early activity, including the conversion of 61% of etripamil patients compared to 45% of placebo patients within 45
minutes after study drug administration (p=0.02), a time period consistent with the pharmacological activity of etripamil,
results from the latter part of the analysis confounded the statistical analysis of the primary endpoint.

In July 2020, we announced that we received agreement from the U.S. FDA, on our proposal to alter the size, design and
analysis plan of a then ongoing study, NODE-301 part 2, as well as the overall program based on the data from the NODE-

7

Table of Contents

301 trial. We renamed the NODE-301 part 2 trial to the RAPID trial and increased the number of patients and clinical study
sites.  The FDA indicated that two studies, the RAPID study and the completed NODE-301 study, could potentially fulfill
the efficacy requirement for our planned NDA for etripamil in patients with PSVT.

Under  an  updated  statistical  analysis  plan,  or  SAP,  the  primary  efficacy  endpoint  for  both  the  RAPID  and  NODE-301
studies will be defined as time to conversion over the first 30 minutes, with a target p-value of less than 0.05 for each study.
We believe this endpoint supports the desire of patients to rapidly address their PSVT symptoms during an episode and
ideally avoid visiting the emergency department. Based on interactions with PSVT treating physicians and cardiovascular
thought  leaders,  we  believe  that  a  50%  conversion  rate  within  60  minutes  is  a  clinically  meaningful  outcome  given  the
symptomatic nature of SVT episodes and the lack of approved at-home treatments.

When employing the updated SAP retrospectively to the NODE-301 data, 54% of etripamil patients vs. 35% of placebo
patients  converted  within  30  minutes  (HR  1.87,  p=0.02).    Applying  the  same  primary  endpoint  to  the  RAPID  study,
powering the study at 90% and using alpha of 0.05 to detect a 19% difference of etripamil versus placebo in 30 minute time
to conversion that was observed in the NODE-301 study results in the size of 180 confirmed PSVT events.

The RAPID study is designed very similarly to NODE-301, but will introduce a new treatment regimen to the program.
Based  on  discussions  with  the  FDA  regarding  maximizing  the  treatment  effect  of  etripamil,  the  RAPID  trial  allows  for
repeat administration of study drug (either 70 mg of etripamil or placebo) for patients who have not experienced symptom
relief within ten minutes of the first study drug administration. This repeat dose regimen, which is similar to current PSVT
treatment practices in the emergency department setting, is tailored to the pharmacokinetic profile of etripamil to deliver
increased  exposure  over  approximately  the  first  30  minutes  following  initial  administration.  We  believe  that  the  repeat
administration could benefit a broader group of patients, including those with more persistent episodes.

In  the  NODE-301  study,  32%  of  etripamil  patients  and  14%  of  placebo  patients  converted  to  sinus  rhythm  within  10
minutes. The FDA agreed that the single and repeat administrations of etripamil could be pooled and compared to placebo
for the primary analysis, resulting in no increase in the sample size.  

Safety Studies

NODE-303 is a Phase 3, multi-center, open-label safety trial, evaluating the safety of etripamil when self-administered
without medical supervision, and evaluating the treatment safety and efficacy of etripamil on multiple SVT episodes.
The study initiated with the etripamil 70 mg single dose regimen and the 70 mg repeat dose regimen was introduced
into the trial starting in the second half of 2021 following FDA acceptance of the protocol change.  The trial is designed
to add to the safety data from the remainder of the development program, including both the NODE-301 and RAPID
trials, in order to fulfill the safety data set needed for NDA filing. Our plan is to ascertain the final sizing of the trial
following future discussions with the FDA and other regulatory authorities.

We are conducting patient access programs to provide further access to etripamil to patients who have participated in the
clinical development registration trials to treat future SVT episodes. These programs are tailored to meet the regulatory
requirements in the territories in which the clinical sites are located.

Phase 2 Proof of Concept Trial in AFib-RVR

We began enrollment of patients in a Phase 2 proof-of-concept clinical trial titled ReVeRA in the first quarter of 2021 to
evaluate the potential effectiveness of etripamil to reduce ventricular rate in AFib-RVR episodes. The Phase 2 double blind,
placebo controlled, proof-of-concept study, which is being conducted in Canada in collaboration with the Montreal Heart
Institute and other research centers, is expected to enroll approximately 50 patients randomized 1:1 to receive either 70 mg
of  etripamil  nasal  spray  or  placebo.  The  primary  endpoint  will  assess  reduction  in  ventricular  rate,  with  key  secondary
endpoints  including  the  time  to  achieve  the  maximum  reduction  in  rate  and  the  duration  of  the  effect.  The  trial  is  being
conducted in the hospital or emergency department setting under medical supervision. The COVID-19 pandemic

8

Table of Contents

and  its  impact  on  emergency  departments  and  hospital  personnel  has  resulted  in  significantly  slower  than  expected
enrollment for this trial.

As we generate more data on the safety and efficacy profile of etripamil in PSVT and assess the proof-of-concept results
from the ReVeRA trial, we will continue to assess whether etripamil could be further developed in PSVT, AFib-RVR, and
other areas of unmet medical need.

Our Strategy

Our goal is to identify, develop and commercialize innovative cardiovascular medicines, including etripamil for the
treatment of PSVT, AFib-RVR and other cardiovascular indications, and additional clinical stage compounds for other
cardiovascular conditions. The key elements of our business strategy to achieve this goal include the following:

•

•

Successfully complete development and obtain regulatory approval of etripamil for the treatment of PSVT.  
We are focused on efficiently developing and obtaining approval for etripamil to treat patients with PSVT. We
are maintaining our guidance of achieving topline data from the RAPID trial in mid-second half 2022. We
intend to first seek regulatory approval in the United States, followed by Europe and other major markets.

Expand the scope of cardiovascular indications for etripamil beyond PSVT.  We are investigating the use of
etripamil for the treatment of patients with AFib-RVR. We believe that etripamil could benefit patients with
AFib-RVR based on the approved use of intravenous, or IV, calcium channel blockers in this indication. We
began enrollment of our Phase 2 proof-of-concept clinical trial in patients with AFib-RVR in the first quarter
of 2021. We are also exploring the additional cardiovascular opportunities for the use of etripamil.

• Maximize the value of our programs by maintaining flexibility to commercialize our product candidates 
independently or through collaborative partnerships.  We currently have exclusive development and
commercialization rights for etripamil for our initial indications of PSVT and AFib-RVR. We plan to
establish commercialization and marketing capabilities using a direct sales force to commercialize etripamil
in the United States. Outside of the United States, we are considering commercialization strategies that may
include collaborations with other companies.

•

Leverage our expertise and experience to expand our pipeline of product candidates.  We seek to maximize
our commercial opportunities by acquiring or in-licensing product candidates for indications with significant
unmet need with a focus on novel treatments for cardiovascular or other conditions. Our leadership team has
extensive experience in developing and commercializing successful drugs. We intend to leverage the
collective talent within our organization and our network to guide our development plans and pipeline
expansion.

Cardiac Conduction

Normal Conduction

Within the right atrium, one of the heart’s upper chambers, sits a specialized structure called the sinus node. The sinus node
generates its own electrical signal, which spreads throughout both atria and is transmitted down to the lower chambers, the
ventricles, and over another piece of electrical tissue called the atrio-ventricular, or AV, node, which is shown in the figure
below. Once the signal reaches the ventricles, it causes them to contract, pumping blood out to the body. Another heartbeat
does not occur until a new signal is generated from the sinus node and the cycle repeats. Under normal conditions, passage
from  the  sinus  node  over  the  AV  node  is  the  only  way  for  the  electrical  impulse  to  travel  from  the  atria  down  to  the
ventricles.

9

Table of Contents

The electrical signal of each heartbeat can be detected by placing sensors known as electrodes over the skin, and recorded
over  time  in  a  tracing  known  as  an  electrocardiogram,  or  ECG.  The  ECG  measures  signal  voltage  and  duration.  To  the
trained interpreter, an ECG conveys a large amount of information about the structure and function of the heart, including
among other things, heart rate and rhythm. Under normal physiologic conditions, an ECG has a characteristic pattern of
waves corresponding to the electrical activity, contraction and relaxation of each heart chamber. This normal functioning is
referred to as sinus rhythm and occurs at a heart rate of between 60 and 100 beats per minute at regular intervals.

As  seen  in  the  figure  below,  the  various  waves  of  an  ECG  tracing  corresponding  to  the  events  of  a  single  heartbeat  are
named with the letters P, Q, R, S and T. The interval between the P wave and the R wave, known as the PR interval, is a
measure of conduction over the AV node. A normal PR interval is 0.12-0.20 seconds in duration.

ECG Tracing Graph – Event Single Heartbeat

Arrhythmias

A  disruption  in  the  heart’s  normal  rate  or  rhythm  is  called  an  arrhythmia.  With  an  arrhythmia,  the  heart  can  beat  too
quickly, too slowly or with an irregular pattern. A faster than normal heat rate is called tachycardia; a slower than normal
heart rate is called bradycardia. Symptoms of an arrhythmia can include palpitations, lightheadedness or dizziness, chest

10

Table of Contents

pain, shortness of breath or sweating. PSVT and atrial fibrillation are two of the most commonly occurring arrhythmias.
While PSVT is characterized by a faster than normal heart rate where the heart beats at regular intervals, with AFib-RVR
the  heart  often  beats  faster  than  normal  and  always  with  a  random,  irregular  rhythm.  Pharmacologic  treatment  of  PSVT
focuses on terminating the arrhythmia using an agent to slow conduction over the AV node. With AFib-RVR, there are two
approaches to treatment: rate control to reduce the heart rate and rhythm control to restore sinus rhythm and prevent AFib
recurrences.

Etripamil

We designed and are developing etripamil, a novel, potent, rapid-onset and short-acting calcium channel blocker, as a nasal
spray  to  be  administered  by  the  patient  to  terminate  episodes  of  transient  cardiovascular  conditions  as  they  occur.  Short
pharmacological action is sufficient to resolve an episode of SVT. Accordingly, long-lasting drugs that remain in the body
at significant concentrations long after the episode is resolved subject patients to unnecessary risk, given the potential for
prolonged adverse events. Currently, we are in Phase 3 development for PSVT. We are also developing etripamil to provide
rapid  rate  control  for  patients  with  acute  symptomatic  episodes  of  atrial  fibrillation  and  are  exploring  other  therapeutic
applications  where  a  rapid-onset  and  short  acting  non-dihydropyridine  calcium  channel  blocking  agent  could  provide
patient benefit.

In  our  effort  to  develop  potential  therapies,  we  sought  to  create  new  chemical  entities  as  analogs  of  known  molecular
classes with clinically validated mechanisms of action. Our goal was to preserve the beneficial pharmacology of existing
molecules  while  altering  their  pharmacokinetic  profile  with  focused  medicinal  chemistry  to  produce  drugs  that  are  fast
acting  and  rapidly  inactivated.  As  a  result,  we  created  a  series  of  novel  non-dihydropyridine  L  type  calcium  channel
blockers containing chemical ester moieties that preserved the desired pharmacology on the heart but that could be rapidly
metabolized and inactivated in the blood by serum esterases. Etripamil resulted from this effort as a new chemical entity
with  a  short  relevant  pharmacodynamic  effect  for  up  to  50  minutes  in  humans,  compared  with  other  calcium  channel
blockers that have pharmacodynamic effects of several hours.

We believe that the following attributes of etripamil make it a better treatment candidate for certain episodic cardiovascular
conditions than current standards of care:

•

•

•

Action: Etripamil is designed to act upon the desired target for only up to approximately 50 minutes, with the
goal of reducing long-term side effects that may occur with chronic drug therapy.

Absorption:  Etripamil  is  designed  to  be  absorbed  into  the  bloodstream  in  less  than  10  minutes  through  the
inner lining of the nose.

Administration: Etripamil is designed to be self-administered by patients via a nasal spray device.

To  better  understand  the  opportunity  for  etripamil  in  the  United  States  and  Europe,  we  have  completed  multiple  market
research  studies  and  continue  to  conduct  additional  work.  In  2020,  we  conducted  quantitative  research  with  250
cardiologists who . These physicians were shown various product profiles, for etripamil reflecting different efficacy and
dosing scenarios for etripamil. In this research, cCardiologists reported a willingness to prescribe etripamil to 49% of their
patients when exposed to a single administration profile commiseratecommensurate with NODEode- 301 results, and their
w. Willingness to prescribe increased to a range of ~50-55%modestly when exposed to repeat administration scenarios with
higher efficacies.

We  also  commissioned  market  research  in  2019  with  representatives  of  20  regional  and  national  commercial/medicare
payors  and  pharmacy  benefits  managers,  or  PBMs.  In  this  research,  we  asked  these  representatives  to  evaluate  their
receptivity to a product profile of etripamil, which assumes a single dose administration and a hypothetical profile of 70%
conversion within 30 minutes for etripamil vs 30% for placebo. When presented with a range of hypothetical wholesale
acquisition costs and asked about the likelihood of coverage of etripamil, commercial and medicare payors on average

11

Table of Contents

believed it was highly likely to receive broad reimbursement if net pricing was below the specialty tier pricing threshold
for government managed plans.

PSVT

PSVT is a serious and recurring electrical disorder of the heart, which is caused by altered electrical conductivity over the
AV node. PSVT refers to a rapid heart rate condition of the heart’s upper chambers (atria) of abrupt onset and termination.
In the most common form of PSVT called AV nodal reentrant tachycardia, or AVNRT, there is an extra piece of electrical
tissue that allows the electrical signal to travel very rapidly in a circle. As shown in the figure below, when that extra tissue
forms within or near the AV node, the signal can now travel down one part of the AV node and up the other in a small
circle, sending impulses out to both the atria and ventricles along the way. The cycle continues over and over, resulting in a
rapid heart rate.

In the next most common form of PSVT, called atrioventricular reciprocating tachycardia, or AVRT, there is an extra piece
of electrical tissue that directly connects the atria and the ventricles. In AVRT, the electrical signal begins like it would in a
normal heartbeat by traveling from the atria to the ventricles over the AV node. However, as shown in the figure above, in
AVRT, the extra piece of electrical tissue allows the signal to travel back up to the atria, creating a “short circuit.” Once the
signal gets back to the atria, it goes back down to the AV node and the cycle continues over and over, resulting in a rapid
heart rate.

In 2018, we conducted a quantitative survey involving approximately 250 patients with PSVT. This survey indicated that it
takes more than two years after first experiencing symptoms of PSVT for the average patient to receive a formal diagnosis,
suggesting >600,000 undiagnosed patients given the estimated incidence rate of approximately 300,000/year. We believe
this delay in diagnosis is primarily the result of the episodic nature of the disease and the requirement for an ECG when the
patient is experiencing an SVT episode to confirm the diagnosis. From this research and other corroborating sources, we
estimate  that,  overall,  60%  of  patients  with  PSVT  are  women  and  approximately  half  suffer  from  cardiovascular
comorbidities. Patients with PSVT report that SVT episodes can be debilitating, leaving them unable to focus on family or
work during an episode. When in an episode of SVT, patients may experience symptoms including palpitations, sweating,
chest  pressure  or  chest  pain,  shortness  of  breath,  sudden  onset  of  fatigue,  fainting  and  anxiety.  Symptoms  commonly
reported by patients with PSVT mimic other conditions and are often mistaken for anxiety or panic attacks, especially in
women.  Researchers  have  noted  that  up  to  27%  of  patients  with  PSVT  stopped  driving  for  fear  of  temporary  loss  of
consciousness, fainting or passing out. Patients have reported that the duration of SVT episodes varies widely from minutes
to hours, or longer.

12

Table of Contents

To further appreciate the burden of disease in PSVT, we recently completed an important patient reported outcomes (PRO)
market research study that we believe establishes the disease burden for patients and the market opportunity for etripamil.
Approximately  250  patients  participated  in  this  study  for  on  average  8.5  months  and  completed  short  surveys
approximately  every  12  days.  In  total,  over  5,000  episodes  of  PSVT  were  reported  and  characterized.  Patients  who
participated in the study demonstrated a wide range of annual SVT episode frequency (0 to >50), with a median frequency
of 12-15 episodes per year. Of these episodes, approximately 60% lasted longer than 10 minutes and 35% longer than 30
minutes. Over 50% of episodes were reported by the study participants to be moderate or severe in intensity. In addition,
approximately  30%  of  patients  experiencing  episodes  sought  medical  care  for  treatment  of  the  episode,  the  majority  of
which were treated in the emergency department.

We believe that the results of this PRO longitudinal market research study provide increased accuracy of the true disease
burden experienced by patients with PSVT that what was reported from previous patient market research. Patients in the
previous study from 2018 reported episode frequencies that varied from less than one per year to greater than 25 per year,
with a calculated median of four to seven episodes of SVT per year.  The longitudinal PRO study demonstrated a higher
annual SVT episode frequency of 12-15.

Qualitative research with a sample of participants who enrolled in the longitudinal PRO market research uncovered that
this discrepancy is likely attributable to bias of patients to recall ‘significant’ episodes in years past (based on perceived
duration/ intensity). Specifically, the median four to seven episodes per year recalled by patients in the 2018 study were
likely more memorable because they share characteristics of higher disease burden. In the PRO study, approximately 45%
of  episodes  were  both  self-described  by  the  patient  as  moderate/severe  in  intensity  and  greater  than  five  minutes  in
duration.   Applying  this  to  the  overall  study  median  frequency  of  12-15  episodes  results  in  a  median  of  five  to  seven
‘burdensome  episodes’  per  year.    Thus,  we  believe  the  results  of  the  PRO  study  largely  confirm  prior  patient  market
research, after accounting for recall bias associated with only remembering burdensome episodes.

In summary, we now model a target addressable market for etripamil of 60% of patients diagnosed with PSVT categorized
as those who experience multiple moderate or severe 10+ minute episodes each year. Furthermore, we believe that these
target patients will use etripamil to treat a median of 4-6 episodes per year based on the projected number of self-reported
longer or more intense episodes experienced by the patient as well as willingness to pay considerations.

Current Treatment Options for PSVT

Treatment for PSVT depends on the frequency, duration, and severity of the episodes as well as patient preference. Current
options for patients with PSVT to terminate an episode of SVT include vagal maneuvers, IV medication or external shock
delivered  in  the  emergency  department.  Additionally,  some  practitioners  prescribe  oral  medications,  such  as  calcium
channel  blockers,  beta  blockers  and  antiarrhythmic  drugs  to  be  taken  at  the  onset  of  an  episode.  However,  these
interventions are generally not acutely effective. Long-term strategies include chronic drug therapy to reduce the frequency
of  episodes  and  cardiac  ablation  to  potentially  cure  the  disease.  Patients  may  also  elect  to  not  treat  their  symptoms  and
simply endure episodes of SVT when they occur.

Vagal  maneuvers  are  commonly  attempted  to  terminate  an  episode,  with  low  to  modest  success  rates.  These  are
physiological  maneuvers  that  stimulate  the  vagus  nerve,  which  can  terminate  an  SVT  episode.  These  include  gagging,
massaging one carotid artery, holding one’s breath and bearing down (Valsalva maneuver), immersing one’s face in ice-
cold water, or coughing.

Currently approved acute pharmacological therapy for the treatment of an acute episode of SVT includes IV administration
of approved AV nodal-blocking agents in an acute care setting. The current standard of care for treatment of episodes of
SVT is adenosine, but prior to its approval in 1990, episodes of SVT were treated with IV calcium channel blockers, such
as  verapamil  or  diltiazem.  When  given  as  a  rapid  IV  bolus,  adenosine  blocks  conduction  over  the  AV  node,  thereby
interrupting the arrhythmia circuit and restoring the heart back to sinus rhythm. Adenosine temporarily stops the heart and
patients have reported experiencing chest tightness, flushing and a sense of impending death. Physicians report that patients
tell them that they feel like they are going to die. Adenosine is eliminated from the body in less than one minute but cannot

13

Table of Contents

be self-administered as it requires IV access. In-hospital IV administrations are associated with higher healthcare costs and
are also unsettling and inconvenient for the patient. IV calcium channel blockers also slow conduction over the AV node
during the course of several minutes. However, they are associated with the risk of excessive slowing of the heart rate and
low blood pressure. According to treatment guidelines, patients in the acute care setting who fail pharmacologic treatment
for PSVT could then receive direct current cardioversion, where an electric shock is applied to the heart to return it to sinus
rhythm.

In  an  attempt  to  prophylactically  control  the  frequency  and  duration  of  future  SVT  episodes,  many  patients  will  take
chronic  daily  oral  medications  that  modulate  AV  nodal  conduction,  such  as  beta  blockers,  L-type  non-dihydropyridine
calcium channel blockers, or antiarrhythmic drugs. Despite chronic daily oral medication, breakthrough SVT episodes that
require  visits  to  the  emergency  department  may  still  occur,  albeit  for  some  patients  at  a  reduced  frequency.  Chronic
medication can lead to side effects such as sexual dysfunction or fatigue in the case of beta blockers and constipation in the
case of verapamil. Some patients discontinue chronic oral medication due to intolerable side effects. Based on our market
research, we estimate that approximately two thirds of patients with PSVT have been prescribed chronic medications such
as  beta  blockers  or  calcium  channel  blockers  to  prevent  SVT  episodes  or  to  treat  other  concomitant  conditions  such  as
hypertension.

The only potentially curative treatment available at the present time for PSVT is ablation, an invasive procedure, which
works by directly cauterizing or freezing the short circuit that is the cause of the abnormal rhythm. This is achieved in an
electrophysiology lab via catheters that are run through the patient’s groin vessels and into the heart and uses burning or
freezing techniques to destroy the heart’s abnormal electrical tissue. Ablation single-procedure success rates for PSVT are
reported to be 91% to 96%. However, we estimate that less than 10% of patients with PSVT per year choose this option,
which we believe is due primarily to anxiety related to the procedure. Although ablations are generally considered to be
safe by the treating community, as with any invasive procedure there are potential complications, which include bleeding,
blood clots, pericardial tamponade, and transient or permanent heart block, with the latter requiring permanent pacemaker
implantation.

Market Opportunity

We  believe  that  PSVT  is  a  large  and  under-recognized  market  that  we  estimate  affects  approximately  two  million
Americans and results in over 600,000 healthcare claims in the United States alone per year, including more than 150,000
emergency  department  visits  and  hospital  admissions  and  up  to  80,000  ablations.  Furthermore,  we  estimate  that
approximately 300,000 people are diagnosed with PSVT each year in the United States. We derive these estimates from the
analysis of longitudinal claims data, which we believe is the most accurate method available to estimate the epidemiology
of PSVT. A study in the Journal of Clinical Electrophysiology published in 2021 concluded that excluding patients with
comorbid Atrial Fibrillation or Atrial Flutter (AFib/AFL) leads to a conservative estimate of PSVT treated prevalence in
the U.S. of ~1.3M, while including those with comorbid AFib/AFL suggests a U.S. treated prevalence of approximately
2.1M, with approximately 190,000 to 310,000 corresponding new cases each year.

Other  published  sources  that  attempt  to  quantify  the  epidemiology  of  PSVT,  such  as  the  MESA  study  published  in  the
Journal of the American College of Cardiology in 1998, and the PREEMPT study published in the Journal of the American
Heart  Association  in  2018,  provide  important  demographic  and  clinical  characteristic  data  on  patients  with  PSVT.  For
example, in the MESA study, fewer than 40% of the adjudicated incident cases of PSVT would have been detected had the
investigators limited their screening to those patients identified by the PSVT ICD9 Code (427.0). In addition, 21% of the
incident patients with PSVT in the MESA study also had a diagnosis of atrial fibrillation (18%) or atrial flutter (6%). As an
epidemiology  tool,  however,  we  believe  these  studies  underestimate  the  incidence  and  prevalence  of  PSVT  due  to  the
episodic nature of the disease as well as the variability in the duration of the episodes, as the investigators in both studies
relied only on data from patients presenting to healthcare settings acutely, with the episode confirmed on ECG during the
encounter, to estimate the incidence and prevalence of PSVT.

Current treatment for PSVT also consumes significant healthcare resources. Research published in the American Journal of
Cardiology  in  2020  shows  that  costs  for  patients  rose  significantly  in  the  pre-diagnosis  year  due  to  the  difficulty  of
obtaining an accurate diagnosis. In the year following diagnosis, costs triple for those less than 65 years of age and double

14

Table of Contents

for those over 65 years of age, compared to matched controls. Total healthcare expenditures in the year following PSVT
diagnosis  ranged  from  $20,000-$30,000  per  patient,  significantly  higher  than  the  expenditures  observed  for  patients
without PSVT (~$6,500 per patient). Significant increases for both age groups were noted for emergency department visits.
For those less than 65, the average cost of hospitalizations doubled as their inpatient rates quadrupled. Of note, catheter
ablations following diagnosis represent only 23% of this increased spend, meaning the majority of costs are unrelated to
ablations. In total, approximately $3 billion is spent annually in the U.S. on the management of PSVT.

Our Clinical Development Program for the Treatment of PSVT

Current  treatments  do  not  address  the  unmet  medical  need  for  a  rapid-acting,  effective,  and  safe  patient-administered
treatment that can be taken outside of a hospital or acute care setting at the onset of an SVT episode to restore the heart
back to sinus rhythm. We believe that etripamil fills this need. We completed a Phase 1 clinical trial, which supported the
selection  of  four  doses  of  etripamil  for  Phase  2  development,  followed  by  a  Phase  2  clinical  trial  in  adult  patients  to
evaluate  the  effects  of  four  doses  in  patients  with  PSVT.  Both  trials  were  conducted  to  assess  nasally-  administered
etripamil compared to placebo. Based on discussions with the FDA, we initiated a pivotal Phase 3 clinical trial (NODE-
301) in July 2018 to assess the efficacy and safety of etripamil in the at-home setting and released topline data in March of
2020. We have completed a second Phase 1 clinical trial, further characterizing the PK and PD of etripamil in Japanese and
non-Japanese healthy volunteers. We have also completed the conduct portion of an open label Phase 3 safety trial (NODE-
302), which provided further drug access to patients that had previously participated in the NODE-301 trial. The primary
objective of the NODE-302 trial is to assess the safety of etripamil 70 mg in patients over multiple episodes. We are also
conducting  NODE-303,  which  is  an  ongoing  open  label  Phase  3  study  that  has  the  objective  of  collecting  further  safety
data. The FDA has agreed that our Phase 3 clinical program could support an NDA filing in the United States.

Phase 1 Clinical Data

We completed a Phase 1 clinical trial (MSP-2017-1096) in healthy volunteers, which was designed to assess the safety, PK
profile, and cardiac pharmacology of intranasally administered etripamil in a randomized, double-blind, placebo controlled,
single ascending dose trial. The primary objective of this trial was to determine the maximum tolerated dose or maximum
feasible dose of two different formulations of etripamil administered via the nasal route in healthy, adult male subjects. All
doses of etripamil were generally well tolerated, and there was no difference in the safety profile and PK between the two
formulations  of  etripamil,  referred  to  as  MSP2017A  and  MSP2017B.  The  most  commonly  reported  side  effects  were
related to nasal irritation and nasal congestion.  Tolerability areas of focus such as syncope, pre-syncope, lightheadedness,
or decreases in systolic blood pressure below 90 mmHg or AV nodal blocks of second degree or worse were not reported or
observed. The study of MSP2017A was stopped at 60 mg and MSP2017B was further studied at higher doses (105 mg and
140 mg). The Phase 1 results supported the selection of four doses of etripamil for Phase 2 development. We are using this
Phase 1 data to support further clinical development of etripamil in two indications: PSVT and AFib-RVR.

Following  nasal  administration  of  etripamil,  PK  analyses  demonstrated  rapid  absorption  and  elimination,  a  dose
proportional systemic exposure, or area under the curve, and maximum plasma concentration for etripamil and its primary
inactive metabolite. These findings were consistent across a range of seven doses tested up to 140 mg. The 140 mg dose
was  the  maximal  feasible  dose  because  neither  the  concentration  (350  mg/mL)  nor  the  volume  (200  µL)  of  solution
administered  in  each  nostril  could  be  increased.  Due  to  these  characteristics  of  formulation  and  delivery,  a  maximum
tolerated dose of etripamil was not established. The figure below shows the rapid absorption via the nasal route and the
rapid decrease in plasma concentration of etripamil.

15

Table of Contents

Phase 1: (MSP-2017-1096)

Pharmacokinetic Profile of Etripamil Plasma Concentrations

Error bars indicate standard error of the mean

Prolongation  of  the  PR  interval  as  measured  by  ECGs  was  taken  as  the  pharmacodynamic  (PD)  measure.  A  linear
relationship was observed between the dose of etripamil and prolongation of the PR interval. The 60 mg, 105 mg, and 140
mg  doses  demonstrated  a  10%  or  greater  PR  prolongation,  which  is  shown  in  the  figure  below.  This  correlates  with  the
reported  slowing  of  conduction  over  the  AV  node  that  is  necessary  to  convert  an  SVT  episode  to  sinus  rhythm.  Such
slowing  of  conduction  has  already  been  observed  clinically  with  IV  AV  nodal-blocking  agents  such  as  adenosine,
verapamil, and tecadenoson.

16

Table of Contents

Phase 1: (MSP-2017-1096) - Pharmacology

We  completed  a  second  Phase  1  trial,  NODE-102,  comparing  the  PK  and  PD  of  etripamil  35  mg,  70  mg,  and  105  mg
versus placebo in Japanese and non-Japanese healthy volunteers. Once we determined there was no difference in PK and
PD of etripamil between Japanese and non-Japanese participants, we pooled the data from the overall populations into a
single dataset. We believe this trial provides further justification for the selected 70 mg dose in our Phase 3 program and
may be used to support further clinical development of etripamil in Japan.

As shown in the figure below, we observed a correlation between the PK profile of etripamil 70 mg, measured by change in
PR interval from baseline over time, and the plasma concentrations of etripamil.  With regard to pharmacodynamics, we
believe  an  approximately  10%  increase  in  the  PR  interval  is  a  marker  of  meaningful  AV  nodal  conduction  needed  to
terminate an episode of PSVT.  The data as demonstrated on the blue line on the graph below indicates that etripamil 70 mg
is potentially impacting AV nodal conduction at meaningful levels for a period up to approximately 50 minutes.  

17

Table of Contents

Phase 1: (MSP-2017-1205) NODE-102

As  noted  in  the  discussion  of  the  RAPID  study  below,  the  RAPID  study  will  incorporate  a  repeat  dose  administration
regimen of study drug (either 70 mg of etripamil or placebo).  Specifically, patients will be instructed to administer a repeat
administration  of  study  drug  if  they  have  not  experienced  symptom  relief  within  10  minutes  of  the  first  study  drug
administration. This tailored regimen utilizes a repeat-dose similar to current PSVT treatment practices with intravenous
drugs  in  the  emergency  department  setting.   A  similar  regimen,  using  repeat  doses  of  30  mg  etripamil  administered  10
minutes apart, was tested in one cohort of the original phase 1 trial (study MSP-2017-1096).  As shown in the figure below,
this  regimen  allowed  for  greater  systemic  exposure  to  etripamil  in  this  cohort,  as  measured  by  a  second  maximum
concentration after the second administration, as well as a total Area Under the Curve.  We believe this PK data supports
the hypothesis underlying our RAPID trial regimen that a second administration will improve the impact of etripamil on
AV nodal conduction and result in a greater therapeutic effect.

18

Table of Contents

Phase 1: (MSP-2017-1096) -30 mg etripamil administered 10 minutes apart

Phase 2 Clinical Data

We completed a Phase 2 multicenter, randomized, double-blind, placebo controlled clinical trial in the United States and
Canada to evaluate the effects of four different doses of etripamil in patients with PSVT. In order to demonstrate the ability
of etripamil to terminate SVT in a controlled setting, we conducted the study in the electrophysiology, or EP, laboratory
setting, where the SVT episode could be induced in patients scheduled to undergo an EP study and ablation. The primary
objective of this trial was to demonstrate the superiority of at least one dose of etripamil over placebo in terminating SVT.
The secondary objectives were to determine the minimally effective dose of etripamil, to establish a dose related efficacy
trend for etripamil, and to evaluate the safety of etripamil in a clinical setting. The trial was statistically powered at more
than 80% to show a 50% absolute difference of etripamil versus placebo.

The trial enrolled 199 patients, of which 95 withdrew prior to dosing: 70 due to inability to induce (n=42) or sustain (n=28)
SVT, 5 based on physician discretion, 1 lost to follow up, 1 due to withdrawal of consent, and 18 for other reasons. The
mean age of patients was 52.2 years, with the study enrolling patients as young as 19 and as old as 85. As shown in the
figure below, SVT was induced and sustained for 5 minutes in 104 patients, who were randomized into one of five dosing
cohorts.  Four  cohorts  received  active  doses  of  etripamil  (35  mg,  70  mg,  105  mg  or  140  mg)  and  one  cohort  received
placebo.  All  doses  of  the  study  drug  were  delivered  in  a  blind  randomized  fashion  in  which  healthcare  providers
administered  four  100  µL  sprays  from  four  different  single  spray  devices.  There  were  no  imbalances  in  baseline
characteristics across the five treatment groups. The mean heart rate in SVT at time 0 was 177 bpm in the placebo group
and 168 bpm, 173 bpm, 180 bpm and 155 bpm in the etripamil 35 mg, 70 mg, 105 mg and 140 mg groups, respectively.

19

Table of Contents

Phase 2: (MSP-2017-1109) NODE 1  – Clinical Trial Design

The  primary  endpoint  in  this  clinical  trial  was  the  conversion  of  SVT  to  sinus  rhythm  within  15  minutes  after
administration of etripamil or placebo. As shown in the figure below, the percentage of patients in whom SVT converted to
sinus rhythm within 15 minutes of study drug administration was 65% with 35 mg etripamil, 87% with 70 mg, 75% with
105  mg  and  95%  with  140  mg,  compared  with  35%  in  the  placebo  arm.  The  three  highest  doses  of  etripamil  showed
statistically significant conversion rates compared with placebo. Statistical significance expresses the probability that the
results of a particular study could have occurred purely by chance. Statistical significance is assessed by the FDA and other
health  regulatory  agencies  in  evaluating  marketing  approval  applications.  FDA  and  other  regulatory  agencies  review  the
strength  of  the  statistical  evidence  and  whether  it  supports  the  claims  of  the  applicant.  The  primary  endpoint,  statistical
methods for the trial and a p-value boundary for achieving statistical significance for a clinical trial are typically defined
before  the  trial  begins.  If  the  probability  of  observing  the  calculated  statistic  is  smaller  than  the  p-value  boundary,  the
primary  endpoint  is  considered  statistically  significant.  P-value  is  a  conventional  statistical  method  for  measuring  the
statistical significance of clinical results. A p-value of 0.05 or less represents statistical significance, meaning there is a less
than 1in 20 likelihood that the observed results occurred by chance. The FDA utilizes statistical significance, as measured
by p-value, as an evidentiary standard of efficacy and typically requires a p-value of 0.05 or less to demonstrate statistical
significance.

20

Table of Contents

Phase 2: (MSP-2017-1109) NODE 1 - Etripamil Conversion Rates from SVT to Sinus Rhythm

In a post-hoc analysis conducted to help inform our Phase 3 trial design, the patients’ time to conversion to sinus rhythm
was examined. As shown in the following Kaplan Meier plot of patients successfully converting to sinus rhythm during the
15-minute study window, the three highest doses of etripamil (140 mg, 105 mg and 70 mg) showed statistically significant
shorter time to conversion compared with placebo. The 70 mg dose showed a rapid onset of action with a median time to
conversion of less than three minutes after nasal administration of etripamil.

21

Table of Contents

Phase 2: (MSP-2017-1109) NODE 1 – Etripamil Time to Conversion from SVT to Sinus Rhythm

Overall,  etripamil  was  well  tolerated,  and  the  most  common  adverse  events  were  related  to  the  nasal  route  of
administration,  e.g.,  nasal  irritation  or  nasal  congestion,  reported  by  up  to  60%  and  45%  of  patients,  respectively,  after
etripamil  versus  none  after  placebo  administration.  The  70  mg  dose  was  reported  to  have  48%  nasal  irritation  and  26%
nasal congestion. However, these were transient. Most adverse events were mild (44.2%) or moderate (24.0%) across all
treatment groups. At least one adverse event considered related to the study drug, according to the investigator assessment,
was reported in 17 (85.0%) patients in the etripamil 35 mg group, 18 (78.3%) in the 70 mg group, 15 (75.0%) in the 105
mg group, 20 (95.2%) in the 140 mg group and 4 (20.0%) in the placebo group. The incidence of adverse events was not
dose dependent. Hypotension, or low blood pressure, was reported as an adverse event in two patients, one in the 105 mg
dose group of etripamil and one in the 140 mg group.

A total of three patients experienced severe adverse events that were considered possibly related to etripamil. One patient
who received a 35mg dose of etripamil experienced facial flushing, shortness of breath, and chest discomfort. One patient
who received a 105 mg dose of etripamil had nausea and vomiting, as well as a severe and serious cough. One patient who
received  a  140  mg  dose  of  etripamil  experienced  a  severe  adverse  event  of  second-degree  AV  block  with  hypotension
beginning  five  minutes  after  conversion  to  sinus  rhythm.  The  AV  block  resolved  after  43  minutes,  and  ablation  was
subsequently performed. There were no adverse events that led to study discontinuation or death.

Calcium channel blockers have the potential to cause hypotension as a side effect. In our Phase 2 clinical trial, we recorded
vital signs, including heart rate and blood pressure, before induction of SVT and every two minutes for 30 minutes after
study drug was given (see figure below). We observed no meaningful reduction in mean blood pressure in the 35 mg or 70
mg etripamil cohorts but observed a transient decrease in the mean blood pressure in the two highest cohorts, 105 mg and
140 mg. Due to the induction of SVT, the mean systolic blood pressure decreased at time 0 compared to the average at 20
and 10 minutes before SVT induction. Compared to baseline and time 0, systolic blood pressure measurements recorded
from 2 minutes to 16 minutes post study drug administration showed no decrease in mean systolic blood pressure in the
placebo or 35 mg groups, and maximum mean decreases of 2 mmHg four minutes post dose in the 70 mg group, 17

22

Table of Contents

mmHg six minutes post dose in the 105 mg group, and 20 mmHg six minutes and eight minutes post dose in the 140 mg
group.

Phase 2: (MSP-2017-1109) NODE 1 – Etripamil Systolic Blood Pressure Over Time

* p < 0.05 vs baseline.

Baseline is defined as the average of the -20 and -10 minutes pre-dose measurements. Time 0 is defined as the average of
the measurements during SVT between -5 and 0 minutes before study drug administration. Mean and standard error (SEs)
values were calculated based on available data at the relevant time point. MSP-2017 means etripamil. Error bars indicate
standard error of the mean.

Based on the combination of efficacy and safety data from our Phase 2 trial, we selected the 70 mg dose of etripamil for
our subsequent clinical trials.

Ongoing and Planned Clinical Development of PSVT

Based on our interactions with the regulatory agencies, our planned Phase 3 clinical program includes:

•

•

•

•

NODE-301, a pivotal efficacy trial to assess the time to conversion of etripamil compared to placebo in the
at-home setting.

RAPID,  a  confirmatory  pivotal  efficacy  trial  to  assess  the  time  to  conversion  of  etripamil  compared  to
placebo in the at-home setting.

NODE-302, an open-label extension of NODE301 to enroll patients who have completed NODE301 in order
to collect safety data on subsequent episodes in the at-home setting and.

NODE-303, an open-label global safety trial to complete the safety assessment of etripamil in the at-home
setting to support an NDA.

23

Table of Contents

Phase 3 Clinical Trials

RAPID. The RAPID trial was originally an ongoing trial named NODE-301 part 2 and was designed to collect double-
blind  data  from  randomized  patients  who  had  not  yet  experienced  an  SVT  event  after  the  NODE-301  study  reached  its
target  number  of  adjudicated  SVT  events.  After  receiving  guidance  from  the  FDA  on  our  Phase  3  program,  we  have
amended and expanded NODE-301 part 2 and renamed it the RAPID trial.  The RAPID trial will enroll approximately 500
patients  in  total  and  will  be  completed  after  a  total  of  180  confirmed  SVT  events  are  reached.  Patients  enrolled  in  the
RAPID trial are randomized 1:1 (etripamil:placebo). The graphic below shows the design of the RAPID trial. The protocol
amendment changing NODE-301 part 2 to RAPID and incorporating the repeat dose administration was fully implemented
across  all  clinical  study  sites  over  a  time  period  that  completed  in  2021.  Before  the  repeat  dose  amendment  was  fully
implemented,  a  total  of  33  patients  dosed  themselves  with  single  dose  study  drug  of  which  31  were  confirmed  by  the
adjudication committee to be SVT (i.e. groups C+D in the trial design graphic).  The patients in the combined groups C+D
are randomized 2:1 (etripamil:placebo)

Phase 3: (MSP-2017-1138) RAPID  – Trial Design

(1) Arms C and D (single dose) will be only the patients enrolled under NODE-301 who have had an episode prior to the
RAPID Study protocol amendment
(2) Wilcoxon analysis modeling from NODE-301 data

Under  an  updated  statistical  analysis  plan,  or  SAP,  the  primary  efficacy  endpoint  for  both  the  RAPID  and  NODE-301
studies  will  be  defined  as  time  to  conversion  over  the  first  30  minutes,  with  a  target  p-  value  of  less  than  0.05  for  each
study. We believe, this endpoint supports the desire of patients to rapidly address their PSVT symptoms during an episode
and  ideally  avoid  visiting  the  emergency  department.  Based  on  interactions  with  PSVT  treating  physicians  and
cardiovascular thought leaders, we believe that a 50% conversion rate within 60 minutes is a clinically meaningful outcome
given the symptomatic nature of SVT episodes and the lack of approved at-home treatments.

When employing the updated SAP retrospectively to the NODE-301 data, 54% of etripamil patients vs. 35% of placebo
patients converted within 30 minutes (HR 1.87, p=0.02).  Applying the same primary endpoint to the RAPID study and
powering the study at 90% to detect a 19% difference of etripamil versus placebo in 30 minute time to conversion that was
observed in the NODE-301 study results in the size of 180 confirmed PSVT events. A total sample size of 180 patients in
RAPID with a positively adjudicated PSVT episode, randomized at a range of 1:1 to 2:1 ratio (active : control) provides

24

Table of Contents

at least 90% power to detect a significant treatment difference for the primary endpoint at a two-sided significance level of
0.05.  This  sample  size  was  calculated  based  on  internal  modeling  of  the  Part  1  data  where  etripamil  had  a  higher
conversion rate (54% versus 35% at 30 minutes), and also a more rapid conversion rate (32% versus 14% at 10 minutes).
Assuming a type I error rate of alpha = 0.05 and a ratio in the number of positively adjudicated episodes of PSVT etripamil
placebo between 1:1 and 2:1, a minimum of 80 positive conversion events will be required.  Based on internal modeling,
180 patients with a positively adjudicated PSVT episode and 80 positive conversion events will attain greater than 90%
power on the primary variable of time to conversion (using a 2-sided Wilcoxon test). Later and earlier time points for time
to conversion as well as patient reported outcomes and emergency department utilization will also be assessed as part of
secondary analyses to fully characterize the efficacy profile of etripamil.

The  RAPID  study  is  being  conducted  in  North  America  and  in  multiple  countries  in  Europe.   The  trial  was  initiated  in
North  America  during  the  fourth  quarter  of  2020,  amidst  the  COVID-19  pandemic.    The  first  patient  was  dosed  in
November 2020.

NODE-301.    NODE-301  is  a  placebo-controlled  Phase  3  clinical  trial  conducted  in  the  United  States  and  Canada  to
evaluate 70 mg of etripamil versus placebo in terminating an SVT episode in the at-home setting. As shown in the figure
below, the primary endpoint is the time to conversion over a five-hour monitoring period following the administration of
the study drug. Prior to randomization, eligible patients administered a test dose of 70 mg of etripamil in the investigator’s
office while in sinus rhythm in order to assess tolerability. Patients successfully completing the test dose were randomly
assigned to the etripamil or placebo cohorts (2:1 randomization) and sent home with the study drug and a small portable
cardiac monitor to be used during the patient’s subsequent SVT episode. Upon experiencing symptoms of their next SVT
episode,  patients  were  instructed  to  first  apply  the  cardiac  monitoring  device  to  record  ECG  data,  then  attempt  a  vagal
maneuver, and if that was not successful in terminating the episode, to then administer the drug. Patients’ ECG data was
recorded using the cardiac monitoring device for a period of five hours after study drug administration. Patients returned to
the clinic for a follow up visit within one week following their SVT event for collection of further information. NODE-301
enrolled  431  patients  across  65  sites  in  the  United  States  and  Canada,  with  156  patients  (107  etripamil,  49  placebo)
receiving etripamil for an adjudicated true PSVT episode.

In March 2020, we reported topline results of the first part of the NODE-301 trial. The first part of NODE-301 did not meet
its  primary  endpoint  of  time  to  conversion  of  SVT  to  sinus  rhythm  compared  to  placebo  over  the  five-hour  period
following  study  drug  administration.  The  median  time  to  conversion  for  etripamil  was  25  minutes  (95%  CI:  16,  43)
compared to 50 minutes (95% CI: 31,101) for placebo. As shown in the top figure below, despite the activity of etripamil
and  separation  from  placebo  in  the  first  approximately  sixty  minutes  following  study  drug  administration,  a  time  period
consistent  with  the  pharmacological  activity  of  the  drug,  results  from  the  latter  part  of  the  analysis  confounded  the
statistical analysis of the primary endpoint. We also analyzed the first 30 minutes of the Kaplan Meier curve, shown in the
bottom graph below, and the post hoc results at that time point were a 54% rate of conversion for the etripamil patients and
35% for the placebo patients. The results were statistically significant with a hazard ratio of 1.87 and a p-value of 0.02.

25

Table of Contents

Phase 3: (MSP-2017-1138) NODE-301 Part 1 Efficacy – Time to Conversion over 5 Hours
(Post hoc analysis – Time to Conversion over 30 minutes)

26

Table of Contents

The  study  demonstrated  statistically  significant  improvements  in  patients  taking  etripamil  compared  to  those  taking
placebo  in  the  secondary  endpoint  of  patient  reported  treatment  satisfaction,  as  measured  by  a  treatment  satisfaction
questionnaire  for  medication  (TSQM-9),  including  global  satisfaction  (p=0.0069)  and  effectiveness  scores  (p=0.0015).
Additionally,  there  was  a  trend  towards  improvement  in  the  percentage  of  patients  seeking  rescue  medical  intervention,
including  in  the  emergency  department,  with  15%  and  27%  etripamil  and  placebo  patients,  respectively,  reporting  such
intervention (p=0.12).

Phase 

3: 

(MSP-2017-1138) 

NODE-301 

Key 

Secondary 

Efficacy 

Endpoints 

Overall, etripamil was well tolerated when self-administered as a test dose during sinus rhythm or as a post-randomization
dose during symptomatic PSVT. The most common (≥5%) adverse events occurring within 24 hours of a test dose or those
occurring more frequently with etripamil within 24 hours of a randomized dose were nasal discomfort, nasal congestion,
epistaxis,  rhinorrhea,  throat  irritation,  and  increased  lacrimation,  all  of  which  were  related  to  the  nasal  route  of
administration. The incidence of all other adverse events, including those related to abnormal vital signs, laboratory results,
and ECG findings, was balanced between the 2 groups. No serious adverse events were observed within 24 hours of taking
study drug.

NODE-302.  NODE-302 is the open label extension trial of NODE-301. We designed NODE-302 to primarily evaluate the
safety of etripamil when self-administered without medical supervision and to monitor the safety and efficacy of etripamil
for the treatment of multiple episodes of SVT.

Patients who have successfully dosed with the study drug in NODE-301 and completed a study closure visit were eligible
to  enroll  in  NODE-302  to  manage  any  subsequent  episodes  of  SVT.  Eligibility  was  also  contingent  on  satisfying  all
inclusion and exclusion criteria, including not experiencing a serious adverse event related to the study drug or the study
procedure that precludes the self-administration of etripamil.

We initiated NODE-302 in December 2018. The trial completed enrollment in 2020 and the study is in the process of being
published. Overall, the safety and tolerability profile of etripamil 70 mg was favorable and generally consistent with what
was observed in the NODE-301 study.

NODE-303.    NODE-303  is  an  open-label  global  safety  trial  enrolling  patients  who  did  not  participate  in  NODE-301  or
NODE-302 or RAPID in order to collect safety data that when combined with the safety data from the rest of the program

27

Table of Contents

will  form  the  safety  dataset  to  be  evaluated  by  the  FDA  and  other  regulatory  agencies  to  form  the  basis  for  marketing
approval.  We designed NODE-303 to evaluate the safety of etripamil when self-administered without medical supervision,
and to evaluate the safety and efficacy of etripamil on multiple SVT episodes. The NODE-303 trial is designed to more
closely  mimic  the  expected  utilization  of  etripamil  in  the  post  approval  setting  and  for  example  does  not  include  an  in-
office  safety  test  dose  and  includes  a  broad  patient  population,  including  patients  taking  concomitant  betablockers  and
calcium channel blockers In this study, patients have the opportunity to manage up to four episodes of SVT. NODE-303
was initiated in October 2019 utilizing the single 70 mg etripamil administration. In 2021, following FDA’s acceptance, we
initiated the change from the single 70 mg etripamil administration to the 70 mg repeat dose treatment regimen.  The FDA’s
acceptance  was  based  on  initial  safety  data  of  the  repeat  dose  regimen  experience  gained  in  the  RAPID  study  and  the
overall safety data from the etripamil clinical program to date.

Atrial Fibrillation

Atrial fibrillation (AFib) is a common form of arrhythmia with an irregular and often rapid heart rate that can increase the
risk of stroke, heart failure, and other heart-related complications. During AFib, the heart’s two upper chambers, the atria,
beat chaotically and irregularly—out of coordination with the two lower chambers, the ventricles, of the heart, as shown in
the figure below. AFib can occur with or without symptoms, with symptoms often including heart palpitations, shortness of
breath,  and  weakness.  Episodes  of  atrial  fibrillation  can  come  and  go,  or  patients  may  have  AFib  that  does  not  resolve.
Although the heart arrhythmia in AFib itself usually is not life-threatening, it is a serious medical condition that sometimes
requires  emergency  treatment.  Additionally,  AFib  is  associated  with  elevated  risk  of  embolism  and  stroke  and
anticoagulant  medications,  also  called  blood  thinners,  are  commonly  prescribed  to  manage  this  risk.  Uncertainty  around
symptom timing and episode length may impact a patient’s quality of life.

Classification of AF is used to determine the appropriate treatment modality for patients. The American Heart Association,
or AHA, and the American College of Cardiology, or ACC, categorize AFib patients based on disease progression. These
categories are defined as follows: paroxysmal ,which involves AFib episodes that resolve spontaneously within seven days
of symptom onset; persistent, which involves AFib episodes that fail to terminate within seven days of symptom onset and
require treatment to convert back to sinus rhythm; long-standing persistent, which involves atrial fibrillation episodes that
last  longer  than  one  year  despite  continued  attempts  to  restore  sinus  rhythm;  and  permanent,  which  involves  a  joint
decision by the treating provider and patient to no longer pursue cardioversion and leave the patient in AFib, focusing on
rate control and symptom management. Disease progression in AFib is common with approximately 40% of AFib patients
in  the  paroxysmal  stage,  30%  of  AFib  patients  in  the  persistent  and  long-standing  persistent  stage,  and  30%  of  AFib
patients  in  the  permanent  stage.  For  purposes  of  simplicity,  we  do  not  differentiate  the  long-standing  persistent
classification  from  the  persistent  classification  as  the  clinical  impact  of  this  differentiation  has  not  been  characterized.
Concomitant structural heart irregularities including valvular dysfunction and the presence of active symptoms may also
help to characterize patients and influence treatment decisions.

A common complication of atrial fibrillation is rapid ventricular rate which is frequently defined as a heart rate of ≥110
beats per minute. Rapid, irregular, and inefficient contractility induced by rapid ventricular rate accounts for hemodynamic

28

Table of Contents

instability  and  symptoms  of  palpitations.  Frequently,  new-onset  patients  with  atrial  fibrillation  present  with  symptoms
related to rapid ventricular rate.

Current Treatment Options for AFib

There are currently two pharmacological approaches to managing atrial fibrillation: rate control to lower a rapid heart rate
and rhythm control to restore and maintain a regular (sinus) rhythm and prevent recurrent AFib episodes. Either of these
pharmacological management approaches may be administered chronically or acutely, depending on patient preference and
episode frequency and/or severity. The decision to pursue rate and/or rhythm control for AFib episodes is dependent on a
variety  of  factors,  including  episode  severity,  episode  frequency,  patient  preference,  and  safety  and  tolerability  of
treatments. Several rhythm control strategies exist, including electrical cardioversion, catheter ablation and anti-arrhythmic
drug therapy. For rate control, the rapid heart rate of atrial fibrillation is typically treated with AV nodal blocking drugs (for
example, calcium channel blockers, beta blockers, or less commonly digoxin) to control symptoms and improve cardiac
function/hemodynamic stability. Oral rate control drugs used acutely do not provide immediate ventricular rate control due
to  a  30-to-60-minute  delayed  onset  of  action.  Breakthrough  episodes  of  symptomatic  AFib  often  require  urgent  medical
treatment  with  IV  calcium  channel  blockers  and  beta-blockers  under  medical  supervision,  usually  in  the  emergency
department to quickly reduce heart rate before transitioning a patient back to oral therapy.

The  “pill-in-pocket”  anti-arrhythmic  strategy  is  described  by  the  AHA  and  ACC  guidelines  as  the  utilization  of  an  oral
dose  of  flecainide  or  propafenone  as  an  attempt  to  restore  sinus  rhythm  shortly  after  the  onset  of  symptomatic  atrial
fibrillation.  Neither  drug  referenced  in  the  guideline  is  approved  by  any  regulatory  agency  for  the  use  outlined  in  the
guideline.  Pill-in-pocket  rhythm  control  strategies  are  considered  by  physicians  for  patients  who  demonstrate  favorable
outcomes to these medications in the clinic and who are thought to be reliable enough to administer them appropriately.
Initial  administration  of  pill-in-pocket  medication  is  recommended  in  a  monitorable  setting  due  to  potential  AV  node
dysfunction or a proarrhythmic response and may be preceded by beta-blocker or calcium channel blocker therapy if the
patient is not chronically rate controlled.  

Rate controlling agents (for example, calcium channel blockers and beta blockers) may also be administered acutely on an
as needed (or PRN) basis. Though the AHA and ACC guidelines do not explicitly acknowledge this approach, participants
in market research conducted by us indicate a significant share of patients are managed this way. PRN rate control is more
prominently used in paroxysmal patients who do not tolerate chronic medications but experience symptomatic, infrequent
AFib episodes. Our patient market research from 2018 estimated that approximately 40% of patients use an additional rate
control  medication  to  manage  acute  symptoms  of  atrial  fibrillation.  Additionally,  our  physician  market  research
commissioned in 2021 suggests that both clinical/interventional cardiologists and electrophysiologists prescribe PRN rate
control for some of their paroxysmal and persistent patients.

Market Opportunity – AFib

The  American  Heart  Association  estimates  that  in  2016  approximately  five  million  people  suffered  from  AFib  in  the
United  States.  This  estimate  is  projected  to  increase  over  the  next  ten  years;  the  AHA  suggests  a  prevalence  of  seven
million by 2030, while the Centers for Disease Control (CDC) reports this prevalence as increasing to 12 million over the
same time period, representing an approximately 6% annual growth rate. From market research with treating physicians,
we  estimate  that  approximately  40%  of  these  patients  have  paroxysmal  AFib,  30%  have  persistent  AFib,  and  30%  have
permanent AFib. Acute episodes of symptomatic AFib are often treated with the approaches described above. However,
due to the concerning nature of AFib symptoms, patients often present to the emergency department. In the ED, patients
are  treated  with  IV  calcium  channel  blockers  or  beta-blockers  to  quickly  reduce  heart  rate  and/or  anti-arrhythmic  or
electrical  cardioversion  before  transitioning  a  patient  back  to  oral  therapy.  According  to  the  Healthcare  and  Utilization
Project, 660,000 patient visits to the emergency department in 2016 were attributed to AFib (ICD-10 diagnosis codes I48.0,
I48.1, I48.2, I48.91). Additionally, approximately 465,000 patients were admitted to the hospital with AFib (same ICD-10
codes).

Our qualitative and quantitative market research indicates that the target addressable market for etripamil in patients with
AFib-RVR is approximately 30-40% of the five million patients with atrial fibrillation. We derive this percentage estimate

29

Table of Contents

from  2021  market  research  studies  conducted  by  us  that  involved  qualitative  interviews  and  quantitative  surveys  with  a
total of 275 electrophysiologists, general cardiologists, and interventional cardiologists. The physicians in the two studies
were asked to estimate the share of patients experiencing ≥1 symptomatic episode of AFib-RVR requiring treatment per
year.  In  response,  physicians  in  the  quantitative  survey  reported  approximately  40%  of  paroxysmal  patients,  40%  of
persistent  patients,  and  30%  of  permanent  patients  met  this  classification.  This  research  suggests  the  share  of  patients
experiencing ≥1 symptomatic episode of AFib requiring treatment may constitute 30-40% of the prevalent atrial fibrillation
population on a weighted average basis.

We believe that etripamil has the potential to be developed such that it can be used by patients to rapidly reduce their heart
rate in the at-home setting to provide a supplemental option to the acute oral rate or rhythm control strategy their physician
would use. When presented with a target product profile reflecting this potential use case, approximately two thirds of the
physicians in the 2021 market research study perceived utility in the product profile, which could serve as a “bridge” to the
onset of acute oral agents. According to physicians, it can take hours for patients to feel an alleviation of symptoms using
acute oral rate and rhythm control. During this time, patients may experience concerning symptoms that often prompt them
to seek emergent care. We believe that the combination of convenient delivery, potency, rapid onset and short duration of
action of etripamil has the potential to move the current treatment setting for some acute episodes of AFib out of the
burdensome and costly emergency department.

Current atrial fibrillation management consumes significant healthcare resources in the United States. The American Heart
Association published a report in 2016 summarizing the current and projected cost burden of cardiovascular diseases in the
United  States.  This  report  suggests  atrial  fibrillation  resulted  in  $25  billion  in  direct  medical  costs  in  2016  (~7%  of  all
cardiovascular diseases) and another $7 billion in indirect costs (i.e., $32 billion in total costs). Additionally, the forecasted
growth in atrial fibrillation prevalence is anticipated to result in healthcare expenditures of $46 billion in direct costs and
$10 billion in indirect costs in the United States by 2030.

Clinical Development Plan for Atrial Fibrillation

We began enrollment in our Phase 2 proof-of-concept clinical trial, named ReVeRA, in the first quarter of 2021 to evaluate
the  potential  effectiveness  of  etripamil  to  reduce  ventricular  rate  in  patients  with  atrial  fibrillation  and  rapid  ventricular
rate. The ReVeRA Phase 2 double blind, placebo controlled, proof-of-concept trial is conducted in Canada in collaboration
with  the  Montreal  Heart  Institute  and  other  research  centers  and  is  expected  to  enroll  approximately  50  patients
randomized 1:1 to receive either 70 mg of etripamil nasal spray or placebo. The primary endpoint will assess reduction in
ventricular  rate,  with  key  secondary  endpoints  including  the  time  to  achieve  the  maximum  reduction  in  rate  and  the
duration  of  the  effect.  The  trial  is  to  be  conducted  in  the  hospital  or  emergency  department  setting  under  medical
supervision. The COVID-19 pandemic and its impact on emergency departments and hospital personnel has resulted in
significantly slower than expected enrollment for this trial.

Etripamil in Other Therapeutic Applications

Our goal in expanding our pipeline around etripamil is to apply the same paradigm-changing aspiration that we have for
supraventricular  tachycardias  like  PSVT  and  AFib  to  other  cardiac  and  potentially  non-cardiac  conditions  where  we
believe that a rapid-onset, short-acting dihydropyridine L-type calcium channel blocker could potentially deliver significant
clinical and quality of life benefits for patients. We believe that the insights that led to the development of etripamil for the
treatment of PSVT are relevant in other indications where AV-nodal blocking agents with blood vessel widening activity
have demonstrated clinical utility. Both calcium channel blockers and beta blockers are commonly used to manage not only
supraventricular  tachycardias  like  PSVT  or  AFib,  but  also  for  the  treatment  of  chronic  stable  angina  and  angina  due  to
coronary artery spasm.

Sales and Marketing

Given  our  stage  of  development,  we  have  not  yet  established  a  commercial  organization  or  distribution  capabilities.  If
etripamil  receives  marketing  approval,  we  plan  to  commercialize  it  in  the  United  States  with  a  focused,  specialty  sales
force that could consist of our own employees, outsourced sales professionals, or a hybrid model using both internal and

30

Table of Contents

external resources. We believe that this commercial organization at the launch of etripamil will consist of approximately
150  to  200  field  sales  representatives  that  will  call  on  top-prescribing  clinical  cardiologists,  interventional  cardiologists,
electrophysiologists, and high-volume primary care physicians who have a history of prescribing anti-arrhythmic therapies.
We believe an organization of this size would allow us to reach prescribers that collectively care for a substantial portion of
patients diagnosed with PSVT in the United States. Given the importance of increasing awareness and educating patients
with PSVT, we also anticipate deploying focused direct-to-patient marketing campaigns for etripamil. We anticipate that
our sales force could also support the commercialization of additional product candidates treating cardiovascular diseases.
We would expect to conduct most of the buildout of our commercial organization following NDA submission for etripamil.
At this time, we may pursue and believe that we can maximize the value of etripamil by retaining commercialization rights
in the United States and entering into collaboration agreements for certain territories outside the United States, including
the European Union.

Manufacturing

We currently rely on third party contract manufacturing organizations, or CMOs, for all of our required raw materials, nasal
spray  device,  active  pharmaceutical  ingredient  (API)  and  finished  product  for  our  clinical  trials  and  for  our  preclinical
research. We require all of our CMOs to conduct manufacturing activities in compliance with current good manufacturing
practice,  or  cGMP,  requirements.  We  have  assembled  a  team  of  experienced  employees  and  consultants  to  provide  the
necessary  technical,  quality  and  regulatory  oversight  over  our  CMOs  and  have  implemented  a  comprehensive  plan  for
audits  of  our  CMOs.  Currently,  we  have  development  contracts  and  quality  agreements  with  our  CMOs  for  the
manufacturing of etripamil drug substance and drug product. We currently have enough manufactured supply of etripamil
to complete our ongoing registration trials. We also may elect to pursue additional CMOs for manufacturing supplies of
regulatory  starting  materials  in  the  future  and  for  the  filling  of  the  nasal  spray  device,  labeling,  packaging,  storage  and
distribution of investigational drug products. We plan to continue to rely on third party manufacturers for any future trials
and commercialization of etripamil, if approved. We anticipate that these CMOs will have capacity to support commercial
scale production, but we do not have any formal agreements at this time with these CMOs to cover commercial production.
If  etripamil  is  approved  by  any  regulatory  agency,  we  intend  to  enter  into  agreements  with  a  third-party  contract
manufacturer and one or more backup manufacturers for the commercial production of etripamil.

Competition

Drug  development  is  highly  competitive  and  subject  to  rapid  and  significant  technological  advancements.  Our  ability  to
compete will significantly depend upon our ability to complete necessary clinical trials and regulatory approval processes,
and  effectively  market  any  drug  that  we  may  successfully  develop.  Our  current  and  potential  future  competitors  include
pharmaceutical  and  biotechnology  companies,  academic  institutions  and  government  agencies.  The  primary  competitive
factors  that  will  affect  the  commercial  success  of  etripamil  or  any  other  product  candidate  for  which  we  may  receive
marketing  approval  include  differentiation  any  competitor’s  product  regarding  efficacy,  safety,  tolerability,  dosing
convenience, price, coverage and reimbursement. Many of our potential competitors have substantially greater financial,
technical  and  human  resources  than  we  do  and  significantly  greater  experience  in  the  discovery  and  development  of
product  candidates,  as  well  as  in  obtaining  regulatory  approvals  and  commercializing  those  product  candidates  in  the
United States and in foreign countries. It is also possible that a competitor may develop a cure or more effective treatment
method for the diseases we are targeting, which could render our current or future product candidates non-competitive or
obsolete, or reduce the demand for our product candidates before we can recover our development and commercialization
expenses.

We  are  not  aware  of  any  approved  drug  or  any  drug  candidate  in  clinical  development  for  a  patient  with  PSVT  to  self-
administer  treatment  to  terminate  SVT  episodes.  In  the  acute  setting,  IV  treatments  of  generic  drugs  such  as  adenosine,
verapamil and diltiazem, are routinely given. Additionally, some practitioners prescribe oral medications, such as calcium
channel blockers, beta blockers and antiarrhythmics to be taken at the onset of an episode. However, these interventions are
not acutely effective and are not approved by the FDA or other regulatory agencies for this use.

For atrial fibrillation, there are a number of marketed generic antiarrhythmic drugs that are used for chronic and/or acute
rate control, such as metoprolol, propranolol, esmolol, pindolol, atenolol, nadolol, verapamil and diltiazem. We are aware

31

Table of Contents

of  several  drugs  or  new  formulations  of  existing  drugs  under  development  or  recently  under  development  for  atrial
fibrillation, including InRhythm (flecainide), a sodium channel blocker in Phase II from InCarda Therapeutics, Inc., and
Gencaro (bucindolol hydrochloride), a beta blocker in Phase 2 from ARCA biopharma, Inc.

Intellectual Property

We  have  filed  numerous  patent  applications  pertaining  to  etripamil  and  possible  future  product  candidates,  formulations
containing  etripamil,  methods  of  making  such  formulations  and  clinical  use.  We  strive  to  protect  and  enhance  the
proprietary technology, invention and improvements that are commercially important to the development of our business
by  seeking,  maintaining,  and  defending  our  intellectual  property.  We  also  rely  on  know-how,  continuing  technological
innovation and potential in-licensing opportunities to develop, strengthen and maintain our position in the field of cardiac
arrhythmias, such as PSVT, and immediate rate control in atrial fibrillation, as well as other medical conditions affecting
the cardiovascular system. Additionally, we intend to rely on regulatory protection afforded through data exclusivity and
market exclusivity, as well as patent term extensions, where available.

As of March 21, 2022, our patent portfolio as it pertains to etripamil included: 

•      a patent family containing six U.S. patents, projected to expire in 2028, a pending U.S. patent application,
which, if granted, is projected to expire in 2028, as well as corresponding patents in Australia, Brazil, Canada,
China,  Europe,  Hong  Kong,  India,  Japan,  Mexico,  New  Zealand  and  South  Korea,  directed  to  etripamil,
pharmaceutical  compositions  including  etripamil,  and  uses  of  etripamil  such  as  to  treat  angina  or  cardiac
arrhythmias, including PSVT and atrial fibrillation; and 

•      a patent family containing one U.S. patent, projected to expire in 2036, a pending U.S. patent application,
which, if granted, is projected to expire in 2036, as well as corresponding patents in Australia, China, Europe,
Hong Kong, Israel, Japan, Mexico, Russia, South Africa, and Ukraine and corresponding patent applications
in Brazil, Canada, China, Europe, Hong Kong, India, New Zealand, South Africa, and South Korea, directed
to formulations including etripamil, methods of making such formulations, and uses of such formulations to
treat angina or cardiac arrhythmias, such as PSVT and atrial fibrillation. 

•      a patent family containing two pending U.S. provisional patent applications and a pending Canadian patent
application,  which,  if  granted,  is  projected  to  expire  in  2041,  directed  to  uses  of  formulations  including
etripamil to treat angina, cardiac arrhythmias, such as PSVT and atrial fibrillation, or migraines. 

The terms of individual patents may vary based on the countries in which they are obtained. Generally, patents issued for
applications filed in the United States are effective for 20 years from the earliest effective non-provisional filing date in the
absence, for example, of a terminal disclaimer shortening the term of the patent or patent term adjustment increasing the
term  of  the  patent.  In  addition,  in  certain  instances,  a  patent  term  can  be  extended  to  recapture  a  portion  of  the  term
effectively lost as a results of FDA regulatory review periods. The restoration period cannot be longer than five years and
the total term, including the restoration period, must not exceed 14 years following FDA approval. The duration of patents
outside the United States varies in accordance with provisions of applicable local law, but typically is also 20 years from
the earliest non-provisional filing date.

In addition to patents and patent applications that we own, we rely on know-how to develop and maintain our competitive
position.  We  seek  to  protect  our  proprietary  technology  and  processes,  and  obtain  and  maintain  ownership  of  certain
technologies,  in  part,  through  confidentiality  agreements  and  invention  assignment  agreements  with  our  employees,
consultants, scientific advisors, contractors and commercial partners.

Our  future  commercial  success  depends,  in  part,  on  our  ability  to  obtain  and  maintain  patent  and  other  proprietary
protection for commercially important technology, inventions and know-how related to our business; defend and enforce
our patents; and operate without infringing valid enforceable patents and proprietary rights of third parties. Our ability to
stop third parties from making, using, selling, offering to sell or importing our products may depend on the extent to which

32

Table of Contents

we  have  rights  under  valid  and  enforceable  patents  that  cover  these  activities.  With  respect  to  our  owned  intellectual
property, we cannot be sure that patents will issue from any of the pending patent applications which we own or from any
patent applications that we may file in the future, nor can we be sure that any patents that may be issued in the future to us
will  be  commercially  useful  in  protecting  etripamil  or  any  future  product  candidates  and  methods  of  using  or
manufacturing the same. Moreover, we may be unable to obtain patent protection for certain aspects of etripamil or future
product candidates generally, as well as with respect to certain indications. See the section entitled “Risk Factors—Risks
Related to Our Intellectual Property” for a more comprehensive description of risks related to our intellectual property

Government Regulation and Product Approval

Government  authorities  in  the  United  States,  at  the  federal,  state  and  local  levels,  and  in  other  countries,  extensively
regulate, among other things, the research, development, testing, manufacture, packaging, storage, recordkeeping, labeling,
advertising,  promotion,  distribution,  marketing,  import  and  export  of  pharmaceutical  products,  such  as  those  we  are
developing.  The  processes  for  obtaining  regulatory  approvals  in  the  United  States  and  in  foreign  countries,  along  with
subsequent compliance with applicable statutes and regulations, require the expenditure of substantial time and financial
resources.

United States Government Regulation

In  the  United  States,  the  FDA  regulates  drugs  under  the  Federal  Food,  Drug,  and  Cosmetic  Act,  or  FDCA,  and  its
implementing regulations. The process of obtaining regulatory approvals and the subsequent compliance with appropriate
federal, state, local and foreign statutes and regulations requires the expenditure of substantial time and financial resources.
Failure  to  comply  with  the  applicable  United  States  requirements  at  any  time  during  the  drug  development  process,
approval process or after approval, may subject an applicant to a variety of administrative or judicial sanctions, such as the
FDA’s refusal to approve a pending New Drug Application, or NDA, withdrawal of an approval, imposition of a clinical
hold, issuance of warning or untitled letters, product recalls, product seizures, total or partial suspension of production or
distribution, injunctions, fines, refusals of government contracts, restitution, disgorgement or civil or criminal penalties.

The process required by the FDA before a drug may be marketed in the United States generally involves:

•

•

•

•

•

•

•

completion  of  preclinical  laboratory  tests,  animal  studies  and  formulation  studies  in  compliance  with  the
FDA’s good laboratory practice, or GLP, regulations;

submission to the FDA of an IND, which must become effective before human clinical trials may begin;

approval by an independent institutional review board, or IRB, at each clinical site before each trial may be
initiated;

performance of adequate and well controlled clinical trials, in accordance with good clinical practice, or GCP,
requirements to establish the safety and efficacy of the proposed drug for each indication;

submission to the FDA of an NDA;

satisfactory completion of an FDA advisory committee review, if applicable;

satisfactory completion of an FDA inspection of the manufacturing facility or facilities at which the product
is  produced  to  assess  compliance  with  cGMP  requirements,  and  to  assure  that  the  facilities,  methods  and
controls are adequate to preserve the drug’s identity, strength, quality and purity;

33

Table of Contents

•

•

•

satisfactory completion of an FDA inspection of selected clinical sites to assure compliance with GCPs and
the integrity of the clinical data;

payment of user fees; and

FDA review and approval of the NDA.

Preclinical Studies

Preclinical studies include laboratory evaluation of product chemistry, toxicity and formulation, as well as animal studies to
assess  potential  safety  and  efficacy.  An  IND  sponsor  must  submit  the  results  of  the  nonclinical  tests,  together  with
manufacturing information, analytical data and any available clinical data or literature, among other things, to the FDA as
part of an IND. Some nonclinical testing may continue even after the IND is submitted. An IND automatically becomes
effective 30 days after receipt by the FDA, unless before that time the FDA raises concerns or questions related to one or
more proposed clinical trials and places the clinical trial on a clinical hold.

In such a case, the IND sponsor and the FDA must resolve any outstanding concerns before the clinical trial can begin. As
a result, submission of an IND may not result in the FDA allowing clinical trials to commence.

Clinical Trials

Clinical  trials  involve  the  administration  of  the  investigational  new  drug  to  human  subjects  under  the  supervision  of
qualified  investigators  in  accordance  with  GCP  requirements,  which  include  the  requirement  that  all  research  subjects
provide  their  informed  consent  in  writing  for  their  participation  in  any  clinical  trial.  Clinical  trials  are  conducted  under
protocols detailing, among other things, the objectives of the trial, the parameters to be used in monitoring safety and the
effectiveness criteria to be evaluated. A protocol for each clinical trial and any subsequent protocol amendments must be
submitted  to  the  FDA  as  part  of  the  IND.  In  addition,  an  IRB  at  each  institution  participating  in  the  clinical  trial  must
review  and  approve  the  plan  for  any  clinical  trial  before  it  commences  at  that  institution,  and  the  IRB  must  continue  to
oversee  the  clinical  trial  while  it  is  being  conducted.  Information  about  certain  clinical  trials  must  be  submitted  within
specific  timeframes  to  the  National  Institutes  of  Health,  or  NIH,  for  public  dissemination  on  their  ClinicalTrials.gov
website.

Human clinical trials are typically conducted in three sequential phases, which may overlap or be combined. In Phase 1, the
drug is initially introduced into healthy human subjects or patients with the target disease or condition and tested for safety,
dosage  tolerance,  absorption,  metabolism,  distribution,  excretion  and,  if  possible,  to  gain  an  initial  indication  of  its
effectiveness.  In  Phase  2,  the  drug  typically  is  administered  to  a  limited  patient  population  to  identify  possible  adverse
effects and safety risks, to preliminarily evaluate the efficacy of the product for specific targeted diseases and to determine
dosage tolerance and optimal dosage. In Phase 3, the drug is administered to an expanded patient population, generally at
geographically dispersed clinical trial sites, in well controlled clinical trials to generate enough data to statistically evaluate
the safety and efficacy of the product for approval, to establish the overall risk benefit profile of the product and to provide
adequate information for the labeling of the product.

Progress  reports  detailing  the  results  of  the  clinical  trials  must  be  submitted,  at  least  annually,  to  the  FDA,  and  more
frequently if serious adverse events occur. Phase 1, Phase 2 and Phase 3 clinical trials may not be completed successfully
within any specified period, or at all. Furthermore, the FDA or the sponsor may suspend or terminate a clinical trial at any
time on various grounds, including a finding that the research subjects are being exposed to an unacceptable health risk.
Similarly,  an  IRB  can  suspend  or  terminate  approval  of  a  clinical  trial  at  its  institution  if  the  clinical  trial  is  not  being
conducted in accordance with the IRB’s requirements, or if the drug has been associated with unexpected serious harm to
patients.

34

Table of Contents

Marketing Approval

Assuming successful completion of the required clinical testing, the results of the preclinical and clinical studies, together
with  detailed  information  relating  to  the  product’s  chemistry,  manufacture,  controls  and  proposed  labeling,  among  other
things, are submitted to the FDA as part of an NDA requesting approval to market the product for one or more indications.
In most cases, the submission of an NDA is subject to a substantial application user fee. Under the Prescription Drug User
Fee Act, or PDUFA, guidelines that are currently in effect, the FDA has a goal of ten months from the date of “filing” of a
standard NDA for a new molecular entity to review and act on the submission. This review typically takes twelve months
from  the  date  the  NDA  is  submitted  to  the  FDA  because  the  FDA  has  approximately  two  months  to  make  a  “filing”
decision.

In addition, under the Pediatric Research Equity Act, certain NDAs or supplements to an NDA must contain data that are
adequate  to  assess  the  safety  and  effectiveness  of  the  drug  for  the  claimed  indications  in  all  relevant  pediatric
subpopulations, and to support dosing and administration for each pediatric subpopulation for which the product is safe and
effective. The FDA may, on its own initiative or at the request of the applicant, grant deferrals for submission of some or
all  pediatric  data  until  after  approval  of  the  product  for  use  in  adults,  or  full  or  partial  waivers  from  the  pediatric  data
requirements.  Unless  otherwise  required  by  regulation,  the  pediatric  data  requirements  do  not  apply  to  products  with
orphan designation.

The  FDA  also  may  require  submission  of  a  risk  evaluation  and  mitigation  strategy,  or  REMS,  plan  to  ensure  that  the
benefits of the drug outweigh its risks. The REMS plan could include medication guides, physician communication plans,
assessment plans, and/or elements to assure safe use, such as restricted distribution methods, patient registries or other risk
minimization tools.

The FDA conducts a preliminary review of all NDAs within the first 60 days after submission, before accepting them for
filing, to determine whether they are sufficiently complete to permit substantive review. The FDA may request additional
information  rather  than  accept  an  NDA  for  filing.  In  this  event,  the  application  must  be  resubmitted  with  the  additional
information. The resubmitted application is also subject to review before the FDA accepts it for filing. Once the submission
is  accepted  for  filing,  the  FDA  begins  an  in-depth  substantive  review.  The  FDA  reviews  an  NDA  to  determine,  among
other  things,  whether  the  drug  is  safe  and  effective  and  whether  the  facility  in  which  it  is  manufactured,  processed,
packaged or held meets standards designed to assure the product’s continued safety, quality and purity.

The  FDA  may  refer  an  application  for  a  novel  drug  to  an  advisory  committee.  An  advisory  committee  is  a  panel  of
independent  experts,  including  clinicians  and  other  scientific  experts,  that  reviews,  evaluates  and  provides  a
recommendation as to whether the application should be approved and under what conditions. The FDA is not bound by
the recommendations of an advisory committee, but it considers such recommendations carefully when making decisions.

Before approving an NDA, the FDA typically will inspect the facility or facilities where the product is manufactured. The
FDA will not approve an application unless it determines that the manufacturing processes and facilities are in compliance
with  cGMP  requirements  and  adequate  to  assure  consistent  production  of  the  product  within  required  specifications.
Additionally, before approving an NDA, the FDA will typically inspect one or more clinical trial sites to assure compliance
with GCP requirements.

The  testing  and  approval  process  for  an  NDA  requires  substantial  time,  effort  and  financial  resources,  and  takes  several
years to complete. Data obtained from preclinical and clinical testing are not always conclusive and may be susceptible to
varying interpretations, which could delay, limit or prevent regulatory approval. The FDA may not grant approval of an
NDA on a timely basis, or at all.

After  evaluating  the  NDA  and  all  related  information,  including  the  advisory  committee  recommendation,  if  any,  and
inspection reports regarding the manufacturing facilities and clinical trial sites, the FDA may issue an approval letter, or, in
some cases, a complete response letter. A complete response letter generally contains a statement of specific conditions that
must be met in order to secure final approval of the NDA and may require additional clinical or preclinical testing in

35

Table of Contents

order for FDA to reconsider the application. Even with submission of this additional information, the FDA ultimately may
decide that the application does not satisfy the regulatory criteria for approval. If and when those conditions have been met
to  the  FDA’s  satisfaction,  the  FDA  will  typically  issue  an  approval  letter.  An  approval  letter  authorizes  commercial
marketing of the drug with specific prescribing information for specific indications.

Even  if  the  FDA  approves  a  product,  it  may  limit  the  approved  indications  for  use  of  the  product,  require  that
contraindications, warnings or precautions be included in the product labeling, require that post-approval studies, including
Phase  4  clinical  trials,  be  conducted  to  further  assess  a  drug’s  safety  after  approval,  require  testing  and  surveillance
programs  to  monitor  the  product  after  commercialization,  or  impose  other  conditions,  including  distribution  and  use
restrictions  or  other  risk  management  mechanisms  under  a  REMS,  which  can  materially  affect  the  potential  market  and
profitability  of  the  product.  The  FDA  may  prevent  or  limit  further  marketing  of  a  product  based  on  the  results  of  post-
marketing studies or surveillance programs. After approval, some types of changes to the approved product, such as adding
new  indications,  manufacturing  changes,  and  additional  labeling  claims,  are  subject  to  further  testing  requirements  and
FDA review and approval.

Special FDA Expedited Review and Approval Programs

The FDA has various programs, including fast track designation, accelerated approval, priority review, and breakthrough
therapy designation, which are intended to expedite or simplify the process for the development and FDA review of drugs
that  are  intended  for  the  treatment  of  serious  or  life  threatening  diseases  or  conditions  and  demonstrate  the  potential  to
address  unmet  medical  needs.  The  purpose  of  these  programs  is  to  provide  important  new  drugs  to  patients  earlier  than
under standard FDA review procedures.

To be eligible for a fast track designation, the FDA must determine, based on the request of a sponsor, that a product is
intended  to  treat  a  serious  or  life-threatening  disease  or  condition  and  demonstrates  the  potential  to  address  an  unmet
medical need. The FDA will determine that a product will fill an unmet medical need if it will provide a therapy where
none exists or provide a therapy that may be potentially superior to existing therapy based on efficacy or safety factors. The
FDA  may  review  sections  of  the  NDA  for  a  fast  track  product  on  a  rolling  basis  before  the  complete  application  is
submitted.  If  the  sponsor  provides  a  schedule  for  the  submission  of  the  sections  of  the  NDA,  the  FDA  agrees  to  accept
sections  of  the  NDA  and  determines  that  the  schedule  is  acceptable,  and  the  sponsor  pays  any  required  user  fees  upon
submission of the first section of the NDA.

The FDA may give a priority review designation to drugs that are designed to treat serious conditions, and if approved,
would provide a significant improvement in treatment, or provide a treatment where no adequate therapy exists. A priority
review  means  that  the  goal  for  the  FDA  to  review  an  application  is  six  months,  rather  than  the  standard  review  of  ten
months under current PDUFA guidelines. Under the current PDUFA agreement, these six and ten month review periods are
measured  from  the  “filing”  date  rather  than  the  receipt  date  for  NDAs  for  new  molecular  entities,  which  typically  adds
approximately  two  months  to  the  timeline  for  review  and  decision  from  the  date  of  submission.  Most  products  that  are
eligible for fast track designation are also likely to be considered appropriate to receive a priority review.

In  addition,  products  studied  for  their  safety  and  effectiveness  in  treating  serious  or  life-threatening  illnesses  and  that
provide  meaningful  therapeutic  benefit  over  existing  treatments  may  be  eligible  for  accelerated  approval  and  may  be
approved on the basis of adequate and well-controlled clinical trials establishing that the drug product has an effect on a
surrogate endpoint that is reasonably likely to predict clinical benefit, or on a clinical endpoint that can be measured earlier
than irreversible morbidity or mortality, that is reasonably likely to predict an effect on irreversible morbidity or mortality
or other clinical benefit, taking into account the severity, rarity or prevalence of the condition and the availability or lack of
alternative treatments. As a condition of approval, the FDA may require a sponsor of a drug receiving accelerated approval
to perform post-marketing studies to verify and describe the predicted effect on irreversible morbidity or mortality or other
clinical endpoint, and the drug may be subject to accelerated withdrawal procedures.

Breakthrough therapy designation is for a drug that is intended, alone or in combination with one or more other drugs, to
treat a serious or life-threatening disease or condition, and preliminary clinical evidence indicates that the drug may

36

Table of Contents

demonstrate  substantial  improvement  over  existing  therapies  on  one  or  more  clinically  significant  endpoints,  such  as
substantial treatment effects observed early in clinical development. The FDA must take certain actions, such as holding
timely meetings and providing advice, intended to expedite the development and review of an application for approval of a
breakthrough therapy.

Even if a product qualifies for one or more of these programs, the FDA may later decide that the product no longer meets
the conditions for qualification or decide that the time period for FDA review or approval will not be shortened. We may
explore some of these opportunities for our product candidates as appropriate.

Rare  pediatric  disease  designation  by  the  FDA  enables  priority  review  voucher,  or  PRV,  eligibility  upon  U.S.  market
approval of a designated drug for rare pediatric diseases. The RPD-PRV program is intended to encourage development of
therapies to prevent and treat rare pediatric diseases. The voucher, which is awarded upon NDA or BLA approval to the
sponsor of a designated RPD can be sold or transferred to another entity and used by the holder to receive priority review
for  a  future  NDA  or  BLA  submission,  which  reduces  the  FDA  review  time  of  such  future  submission  from  ten  to  six
months.

Post Approval Requirements

Drugs  manufactured  or  distributed  pursuant  to  FDA  approvals  are  subject  to  pervasive  and  continuing  regulation  by  the
FDA,  including,  among  other  things,  requirements  relating  to  recordkeeping,  periodic  reporting,  product  sampling  and
distribution,  advertising  and  promotion  and  reporting  of  adverse  experiences  with  the  product.  After  approval,  most
changes  to  the  approved  product,  such  as  adding  new  indications,  manufacturing  changes  or  other  labeling  claims,  are
subject  to  further  testing  requirements  and  prior  FDA  review  and  approval.  There  also  are  continuing  annual  user  fee
requirements  for  any  marketed  products  and  the  establishments  at  which  such  products  are  manufactured,  as  well  as
application fees for supplemental applications with clinical data.

Even  if  the  FDA  approves  a  product,  it  may  limit  the  approved  indications  for  use  of  the  product,  require  that
contraindications,  warnings  or  precautions  be  included  in  the  product  labeling,  including  a  boxed  warning,  require  that
post-approval studies, including Phase 4 clinical trials, be conducted to further assess a drug’s safety after approval, require
testing  and  surveillance  programs  to  monitor  the  product  after  commercialization,  or  impose  other  conditions,  including
distribution  restrictions  or  other  risk  management  mechanisms  under  a  REMS,  which  can  materially  affect  the  potential
market and profitability of the product. The FDA may prevent or limit further marketing of a product based on the results
of post-marketing studies or surveillance programs.

In  addition,  drug  manufacturers  and  other  entities  involved  in  the  manufacture  and  distribution  of  approved  drugs  are
required  to  register  their  establishments  with  the  FDA  and  state  agencies,  and  are  subject  to  periodic  unannounced
inspections by the FDA and these state agencies for compliance with cGMP requirements. Changes to the manufacturing
process  are  strictly  regulated  and  often  require  prior  FDA  approval  before  being  implemented.  FDA  regulations  also
require investigation and correction of any deviations from cGMP and impose reporting and documentation requirements
upon the sponsor and any third-party manufacturers that the sponsor may decide to use. Accordingly, manufacturers must
continue to expend time, money and effort in the area of production and quality control to maintain cGMP compliance.

Once  an  approval  is  granted,  the  FDA  may  withdraw  the  approval  if  compliance  with  regulatory  requirements  and
standards is not maintained or if problems occur after the product reaches the market.

Later  discovery  of  previously  unknown  problems  with  a  product,  including  adverse  events  of  unanticipated  severity  or
frequency, or with manufacturing processes, or failure to comply with regulatory requirements, may result in mandatory
revisions  to  the  approved  labeling  to  add  new  safety  information;  imposition  of  post-market  studies  or  clinical  trials  to
assess  new  safety  risks;  or  imposition  of  distribution  or  other  restrictions  under  a  REMS  program.  Other  potential
consequences include, among other things:

37

Table of Contents

•

•

•

•

•

restrictions on the marketing or manufacturing of the product, complete withdrawal of the product from the
market or product recalls;

fines, warning letters or holds on post-approval clinical trials;

refusal of the FDA to approve pending NDAs or supplements to approved NDAs, or suspension or revocation
of product approvals;

product seizure or detention, or refusal to permit the import or export of products; or

injunctions or the imposition of civil or criminal penalties.

The FDA strictly regulates marketing, labeling, advertising and promotion of products that are placed on the market. Drugs
may be promoted only for the approved indications and in accordance with the provisions of the approved label, although
physicians,  based  on  their  independent  medical  judgement,  may  prescribe  approved  drugs  for  unapproved  indications.
However,  biopharmaceutical  companies  may  share  truthful  and  not  misleading  information  that  is  otherwise  consistent
with the labeling. The FDA and other agencies actively enforce the laws and regulations prohibiting their promotion of off-
label  uses,  and  a  company  that  is  found  to  have  improperly  promoted  off-label  uses  may  be  subject  to  significant  civil,
criminal and administrative liability.

In addition, the distribution of prescription pharmaceutical products is subject to the Prescription Drug Marketing Act, or
PDMA, which regulates the distribution of drugs and drug samples at the federal level, and sets minimum standards for the
registration  and  regulation  of  drug  distributors  by  the  states.  Both  the  PDMA  and  state  laws  limit  the  distribution  of
prescription pharmaceutical product samples and impose requirements to ensure accountability in distribution.

Federal and State Fraud and Abuse, Data Privacy and Security, and Transparency Laws and Regulations

In addition to FDA restrictions on marketing of pharmaceutical products, federal and state healthcare laws and regulations
restrict business practices in the biopharmaceutical industry. These laws may impact, among other things, our current and
future business operations, including our clinical research activities, and proposed sales, marketing and education programs
and constrain the business or financial arrangements and relationships with healthcare providers and other parties through
which  we  market,  sell  and  distribute  our  products  for  which  we  obtain  marketing  approval.  These  laws  include  anti-
kickback  and  false  claims  laws  and  regulations,  data  privacy  and  security,  and  transparency  laws  and  regulations,
including, without limitation, those laws described below.

The  federal  Anti-Kickback  Statute  prohibits  any  person  or  entity  from,  among  other  things,  knowingly  and  willfully
offering, paying, soliciting or receiving remuneration to induce or in return for purchasing, leasing, ordering or arranging
for or recommending the purchase, lease or order of any item or service reimbursable under Medicare, Medicaid or other
federal  healthcare  programs.  The  term  “remuneration”  has  been  broadly  interpreted  to  include  anything  of  value.  The
federal Anti-Kickback Statute has been interpreted to apply to arrangements between pharmaceutical manufacturers on the
one  hand  and  prescribers,  purchasers  and  formulary  managers  on  the  other.  Although  there  are  a  number  of  statutory
exceptions  and  regulatory  safe  harbors  protecting  some  common  activities  from  prosecution,  the  exceptions  and  safe
harbors are drawn narrowly. Practices that involve remuneration that may be alleged to be intended to induce prescribing,
purchases or recommendations may be subject to scrutiny if they do not qualify for an exception or safe harbor. Several
courts  have  interpreted  the  statute’s  intent  requirement  to  mean  that  if  any  one  purpose  of  an  arrangement  involving
remuneration is to induce referrals of federal healthcare covered business, the statute has been violated.

A person or entity does not need to have actual knowledge of this statute or specific intent to violate it in order to have
committed  a  violation.  In  addition,  the  government  may  assert  that  a  claim  including  items  or  services  resulting  from  a
violation of the federal Anti-Kickback Statute constitutes a false or fraudulent claim for purposes of the federal civil False
Claims Act or the civil monetary penalties laws.

38

Table of Contents

Federal  civil  and  criminal  false  claims  laws,  including  the  federal  civil  False  Claims  Act,  which  can  be  enforced  by
individuals  through  civil  whistleblower  and  qui  tam  actions,  and  civil  monetary  penalties  laws,  prohibits  any  person  or
entity from, among other things, knowingly presenting, or causing to be presented, a false claim for payment to the federal
government or knowingly making, using or causing to be made or used a false record or statement material to a false or
fraudulent claim to the federal government. A claim includes “any request or demand” for money or property presented to
the U.S. government. Several pharmaceutical and other healthcare companies have been prosecuted under these laws for
allegedly providing free product to customers with the expectation that the customers would bill federal programs for the
product.  Other  companies  have  been  prosecuted  for  causing  false  claims  to  be  submitted  because  of  the  companies’
marketing of products for unapproved, and thus non-reimbursable, uses.

The  federal  Health  Insurance  Portability  and  Accountability  Act  of  1996,  or  HIPAA,  created  additional  federal  criminal
statutes that prohibit, among other things, knowingly and willfully executing a scheme to defraud any healthcare benefit
program, including private third-party payors and knowingly and willfully falsifying, concealing or covering up a material
fact  or  making  any  materially  false,  fictitious  or  fraudulent  statement  in  connection  with  the  delivery  of  or  payment  for
healthcare benefits, items or services. Also, many states have similar fraud and abuse statutes or regulations that apply to
items and services reimbursed under Medicaid and other state programs, or, in several states, apply regardless of the payor.

In  addition,  we  may  be  subject  to  data  privacy  and  security  regulation  by  both  the  federal  government  and  the  states  in
which  we  conduct  our  business.  HIPAA,  as  amended  by  the  Health  Information  Technology  for  Economic  and  Clinical
Health Act, or HITECH, and their respective implementing regulations, impose specified requirements on certain types of
individuals  and  entities  relating  to  the  privacy,  security  and  transmission  of  individually  identifiable  health  information.
Among other things, HITECH makes HIPAA’s security standards directly applicable to “business associates,” defined as
independent contractors or agents of covered entities, which include certain healthcare providers, healthcare clearinghouse
and health plans, that create, receive, maintain or transmit individually identifiable health information in connection with
providing a service for or on behalf of a covered entity, and their covered subcontractors. HITECH also increased the civil
and criminal penalties that may be imposed against covered entities, business associates and possibly other persons, and
gave  state  attorneys  general  new  authority  to  file  civil  actions  for  damages  or  injunctions  in  federal  courts  to  enforce
HIPAA and seek attorney’s fees and costs associated with pursuing federal civil actions. In addition, state laws govern the
privacy and security of health information in certain circumstances, many of which are not pre-empted by HIPAA, differ
from each other in significant ways and may not have the same effect, thus complicating compliance efforts.

The  federal  Physician  Payments  Sunshine  Act  requires  certain  manufacturers  of  drugs,  devices,  biologics  and  medical
supplies  for  which  payment  is  available  under  Medicare,  Medicaid  or  the  Children’s  Health  Insurance  Program,  with
specific exceptions, to report annually to the Centers for Medicare & Medicaid Services, or CMS, information related to
payments or other transfers of value made to physicians (defined to include doctors, dentists, optometrists, podiatrists and
chiropractors), other healthcare professionals (such as physician assistants and nurse practitioners), and teaching hospitals,
and  applicable  manufacturers  and  applicable  group  purchasing  organizations  to  report  annually  to  CMS  ownership  and
investment interests held by physicians and their immediate family members.

We may also be subject to state laws that require pharmaceutical companies to comply with the pharmaceutical industry’s
voluntary compliance guidelines and the relevant compliance guidance promulgated by the federal government, state laws
that  require  drug  manufacturers  to  report  information  related  to  payments  and  other  transfers  of  value  to  physicians  and
other healthcare providers or marketing expenditures, state laws that require drug manufacturers to report information on
the pricing of certain drugs, and state and local laws that require the registration of pharmaceutical sales representatives.

Because of the breadth of these laws and the narrowness of available statutory exceptions and regulatory safe harbors, it is
possible that some of our business activities could be subject to challenge under one or more of such laws. If our operations
are found to be in violation of any of the federal and state laws described above or any other governmental regulations that
apply  to  us,  we  may  be  subject  to  significant  criminal,  civil  and  administrative  penalties  including  damages,  fines,
imprisonment, additional reporting requirements and oversight if we become subject to a corporate integrity agreement or
similar  agreement  to  resolve  allegations  of  non-compliance  with  these  laws,  contractual  damages,  reputational  harm,
diminished profits and future earnings, disgorgement, exclusion from participation in government healthcare programs and
the curtailment or restructuring of our operations, any of which could adversely affect our ability

39

Table of Contents

to operate our business and our results of operations. To the extent that any of our products are sold in a foreign country, we
may  be  subject  to  similar  foreign  laws  and  regulations,  which  may  include,  for  instance,  applicable  post-marketing
requirements, including safety surveillance, anti-fraud and abuse laws, implementation of corporate compliance programs,
reporting  of  payments  or  transfers  of  value  to  healthcare  professionals,  and  additional  data  privacy  and  security
requirements.

Coverage and Reimbursement

The future commercial success of our, or any of our collaborators’, product candidates, if approved, will depend in part on
the  extent  to  which  third-party  payors,  such  as  governmental  payor  programs  at  the  federal  and  state  levels,  including
Medicare and Medicaid, private health insurers and other third-party payors, provide coverage of and establish adequate
reimbursement levels for our product candidates. Third-party payors generally decide which products they will pay for and
establish reimbursement levels for those products. In particular, in the United States, no uniform policy for coverage and
reimbursement exists. Private health insurers and other third-party payors often provide coverage and reimbursement for
products  based  on  the  level  at  which  the  government,  through  the  Medicare  program,  provides  coverage  and
reimbursement  for  such  products,  but  also  have  their  own  methods  and  approval  process  apart  from  Medicare
determinations. Therefore, coverage and reimbursement can differ significantly from payor to payor.

In  the  United  States,  the  European  Union,  or  EU,  and  other  potentially  significant  markets  for  our  product  candidates,
government  authorities  and  third-party  payors  are  increasingly  attempting  to  limit  or  regulate  the  price  of  products,
particularly  for  new  and  innovative  products,  which  often  has  resulted  in  average  selling  prices  lower  than  they  would
otherwise  be.  Further,  the  increased  emphasis  on  managed  healthcare  in  the  United  States  and  on  country  and  regional
pricing and reimbursement controls in the EU will put additional pressure on product pricing, reimbursement and usage.
These  pressures  can  arise  from  rules  and  practices  of  managed  care  groups,  judicial  decisions  and  laws  and  regulations
related to Medicare, Medicaid and healthcare reform, pharmaceutical coverage and reimbursement policies and pricing in
general.

Third-party  payors  are  increasingly  imposing  additional  requirements  and  restrictions  on  coverage  and  limiting
reimbursement  levels  for  products.  For  example,  federal  and  state  governments  reimburse  products  at  varying  rates
generally below average wholesale price. These restrictions and limitations influence the purchase of products. Third-party
payors may limit coverage to specific products on an approved list, or formulary, which might not include all of the FDA-
approved products for a particular indication. Third-party payors are increasingly challenging the price and examining the
medical  necessity  and  cost-effectiveness  of  products,  in  addition  to  their  safety  and  efficacy.  We  may  need  to  conduct
expensive pharmacoeconomic studies in order to demonstrate the medical necessity and cost-effectiveness of our product
candidates, in addition to the costs required to obtain the FDA approvals. Our product candidates may not be considered
medically necessary or cost-effective. A payor’s decision to provide coverage for a product does not imply that an adequate
reimbursement  rate  will  be  approved.  Adequate  third-party  payor  reimbursement  may  not  be  available  to  enable  us  to
realize  an  appropriate  return  on  our  investment  in  product  development.  Legislative  proposals  to  reform  healthcare  or
reduce  costs  under  government  insurance  programs  may  result  in  lower  reimbursement  for  our  product  candidates,  if
approved, or exclusion of our product candidates from coverage and reimbursement. The cost containment measures that
third-party payors and providers are instituting and any healthcare reform could significantly reduce our revenues from the
sale of any approved product candidates.

Healthcare Reform

The  United  States  and  some  foreign  jurisdictions  are  considering  enacting  or  have  enacted  a  number  of  additional
legislative and regulatory proposals to change the healthcare system in ways that could affect our ability to sell our product
candidates profitably, if approved. Among policy makers and payors in the United States and elsewhere, there is significant
interest in promoting changes in healthcare systems with the stated goals of containing healthcare costs, improving quality
and expanding access. In the United States, the pharmaceutical industry has been a particular focus of these efforts, which
include major legislative initiatives to reduce the cost of care through changes in the healthcare system, including limits on
the pricing, coverage, and reimbursement of pharmaceutical and biopharmaceutical products, especially under government-
funded health care programs, and increased governmental control of drug pricing.

40

Table of Contents

There have been several U.S. government initiatives over the past few years to fund and incentivize certain comparative
effectiveness research, including creation of the Patient-Centered Outcomes Research Institute under the Patient Protection
and  Affordable  Care  Act  of  2010,  as  amended  by  the  Health  Care  and  Education  Reconciliation  Act  of  2010,  or
collectively the PPACA. It is also possible that comparative effectiveness research demonstrating benefits in a competitor’s
product could adversely affect the sales of our product candidates.

The  PPACA  became  law  in  March  2010  and  substantially  changed  the  way  healthcare  is  financed  by  both  third-party
payors. Among other measures that may have an impact on our business, the PPACA establishes an annual, nondeductible
fee on any entity that manufactures or imports specified branded prescription drugs and biologic agents; a new Medicare
Part D coverage gap discount program; and a new formula that increases the rebates a manufacturer must pay under the
Medicaid  Drug  Rebate  Program.  Additionally,  the  PPACA  extends  manufacturers’  Medicaid  rebate  liability,  expands
eligibility criteria for Medicaid programs, and expands entities eligible for discounts under the Public Health Service Act.
At this time, we are unsure of the full impact that the PPACA will have on our business.

There have been executive, judicial and Congressional challenges to certain aspects of the PPACA. While Congress has not
passed comprehensive repeal legislation, several bills affecting the implementation of certain taxes under the PPACA have
been  signed  into  law.  The  Tax  Cuts  and  Jobs  Act  of  2017,  or  Tax  Act,  included  a  provision  that  repealed,  effective
January  1,  2019,  the  tax-based  shared  responsibility  payment  imposed  by  the  PPACA  on  certain  individuals  who  fail  to
maintain qualifying health coverage for all or part of a year that is commonly referred to as the “individual mandate.” In
addition,  the  2020  federal  spending  package  permanently  eliminated,  effective  January  1,  2020,  the  PPACA-mandated
“Cadillac”  tax  on  high-cost  employer-sponsored  health  coverage  and  medical  device  tax  and,  effective  January  1,  2021,
also eliminated the health insurer tax. The Bipartisan Budget Act of 2018, or the BBA, among other things, amended the
PPACA, effective January 1, 2019, to increase from 50% to 70% the point-of-sale discount that is owed by pharmaceutical
manufacturers who participate in Medicare Part D and to close the coverage gap in most Medicare drug plans, commonly
referred to as the “donut hole.” On June 17, 2021 the U.S. Supreme Court dismissed a challenge on procedural grounds that
argued the PPACA is unconstitutional in its entirety because the “individual mandate” was repealed by Congress. Thus, the
PPACA will remain in effect in its current form. Prior to the U.S. Supreme Court ruling, on January 28, 2021, President
Biden  issued  an  executive  order  that  initiated  a  special  enrollment  period  for  purposes  of  obtaining  health  insurance
coverage  through  the  PPACA  marketplace.  The  executive  order  also  instructed  certain  governmental  agencies  to  review
and  reconsider  their  existing  policies  and  rules  that  limit  access  to  healthcare,  including  among  others,  reexamining
Medicaid demonstration projects and waiver programs that include work requirements, and policies that create unnecessary
barriers to obtaining access to health insurance coverage through Medicaid or the PPACA. It is possible that the PPACA
will be subject to judicial or Congressional challenges in the future. It is unclear how such challenges and the healthcare
reform measures of the Biden administration will impact the PPACA.

In addition, other legislative changes have been proposed and adopted since the PPACA was enacted. In August 2011, the
President  signed  into  law  the  Budget  Control  Act  of  2011,  as  amended,  which,  among  other  things,  included  aggregate
reductions  to  Medicare  payments  to  providers  of  2%  per  fiscal  year,  which  began  in  2013  and,  following  passage  of
subsequent legislation, including the BBA and the Infrastructure Investment and Jobs Act, will continue through 2031 with
the  exception  of  a  temporary  suspension  from  May  1,  2020  through  March  31,  2022  due  to  the  COVID-19  pandemic,
unless additional Congressional action is taken. Under current legislation, the actual reduction in Medicare payments will
vary  from  1%  in  2022  to  up  to  3%  in  the  final  fiscal  year  of  this  sequester.  Additionally,  on  March  11,  2021,  President
Biden signed the American Rescue Plan Act of 2021 into law, which eliminates the statutory Medicaid drug rebate cap,
currently  set  at  100%  of  a  drug’s  average  manufacturer  price,  for  single  source  and  innovator  multiple  source  drugs,
beginning  January  1,  2024.  In  January  2013,  the  American  Taxpayer  Relief  Act  of  2012  was  enacted  and,  among  other
things, reduced Medicare payments to several providers and increased the statute of limitations period for the government
to recover overpayments to providers from three to five years.

Further,  there  has  been  increasing  legislative  and  enforcement  interest  in  the  United  States  with  respect  to  drug  pricing
practices. Specifically, there have been several recent U.S. Congressional inquiries and proposed and enacted federal and
state legislation designed to, among other things, bring more transparency to drug pricing, review the relationship between
pricing and manufacturer patient programs, and reform government program reimbursement methodologies for drugs. At
the federal level, the Trump administration used several means to propose or implement drug pricing reform, including

41

Table of Contents

through federal budget proposals, executive orders and policy initiatives. For example, on July 24, 2020 and September 13,
2020, the Trump administration announced several executive orders related to prescription drug pricing that attempted to
implement several of the administration’s proposals. As a result, the FDA concurrently released a final rule and guidance in
September  2020  implementing  a  portion  of  the  importation  executive  order  providing  pathways  for  states  to  build  and
submit  importation  plans  for  drugs  from  Canada.  Further,  on  November  20,  2020,  the  U.S.  Department  of  Health  and
Human Services, or HHS, finalized a regulation removing safe harbor protection for price reductions from pharmaceutical
manufacturers  to  plan  sponsors  under  Part  D,  either  directly  or  through  pharmacy  benefit  managers,  unless  the  price
reduction is required by law. The rule also creates a new safe harbor for price reductions reflected at the point-of-sale, as
well as a new safe harbor for certain fixed fee arrangements between pharmacy benefit managers and manufacturers. The
implementation of the rule has been delayed until January 1, 2026. On November 20, 2020, CMS issued an interim final
rule  implementing  the  Trump  administration’s  Most  Favored  Nation  executive  order,  which  would  tie  Medicare  Part  B
payments  for  certain  physician-administered  drugs  to  the  lowest  price  paid  in  other  economically  advanced  countries,
effective  January  1,  2021.  As  a  result  of  litigation  challenging  the  Most  Favored  Nation  model,  on  December  27,  2021,
CMS  published  a  final  rule  that  rescinded  the  Most  Favored  Nation  model  interim  final  rule.  In  July  2021,  the  Biden
administration released an executive order, “Promoting Competition in the American Economy,” with multiple provisions
aimed at prescription drugs. In response to Biden’s executive order, on September 9, 2021, HHS released a Comprehensive
Plan for Addressing High Drug Prices that outlines principles for drug pricing reform and sets out a variety of potential
legislative policies that Congress could pursue as well as potential administrative actions HHS can take to advance these
principles. No legislation or administrative actions have been finalized to implement these principles. In addition, Congress
is considering drug pricing as part of other reform initiatives. It is unclear whether these or  similar policy initiatives will be
implemented in the future.  At the state level, legislatures have increasingly passed legislation and implemented regulations
designed  to  control  pharmaceutical  and  biological  product  pricing,  including  price  or  patient  reimbursement  constraints,
discounts,  restrictions  on  certain  product  access  and  marketing  cost  disclosure  and  transparency  measures,  and,  in  some
cases, designed to encourage importation from other countries and bulk purchasing. It is also possible that governmental
action will be taken in response to the COVID-19 pandemic.

Foreign Regulation

In  order  to  market  any  product  outside  of  the  United  States,  we  would  need  to  comply  with  numerous  and  varying
regulatory requirements of other countries regarding safety and efficacy and governing, among other things, clinical trials,
marketing  authorization,  commercial  sales  and  distribution  of  our  product  candidates.  For  example,  in  the  EU,  we  must
obtain authorization of a clinical trial application, or CTA, in each member state in which we intend to conduct a clinical
trial.  Whether  or  not  we  obtain  FDA  approval  for  a  drug,  we  would  need  to  obtain  the  necessary  approvals  by  the
comparable regulatory authorities of foreign countries before we can commence clinical trials or marketing of the drug in
those  countries.  The  approval  process  varies  from  country  to  country  and  can  involve  additional  product  testing  and
additional administrative review periods. The time required to obtain approval in other countries might differ from and be
longer than that required to obtain FDA approval. Regulatory approval in one country does not ensure regulatory approval
in  another,  but  a  failure  or  delay  in  obtaining  regulatory  approval  in  one  country  may  negatively  impact  the  regulatory
process in others.

Employees and Human Capital

Patients inspire all we do. Milestone employees are passionate about creating a solution for patients who suffer from PSVT
and other related illness as we work together on our mission to develop innovative cardiovascular medicines. We have built
a culture of high performance based on our core values:

◾ Patients First: Everything we do is with the patient in mind. We listen to and partner with patients and place their

well-being at the core of all our initiatives.
Our patients inspire us.

◾ Teamwork: Milestone employees support, challenge and care for each other.

Employees  engage  with  one  another  through  their  teams,  but  also  through  our  weekly  gatherings,  outings  and

friendly competitions and challenges.

42

Table of Contents

Collaboration is key.

◾ Entrepreneurial Mindset:  Milestone places a high value on grit, courage and resolve. Milestone’s organizational

energy has the sense of a startup.
Employees are encouraged to think like an owner.

◾ Every Idea Matters: Sometimes the best ideas evolve from where it is least expected.

All ideas are welcome.

◾ Humility, Empathy and Integrity: We act individually and as a team with these three attributes in mind in all we

do.
We care to do what is right.

Our  human  capital  objectives  include,  as  applicable,  identifying,  recruiting,  retaining,  incentivizing  and  integrating  our
existing and additional employees. The principal purposes of our equity incentive plans are to attract, retain and motivate
selected employees, consultants and directors through the granting of stock-based compensation awards.

As  of  December  31,  2021,  we  had  29  full-time  employees,  15  of  whom  were  primarily  engaged  in  research  and
development activities. Seven of these employees have an M.D. or Ph.D. degree. None of our employees is represented by
a labor union and we consider our employee relations to be excellent.

Facilities

Our headquarters is currently located in Montréal (Québec), Canada and consists of 7,700 square feet of leased office space
under  a  lease  that  expires  in  November  2025  with  an  option  to  terminate  in  November  2023.  We  also  have  a  U.S.
subsidiary in Charlotte, North Carolina that occupies 5,116 square feet of leased office space under a lease that expires in
July 2022. We  plan to expand the office space in Charlotte, NC to meet the future needs of our growing U.S. subsidiary for
preparation of commercialization.

Legal Proceedings

From time to time, we may become involved in legal proceedings arising in the ordinary course of our business. We are not
currently a party to any material legal proceedings, and we are not aware of any pending or threatened legal proceeding
against us that we believe could have an adverse effect on our business, operating results or financial condition.

Corporate Information

Our  principal  executive  offices  are  located  at  1111  Dr.  Frederik-Philips  Blvd.,  Suite  420,  Montréal,  Québec,  Canada
H4M 2X6, and our telephone number is (514) 336-0444. Our US offices are located at 7422 Carmel Executive Park Drive,
Suite 300 Charlotte, NC 28226 and our telephone number is (704) 848-5316.

Available Information

We maintain an internet website at www.milestonepharma.com and make available free of charge through our website our
Annual Reports on Form 10-K, Quarterly Reports on Form 10-Q, Current Reports on Form 8-K and amendments to those
reports  filed  or  furnished  pursuant  to  Sections  13(a)  and  15(d)  of  the  Exchange  Act  of  1934  (the  “Exchange  Act”).  We
make these reports available through our website as soon as reasonably practicable after we electronically file such reports
with, or furnish such reports to, the Securities and Exchange Commission (the “SEC”). You can review our electronically
filed reports and other information that we file with the SEC on the SEC’s web site at http://www.sec.gov. We also make
available,  free  of  charge  on  our  website,  the  reports  filed  with  the  SEC  by  our  executive  officers,  directors  and  10%
stockholders pursuant to Section 16 under the Exchange Act as soon as reasonably practicable after copies of those filings
are provided to us by those persons. In addition, we regularly use our website to post information regarding our business,

43

Table of Contents

product  development  programs  and  governance,  and  we  encourage  investors  to  use  our  website,  particularly  the
information in the section entitled “Investors,” as a source of information about us.

The information on our website is not incorporated by reference into this Annual Report on Form 10-K and should not be
considered  to  be  a  part  of  this  Annual  Report  on  Form  10-K.  Our  website  address  is  included  in  this  Annual  Report  on
Form 10-K as an inactive technical reference only.

Investors  and  others  should  note  that  we  announce  material  information  to  our  investors  using  one  or  more  of  the
following: SEC filings, press releases and our corporate website, including without limitation the “Investors” and “Events
and Presentations” sections of our website. We use these channels, as well as social media channels such as LinkedIn, in
order to achieve broad, non-exclusionary distribution of information to the public and for complying with our disclosure
obligations under Regulation FD. It is possible that the information we post on our corporate website or other social media
could  be  deemed  to  be  material  information.  Therefore,  we  encourage  investors,  the  media,  and  others  interested  in  our
company to review the information we post on the “Investors” and “Events and Presentations” sections of our corporate
website  and  on  our  social  media  channels.  The  contents  of  our  corporate  website  and  social  media  channels  are  not,
however, a part of this Annual Report. 

44

Table of Contents

ITEM 1A.     RISK FACTORS

An investment in shares of our common shares involves a high degree of risk. You should carefully consider the following
information about these risks, together with the other information appearing elsewhere in this Annual Report on Form 10-
K, consolidated financial statements and related notes thereto and “Management’s Discussion and Analysis of Financial
Condition  and  Results  of  Operations,”  before  deciding  to  invest  in  our  common  shares.  The  occurrence  of  any  of  the
following risks could have a material adverse effect on our business, financial condition, results of operations and future
growth prospects or cause our actual results to differ materially from those contained in forward-looking statements we
have made in this report and those we may make from time to time. In these circumstances, the market price of our common
shares  could  decline,  and  you  may  lose  all  or  part  of  your  investment.  We  cannot  assure  you  that  any  of  the  events
discussed below will not occur. Such risks may be amplified by the ongoing COVID-19 pandemic and its potential impact
on our business and the global economy.

Risks Related to Our Financial Position and Capital Needs

We have incurred significant operating losses since inception and anticipate that we will continue to incur substantial
operating losses for the foreseeable future and may never achieve or maintain profitability.

Since inception in 2003, we have incurred significant operating losses. Our net loss was $42.9 million and $50.0 million
for the years ended December 31, 2021 and 2020, respectively. As of December 31, 2021, we had an accumulated deficit of
$206.3  million  We  expect  to  continue  to  incur  significant  expenses  and  increasing  operating  losses  for  the  foreseeable
future. Since inception, we have devoted substantially all of our efforts to research and preclinical and clinical development
of etripamil, as well as to expanding our management team and infrastructure. It could be several years, if ever, before we
have a commercialized drug. The ongoing COVID-19 pandemic has had an impact on our business, operations and clinical
development  timelines.  Government  orders  and  restrictions  in  order  to  control  the  spread  of  the  disease  have  impacted
patient recruitment, enrollment and follow-up visits at clinical sites. At the date of the publication of this annual report, it is
not possible to reliably estimate the length and severity of these developments. We expect that our existing cash and cash
equivalents to be sufficient to fund our operations under our current operating plan.

The net losses we incur may fluctuate significantly from quarter to quarter and year to year. We anticipate that our expenses
will increase substantially if, and as, we:

•

•

•

•

•

continue our ongoing and planned development of etripamil, including our Phase 3 clinical trials of etripamil
for the treatment of paroxysmal supraventricular tachycardia, or PSVT, and our ongoing Phase 2 clinical trial
of etripamil for the treatment of atrial fibrillation and rapid ventricular rate, or AFib-RVR;

seek  marketing  approvals  for  etripamil  for  the  treatment  of  PSVT  and  other  cardiovascular  indications  and
any future product candidates that successfully complete clinical trials;

establish a sales, marketing, manufacturing and distribution capability, either directly or indirectly with third
parties,  to  commercialize  etripamil  or  any  future  product  candidate  for  which  we  may  obtain  marketing
approval;

build a portfolio of product candidates through development, or the acquisition or in-license of drugs, product
candidates or technologies;

initiate preclinical studies and clinical trials for etripamil for any additional indications we may pursue, and
for any additional product candidates that we may pursue in the future;

• maintain, protect and expand our intellectual property portfolio;

•

hire additional clinical, regulatory and scientific personnel;

45

Table of Contents

•

•

add  operational,  financial  and  management  information  systems  and  personnel,  including  personnel  to
support our product development and planned future commercialization efforts; and

incur additional legal, insurance related, accounting and other expenses associated with operating as a public
company.

To  become  and  remain  profitable,  we  must  succeed  in  developing  and  eventually  commercializing  drugs  that  generate
significant revenue. This will require us to be successful in a range of challenging activities, including completing clinical
trials  of  etripamil  and  any  future  product  candidates  that  way  may  pursue,  obtaining  regulatory  approval,  procuring
commercial-scale  manufacturing,  marketing  and  selling  etripamil  and  any  future  products  for  which  we  may  obtain
regulatory approval, as well as discovering or acquiring and then developing additional product candidates. We are only in
the preliminary stages of some of these activities, and we have recently encountered setbacks in our clinical development
program for etripamil, as our NODE-301 trial did not meet its primary endpoint. We may never succeed in these activities
and, even if we do, may never generate revenues that are significant enough to achieve profitability.

Because of the numerous risks and uncertainties associated with drug development, we are unable to accurately predict the
timing or amount of expenses or when, or if, we will be able to achieve profitability.

Our  expenses  could  increase  beyond  our  expectations  if  we  are  required  by  the  U.S.  Food  and  Drug  Administration,  or
FDA, the European Medicines Agency or other regulatory authorities to perform studies in addition to those we currently
expect, or if there are any delays in the initiation and completion of our clinical trials or the development of etripamil or
any future product candidates.

Even if we do achieve profitability, we may not be able to sustain or increase profitability on a quarterly or annual basis.
Our failure to become and remain profitable would decrease the value of our company and could impair our ability to raise
capital, maintain our research and development efforts, expand our business or continue our operations. A decline in the
value of our common shares could also cause you to lose all or part of your investment.

Our limited operating history may make it difficult for you to evaluate the success of our business to date and to assess
our future viability.

We are a clinical-stage company founded in 2003, and our operations to date have been largely focused on raising capital,
organizing,  staffing  our  company  and  undertaking  preclinical  studies  and  conducting  clinical  trials  for  etripamil.  As  an
organization,  we  have  not  yet  demonstrated  an  ability  to  successfully  complete  clinical  development,  obtain  regulatory
approvals, manufacture a commercial-scale product or arrange for a third party to do so on our behalf, or conduct sales and
marketing activities necessary for successful commercialization. Consequently, any predictions about our future success or
viability may not be as accurate as they could be if we had a longer operating history or a history of successful clinical
development and commercialization of products.

We  may  encounter  unforeseen  expenses,  difficulties,  complications,  delays  and  other  known  or  unknown  factors  in
achieving  our  business  objectives.  We  will  need  to  transition  at  some  point  from  a  company  with  a  research  and
development  focus  to  a  company  capable  of  supporting  commercial  activities.  We  may  not  be  successful  in  such  a
transition.

Additionally, we expect our financial condition and operating results to continue to fluctuate from quarter to quarter and
year to year due to a variety of factors, many of which are beyond our control. Accordingly, you should not rely upon the
results of any quarterly or annual periods as indications of future operating performance.

46

Table of Contents

We will require substantial additional funding to finance our operations. If we are unable to raise capital when needed,
we could be forced to delay, reduce or terminate our development of etripamil or other operations.

Based on our research and development plans, we expect that our existing cash and cash equivalents will be sufficient to
fund  our  operations  for  at  least  the  next  12  months.  However,  we  will  need  to  obtain  substantial  additional  funding  in
connection  with  our  continuing  operations  and  planned  activities.  Our  future  capital  requirements  will  depend  on  many
factors, including:

•

•

•

•

•

•

•

•

•

•

the timing, progress and results of our ongoing and planned clinical trials of etripamil in PSVT, AFib-RVR
and in other cardiovascular indications;

the  scope,  progress,  results  and  costs  of  preclinical  development,  laboratory  testing  and  clinical  trials  of
etripamil for additional indications or any future product candidates that we may pursue;

our ability to establish collaborations on favorable terms, if at all;

the ability of vendors who we rely on to accurately forecast expenses and deliver on expectations;

the costs, timing and outcome of regulatory review of etripamil and any future product candidates;

the costs and timing of future commercialization activities, including product manufacturing, marketing, sales
and distribution, for etripamil and any future product candidates for which we receive marketing approval;

the revenue, if any, received from commercial sales of etripamil and any future product candidates for which
we receive marketing approval;

the costs and timing of preparing, filing and prosecuting patent applications, maintaining and enforcing our
intellectual property rights and defending any intellectual property-related claims;

the extent to which we acquire or in-license other product candidates and technologies; and

the costs of operating as a public company.

47

Table of Contents

Identifying  potential  product  candidates  and  conducting  preclinical  testing  and  clinical  trials  is  a  time-consuming,
expensive  and  uncertain  process  that  takes  years  to  complete,  and  we  may  never  generate  the  necessary  data  or  results
required  to  obtain  regulatory  approval  and  achieve  product  sales.  For  example,  we  recently  announced  that  the  pivotal
NODE-301 trial of etripamil for PSVT did not meet its primary endpoint. There can be no guarantee that the RAPID trial
or  our  clinical  trial  of  etripamil  for  AFib-RVR  will  meet  their  primary  endpoints.  In  addition,  etripamil  and  any  future
product candidates, if approved, may not achieve commercial success. Our commercial revenues, if any, will be derived
from sales of drugs that we do not expect to be commercially available for several years, if at all. Accordingly, we will
need to continue to rely on additional financing to achieve our business objectives. Adequate additional financing may not
be  available  to  us  on  acceptable  terms,  or  at  all.  In  addition,  we  may  seek  additional  capital  due  to  favorable  market
conditions or strategic considerations even if we believe we have sufficient funds for our current or future operating plans.
If  we  are  unable  to  raise  capital  when  needed  or  on  attractive  terms,  we  could  be  forced  to  delay,  reduce  or  altogether
terminate our research and development programs or future commercialization efforts.

Economic uncertainty, including related to inflation, may adversely affect our results of operations.

Our results of operations may be materially affected by global economic conditions, including inflation, which has recently
increased  at  the  fastest  pace  in  nearly  40  years,  sustained  uncertainty  regarding  future  economic  conditions,  prolonged
tightening of credit markets and changes in tax rates. In recent years, the U.S. and other significant economic markets have
experienced  cyclical  downturns,  and  worldwide  economic  conditions  remain  uncertain.  While  such  uncertainty  persists,
investor concerns over inflation, market volatility and the ongoing COVID-19 pandemic may cause deteriorating market
conditions with adverse effects on our business, financial condition and operating results.

Raising  additional  capital  may  cause  dilution  to  our  shareholders,  restrict  our  operations  or  require  us  to  relinquish
rights to our product candidates.

Until such time, if ever, as we can generate substantial product revenue, we expect to finance our cash needs through public
or  private  equity  or  debt  financings,  third-party  funding,  marketing  and  distribution  arrangements,  as  well  as  other
collaborations, strategic alliances and licensing arrangements, or any combination of these approaches. We do not have any
committed external source of funds. To the extent that we raise additional capital through the sale of equity or convertible
debt securities, your ownership interest may be diluted, and the terms of these securities may include liquidation or other
preferences  that  adversely  affect  your  rights  as  a  shareholder.  Debt  and  equity  financings,  if  available,  may  involve
agreements that include covenants limiting or restricting our ability to take specific actions, such as redeeming our shares,
making investments, incurring additional debt, making capital expenditures, declaring dividends or placing limitations on
our ability to acquire, sell or license intellectual property rights.

If  we  raise  additional  capital  through  future  collaborations,  strategic  alliances  or  third-party  licensing  arrangements,  we
may have to relinquish valuable rights to our intellectual property, future revenue streams, research programs or product
candidates, or grant licenses on terms that may not be favorable to us. If we are unable to raise additional capital when
needed, we may be required to delay, limit, reduce or terminate our drug development or future commercialization efforts,
or grant rights to develop and market product candidates that we would otherwise develop and market ourselves.

Our  ability  to  use  our  non-capital  loss  carryforwards  to  offset  future  taxable  income  may  be  subject  to  certain
limitations.

In  general,  where  control  of  a  corporation  has  been  acquired  by  a  person  or  group  of  persons,  subsection  111(5)  of  the
Income  Tax  Act  (Canada),  or  the  Canadian  Tax  Act,  and  equivalent  provincial  income  tax  legislation  restrict  the
corporation’s ability to carry forward non-capital losses from preceding taxation years. We have not performed a detailed
analysis to determine whether an acquisition of control for the purposes of subsection 111(5) of the Canadian Tax Act has
occurred  after  each  of  our  previous  issuances  of  common  shares  or  preferred  shares.  In  addition,  if  we  undergo  an
acquisition of control, our ability to utilize non-capital losses could be limited by subsection 111(5) of the Canadian Tax
Act. As of December 31, 2021, we had Canadian federal and provincial non-capital loss carry forwards of $149.0 million
and $146.7 million, respectively, which expire beginning in 2027 through 2041. In addition, we also have scientific

48

Table of Contents

research and experimental development expenditures of $18.1 million and $22.2 million, respectively, for Canadian federal
and  provincial  income  tax  purposes,  which  have  not  been  deducted.  These  expenditures  are  available  to  reduce  future
taxable income and have an unlimited carry-forward period. Research and development tax credits and expenditures are
subject  to  verification  by  the  tax  authorities,  and,  accordingly,  these  amounts  may  vary.  Future  changes  in  our  share
ownership, some of which are outside of our control, could result in an acquisition of control for the purposes of subsection
111(5) of the Canadian Tax Act. Furthermore, our ability to utilize non-capital losses (or U.S. equivalents) of companies
that  we  may  acquire  in  the  future  may  be  subject  to  limitations.  As  a  result,  even  if  we  attain  profitability,  we  may  be
unable to use a material portion of our non-capital losses and other tax attributes, which could negatively impact our future
cash flows.

Our subsidiary’s ability to use its U.S. net operating loss carryforwards and certain other tax attributes for U.S. income
tax purposes may be limited.

As of December 31, 2021, we had U.S. federal net operating loss carryforwards, or NOLs, of $26.3 million as a result of
expenses incurred by Milestone Pharmaceuticals USA, Inc., our wholly owned subsidiary. Under current U.S. federal tax
law,  NOLs  incurred  in  taxable  years  ending  beginning  after  December  31,  2017  may  be  carried  forward  indefinitely.
However, the deductibility of such NOLs in taxable years beginning after December 31, 2021 is limited to 80% of taxable
income. It is uncertain if and to what extent various states will conform to the federal law. In addition, under Sections 382
and  383  of  the  Internal  Revenue  Code  of  1986,  as  amended,  and  corresponding  provisions  of  state  law,  if  a  corporation
undergoes  an  “ownership  change,”  which  is  generally  defined  as  a  greater  than  50%  change  (by  value)  in  its  equity
ownership over a three year period, the corporation’s ability to use its pre change NOL carryforwards and other pre change
tax  attributes  (such  as  research  tax  credits)  to  offset  its  post  change  income  may  be  limited.  It  is  possible  that  we  have
experienced  one  or  more  ownership  changes  in  the  past.  In  addition,  we  may  also  experience  ownership  changes  in  the
future as a result of subsequent shifts in our share ownership some of which may be outside of our control. As a result, if
we earn net taxable income, our ability to use our pre ownership change NOL carryforwards to offset U.S. federal taxable
income may be subject to limitations, which could potentially result in increased future tax liability to us. In addition, at the
state level, there may be periods during which the use of NOLs is suspended or otherwise limited, which could accelerate
or permanently increase state taxes owed.

Risks Related to the Development of Our Product Candidates

We have only one product candidate, etripamil, for which we are currently pursuing clinical development. Our future
success is substantially dependent on the successful clinical development and regulatory approval of etripamil. If we are
not able to obtain required regulatory approvals for etripamil or any future product candidates, we will not be able to
commercialize etripamil or any future product candidates and our ability to generate revenue will be adversely affected.

Etripamil is currently our only product candidate. We have not obtained regulatory approval for etripamil or any product
candidate, and it is possible that neither etripamil nor any product candidates we may seek to develop in the future will ever
obtain regulatory approval. Neither we nor any future collaborator is permitted to market any drug product candidates in
the  United  States  or  other  countries  until  we  receive  regulatory  approval  from  the  FDA  or  applicable  foreign  regulatory
agency.  The  time  required  to  obtain  approval  or  other  marketing  authorizations  by  the  FDA  and  comparable  foreign
regulatory authorities is unpredictable but typically takes many years following the commencement of clinical trials and
depends  upon  numerous  factors,  including  the  substantial  discretion  of  the  regulatory  authorities.  In  addition,  approval
policies, regulations or the type and amount of clinical data necessary to gain approval may change during the course of a
product candidate’s clinical development and may vary among jurisdictions. For example, in July 2020, we announced that
the  FDA  indicated  that  two  studies,  the  RAPID  study  and  the  completed  NODE-301  study,  could  potentially  fulfill  the
efficacy requirement for our NDA for etripamil in patients with PSVT. We proposed certain program changes to the FDA
and they agreed.

Prior  to  obtaining  approval  to  commercialize  etripamil  and  any  other  drug  product  candidate  in  the  United  States  or
elsewhere, we must demonstrate with substantial evidence from well controlled clinical trials, and to the satisfaction of the
FDA or comparable foreign regulatory authorities, that such product candidates are safe and effective for their intended

49

Table of Contents

uses.  Results  from  nonclinical  studies  and  clinical  trials  can  be  interpreted  in  different  ways.  Even  if  we  believe  the
nonclinical or clinical data for our product candidates are promising, such data may not be sufficient to support approval by
the FDA and other regulatory authorities. The FDA may also require us to conduct additional nonclinical studies, including
human  factor  studies,  or  clinical  trials  for  our  product  candidates  either  prior  to  or  post-approval,  or  it  may  object  to
elements  of  our  clinical  development  program.  In  addition,  the  FDA  typically  refers  applications  for  novel  drugs,  like
etripamil and potentially any future product candidates, to an advisory committee composed of outside experts. The FDA is
not  bound  by  the  recommendation  of  the  advisory  committee,  but  it  considers  such  recommendation  when  making  its
decision.

Of the large number of products in development, only a small percentage successfully complete the FDA or comparable
foreign  regulatory  authorities’  approval  processes  and  are  commercialized.  The  lengthy  approval  or  marketing
authorization  process  as  well  as  the  unpredictability  of  future  clinical  trial  results  may  result  in  our  failing  to  obtain
regulatory  approval  or  marketing  authorization  to  market  etripamil  or  any  future  product  candidates,  which  would
significantly harm our business, financial condition, results of operations and prospects.

We have invested a significant portion of our time and financial resources in the development of etripamil. Our business is
dependent  on  our  ability  to  successfully  complete  development  of,  obtain  regulatory  approval  for,  and,  if  approved,
successfully commercialize etripamil and any future product candidates in a timely manner.

Even  if  we  eventually  complete  clinical  testing  and  receive  approval  of  a  new  drug  application,  or  NDA,  or  foreign
marketing  application  for  etripamil  and  any  future  product  candidates,  the  FDA  or  the  comparable  foreign  regulatory
authorities may grant approval or other marketing authorization contingent on the performance of costly additional clinical
trials, including post-market clinical trials. The FDA or the comparable foreign regulatory authorities also may approve or
authorize for marketing a product candidate for a more limited indication or patient population that we originally request,
and  the  FDA  or  comparable  foreign  regulatory  authorities  may  not  approve  or  authorize  the  labeling  that  we  believe  is
necessary or desirable for the successful commercialization of a product candidate. Any delay in obtaining, or inability to
obtain, applicable regulatory approval or other marketing authorization would delay or prevent commercialization of that
product candidate and would materially adversely impact our business and prospects.

In addition, the FDA and comparable foreign regulatory authorities may change their policies, adopt additional regulations
or  revise  existing  regulations  or  take  other  actions,  which  may  prevent  or  delay  approval  of  our  future  products  under
development on a timely basis. Such policy or regulatory changes could impose additional requirements upon us that could
delay  our  ability  to  obtain  approvals,  increase  the  costs  of  compliance  or  restrict  our  ability  to  maintain  any  marketing
authorizations we may have obtained.

We may not be successful in our efforts to expand our pipeline of product candidates beyond etripamil for PSVT.

We  intend  to  build  a  pipeline  of  product  candidates  beyond  etripamil  for  PSVT  and  progress  these  product  candidates
through  clinical  development.  For  example,  we  recently  began  enrollment  in  a  Phase  2  clinical  trial  of  etripamil  for  the
treatment of AFib-RVR. We may not be able to successfully expand the scope of cardiovascular indications for etripamil
beyond PSVT, or leverage our expertise and experience with etripamil in PSVT to other product candidates. We may not be
able  to  in-license,  acquire  or  develop  future  product  candidates  that  are  safe  and  effective.  Even  if  we  are  successful  in
continuing to expand etripamil to other indications and further build our pipeline, the potential product candidates that we
identify  may  not  be  suitable  for  clinical  development,  including  as  a  result  of  safety,  tolerability,  efficacy  or  other
characteristics  that  indicate  that  they  are  unlikely  to  be  drugs  that  will  receive  marketing  approval,  achieve  market
acceptance  or  obtain  reimbursements  from  third-party  payors.  If  we  do  not  successfully  execute  on  our  strategy  of
expanding our product pipeline, it could significantly harm our financial position and adversely affect the trading price of
our common shares.

50

Table of Contents

The development of additional product candidates is risky and uncertain.

Efforts to identify, acquire or in-license, and then develop product candidates require substantial technical, financial and
human resources, whether or not any product candidates are ultimately identified. Our efforts may initially show promise in
identifying potential product candidates, yet fail to yield product candidates for clinical development, approved products or
commercial revenues for many reasons, including the following:

•

•

•

•

•

•

the methodology used may not be successful in identifying potential product candidates;

competitors may develop alternatives that render any product candidates we develop obsolete;

any product candidates we develop may nevertheless be covered by third parties’ patents or other exclusive
rights;

a  product  candidate  may  be  shown  to  have  harmful  side  effects  or  other  characteristics  that  indicate  it  is
unlikely to be effective or otherwise does not meet applicable regulatory criteria;

a product candidate may not be capable of being produced in commercial quantities at an acceptable cost, or
at all; and

a product candidate may not be accepted as safe and effective by physicians, patients, the medical community
or third-party payors.

We have limited financial and management resources and, as a result, we may forego or delay pursuit of opportunities with
other product candidates or for other indications that later prove to have greater market potential. Our resource allocation
decisions  may  cause  us  to  fail  to  capitalize  on  viable  commercial  drugs  or  profitable  market  opportunities.  If  we  do  not
accurately  evaluate  the  commercial  potential  or  target  market  for  a  particular  product  candidate,  we  may  relinquish
valuable rights to that product candidate through collaboration, licensing or other royalty arrangements in circumstances
under which it would have been more advantageous for us to retain sole development and commercialization rights to such
product candidate. If we are unsuccessful in identifying and developing additional product candidates or are unable to do
so, our business may be harmed.

Success in preclinical studies or earlier clinical trials may not be indicative of results in future clinical trials and we
cannot  assure  you  that  any  ongoing,  planned  or  future  clinical  trials  will  lead  to  results  sufficient  for  the  necessary
regulatory approvals.

Success in preclinical testing and earlier clinical trials does not ensure that later clinical trials will generate the same results
or  otherwise  provide  adequate  data  to  demonstrate  the  efficacy  and  safety  of  a  product  candidate.  Preclinical  tests  and
Phase 1 and Phase 2 clinical trials are primarily designed to test safety, to study pharmacokinetics and pharmacodynamics
and to understand the side effects of product candidates at various doses and schedules. Success in preclinical studies and
earlier  clinical  trials  does  not  ensure  that  later  efficacy  trials  will  be  successful,  nor  does  it  predict  final  results.  For
example, our Phase 2 clinical trial of etripamil for PSVT was conducted in an electrophysiology lab, a controlled setting, in
which  episodes  of  supraventricular  tachycardia,  or  SVT,  were  induced  and  etripamil  was  administered  by  healthcare
providers. Our Phase 3 clinical trials are being conducted in an at-home setting with patients self-administering etripamil
and monitoring their cardiac activity as episodes of SVT occur. Additionally, in our Phase 2 clinical trial, four sprays of
study drug were dispensed to patients using four separate FDA approved single spray devices. In our Phase 3 clinical trials,
patients self-administer two to four sprays of study drug from an FDA approved device that is capable of delivering two
separate sprays. Accordingly, the results of our Phase 2 trial of etripamil may not be replicated in the at-home setting of our
Phase 3 clinical trials, and notably, our NODE-301 clinical trial did not meet its primary endpoint. Etripamil and any future
product  candidates  may  fail  to  show  the  desired  safety  and  efficacy  in  clinical  development  despite  positive  results  in
preclinical studies or having successfully advanced through earlier clinical trials.

51

Table of Contents

In addition, the design of a clinical trial can determine whether its results will support approval of a product, and flaws in
the design of a clinical trial may not become apparent until the clinical trial is well advanced. Clinical trial design flaws are
more likely in therapy areas, such as PSVT, where there are limited previous trials from which to learn and model clinical
trials. As an organization, we have limited experience designing clinical trials and may be unable to design and execute a
clinical  trial  to  support  regulatory  approval.  Many  companies  in  the  pharmaceutical  and  biotechnology  industries  have
suffered  significant  setbacks  in  late-stage  clinical  trials  even  after  achieving  promising  results  in  preclinical  testing  and
earlier clinical trials. Data obtained from preclinical and clinical activities are subject to varying interpretations, which may
delay, limit or prevent regulatory approval. In addition, we may experience regulatory delays or rejections as a result of
many factors, including changes in regulatory policy during the period of our product candidate development. Any such
delays could negatively impact our business, financial condition, results of operations and prospects.

Our  business,  operations  and  clinical  development  timelines  and  plans  have  been  adversely  affected  by  the  effects  of
health epidemics, including the ongoing COVID-19 pandemic, and could be affected by future health epidemics.

Our  business,  operations  and  clinical  development  timelines  and  plans  have  been,  and  could  in  the  future  be  adversely
affected by health epidemics in regions where we have concentrations of clinical trial sites or other business operations,
and could cause significant disruption in the operations of CROs and manufacturers upon whom we rely.

The  ongoing  COVID-19  pandemic  has  resulted  in  many  state,  local  and  foreign  governments  implementing  various
quarantines, executive orders, shelter-in-place orders and similar government orders and restrictions in order to control the
spread  of  the  disease,  which  changing  restrictions  have  resulted  in  periods  of  business  closures,  work  stoppages,
slowdowns and delays, work-from-home policies, travel restrictions and cancellation of events.  We implemented a work-
from-home policy for all employees, which is no longer in place, we now have a hybrid model, and we may take further
actions that alter our operations as may be required by federal, state or local authorities, or which we determine are in the
best  interests  of  our  employees.  While  the  situation  continues  to  evolve  and  certain  locations  have  reduced  some  of  the
restrictions  initially  adopted  in  response  to  the  pandemic,  new  restrictions  could  be  implemented,  or  prior  restrictions
reinstated in order to address any resurgences in cases of COVID-19, including those related to newer strains such as the
Delta and Omicron variants. These actions, and the uncertainty about the ever evolving landscape, could negatively impact
productivity and disrupt our business and operations.

Moreover,  our  clinical  development  timelines  and  plans  have  been  and  could  continue  to  be  affected  by  the  COVID-19
pandemic. We rely on contract research organizations or other third parties to assist us with clinical trials, and we cannot
guarantee that they will continue to perform their contractual duties in a timely and satisfactory manner as a result of the
COVID-19  pandemic.  Clinical  trial  site  initiations  and  patient  enrollment  have  been  and  may  be  further  delayed  or
suspended due to the desire to protect potential study patients and study personnel. For example, some sites for our NODE-
303  and  RAPID  studies  have  closed  their  practices  to  further  enrollment  at  this  time.  Furthermore,  the  initiation  of
enrollment  in  our  Phase  2  clinical  trial  of  etripamil  for  the  treatment  of  AFib-RVR  has  been  delayed  due  to  closures  of
clinical trial sites.  In addition, already-enrolled patients may not be able to comply with clinical trial protocols or attend
follow up visits if quarantines impede patient movement or interrupt healthcare services. Similarly, our ability to recruit
and retain patients and principal investigators and site staff who, as healthcare providers, may have heightened exposure to
COVID-19  could  be  adversely  impacted.  As  a  result,  we  may  face  delays  in  meeting  the  anticipated  timelines  for  our
ongoing and planned clinical trials.

Further,  if  the  business  operations  of  our  third-party  manufacturers  and  suppliers  are  interrupted,  this  could  disrupt  our
supply chain and impact our ongoing preclinical studies and clinical trials. In addition, disruptions or delays in chemistry,
manufacturing and control activities for current or future product candidates in general may result in delays and challenges
in numerous areas of the drug development lifecycle, including preclinical drug development, clinical stage validation and
testing and manufacturing.

In addition, the spread of COVID-19, which has caused a broad impact globally, may materially affect us economically.
While the full extent of the economic impact brought by and the duration of the panedmic may be difficult to assess or
predict, the pandemic could result in future periods of significant disruption of global financial markets, reducing our

52

Table of Contents

ability to access capital, which could in the future negatively affect our liquidity. In addition, further recessions or market
correction resulting from the sustained pandemic could materially affect our business and the value of our common shares.

The ultimate impact of the pandemic or a similar health epidemic is highly uncertain and subject to future developments
that are highly uncertain, including as a result of evolving variants of the disease, the actions taken to contain or treat it,
including  the  likelihood  of  achieving  widespread  global  vaccination  rates,  and  the  duration  and  intensity  of  the  related
effects of the pandemic and the uncertainty of the timing of the broader economic recovery to pre-pandemic levels. We do
not yet know the full extent of the potential impacts on our business, our clinical trials, healthcare systems or the global
economy as a whole.

We may encounter substantial delays or difficulties in our clinical trials.

We may not commercialize, market, promote or sell any product candidate without obtaining marketing approval from the
FDA or comparable foreign regulatory authorities, and we may never receive such approvals. It is impossible to predict
when  or  if  any  of  our  product  candidates  will  prove  effective  or  safe  in  humans  and  will  receive  regulatory  approval.
Before obtaining marketing approval from regulatory authorities for the sale of our product candidates, we must complete
preclinical  development  and  then  conduct  extensive  clinical  trials  to  demonstrate  the  safety  and  efficacy  of  our  product
candidates in humans. Clinical testing is expensive, difficult to design and implement, can take many years to complete and
is uncertain as to outcome. A failure of one or more clinical trials can occur at any stage of testing. For example, in March
2020, we reported that the first our NODE-301 trial did not meet its primary endpoint.  With agreement from the FDA, we
have  revised  the  second  part,  and  renamed  it  the  RAPID  trial,  but  there  can  be  no  guarantee  that  the  recently  initiated
RAPID  trial  will  meet  its  primary  endpoints.  Moreover,  preclinical  and  clinical  data  are  often  susceptible  to  varying
interpretations and analyses, and many companies that have believed their product candidates performed satisfactorily in
preclinical studies and clinical trials have nonetheless failed to obtain marketing approval of their products.

We may experience numerous unforeseen events prior to, during, or as a result of, clinical trials that could delay or prevent
our ability to receive marketing approval or commercialize etripamil and any future product candidates, including:

•

•

•

•

•

•

•

•

delays in reaching a consensus with regulatory authorities on design or implementation of our clinical trials;

regulators or institutional review boards, or IRBs, may not authorize us or our investigators to commence a
clinical trial or conduct a clinical trial at a prospective trial site;

delays in reaching agreement on acceptable terms with prospective clinical research organizations, or CROs,
and clinical trial sites;

the number of patients required for clinical trials of our product candidates may be larger than we anticipate,
enrollment in these clinical trials may be slower than we anticipate, patients may drop out of these clinical
trials at a higher rate than we anticipate or fail to return for post-treatment follow-up or we may fail to recruit
suitable patients to participate in a trial;

clinical trials of our product candidates may produce negative or inconclusive results;

imposition of a clinical hold by regulatory authorities as a result of a serious adverse event, concerns with a
class of product candidates or after an inspection of our clinical trial operations, trial sites or manufacturing
facilities;

occurrence  of  serious  adverse  events  associated  with  the  product  candidate  that  are  viewed  to  outweigh  its
potential benefits;

changes in regulatory requirements and guidance that require amending or submitting new clinical protocols;

53

Table of Contents

•

•

interruptions resulting from public health emergencies, including those related to the COVID-19 pandemic,
or other geopolitical tensions, such as Russia’s recent incursion into Ukraine,; or

we  may  decide,  or  regulators  may  require  us,  to  conduct  additional  clinical  trials  or  abandon  product
development programs.

Any inability to successfully complete preclinical and clinical development could result in additional costs to us or impair
our  ability  to  generate  revenue  from  future  drug  sales  or  other  sources.  In  addition,  if  we  make  manufacturing  or
formulation changes to our product candidates, we may need to conduct additional testing to bridge our modified product
candidate to earlier versions. Clinical trial delays could also shorten any periods during which we may have the exclusive
right to commercialize our product candidates, if approved, or allow our competitors to bring competing drugs to market
before  we  do,  which  could  impair  our  ability  to  successfully  commercialize  our  product  candidates  and  may  harm  our
business, financial condition, results of operations and prospects.

Additionally, if the results of our clinical trials are inconclusive or if there are safety concerns or serious adverse events
associated with our product candidates, we may:

•

•

•

•

•

•

•

•

•

be delayed in obtaining marketing approval, if at all;

obtain approval for indications or patient populations that are not as broad as intended or desired;

obtain approval with labeling that includes significant use or distribution restrictions or safety warnings;

be subject to additional post-marketing testing requirements;

be required to perform additional clinical trials to support approval or be subject to additional post-marketing
testing requirements;

have  regulatory  authorities  withdraw,  or  suspend,  their  approval  of  the  drug  or  impose  restrictions  on  its
distribution in the form of a modified risk evaluation and mitigation strategy, or REMS;

be subject to the addition of labeling statements, such as warnings or contraindications;

be sued; or

experience damage to our reputation.

Our product development costs will also increase if we experience delays in testing or obtaining marketing approvals. We
do not know whether any of our preclinical studies or clinical trials will begin as planned, need to be restructured or be
completed on schedule, if at all.

Further, we, the FDA or an IRB may suspend our clinical trials at any time if it appears that we or our collaborators are
failing to conduct a trial in accordance with regulatory requirements, including the FDA’s current Good Clinical Practice,
or GCP, regulations, that we are exposing participants to unacceptable health risks, or if the FDA finds deficiencies in our
investigational  new  drug  applications,  or  INDs,  or  the  conduct  of  these  trials.  Therefore,  we  cannot  predict  with  any
certainty  the  schedule  for  commencement  and  completion  of  future  clinical  trials.  If  we  experience  delays  in  the
commencement or completion of our clinical trials, or if we terminate a clinical trial prior to completion, the commercial
prospects of our product candidates could be negatively impacted, and our ability to generate revenues from our product
candidates may be delayed.

54

Table of Contents

Clinical trials are very expensive, time consuming and difficult to design and implement.

Our product candidates will require clinical testing before we are prepared to submit an NDA, or comparable application to
foreign regulatory authorities, for regulatory approval. We cannot predict with any certainty if or when we might submit an
application for regulatory approval for any of our product candidates or whether any such application will be approved by
the FDA or foreign regulatory authority. Human clinical trials are very expensive and difficult to design and implement, in
part  because  they  are  subject  to  rigorous  regulatory  requirements.  For  instance,  the  FDA  or  foreign  regulatory  authority
may  not  agree  with  our  proposed  endpoints  for  any  future  clinical  trial  of  our  product  candidates,  which  may  delay  the
commencement of our clinical trials. In addition, we may not succeed in developing and validating disease relevant clinical
endpoints  based  on  insights  regarding  biological  pathways  for  the  diseases  we  are  studying.  The  clinical  trial  process  is
also  time  consuming.  We  estimate  that  the  successful  completion  of  clinical  trials  for  etripamil  and  any  future  product
candidates  will  take  several  years  to  complete.  Furthermore,  failure  can  occur  at  any  stage,  and  we  could  encounter
problems that cause us to abandon or repeat clinical trials. For example, the pivotal NODE-301 trial of etripamil for PSVT
did  not  meet  its  primary  endpoint.  As  a  result,  we  were  required  to  submit  a  protocol  amendment  to  the  FDA  for  the
RAPID trial.

Enrollment and retention of patients in clinical trials is an expensive and time-consuming process and could be delayed,
made more difficult or rendered impossible by multiple factors outside our control.

Identifying  and  qualifying  patients  to  participate  in  our  clinical  trials  is  critical  to  our  success.  If  the  actual  number  of
patients with PSVT, AFib-RVR or any other indications that we may pursue for etripamil or future product candidates, is
smaller  than  we  anticipate,  we  may  encounter  difficulties  in  enrolling  patients  in  our  clinical  trials,  thereby  delaying  or
preventing  development  and  approval  of  etripamil  and  any  future  product  candidates.  Even  once  enrolled  we  may  be
unable to retain a sufficient number of patients to complete any of our trials. Patient enrollment and retention in clinical
trials  depends  on  many  factors,  including  the  size  of  the  patient  population,  the  nature  of  the  trial  protocol,  the  existing
body of safety and efficacy data, the number and nature of competing treatments and ongoing clinical trials of competing
therapies for the same indication, the proximity of patients to clinical sites, the experience and capabilities of the clinical
sites to recruit the correct patients, and the eligibility criteria for the trial. In our Phase 3 clinical trials, we are attempting to
enroll  elderly  patients  and  patients  taking  concomitant  medications  that  impact  the  heart,  such  as  other  calcium  channel
blockers and beta blockers. We are doing this in order to obtain efficacy and safety data on patients representing the subset
of  our  intended  population  that  is  most  vulnerable  to  safety  concerns  with  the  use  of  etripamil.  Such  patients  may  be
difficult to enroll in this trial, and the lack of data on these patients may negatively impact the approvability or labeling of
etripamil. Patient enrollment may also continue to be affected by the ongoing COVID-19 pandemic, which could be due to
the  prioritization  of  hospitalization  resources  toward  this  pandemic,  exposure  of  healthcare  providers  to  COVID-19  and
difficulties for patients to access clinical trial sites and comply with clinical trial protocols. For example, some sites for our
NODE-303 study have closed their practices to further enrollment.

In our Phase 2 clinical trial of etripamil for the treatment of PSVT, only 104 of 199 enrolled patients completed the trials,
with 70 patients unable to induce or sustain episodes of SVT during the trial period. The first Phase 3 trial of PSVT for
etripamil enrolled over 400 diagnosed patients with PSVT meeting inclusion and exclusion criteria in order to achieve the
required  treatment  of  150  confirmed  PSVT  episodes.    PSVT  is  episodic  and  unpredictable,  and  all  of  our  Phase  3  trial
designs depend on patients experiencing and recognizing an episode of SVT, self-administering etripamil and monitoring
their cardiac activity using a monitoring device. We cannot control the timing of these episodes or guarantee that patients
will  correctly  recognize  the  episode,  self-administer  etripamil  and  use  the  cardiac  monitor  as  directed.  We  also  cannot
predict with certainty the number or timing of any SVT episodes for those patients that enroll in the trial. Conducting a
Phase 3 clinical trial for a PSVT treatment in an at-home setting is paradigm changing, and subject to a number of risks.
There is limited, if any, meaningful precedent from which to inform our trial design and make assumptions about patient
enrollment and compliance. Accordingly, our Phase 3 trial design is subject to significantly more risks than if there were
numerous  studies  upon  which  we  could  model  our  protocols.  Our  efficacy  and  safety  databases  could  take  significantly
longer to populate than projected, which would add cost to our development program and delay any potential approval of
etripamil.

55

Table of Contents

Furthermore, our efforts to build relationships with patient communities may not succeed, which could result in delays in
patient enrollment in our clinical trials. In addition, any negative results we may report in clinical trials of etripamil and any
future product candidate may make it difficult or impossible to recruit and retain patients in other clinical trials of that same
product candidate. For example, we reported a failed primary endpoint from our NODE-301 trial in March 2020. Delays or
failures in planned patient enrollment or retention may result in increased costs, program delays or both, which could have
a harmful effect on our ability to develop etripamil or any future product candidates or could render further development
impossible. In addition, we expect to rely on CROs and clinical trial sites to ensure proper and timely conduct of our future
clinical trials and, while we intend to enter into agreements governing their services, we will be limited in our ability to
compel their actual performance. Similarly, our formulation of etripamil is designed to be self-administered as a nasal spray
during an SVT episode by patients enrolled in our Phase 3 trials, or during a AFib-RVR episode by patients in our Phase 2
trial. While we expect enrolled patients to adhere to the protocol, our ability to ensure patient compliance is limited.

Our  product  candidates  may  cause  undesirable  side  effects  or  have  other  properties  that  could  delay  or  prevent  their
regulatory  approval,  limit  the  commercial  potential  or  result  in  significant  negative  consequences  following  any
potential marketing approval.

During the conduct of clinical trials, patients report changes in their health, including illnesses, injuries and discomforts, to
their  doctor.  Often,  it  is  not  possible  to  determine  whether  or  not  the  product  candidate  being  studied  caused  these
conditions.  Regulatory  authorities  may  draw  different  conclusions  or  require  additional  testing  to  confirm  these
determinations, if they occur. For example, in our Phase 2 clinical trial for PSVT, three serious adverse events, or SAEs,
were  considered  possibly  related  to  etripamil,  including  a  second  degree  AV  block  that  subsequently  resolved.  Calcium
channel  blockers  have  known  side  effects,  such  as  slowing  the  heart  rate  below  normal  levels  and  hypotension,  or  low
blood pressure. While we designed etripamil to have a short pharmacodynamic effect to lower these risks, if etripamil is
not quickly metabolized as designed, these known side effects may become more pronounced in patients who use etripamil.

In  addition,  it  is  possible  that  as  we  test  etripamil  or  any  future  product  candidates  in  larger,  longer  and  more  extensive
clinical  trials,  such  as  our  Phase  3  clinical  trials,  or  as  use  of  etripamil  or  any  future  product  candidates  becomes  more
widespread if they receive regulatory approval, illnesses, injuries, discomforts and other adverse events that were observed
in earlier trials, as well as conditions that did not occur or went undetected in previous trials, will be reported by subjects or
patients. Many times, side effects are only detectable after investigational drugs are tested in large-scale pivotal trials or, in
some cases, after they are made available to patients on a commercial scale after approval. If additional clinical experience
indicates that etripamil or any future product candidates have side effects or causes serious or life-threatening side effects,
the  development  of  the  product  candidate  may  fail  or  be  delayed,  or,  if  the  product  candidate  has  received  regulatory
approval,  such  approval  may  be  revoked,  which  would  harm  our  business,  prospects,  operating  results  and  financial
condition.

Interim, “top-line” and preliminary data from our clinical trials that we announce or publish from time to time may
change as more patient data become available and are subject to audit and verification procedures that could result in
material changes in the final data.

From  time  to  time,  we  may  publish  interim,  “top-line”  or  preliminary  data  from  our  clinical  trials.  Interim  data  from
clinical trials that we may complete are subject to the risk that one or more of the clinical outcomes may materially change
as patient enrollment continues and more patient data become available. Preliminary or “top-line” data also remain subject
to audit and verification procedures that may result in the final data being materially different from the preliminary data we
previously  published.  As  a  result,  interim  and  preliminary  data  should  be  viewed  with  caution  until  the  final  data  are
available. Differences between preliminary or interim data and final data could significantly harm our business prospects
and may cause the trading price of our common shares to fluctuate significantly.

56

Table of Contents

As an organization, we have never successfully completed pivotal clinical trials, and we may be unable to do so for any
product candidates we may develop, including our pivotal Phase 3 clinical trials for the treatment of PSVT.

We will need to successfully complete pivotal clinical trials in order to obtain the approval of the FDA and other regulatory
agencies  to  market  etripamil  or  any  of  our  other  product  candidates.  Carrying  out  later-stage  clinical  trials  and  the
submission  of  a  successful  NDA  is  a  complicated  process.  As  an  organization,  we  have  only  completed  one  Phase  3
clinical  trial,  we  have  other  trials  ongoing,  and  we  have  limited  experience  in  preparing,  submitting  and  prosecuting
regulatory filings. Due to our limited experience with later stage trials, we may be unable to successfully and efficiently
execute  and  complete  necessary  clinical  trials  in  a  way  that  leads  to  NDA  submission  and  approval  of  etripamil  for  the
treatment  of  PSVT.  We  may  require  more  time  and  incur  greater  costs  than  our  competitors  and  may  not  succeed  in
obtaining regulatory approvals of product candidates that we develop. Failure to commence or complete, or delays in, our
planned clinical trials could prevent us from or delay us in commercializing etripamil for the treatment of PSVT.

We  may  explore  strategic  collaborations  that  may  never  materialize,  or  we  may  be  required  to  relinquish  important
rights to and control over the development of our product candidates to any future collaborators.

We  intend  to  continue  to  periodically  explore  a  variety  of  possible  strategic  collaborations  in  an  effort  to  gain  access  to
additional  product  candidates  or  resources.  We  are  likely  to  face  significant  competition  in  seeking  appropriate  strategic
collaborators, and strategic collaborations can be complicated and time consuming to negotiate and document. We may not
be able to negotiate strategic collaborations on acceptable terms, or at all. We are unable to predict when, if ever, we will
enter into any strategic collaborations because of the numerous risks and uncertainties associated with establishing them.

Future collaborations could subject us to a number of risks, including:

•

•

•

•

•

•

•

•

•

we  may  be  required  to  undertake  the  expenditure  of  substantial  operational,  financial  and  management
resources;

we may be required to issue equity securities that would dilute our shareholders’ percentage ownership of our
company;

we may be required to assume substantial actual or contingent liabilities;

we may not be able to control the amount and timing of resources that our strategic collaborators devote to
the development or commercialization of our product candidates;

strategic collaborators may select indications or design clinical trials in a way that may be less successful than
if we were doing so;

strategic  collaborators  may  delay  clinical  trials,  provide  insufficient  funding,  terminate  a  clinical  trial  or
abandon  a  product  candidate,  repeat  or  conduct  new  clinical  trials  or  require  a  new  version  of  a  product
candidate for clinical testing;

strategic  collaborators  may  not  pursue  further  development  of  products  resulting  from  the  strategic
collaboration arrangement or may elect to discontinue research and development programs;

strategic collaborators may not commit adequate resources to the marketing and distribution of our product
candidates, limiting our potential revenues from these products;

disputes  may  arise  between  us  and  our  strategic  collaborators  that  result  in  the  delay  or  termination  of  the
research or development of our product candidates or that result in costly litigation or arbitration that diverts
management’s attention and consumes resources;

57

Table of Contents

•

•

•

•

•

strategic collaborators may experience financial difficulties;

strategic  collaborators  may  not  properly  maintain  or  defend  our  intellectual  property  rights  or  may  use  our
proprietary information in a manner that could jeopardize or invalidate our proprietary information or expose
us to potential litigation;

business  combinations  or  significant  changes  in  a  strategic  collaborator’s  business  strategy  may  adversely
affect a strategic collaborator’s willingness or ability to complete its obligations under any arrangement;

strategic  collaborators  could  decide  to  move  forward  with  a  competing  product  candidate  developed  either
independently or in collaboration with others, including our competitors; and

strategic  collaborators  could  terminate  the  arrangement  or  allow  it  to  expire,  which  would  delay  the
development and may increase the cost of developing our product candidates.

Risks Related to the Commercialization of Our Product Candidates

If we are unable to establish sales and marketing capabilities or enter into agreements with third parties to market and
sell etripamil or any future product candidates, we may not be successful in commercializing etripamil or any future
product candidates, if and when they are approved.

To successfully commercialize etripamil or any future product candidate that may result from our development programs,
we  will  need  to  build  out  our  sales  and  marketing  capabilities,  either  on  our  own  or  with  others.  The  establishment  and
development of our own commercial team or the establishment of a contract field force to market any product candidate we
may develop will be expensive and time consuming and could delay any drug launch. Moreover, we cannot be certain that
we will be able to successfully develop this capability. We may seek to enter into collaborations with other entities to use
their established marketing and distribution capabilities, but we may be unable to enter into such agreements on favorable
terms,  if  at  all.  If  any  current  or  future  collaborators  do  not  commit  sufficient  resources  to  commercialize  our  product
candidates,  or  we  are  unable  to  develop  the  necessary  capabilities  on  our  own,  we  may  be  unable  to  generate  sufficient
revenue to sustain our business. We may compete with many companies that currently have extensive, experienced, and
well-funded marketing and sales operations to recruit, hire, train and retain marketing and sales personnel. We will likely
also face competition if we seek third parties to assist us with the sales and marketing efforts of etripamil and any future
product candidates. Without an internal team or the support of a third party to perform marketing and sales functions, we
may be unable to compete successfully against these more established companies.

Even  if  etripamil  or  any  future  product  candidates  receive  marketing  approval,  they  may  fail  to  achieve  market
acceptance  by  physicians,  patients,  third-party  payors  or  others  in  the  medical  community  necessary  for  commercial
success.

Even if etripamil or any future product candidates receive marketing approval, they may fail to gain market acceptance by
physicians, patients, third-party payors and others in the medical community. If such product candidates do not achieve an
adequate level of acceptance, we may not generate significant drug revenue and may not become profitable. The degree of
market acceptance of etripamil or any future product candidates, if approved for commercial sale, will depend on a number
of factors, including but not limited to:

•

•

•

the convenience and ease of administration compared to alternative treatments and therapies;

the  willingness  of  the  target  patient  population  to  try  new  therapies  and  of  physicians  to  prescribe  these
therapies;

the efficacy and potential advantages compared to alternative treatments and therapies;

58

Table of Contents

•

•

•

•

•

•

•

the effectiveness of sales and marketing efforts;

the prevalence and severity of any side effects;

the strength of our relationships with patient communities;

the  cost  of  treatment  in  relation  to  alternative  treatments  and  therapies,  including  any  similar  generic
treatments;

our ability to offer such drug for sale at competitive prices;

the strength of marketing and distribution support;

the availability of third-party coverage and adequate reimbursement; any restrictions on the use of the drug
together with other medications; and the awareness and support from key opinion leaders in cardiology.

Our  efforts  to  educate  physicians,  patients,  third-party  payors  and  others  in  the  medical  community  on  the  benefits  of
etripamil or any future product candidates may require significant resources and may never be successful. Such efforts may
require more resources than are typically required due to the potential of etripamil to shift the treatment paradigm away
from acute-care settings to self-administration. Because we expect sales of etripamil or any future product candidates, if
approved, to generate substantially all of our revenues for the foreseeable future, the failure of these product candidates to
find market acceptance would harm our business.

Even if we successfully obtain approval for etripamil, its success will be dependent on its proper use.

While we have designed etripamil to be self-administered, we cannot control the successful use of the product. While we
have conducted, and intend in the future to conduct, human factors studies to determine how to optimize the instructions
for use, the results in our clinical trials may not be replicated by users in the future. If we are not successful in promoting
the proper use of etripamil, if approved, we may not be able to achieve market acceptance or effectively commercialize the
drug.  In  addition,  even  in  the  event  of  proper  use  of  etripamil,  individual  devices  may  fail.  Increasing  the  scale  of
production inherently creates increased risk of manufacturing errors, and we may not be able to adequately inspect every
device that is produced, and it is possible that individual devices may fail to perform as designed. Manufacturing errors
could negatively impact market acceptance of any of our product candidates that receive approval, result in negative press
coverage, or increase our liability.

If the market opportunities for etripamil and any future product candidates are smaller than we estimate, our business
may suffer.

Our eligible patient population may differ significantly from the actual market addressable by our product candidates. Our
projections of both the number of people who have these conditions, as well as the subset of people with these diseases
who have the potential to benefit from treatment with our product candidates, are based on our beliefs and estimates. These
estimates  have  been  derived  from  a  variety  of  sources,  including  the  scientific  literature,  insurance  claims  databases  or
market research, and may prove to be incorrect. Further, new studies may change the estimated incidence or prevalence of
these  diseases.  The  number  of  patients  may  turn  out  to  be  lower  than  expected.  Likewise,  the  potentially  addressable
patient population for each of our product candidates may be limited or may not be amenable to treatment with our product
candidates, and new patients may become increasingly difficult to identify or access. If the market opportunities for our
product candidates are smaller than we estimate, our business and results of operations could be adversely affected.

59

Table of Contents

We may face substantial competition, which may result in others developing or commercializing drugs before or more
successfully than us.

The  development  and  commercialization  of  new  drugs  is  highly  competitive.  We  may  face  competition  from  major
pharmaceutical  companies,  specialty  pharmaceutical  companies  and  biotechnology  companies  worldwide.  Potential
competitors  also  include  academic  institutions,  government  agencies  and  other  public  and  private  research  organizations
that  conduct  research,  seek  patent  protection  and  establish  collaborative  arrangements  for  research,  development,
manufacturing and commercialization.

More established companies may have a competitive advantage over us due to their greater size, resources and institutional
experience. In particular, these companies have greater experience and expertise in securing reimbursement, government
contracts  and  relationships  with  key  opinion  leaders,  conducting  testing  and  clinical  trials,  obtaining  and  maintaining
regulatory  approvals  and  distribution  relationships  to  market  products  and  marketing  approved  drugs.  These  companies
also have significantly greater research and marketing capabilities than we do. If we are not able to compete effectively
against existing and potential competitors, our business and financial condition may be harmed.

As a result of these factors, our competitors may obtain regulatory approval of their drugs before we are able to, which may
limit  our  ability  to  develop  or  commercialize  etripamil  and  any  future  product  candidates.  Our  competitors  may  also
develop therapies that are safer, more effective, more widely accepted or less expensive than ours, and may also be more
successful  than  we  in  manufacturing  and  marketing  their  drugs.  These  advantages  could  render  our  product  candidates
obsolete  or  non-competitive  before  we  can  recover  the  costs  of  such  product  candidates’  development  and
commercialization.

Mergers  and  acquisitions  in  the  pharmaceutical  and  biotechnology  industries  may  result  in  even  more  resources  being
concentrated  among  a  smaller  number  of  our  competitors.  Smaller  and  early  stage  companies  may  also  prove  to  be
significant competitors, particularly through collaborative arrangements with large and established companies. These third
parties  compete  with  us  in  recruiting  and  retaining  qualified  scientific,  management  and  commercial  personnel,
establishing  clinical  trial  sites  and  subject  registration  for  clinical  trials,  as  well  as  in  acquiring  technologies
complementary to, or necessary for, our programs.

If we commercialize etripamil or any future product candidates outside of the United States, a variety of risks associated
with international operations could harm our business.

We intend to seek approval to market etripamil outside of the United States and may do so for future product candidates. If
we  market  approved  products  outside  of  the  United  States,  we  expect  that  we  will  be  subject  to  additional  risks  in
commercialization including:

•

•

•

•

•

•

•

different regulatory requirements for approval of therapies in foreign countries;

reduced protection for intellectual property rights;

unexpected changes in tariffs, trade barriers and regulatory requirements;

economic weakness, including inflation, or political instability in particular foreign economies and markets;

compliance with tax, employment, immigration and labor laws for employees living or traveling abroad;

foreign currency fluctuations, which could result in increased operating expenses and reduced revenues, and
other obligations incident to doing business in another country;

foreign reimbursement, pricing and insurance regimes;

60

Table of Contents

•

•

•

workforce uncertainty in countries where labor unrest is more common than in the United States;

production  shortages  resulting  from  any  events  affecting  raw  material  supply  or  manufacturing  capabilities
abroad; and

business  interruptions  resulting  from  pandemics  and  public  health  emergencies,  including  those  related  to
COVID-19  coronavirus,  geopolitical  actions,  including  war  and  terrorism  or  natural  disasters  including
earthquakes, typhoons, floods and fires.

We  have  no  prior  experience  in  these  areas.  In  addition,  there  are  complex  regulatory,  tax,  labor  and  other  legal
requirements imposed by many of the individual countries in and outside of Europe with which we will need to comply.
Many biopharmaceutical companies have found the process of marketing their own products in foreign countries to be very
challenging.

Coverage  and  adequate  reimbursement  may  not  be  available  for  etripamil  or  any  future  product  candidates,  which
could make it difficult for us to gain market acceptance.

Market  acceptance  and  sales  of  any  product  candidates  that  we  commercialize,  if  approved,  will  depend  in  part  on  the
extent to which reimbursement for these drugs and related treatments will be available from third-party payors, including
government  health  administration  authorities,  managed  care  organizations  and  other  private  health  insurers.  Third-party
payors  decide  for  which  therapies  and  establish  reimbursement  levels.  While  no  uniform  policy  for  coverage  and
reimbursement  exists  in  the  United  States,  third-party  payors  often  rely  upon  Medicare  coverage  policy  and  payment
limitations in setting their own coverage and reimbursement policies. However, decisions regarding the extent of coverage
and amount of reimbursement to be provided for any product candidates that we develop will be made on a payor-by-payor
basis.  Therefore,  one  payor’s  determination  to  provide  coverage  for  a  drug  does  not  assure  that  other  payors  will  also
provide  coverage,  and  adequate  reimbursement,  for  the  drug.  Additionally,  a  third-party  payor’s  decision  to  provide
coverage  for  a  therapy  does  not  imply  that  an  adequate  reimbursement  rate  will  be  approved.  Each  payor  determines
whether or not it will provide coverage for a therapy, what amount it will pay the manufacturer for the therapy, and on what
tier of its formulary it will be placed. The position on a payor’s list of covered drugs, or formulary, generally determines
the  co-payment  that  a  patient  will  need  to  make  to  obtain  the  therapy  and  can  strongly  influence  the  adoption  of  such
therapy by patients and physicians. Patients who are prescribed treatments for their conditions and providers prescribing
such services generally rely on third-party payors to reimburse all or part of the associated healthcare costs. Patients are
unlikely to use our products unless coverage is provided and reimbursement is adequate to cover a significant portion of
the cost of our products.

Third-party payors have attempted to control costs by limiting coverage and the amount of reimbursement for particular
medications.  We  cannot  be  sure  that  coverage  and  reimbursement  will  be  available  for  any  drug  that  we  commercialize
and, if reimbursement is available, what the level of reimbursement will be. Inadequate coverage and reimbursement may
impact  the  demand  for,  or  the  price  of,  any  drug  for  which  we  obtain  marketing  approval.  If  coverage  and  adequate
reimbursement are not available, or are available only to limited levels, we may not be able to successfully commercialize
etripamil or any future product candidates that we develop.

In addition, we expect that the increased emphasis on managed care and cost containment measures in the United States by
third-party payors and government authorities to continue and will place pressure on pharmaceutical pricing and coverage.
Coverage policies and third-party reimbursement rates may change at any time. Therefore, even if favorable coverage and
reimbursement status is attained for one or more drug products for which we receive regulatory approval, less favorable
coverage  policies  and  reimbursement  rates  may  be  implemented  in  the  future.  If  we  are  unable  to  obtain  and  maintain
sufficient  third-party  coverage  and  adequate  reimbursement  for  our  drug  products,  the  commercial  success  of  our  drug
products  may  be  greatly  hindered  and  our  financial  condition  and  results  of  operations  may  be  materially  and  adversely
affected.

61

Table of Contents

Product liability lawsuits against us could cause us to incur substantial liabilities and could limit commercialization of
any product candidates that we may develop.

We face an inherent risk of product liability exposure related to the testing of etripamil or any future product candidates in
clinical trials and may face an even greater risk if we commercialize any product candidate that we may develop. If we
cannot  successfully  defend  ourselves  against  claims  that  any  such  product  candidates  caused  injuries,  we  could  incur
substantial liabilities. Regardless of merit or eventual outcome, liability claims may result in:

•

•

•

•

•

•

•

decreased demand for any product candidate that we may develop;

loss of revenue;

substantial monetary awards to trial participants or patients;

significant time and costs to defend the related litigation;

withdrawal of clinical trial participants;

increased insurance costs;

the inability to commercialize any product candidate that we may develop; and injury to our reputation and
significant negative media attention.

Although we maintain clinical trial liability insurance coverage with maximum coverage of $10 million per incident and an
aggregate loss limit of $10 million such insurance may not be adequate to cover all liabilities that we may incur with a
medical product during the clinical trials. We anticipate that we will need to increase our insurance coverage each time we
commence  a  clinical  trial  and  maintain  a  product  liability  insurance  if  we  successfully  commercialize  any  product
candidate.  Insurance  coverage  is  increasingly  expensive.  We  may  not  be  able  to  maintain  insurance  coverage  at  a
reasonable cost or in an amount adequate to satisfy any liability that may arise.

Risks Related to Regulatory Compliance

Even if we obtain and maintain approval for etripamil or any future product candidates from the FDA, we may never
obtain  approval  of  etripamil  or  any  future  product  candidates  outside  of  the  United  States,  which  would  limit  our
market opportunities and could harm our business.

Approval of a product candidate in the United States by the FDA does not ensure approval of such product candidate by
regulatory authorities in other countries or jurisdictions, and approval by one foreign regulatory authority does not ensure
approval  by  regulatory  authorities  in  other  foreign  countries  or  by  the  FDA.  Sales  of  etripamil  or  any  future  product
candidates  outside  of  the  United  States  will  be  subject  to  foreign  regulatory  requirements  governing  clinical  trials  and
marketing  approval.  Even  if  the  FDA  grants  marketing  approval  for  a  product  candidate,  comparable  foreign  regulatory
authorities  also  must  approve  the  manufacturing  and  marketing  of  the  product  candidate  in  those  countries.  Approval
procedures vary among jurisdictions and can involve requirements and administrative review periods different from, and
more onerous than, those in the United States, including additional preclinical studies or clinical trials. In many countries
outside the United States, a product candidate must be approved for reimbursement before it can be approved for sale in
that country. In some cases, the price that we intend to charge for any product candidates, if approved, is also subject to
approval.  Obtaining  approval  for  etripamil  or  any  future  product  candidates  in  the  European  Union  from  the  European
Commission following the opinion of the European Medicines Agency, if we choose to submit a marketing authorization
application  there,  would  be  a  lengthy  and  expensive  process.  Even  if  a  product  candidate  is  approved,  the  FDA  or  the
European  Commission,  as  the  case  may  be,  may  limit  the  indications  for  which  the  drug  may  be  marketed,  require
extensive warnings on the drug labeling or require expensive and time-consuming additional clinical trials or reporting as
conditions of approval. Obtaining foreign regulatory approvals and compliance with foreign regulatory requirements could
result in

62

Table of Contents

significant  delays,  difficulties  and  costs  for  us  and  could  delay  or  prevent  the  introduction  of  etripamil  or  any  future
product candidates in certain countries.

Further,  clinical  trials  conducted  in  one  country  may  not  be  accepted  by  regulatory  authorities  in  other  countries.  Also,
regulatory approval for our product candidates may be withdrawn. If we fail to comply with the regulatory requirements,
our  target  market  will  be  reduced  and  our  ability  to  realize  the  full  market  potential  of  etripamil  or  any  future  product
candidates will be harmed and our business, financial condition, results of operations and prospects could be harmed.

Even  if  we  obtain  regulatory  approval  for  etripamil  or  any  future  product  candidates,  they  will  remain  subject  to
ongoing regulatory oversight.

Even  if  we  obtain  regulatory  approvals  for  etripamil  or  any  future  product  candidates,  such  approvals  will  be  subject  to
ongoing regulatory requirements for manufacturing, labeling, packaging, storage, advertising, promotion, sampling, record-
keeping  and  submission  of  safety  and  other  post-market  information.  Any  regulatory  approvals  that  we  receive  for
etripamil or any future product candidates may also be subject to a REMS, limitations on the approved indicated uses for
which  the  drug  may  be  marketed  or  to  the  conditions  of  approval,  or  contain  requirements  for  potentially  costly  post-
marketing testing, including Phase 4 trials, and surveillance to monitor the quality, safety and efficacy of the drug. Such
regulatory requirements may differ from country to country depending on where we have received regulatory approval.

In addition, drug manufacturers and their facilities are subject to payment of user fees and continual review and periodic
inspections  by  the  FDA  and  other  regulatory  authorities  for  compliance  with  cGMP  requirements  and  adherence  to
commitments  made  in  the  NDA  or  foreign  marketing  application.  If  we,  or  a  regulatory  authority,  discover  previously
unknown problems with a drug, such as adverse events of unanticipated severity or frequency, or problems with the facility
where  the  drug  is  manufactured  or  if  a  regulatory  authority  disagrees  with  the  promotion,  marketing  or  labeling  of  that
drug,  a  regulatory  authority  may  impose  restrictions  relative  to  that  drug,  the  manufacturing  facility  or  us,  including
requesting a recall or requiring withdrawal of the drug from the market or suspension of manufacturing.

If  we  fail  to  comply  with  applicable  regulatory  requirements  following  approval  of  etripamil  or  any  future  product
candidates, a regulatory authority may:

•

•

•

•

•

•

•

•

•

issue an untitled letter or warning letter asserting that we are in violation of the law;

seek an injunction or impose administrative, civil or criminal penalties or monetary fines;

suspend or withdraw regulatory approval;

suspend any ongoing clinical trials;

refuse to approve a pending NDA or comparable foreign marketing application or any supplements thereto
submitted by us or our partners;

restrict the marketing or manufacturing of the drug;

seize or detain the drug or otherwise require the withdrawal of the drug from the market;

refuse to permit the import or export of product candidates; or

refuse to allow us to enter into supply contracts, including government contracts.

Moreover, the FDA strictly regulates the promotional claims that may be made about drug products. In particular, a product
may not be promoted for uses that are not approved by the FDA as reflected in the product’s approved labeling. Physicians,

63

Table of Contents

on  the  other  hand,  may  prescribe  products  for  off-label  uses.  Although  the  FDA  and  other  regulatory  agencies  do  not
regulate  a  physician’s  choice  of  drug  treatment  made  in  the  physician’s  independent  medical  judgment,  they  do  restrict
promotional  communications  from  companies  or  their  sales  force  with  respect  to  off-label  uses  of  products  for  which
marketing  clearance  has  not  been  issued.  However,  biopharmaceutical  companies  may  share  truthful  and  not  misleading
information  that  is  otherwise  consistent  with  the  labeling.  The  FDA  and  other  agencies  actively  enforce  the  laws  and
regulations prohibiting the promotion of off-label uses, and a company that is found to have improperly promoted off-label
uses may be subject to significant civil, criminal and administrative penalties.

Any  government  investigation  of  alleged  violations  of  law  could  require  us  to  expend  significant  time  and  resources  in
response and could generate negative publicity. The occurrence of any event or penalty described above may inhibit our
ability to commercialize etripamil or any future product candidates and harm our business, financial condition, results of
operations and prospects.

The FDA’s and other regulatory authorities’ policies may change, and additional government regulations may be enacted
that  could  prevent,  limit  or  delay  regulatory  approval  of  our  product  candidates.  If  we  are  slow  or  unable  to  adapt  to
changes  in  existing  requirements  or  the  adoption  of  new  requirements  or  policies,  or  if  we  are  not  able  to  maintain
regulatory compliance, we may lose any marketing approval that we may have obtained and we may not achieve or sustain
profitability, which would adversely affect our business, prospects, financial condition and results of operations.

In  addition,  we  cannot  predict  the  likelihood,  nature  or  extent  of  government  regulation  that  may  arise  from  future
legislation or administrative or executive action, either in the United States or abroad.

Our relationships with customers, physicians, and third-party payors are subject, directly or indirectly, to federal and
state  healthcare  fraud  and  abuse  laws,  false  claims  laws,  health  information  privacy  and  security  laws,  and  other
healthcare laws and regulations. If we are unable to comply, or have not fully complied, with such laws, we could face
substantial penalties.

Healthcare providers, including physicians and third-party payors in the United States and elsewhere will play a primary
role  in  the  recommendation  and  prescription  of  any  product  candidates  for  which  we  obtain  marketing  approval.  Our
current  and  future  arrangements  with  healthcare  professionals,  principal  investigators,  consultants,  customers  and  third-
party payors subject us to various federal and state fraud and abuse laws, data privacy and security laws, transparency laws
and other healthcare laws that may constrain the business or financial arrangements and relationships through which we
research, sell, market, and distribute our products, if we obtain marketing approval.

The federal Anti-Kickback Statute prohibits the offer, receipt, or payment of remuneration in exchange for or to induce the
referral of patients or the use of products or services that would be paid for in whole or part by Medicare, Medicaid or other
federal  healthcare  programs.  Remuneration  has  been  broadly  defined  to  include  anything  of  value,  including  cash,
improper discounts, and free or reduced price items and services. Additionally, the intent standard under the federal Anti-
Kickback  Statute  was  amended  by  the  Patient  Protection  and  Affordable  Care  Act,  as  amended  by  the  Health  Care  and
Education Reconciliation Act of 2010, or collectively, PPACA, to a stricter standard such that a person or entity does not
need to have actual knowledge of the statute or specific intent to violate it in order to have committed a violation. Further,
PPACA codified case law that a claim including items or services resulting from a violation of the federal Anti-Kickback
Statute constitutes a false or fraudulent claim for purposes of the False Claims Act.

The federal false claims, including the False Claims Act, and civil monetary penalties laws, which prohibit individuals or
entities from, among other things, knowingly presenting, or causing to be presented, false or fraudulent claims for payment
of federal funds, and knowingly making, or causing to be made, a false record or statement material to a false or fraudulent
claim to avoid, decrease or conceal an obligation to pay money to the federal government.

The federal Health Information Insurance Portability and Accountability Act of 1996, or HIPAA, prohibits, among other
things, knowingly and willfully executing, or attempting to execute, a scheme to defraud any healthcare benefit program,
or knowingly and willfully falsifying, concealing or covering up a material fact or making any materially false statement,

64

Table of Contents

in connection with the delivery of, or payment for, healthcare benefits, items or services. Similar to the U.S. federal Anti-
Kickback Statute, a person or entity does not need to have actual knowledge of the statute or specific intent to violate it in
order to have committed a violation.

HIPAA, as amended by the Health Information Technology for Economic and Clinical Health Act of 2009, or HITECH,
also  imposes,  among  other  things,  certain  standards  and  obligations  on  covered  entities  including  certain  healthcare
providers,  health  plans  and  healthcare  clearinghouses,  and  their  respective  business  associates  that  create,  receive,
maintain,  or  transmit  individually  identifiable  health  information  for  or  on  behalf  of  a  covered  entity  as  well  as  their
covered  subcontractors  relating  to  the  privacy,  security,  transmission  and  breach  reporting  of  individually  identifiable
health information.

The federal Physician Payments Sunshine Act, and its implementing regulations, require certain manufacturers of drugs,
devices,  biologics  and  medical  supplies  that  are  reimbursable  under  Medicare,  Medicaid,  or  the  Children’s  Health
Insurance Program to report annually to Centers for Medicare & Medicaid Services information related to certain payments
and other transfers of value to physicians (defined to include doctors, dentists, optometrists, podiatrists and chiropractors),
  other  healthcare  professionals  (such  as  physician  assistants  and  nurse  practitioners),  and  teaching  hospitals,  as  well  as
ownership and investment interests held by the physicians described above and their immediate family members.

We will also be subject to healthcare regulation and enforcement by the U.S. federal government and the states and any
other countries in which we conduct our business, including our research, and the sales, marketing and distribution of our
product candidates and products once they have obtained marketing authorization.

Analogous state and foreign anti-kickback and false claims laws that may apply to sales or marketing arrangements and
claims  involving  healthcare  items  or  services  reimbursed  by  non-governmental  third  party  payors,  including  private
insurers,  or  that  apply  regardless  of  payor;  state  laws  that  require  pharmaceutical  companies  to  comply  with  the
pharmaceutical  industry’s  voluntary  compliance  guidelines  and  the  relevant  compliance  guidance  promulgated  by  the
federal  government;  state  and  local  laws  that  require  drug  manufacturers  to  report  information  related  to  payments  and
other transfers of value to physicians and other healthcare providers or marketing expenditures; state laws that require the
reporting  of  information  related  to  drug  pricing;  state  and  local  laws  requiring  the  registration  of  pharmaceutical  sales
representatives; and state and foreign laws governing the privacy and security of health information in some circumstances,
many  of  which  differ  from  each  other  in  significant  ways  and  often  are  not  preempted  by  HIPAA,  thus  complicating
compliance efforts.

Ensuring  that  our  business  arrangements  with  third  parties  comply  with  applicable  healthcare  laws  and  regulations  will
likely be costly. It is possible that governmental authorities will conclude that our business practices may not comply with
current  or  future  statutes,  regulations  or  case  law  involving  applicable  fraud  and  abuse  or  other  healthcare  laws  and
regulations. If our operations are found to be in violation of any of these laws or any other governmental regulations that
may  apply  to  us,  we  may  be  subject  to  significant  civil,  criminal  and  administrative  penalties,  damages,  fines,
disgorgement,  imprisonment,  exclusion  from  participating  in  government  funded  healthcare  programs,  such  as  Medicare
and Medicaid, additional reporting requirements and oversight if we become subject to a corporate integrity agreement or
similar agreement to resolve allegations of non-compliance with these laws, contractual damages, reputational harm and
the curtailment or restructuring of our operations.

If the physicians or other providers or entities with whom we expect to do business are found not to be in compliance with
applicable laws, they may be subject to significant criminal, civil or administrative sanctions, including exclusions from
government  funded  healthcare  programs.  Even  if  resolved  in  our  favor,  litigation  or  other  legal  proceedings  relating  to
healthcare  laws  and  regulations  may  cause  us  to  incur  significant  expenses  and  could  distract  our  technical  and
management personnel from their normal responsibilities. In addition, there could be public announcements of the results
of hearings, motions or other interim proceedings or developments. If securities analysts or investors perceive these results
to be negative, it could have a substantial adverse effect on the price of our common shares. Such litigation or proceedings
could substantially increase our operating losses and reduce the resources available for development, manufacturing, sales,
marketing or distribution activities. Uncertainties resulting from the initiation and continuation of litigation or other

65

Table of Contents

proceedings  relating  to  applicable  healthcare  laws  and  regulations  could  have  a  material  adverse  effect  on  our  ability  to
compete in the marketplace.

Healthcare legislative reform measures may have a negative impact on our business and results of operations.

In the United States and some foreign jurisdictions, there have been, and continue to be, several legislative and regulatory
changes and proposed changes regarding the healthcare system that could prevent or delay marketing approval of product
candidates, restrict or regulate post approval activities, and affect our ability to profitably sell any product candidates for
which we obtain marketing approval. In particular, there have been and continue to be a number of initiatives at the U.S.
federal and state levels that seek to reduce healthcare costs and improve the quality of healthcare. For example, in March
2010  the  PPACA,  was  passed,  which  substantially  changed  the  way  healthcare  is  financed  by  both  governmental  and
private payors in the United States. There have been executive, judicial and Congressional challenges to certain aspects of
the PPACA. For example, the Tax Cuts and Jobs Act of 2017, or the Tax Act, was enacted, which included a provision that
repealed,  effective  January  1,  2019,  the  tax  based  shared  responsibility  payment  imposed  by  the  PPACA  on  certain
individuals  who  fail  to  maintain  qualifying  health  coverage  for  all  or  part  of  a  year  that  is  commonly  referred  to  as  the
“individual mandate.” In addition, the 2020 federal spending package permanently eliminated, effective January 1, 2020,
the  PPACA  mandated  “Cadillac”  tax  on  high  cost  employer  sponsored  health  coverage  and  medical  device  tax  and,
effective January 1, 2021, also eliminated the health insurer tax. On December 14, 2018, a Texas U.S. District Court Judge
ruled that the PPACA is unconstitutional in its entirety because the “individual mandate” was repealed by Congress as part
of the Tax Act. Additionally, on June 17, 2021, the U.S. Supreme Court dismissed a challenge on procedural grounds that
argued the PPACA is unconstitutional in its entirety because the “individual mandate” was repealed by Congress. Thus, the
PPACA will remain in effect in its current form. Moreover, prior to the U.S. Supreme Court ruling, on January 28, 2021,
President  Biden  issued  an  executive  order  that  initiated  a  special  enrollment  period  for  purposes  of  obtaining  health
insurance coverage through the PPACA marketplace. The executive order also instructed certain governmental agencies to
review and reconsider their existing policies and rules that limit access to healthcare, including among others, reexamining
Medicaid demonstration projects and waiver programs that include work requirements, and policies that create unnecessary
barriers to obtaining access to health insurance coverage through Medicaid or the PPACA. It is possible that the PPACA
will  be  subject  to  judicial  or  Congressional  challenges  in  the  future.  It  is  unclear  how  any  such  challenges  and  the
healthcare reform measures of the Biden administration will impact the PPACA and our business.

Further, in the United States there has been heightened governmental scrutiny over the manner in which manufacturers set
prices for their marketed products, which has resulted in several Congressional inquiries and proposed and enacted federal
and  state  legislation  designed  to,  among  other  things,  bring  more  transparency  to  drug  pricing,  reduce  the  cost  of
prescription  drugs  under  government  payor  programs,  and  review  the  relationship  between  pricing  and  manufacturer
patient programs. At the federal level, the Trump administration used several means to propose or implement drug pricing
reform, including through federal budget proposals, executive orders and policy initiatives. For example, on July 24, 2020
and September 13, 2020, the Trump administration announced several executive orders related to prescription drug pricing
that  attempted  to  implement  several  of  the  administration’s  proposals.  The  FDA  concurrently  released  a  final  rule  and
guidance in September 2020 implementing a portion of the importation executive order providing pathways for states to
build and submit importation plans for drugs from Canada. Further, on November 20, 2020, the U.S. Department of Health
and  Human  Services,  or  HHS,  finalized  a  regulation  removing  safe  harbor  protection  for  price  reductions  from
pharmaceutical manufacturers to plan sponsors under Part D, either directly or through pharmacy benefit managers, unless
the price reduction is required by law. The rule also creates a new safe harbor for price reductions reflected at the point-of-
sale,  as  well  as  a  new  safe  harbor  for  certain  fixed  fee  arrangements  between  pharmacy  benefit  managers  and
manufacturers. The implementation of the rule has been delayed until January 1, 2026. On November 20, 2020, the Centers
for Medicare & Medicaid Services, or CMS, issued an interim final rule implementing the Trump Administration’s Most
Favored Nation executive order, which would tie Medicare Part B payments for certain physician-administered drugs to the
lowest price paid in other economically advanced countries, effective January 1, 2021. As a result of litigation challenging
the  Most  Favored  Nation  model,  on  December  27,  2021,  CMS  published  a  final  rule  that  rescinded  the  Most  Favored
Nation  model  interim  final  rule.  In  July  2021,  the  Biden  administration  released  an  executive  order,  “Promoting
Competition  in  the  American  Economy,”  with  multiple  provisions  aimed  at  prescription  drugs.  In  response  to  Biden’s
executive order, on September 9, 2021, HHS released a Comprehensive Plan for Addressing High Drug Prices that outlines
principles for drug pricing reform and sets out a variety of potential legislative policies that Congress could pursue as well

66

Table of Contents

as potential administrative actions HHS can take to advance these principles. No legislation or administrative actions have
been  finalized  to  implement  these  principles.  In  addition,  Congress  is  considering  drug  pricing  as  part  of  other  reform
initiatives.  It  is  unclear  whether  these  or  similar  policy  initiatives  will  be  implemented  in  the  future.  At  the  state  level,
legislatures  have  increasingly  passed  legislation  and  implemented  regulations  designed  to  control  pharmaceutical  and
biological product pricing, including price or patient reimbursement constraints, discounts, restrictions on certain product
access and marketing cost disclosure and transparency measures, and, in some cases, designed to encourage importation
from other countries and bulk purchasing. We expect that additional U.S. healthcare reform measures will be adopted in the
future,  any  of  which  could  limit  the  amounts  that  the  U.S.  federal  government  will  pay  for  healthcare  products  and
services,  which  could  result  in  reduced  demand  for  etripamil  or  any  future  product  candidates  or  additional  pricing
pressures. It is also possible that additional governmental action will be taken in response to the COVID-19 pandemic.

In addition, other legislative changes have been proposed and adopted since the PPACA was enacted. On August 2, 2011,
the Budget Control Act of 2011 was signed into law, which includes reductions to Medicare payments to providers of 2%
per  fiscal  year,  which  went  into  effect  on  April  1,  2013  and,  due  to  subsequent  legislative  amendments  to  the  statute,
including the Infrastructure Investment and Jobs Act, will remain in effect through 2031 with the exception of a temporary
suspension  from  May  1,  2020  through  March  31,  2022  due  to  the  ongoing  COVID-19  pandemic,  unless  additional
Congressional action is taken. Under current legislation the actual reduction in Medicare payments will vary from 1% in
2022  to  up  to  3%  in  the  final  fiscal  year  of  this  sequester.  Additionally,  on  March  11,  2021,  President  Biden  signed  the
American  Rescue  Plan  Act  of  2021  into  law,  which  eliminates  the  statutory  Medicaid  drug  rebate  cap,  currently  set  at
100% of a drug’s average manufacturer price, for single source and innovator multiple source drugs, beginning January 1,
2024.  On  January  2,  2013,  the  American  Taxpayer  Relief  Act  of  2012  was  signed  into  law,  which,  among  other  things,
reduced Medicare payments to several providers, including hospitals, and increased the statute of limitations period for the
government to recover overpayments to providers from three to five years.

We  cannot  predict  the  likelihood,  nature  or  extent  of  health  reform  initiatives  that  may  arise  from  future  legislation  or
administrative action in the United States or any other jurisdiction. If we or any third parties we may engage are slow or
unable to adapt to changes in existing or new requirements or policies, or if we or such third parties are not able to maintain
regulatory compliance, etripamil or any future product candidates we may develop may lose any regulatory approval that
may have been obtained and we may not achieve or sustain profitability.

Our  business  involves  the  use  of  hazardous  materials  and  we  and  our  third-party  manufacturers  and  suppliers  must
comply with environmental laws and regulations, which can be expensive and restrict how we do business.

Our research and development activities and our third-party manufacturers’ and suppliers’ activities involve the controlled
storage,  use  and  disposal  of  hazardous  materials  owned  by  us,  including  the  components  of  etripamil  and  any  future
product  candidates  and  other  hazardous  compounds.  We  and  our  manufacturers  and  suppliers  are  subject  to  laws  and
regulations  governing  the  use,  manufacture,  storage,  handling  and  disposal  of  these  hazardous  materials.  In  some  cases,
these  hazardous  materials  and  various  wastes  resulting  from  their  use  are  stored  at  our  and  our  manufacturers’  facilities
pending their use and disposal. We cannot eliminate the risk of contamination, which could cause an interruption of our
commercialization  efforts,  research  and  development  efforts  and  business  operations,  environmental  damage  resulting  in
costly clean-up and liabilities under applicable laws and regulations governing the use, storage, handling and disposal of
these  materials  and  specified  waste  products.  Although  we  believe  that  the  safety  procedures  utilized  by  our  third-party
manufacturers for handling and disposing of these materials generally comply with the standards prescribed by these laws
and regulations, we cannot guarantee that this is the case or eliminate the risk of accidental contamination or injury from
these  materials.  In  such  an  event,  we  may  be  held  liable  for  any  resulting  damages  and  such  liability  could  exceed  our
resources and state or federal or other applicable authorities may curtail our use of certain materials and/or interrupt our
business operations. Furthermore, environmental laws and regulations are complex, change frequently and have tended to
become more stringent. We cannot predict the impact of such changes and cannot be certain of our future compliance. We
do not currently carry hazardous waste insurance coverage.

67

Table of Contents

Risks Related to Our Dependence on Third Parties

We  will  rely  on  third  parties  to  produce  clinical  and  commercial  supplies  of  etripamil  and  any  future  product
candidates.

We do not own or operate facilities for drug manufacturing, storage and distribution, or testing. We are dependent on third
parties  to  manufacture  the  clinical  supplies  of  etripamil  and  any  future  product  candidates.  The  facilities  used  by  our
contract manufacturers to manufacture etripamil and any future product candidates must be approved by the FDA pursuant
to inspections that will be conducted after we submit our NDA to the FDA. We do not control the manufacturing process
of, and are completely dependent on, our contract manufacturing partners for compliance with the regulatory requirements,
known as cGMPs for manufacture of active drug substances, nasal spray device, and finished product candidates. If our
contract  manufacturers  cannot  successfully  manufacture  material  that  conforms  to  our  specifications  and  the  strict
regulatory requirements of the FDA or others, we will not be able to secure and/or maintain regulatory approval for our
product  candidates.  In  addition,  we  have  no  control  over  the  ability  of  our  contract  manufacturers  to  maintain  adequate
quality control, quality assurance and qualified personnel. We intend to use multiple contract manufacturers for clinical and
commercial supply of our drug product and drug substance. As such, we will need to demonstrate to the FDA that the drug
product and drug substance from these contract manufacturers are comparable, which may include conducting additional
equivalence  studies.  If  the  FDA  or  a  comparable  foreign  regulatory  authority  does  not  approve  these  facilities  for  the
manufacture of our product candidates or if it withdraws any such approval in the future, we may need to find alternative
manufacturing facilities, which would significantly impact our ability to develop, obtain regulatory approval for or market
our  product  candidates,  if  approved.  Any  significant  delay  in  the  supply  of  a  product  candidate,  or  the  raw  material
components thereof, for an ongoing clinical trial due to the need to replace a third-party manufacturer could considerably
delay completion of our clinical trials, product testing and potential regulatory approval of our product candidates.

Further, we also will rely on third-party manufacturers to supply us with sufficient quantities of etripamil and any future
product  candidates,  if  approved,  for  commercialization.  We  do  not  yet  have  a  commercial  supply  agreement  for
commercial quantities of drug substance, drug product or nasal spray device. If we are not able to meet market demand for
any  approved  product,  it  would  negatively  affect  our  ability  to  generate  revenue,  harm  our  reputation,  and  could  have  a
material and adverse effect on our business and financial condition. Increasing the scale of production inherently creates
increased risk of manufacturing errors, and we may not be able to adequately inspect every device that is produced, and it
is possible that individual devices may fail to perform as designed. Manufacturing errors could negatively impact market
acceptance  of  any  of  our  product  candidates  that  receive  approval,  result  in  negative  press  coverage,  or  increase  our
liability.

Further,  our  reliance  on  third-party  manufacturers  entails  risks  to  which  we  would  not  be  subject  if  we  manufactured
product candidates ourselves, including:

•

•

•

•

•

•

inability to meet our product specifications and quality requirements consistently;

delay or inability to procure or expand sufficient manufacturing capacity;

issues related to scale-up of manufacturing;

costs and validation of new equipment and facilities required for scale-up;

our third-party manufacturers may not be able to execute our manufacturing procedures and other logistical
support requirements appropriately;

our third-party manufacturers may fail to comply with cGMP-compliance and other inspections by the FDA
or other comparable regulatory authorities;

68

Table of Contents

•

•

•

•

•

•

our inability to negotiate manufacturing agreements with third parties under commercially reasonable terms,
if at all;

breach, termination or nonrenewal of manufacturing agreements with third parties in a manner or at a time
that is costly or damaging to us;

reliance on a single source for the nasal spray device;

our third-party manufacturers may not devote sufficient resources to our product candidates;

we  may  not  own,  or  may  have  to  share,  the  intellectual  property  rights  to  any  improvements  made  by  our
third-party manufacturers in the manufacturing process for our product candidates;

operations  of  our  third  party  manufacturers  or  suppliers  could  be  disrupted  by  conditions  unrelated  to  our
business  or  operations,  including  public  health  emergencies,  such  as  the  COVID-19  pandemic,  natural
disasters,  such  as  earthquakes,  fires  or  floods,  the  bankruptcy  of  the  manufacturer  or  supplier,  carrier
disruptions or increased costs that are beyond our control, and global macro uncertainty related to the Ukraine
– Russia crisis.

In addition, if we enter into a strategic collaboration with a third party for the commercialization of etripamil or any future
product candidate, we will not be able to control the amount of time or resources that they devote to such efforts. If any
strategic  collaborator  does  not  commit  adequate  resources  to  the  marketing  and  distribution  of  etripamil  or  any  future
product candidate, it could limit our potential revenues.

Any  of  these  events  could  lead  to  clinical  trial  delays,  failure  to  obtain  regulatory  approval  or  affect  our  ability  to
successfully commercialize etripamil or any future product candidates once approved. Some of these events could be the
basis for FDA action, including injunction, request for recall, seizure, or total or partial suspension of production.

We rely on third parties to conduct, supervise and monitor our preclinical studies and clinical trials, and if those third
parties perform in an unsatisfactory manner, it may harm our business.

We  have  engaged  CROs  to  conduct  our  Phase  3  clinical  trials  of  etripamil  for  the  treatment  of  PSVT,  and  our  Phase  2
clinical  trial  of  etripamil  for  the  treatment  of  AFib-RVR,  and  we  expect  to  engage  a  CRO  for  future  clinical  trials  of
etripamil  and  any  future  product  candidates.  We  do  not  currently  have  the  ability  to  independently  conduct  any  clinical
trials.  We  rely  on  CROs  and  clinical  trial  sites  to  ensure  the  proper  and  timely  conduct  of  our  preclinical  studies  and
clinical trials, and we expect to have limited influence over their actual performance. We rely upon CROs to monitor and
manage  data  for  our  clinical  programs,  as  well  as  the  execution  of  future  nonclinical  studies.  We  expect  to  control  only
certain  aspects  of  our  CROs’  activities.  Nevertheless,  we  will  be  responsible  for  ensuring  that  each  of  our  preclinical
studies and clinical trials is conducted in accordance with the applicable protocol, legal, regulatory and scientific standards,
and our reliance on the CROs does not relieve us of our regulatory responsibilities.

We and our CROs are required to comply with the good laboratory practices, or GLPs, and GCPs, which are regulations
and guidelines enforced by the FDA and comparable foreign regulatory authorities in the form of International Conference
on  Harmonization  guidelines  for  any  of  our  product  candidates  that  are  in  preclinical  and  clinical  development.  The
regulatory authorities enforce GCPs through periodic inspections of trial sponsors, principal investigators and clinical trial
sites. Although we rely on CROs to conduct GCP-compliant clinical trials, we remain responsible for ensuring that each of
our  GLP  preclinical  studies  and  clinical  trials  is  conducted  in  accordance  with  its  investigational  plan  and  protocol  and
applicable laws and regulations, and our reliance on the CROs does not relieve us of our regulatory responsibilities. If we
or our CROs fail to comply with GCPs, the clinical data generated in our clinical trials may be deemed unreliable, and the
FDA or comparable foreign regulatory authorities may require us to perform additional clinical trials before approving our
marketing applications. Accordingly, if our CROs fail to comply with these regulations or fail to recruit a sufficient number
of subjects, we may be required to repeat clinical trials, which would delay the regulatory approval process.

69

Table of Contents

Our  reliance  on  third  parties  to  conduct  clinical  trials  will  result  in  less  direct  control  over  the  management  of  data
developed through clinical trials than would be the case if we were relying entirely upon our own staff. Any failure by third
parties to prevent unauthorized access, use or disclosure of data, including personal information regarding our patients or
employees, could harm our reputation, cause us not to comply with federal and/or state breach notification laws and foreign
law  equivalents  and  otherwise  subject  us  to  liability  under  laws  and  regulations  that  protect  the  privacy  and  security  of
personal information.

Communicating with CROs and other third parties can be challenging, potentially leading to mistakes as well as difficulties
in coordinating activities. Such parties may:

•

•

•

•

•

have staffing difficulties;

fail to comply with contractual obligations;

experience regulatory compliance issues;

experience  business  disruptions  from  public  health  emergencies,  such  as  the  COVID-19  pandemic,  and
accompanying shelter in place orders; or

undergo changes in priorities or become financially distressed.

These factors may materially adversely affect the willingness or ability of third parties to conduct our clinical trials and
may subject us to unexpected cost increases that are beyond our control. If our CROs do not successfully carry out their
contractual  duties  or  obligations,  fail  to  meet  expected  deadlines,  fail  to  comply  with  regulatory  requirements,  or  if  the
quality or accuracy of the clinical data they obtain is compromised due to the failure to adhere to our clinical protocols or
regulatory requirements or for any other reasons, our clinical trials may be extended, delayed or terminated, and we may
not be able to obtain regulatory approval for, or successfully commercialize, any product candidate that we develop. As a
result, our financial results and the commercial prospects for any product candidate that we develop would be harmed, our
costs could increase, and our ability to generate revenue could be delayed. While we will have agreements governing their
activities,  our  CROs  will  not  be  our  employees,  and  we  will  not  control  whether  or  not  they  devote  sufficient  time  and
resources to our future clinical and nonclinical programs. These CROs may also have relationships with other commercial
entities,  including  our  competitors,  for  whom  they  may  also  be  conducting  clinical  trials,  or  other  drug  development
activities  that  could  harm  our  business.  We  face  the  risk  of  potential  unauthorized  disclosure  or  misappropriation  of  our
intellectual property by CROs, which may reduce our trade secret protection and allow our potential competitors to access
and exploit our proprietary technology.

If  our  relationship  with  any  of  these  CROs  terminates,  we  may  not  be  able  to  enter  into  arrangements  with  alternative
CROs  or  do  so  on  commercially  reasonable  terms.  Switching  or  adding  additional  CROs  involves  substantial  cost  and
requires management time and focus. In addition, there is a natural transition period when a new CRO commences work.
As  a  result,  delays  occur,  which  can  negatively  affect  our  ability  to  meet  our  desired  clinical  development  timelines.
Though  we  intend  to  manage  carefully  our  relationships  with  our  CROs,  there  can  be  no  assurance  that  we  will  not
encounter  challenges  or  delays  in  the  future  or  that  these  delays  or  challenges  will  not  have  a  negative  impact  on  our
business, financial condition and prospects.

In addition, principal investigators for our clinical trials may serve as scientific advisors or consultants to us from time to
time  and  receive  compensation  in  connection  with  such  services.  Under  certain  circumstances,  we  may  be  required  to
report  some  of  these  relationships  to  the  FDA.  The  FDA  may  conclude  that  a  financial  relationship  between  us  and  a
principal  investigator  has  created  a  conflict  of  interest  or  otherwise  affected  interpretation  of  the  trial.  The  FDA  may
therefore question the integrity of the data generated at the applicable clinical trial site and the utility of the clinical trial
itself may be jeopardized. This could result in a delay in approval, or rejection, of our marketing applications by the FDA
and may ultimately lead to the denial of marketing approval of etripamil and any future product candidates.

70

Table of Contents

Etripamil is intended to be used with a nasal-spray device, which may result in additional regulatory and supply risks.

Etripamil is administered through a nasal-spray device that we obtain from a single source supplier, and that supplier is
relying on multiple component suppliers, some of whom are single source suppliers. There are a limited number of device
suppliers that address our particular design requirements. While we intend to explore alternative nasal spray devices for the
delivery of etripamil that are produced by other suppliers to have backup sources for future commercial needs, we may not
identify other nasal device suppliers that meet our requirements, and such alternative devices may not be as effective at the
delivery of etripamil as our current supplier’s device. We do not currently have a formal supply agreement with our current
sole nasal spray device supplier, and obtain such devices as needed. Even if we reach agreement for commercial supply, if
we  do  not  have  additional  nasal  spray  device  suppliers,  our  sole  supplier  may  be  unable  to  meet  our  demands.
Unpredictability of supply could have a material adverse effect on our commercialization plans for etripamil, if approved,
and could have a material adverse effect on our business and financial condition.

Our finished drug product in the intra-nasal delivery system will be regulated as a drug/device combination product. We
may experience delays in obtaining regulatory approval of etripamil given the increased complexity of the review process
when approval of the product and a delivery device is sought under a single marketing application. In the United States,
each  component  of  a  combination  product  is  subject  to  the  requirements  established  by  the  FDA  for  that  type  of
component, whether a drug, biologic, or device. The delivery system device would be subject to FDA device requirements
regarding design, performance and validation as well as human factors testing, among other things.

Delays in or failure of the studies conducted by us, or failure of our company, our collaborators, if any, or the third-party
providers or suppliers to obtain or maintain regulatory approval could result in increased development costs, delays in or
failure to obtain regulatory approval, and associated delays in etripamil reaching the market. Further, failure to successfully
develop or supply the device, or to gain or maintain its approval, could adversely affect sales of etripamil.

Risks Related to Our Intellectual Property

If we are unable to obtain and maintain patent protection for etripamil or any future product candidates, or if the scope
of  the  patent  protection  obtained  is  not  sufficiently  broad,  our  competitors  could  develop  and  commercialize  drugs
similar or identical to ours, and our ability to commercialize successfully our product candidates may be impaired.

Our  success  depends  in  large  part  on  our  ability  to  obtain  and  maintain  patent  protection  in  the  United  States  and  other
countries with respect to etripamil and any future product candidates. We seek to protect our proprietary position by filing
patent  applications  in  the  United  States  and  abroad  related  to  our  product  candidates.  The  patent  application  and
prosecution process is expensive and time-consuming. We may not be able to file and prosecute all necessary or desirable
patent  applications  at  a  reasonable  cost  or  in  a  timely  manner.  We  may  also  fail  to  identify  patentable  aspects  of  our
research  and  development  before  it  is  too  late  to  obtain  patent  protection.  Therefore,  these  and  any  of  our  patents  and
applications  may  not  be  prosecuted  and  enforced  in  a  manner  consistent  with  the  best  interests  of  our  business.  It  is
possible that defects of form in the preparation or filing of our patents or patent applications may exist, or may arise in the
future, such as with respect to proper priority claims, inventorship, claim scope or patent term adjustments. If any future
licensors or licensees are not fully cooperative or disagree with us as to the prosecution, maintenance or enforcement of
any patent rights, such patent rights could be compromised and we might not be able to prevent third parties from making,
using  and  selling  competing  products.  If  there  are  material  defects  in  the  form  or  preparation  of  our  patents  or  patent
applications, such patents or applications may be invalid and unenforceable. Moreover, our competitors may independently
develop  equivalent  knowledge,  methods  and  know-how.  Any  of  these  outcomes  could  impair  our  ability  to  prevent
competition from third parties.

The patent position of biotechnology and pharmaceutical companies generally is highly uncertain. Changes in either the
patent  laws  or  interpretation  of  the  patent  laws  in  the  United  States  and  other  countries  may  diminish  the  value  of  our
patents or narrow the scope of our patent protection. In addition, the laws of foreign countries may not protect our rights to
the  same  extent  as  the  laws  of  the  United  States.  No  consistent  policy  regarding  the  breadth  of  claims  allowed  in
biotechnology and pharmaceutical patents has emerged to date in the United States or in many foreign jurisdictions. In

71

Table of Contents

addition,  the  determination  of  patent  rights  with  respect  to  pharmaceutical  compounds  and  technologies  commonly
involves complex legal and factual questions, which has in recent years been the subject of much litigation. As a result, the
issuance, scope, validity, enforceability and commercial value of our patent rights are highly uncertain. Furthermore, recent
changes in patent laws in the United States, including the America Invents Act of 2011, may affect the scope, strength and
enforceability of our patent rights or the nature of proceedings that may be brought by us related to our patent rights.

We may not be aware of all third-party intellectual property rights potentially relating to etripamil or any future product
candidates.  Publications  of  discoveries  in  the  scientific  literature  often  lag  behind  the  actual  discoveries,  and  patent
applications in the United States and other jurisdictions are typically not published until 18 months after filing, or in some
cases not at all. For example, U.S. applications filed before November 28, 2000 and certain U.S. applications filed after
that date that will not be filed outside the United States remain confidential until a patent issues. Therefore, we cannot be
certain that we were the first to make the inventions claimed in our patents or pending patent applications, or that we were
the first to file for patent protection of such inventions. Similarly, should we own any patents or patent applications in the
future, we may not be certain that we were the first to file for patent protection for the inventions claimed in such patents or
patent applications. As a result, the issuance, scope, validity and commercial value of our patent rights cannot be predicted
with any certainty. Moreover, we may be subject to a third-party pre-issuance submission of prior art to the U.S. Patent and
Trademark Office, or USPTO, or become involved in opposition, derivation, reexamination, inter parties review, post grant
review, or interference proceedings, in the United States or elsewhere, challenging our patent rights or the patent rights of
others. An adverse determination in any such submission, proceeding or litigation could reduce the scope of, or invalidate,
our patent rights, allow third parties to commercialize our technology or product candidates and compete directly with us,
without payment to us, or result in our inability to manufacture or commercialize products without infringing third-party
patent rights.

Our pending and future patent applications may not result in patents being issued that protect our technology or product
candidates,  in  whole  or  in  part,  or  which  effectively  prevent  others  from  commercializing  competitive  technologies  and
products.  Even  if  our  patent  applications  issue  as  patents,  they  may  not  issue  in  a  form  that  will  provide  us  with  any
meaningful  protection  against  competing  products  or  processes  sufficient  to  achieve  our  business  objectives,  prevent
competitors from competing with us or otherwise provide us with any competitive advantage. Our competitors may be able
to  circumvent  our  owned  or  licensed  patents  by  developing  similar  or  alternative  technologies  or  products  in  a  non-
infringing  manner.  Our  competitors  may  seek  to  market  generic  versions  of  any  approved  products  by  submitting
abbreviated  new  drug  applications  to  the  FDA  in  which  they  claim  that  patents  owned  or  licensed  by  us  are  invalid,
unenforceable and/or not infringed. Alternatively, our competitors may seek approval to market their own products similar
to or otherwise competitive with our products. In these circumstances, we may need to defend and/or assert our patents,
including by filing lawsuits alleging patent infringement. In any of these types of proceedings, a court or other agency with
jurisdiction may find our patents invalid and/or unenforceable.

The  issuance  of  a  patent  is  not  conclusive  as  to  its  inventorship,  scope,  validity  or  enforceability,  and  our  owned  and
licensed patents may be challenged in the courts or patent offices in the United States and abroad. Such challenges may
result in loss of exclusivity or freedom to operate or in patent claims being narrowed, invalidated or held unenforceable, in
whole or in part, which could limit our ability to stop others from using or commercializing similar or identical technology
and products, or limit the duration of the patent protection of our technology and products. In addition, given the amount of
time  required  for  the  development,  testing  and  regulatory  review  of  new  product  candidates,  patents  protecting  such
candidates might expire before or shortly after such candidates are commercialized.

Obtaining  and  maintaining  our  patent  protection  depends  on  compliance  with  various  procedural,  document
submission,  fee  payment  and  other  requirements  imposed  by  government  patent  agencies,  and  our  patent  protection
could be reduced or eliminated for non-compliance with these requirements.

The  USPTO  and  various  foreign  governmental  patent  agencies  require  compliance  with  a  number  of  procedural,
documentary,  fee  payment  and  other  similar  provisions  during  the  patent  application  process.  In  addition,  periodic
maintenance fees, renewal fees, annuity fees and various other government fees on patents and/or applications will have to
be paid to the USPTO and various government patent agencies outside of the United States over the lifetime of our

72

Table of Contents

owned  patents  and/or  applications  and  any  patent  rights  we  may  own  or  license  in  the  future.  We  rely  on  our  outside
counsel to pay these fees due to non-U.S. patent agencies. The USPTO and various non-U.S. government patent agencies
require  compliance  with  several  procedural,  documentary,  fee  payment  and  other  similar  provisions  during  the  patent
application process. We employ reputable law firms and other professionals to help us comply.

Non-compliance  events  that  could  result  in  abandonment  or  lapse  of  a  patent  or  patent  application  include,  but  are  not
limited to, failure to respond to official actions within prescribed time limits, non-payment of fees and failure to properly
legalize and submit formal documents. If we fail to maintain the patents and patent applications covering our products or
technologies, we may not be able to stop a competitor from marketing products that are the same as or similar to etripamil
or  any  future  product  candidates,  which  would  have  a  material  adverse  effect  on  our  business.  In  many  cases,  an
inadvertent lapse can be cured by payment of a late fee or by other means in accordance with the applicable rules. There
are situations, however, in which non-compliance can result in abandonment or lapse of the patent or patent application,
resulting  in  partial  or  complete  loss  of  patent  rights  in  the  relevant  jurisdiction.  In  such  an  event,  potential  competitors
might be able to enter the market and this circumstance could harm our business.

Patent terms may be inadequate to protect our competitive position on our product candidates for an adequate amount
of time.

Given the amount of time required for the development, testing and regulatory review of new product candidates, such as
etripamil, patents protecting such candidates might expire before or shortly after such candidates are commercialized. We
expect to seek extensions of patent terms in the United States and, if available, in other countries where we are prosecuting
patents. In the United States, the Drug Price Competition and Patent Term Restoration Act of 1984 permits a patent term
extension of up to five years beyond the normal expiration of the patent, which is limited to the approved indication (or any
additional  indications  approved  during  the  period  of  extension).  However,  the  applicable  authorities,  including  the  FDA
and the USPTO in the United States, and any equivalent regulatory authority in other countries, may not agree with our
assessment of whether such extensions are available, and may refuse to grant extensions to our patents, or may grant more
limited  extensions  than  we  request.  If  this  occurs,  our  competitors  may  be  able  to  take  advantage  of  our  investment  in
development  and  clinical  trials  by  referencing  our  clinical  and  preclinical  data  and  launch  their  drug  earlier  than  might
otherwise be the case.

Intellectual property rights do not necessarily address all potential threats to our business.

The degree of future protection afforded by our intellectual property rights is uncertain because intellectual property rights
have limitations and may not adequately protect our business. The following examples are illustrative:

•

•

•

•

•

•

others  may  be  able  to  make  compounds  or  formulations  that  are  similar  to  etripamil  or  formulations  of
etripamil or our future product candidates but that are not covered by the claims of any patents, should they
issue, that we own or control;

we  or  any  strategic  partners  might  not  have  been  the  first  to  make  the  inventions  covered  by  the  issued
patents or pending patent applications that we own or control;

we might not have been the first to file patent applications covering certain of our inventions;

others  may  independently  develop  similar  or  alternative  technologies  or  duplicate  any  of  our  technologies
without infringing our intellectual property rights;

it is possible that our pending patent applications will not lead to issued patents;

issued patents that we own or control may not provide us with any competitive advantages, or may be held
invalid or unenforceable as a result of legal challenges;

73

Table of Contents

•

•

our competitors might conduct research and development activities in the United States and other countries
that provide a safe harbor from patent infringement claims for certain research and development activities, as
well  as  in  countries  where  we  do  not  have  patent  rights  and  then  use  the  information  learned  from  such
activities to develop competitive drugs for sale in our major commercial markets;

we  may  not  develop  additional  proprietary  technologies  that  are  patentable;  and  the  patents  of  others  may
have an adverse effect on our business.

Should any of these events occur, they could have a material adverse effect on our business, financial condition, results of
operations and prospects.

We may become involved in lawsuits to protect or enforce our patents or other intellectual property rights, which could
be expensive, time consuming and unsuccessful.

Competitors  may  infringe  our  issued  patents,  future  trademarks,  copyrights  or  other  intellectual  property.  To  counter
infringement  or  unauthorized  use,  we  may  be  required  to  file  infringement  claims,  which  can  be  expensive  and  time-
consuming  and  divert  the  time  and  attention  of  our  management  and  scientific  personnel.  Any  claims  we  assert  against
perceived infringers could provoke these parties to assert counterclaims against us alleging that we infringe their patents,
trademarks, copyrights or other intellectual property. In addition, in a patent infringement proceeding, there is a risk that a
court will decide that a patent of ours is invalid or unenforceable, in whole or in part, and that we do not have the right to
stop the other party from using the invention at issue. There is also a risk that, even if the validity of such patents is upheld,
the court will construe the patent’s claims narrowly or decide that we do not have the right to stop the other party from
using the invention at issue on the grounds that our patents do not cover the invention. An adverse outcome in a litigation
or proceeding involving our patents could limit our ability to assert our patents against those parties or other competitors,
and may curtail or preclude our ability to exclude third parties from making and selling similar or competitive products.
Similarly, if we assert trademark infringement claims, a court may determine that the marks we have asserted are invalid or
unenforceable, or that the party against whom we have asserted trademark infringement has superior rights to the marks in
question. In this case, we could ultimately be forced to cease use of such trademarks.

In  any  infringement  litigation,  any  award  of  monetary  damages  we  receive  may  not  be  commercially  valuable.
Furthermore,  because  of  the  substantial  amount  of  discovery  required  in  connection  with  intellectual  property  litigation,
there is a risk that some of our confidential information could be compromised by disclosure during litigation. In addition,
there could be public announcements of the results of hearings, motions or other interim proceedings or developments and
if securities analysts or investors perceive these results to be negative, it could have a substantial adverse effect on the price
of our common shares. Moreover, there can be no assurance that we will have sufficient financial or other resources to file
and pursue such infringement claims, which typically last for years before they are concluded. Some of our competitors
may  be  able  to  sustain  the  costs  of  such  litigation  or  proceedings  more  effectively  than  we  can  because  of  their  greater
financial resources and more mature and developed intellectual property portfolios. Even if we ultimately prevail in such
claims, the monetary cost of such litigation and the diversion of the attention of our management and scientific personnel
could outweigh any benefit we receive as a result of the proceedings. Accordingly, despite our efforts, we may not be able
to  prevent  third  parties  from  infringing,  misappropriating  or  successfully  challenging  our  intellectual  property  rights.
Uncertainties resulting from the initiation and continuation of patent litigation or other proceedings could have a negative
impact on our ability to compete in the marketplace.

Third  parties  may  initiate  legal  proceedings  alleging  that  we  are  infringing  their  intellectual  property  rights,  the
outcome of which would be uncertain and could have a negative impact on the success of our business.

Our  commercial  success  depends,  in  part,  upon  our  ability  and  the  ability  of  future  collaborators,  if  any,  to  develop,
manufacture,  market  and  sell  etripamil  and  any  future  product  candidates  and  use  our  proprietary  technologies  without
infringing the proprietary rights and intellectual property of third parties. The biotechnology and pharmaceutical industries
are characterized by extensive and complex litigation regarding patents and other intellectual property rights. We may in
the future become party to, or be threatened with, adversarial proceedings or litigation regarding intellectual property rights

74

Table of Contents

with respect to etripamil and any future product candidates and technology, including interference proceedings, post grant
review  and  inter  partes  review  before  the  USPTO.  Third  parties  may  assert  infringement  claims  against  us  based  on
existing patents or patents that may be granted in the future, regardless of their merit. There is a risk that third parties may
choose to engage in litigation with us to enforce or to otherwise assert their patent rights against us. Even if we believe
such  claims  are  without  merit,  a  court  of  competent  jurisdiction  could  hold  that  these  third-party  patents  are  valid,
enforceable and infringed, which could have a negative impact on our ability to commercialize our current and any future
product candidates. In order to successfully challenge the validity of any such U.S. patent in federal court, we would need
to overcome a presumption of validity. As this burden is a high one requiring us to present clear and convincing evidence
as  to  the  invalidity  of  any  such  U.S.  patent  claim,  there  is  no  assurance  that  a  court  of  competent  jurisdiction  would
invalidate the claims of any such U.S. patent. If we are found to infringe a third party’s valid and enforceable intellectual
property rights, we could be required to obtain a license from such third party to continue developing, manufacturing and
marketing  our  product  candidate(s)  and  technology.  However,  we  may  not  be  able  to  obtain  any  required  license  on
commercially reasonable terms or at all. Even if we were able to obtain a license, it could be non-exclusive, thereby giving
our  competitors  and  other  third  parties  access  to  the  same  technologies  licensed  to  us,  and  it  could  require  us  to  make
substantial  licensing  and  royalty  payments.  We  could  be  forced,  including  by  court  order,  to  cease  developing,
manufacturing and commercializing the infringing technology or product candidate. In addition, we could be found liable
for monetary damages, including treble damages and attorneys’ fees, if we are found to have willfully infringed a patent or
other  intellectual  property  right.  A  finding  of  infringement  could  prevent  us  from  manufacturing  and  commercializing
etripamil  or  any  future  product  candidates  or  force  us  to  cease  some  or  all  of  our  business  operations,  which  could
materially harm our business. Claims that we have misappropriated the confidential information or trade secrets of third
parties could have a similar negative impact on our business, financial condition, results of operations and prospects. See
the section herein titled “Legal Proceedings” for additional information.

We may need to license intellectual property from third parties, and such licenses may not be available or may not be
available on commercially reasonable terms.

A  third  party  may  hold  intellectual  property  rights,  including  patent  rights,  that  are  important  or  necessary  to  the
development of etripamil or any future product candidates. It may be necessary for us to use the patented or proprietary
technology of third parties to commercialize our product candidates, in which case we would be required to obtain a license
from these third parties. Such a license may not be available on commercially reasonable terms, or at all, and we could be
forced to accept unfavorable contractual terms. If we are unable to obtain such licenses on commercially reasonable terms,
our business could be harmed.

We  may  be  subject  to  claims  asserting  that  our  employees,  consultants  or  advisors  have  wrongfully  used  or  disclosed
alleged trade secrets of their current or former employers or claims asserting ownership of what we regard as our own
intellectual property.

Many  of  our  employees,  consultants  or  advisors  are  currently,  or  were  previously,  employed  at  universities  or  other
biotechnology or pharmaceutical companies, including our competitors or potential competitors. Although we try to ensure
that our employees, consultants and advisors do not use the proprietary information or know-how of others in their work
for us, we may be subject to claims that these individuals or we have used or disclosed intellectual property, including trade
secrets or other proprietary information, of any such individual’s current or former employer. Litigation may be necessary
to defend against these claims. If we fail in defending any such claims, in addition to paying monetary damages, we may
lose valuable intellectual property rights or personnel. Even if we are successful in defending against such claims, litigation
could result in substantial costs and be a distraction to management.

In addition, we may in the future be subject to claims by our former employees or consultants asserting an ownership right
in  our  patents  or  patent  applications,  as  a  result  of  the  work  they  performed  on  our  behalf.  Although  it  is  our  policy  to
require  our  employees  and  contractors  who  may  be  involved  in  the  development  of  intellectual  property  to  execute
agreements assigning such intellectual property to us, we may be unsuccessful in executing such an agreement with each
party who, in fact, conceives or develops intellectual property that we regard as our own, and we cannot be certain that our
agreements with such parties will be upheld in the face of a potential challenge or that they will not be breached, for which
we may not have an adequate remedy. The assignment of intellectual property rights may not be self-executing or

75

Table of Contents

the assignment agreements may be breached, and we may be forced to bring claims against third parties, or defend claims
that they may bring against us, to determine the ownership of what we regard as our intellectual property.

Changes in U.S. patent law or the patent law of other countries or jurisdictions could diminish the value of patents in
general, thereby impairing our ability to protect etripamil and any future product candidates.

The United States has recently enacted and implemented wide ranging patent reform legislation. The U.S. Supreme Court
has  ruled  on  several  patent  cases  in  recent  years,  either  narrowing  the  scope  of  patent  protection  available  in  certain
circumstances  or  weakening  the  rights  of  patent  owners  in  certain  situations.  In  addition  to  increasing  uncertainty  with
regard to our ability to obtain patents in the future, this combination of events has created uncertainty with respect to the
value of patents, once obtained. Depending on actions by the U.S. Congress, the federal courts, and the USPTO, the laws
and regulations governing patents could change in unpredictable ways that could weaken our ability to obtain new patents
or  to  enforce  patents  that  we  have  licensed  or  that  we  might  obtain  in  the  future.  Similarly,  changes  in  patent  law  and
regulations in other countries or jurisdictions, changes in the governmental bodies that enforce them or changes in how the
relevant  governmental  authority  enforces  patent  laws  or  regulations  may  weaken  our  ability  to  obtain  new  patents  or  to
enforce patents that we have licensed or that we may obtain in the future.

We may not be able to protect our intellectual property rights throughout the world, which could negatively impact our
business.

Filing,  prosecuting  and  defending  patents  on  product  candidates  in  all  countries  throughout  the  world  would  be
prohibitively  expensive,  and  our  intellectual  property  rights  in  some  countries  outside  the  United  States  could  be  less
extensive  than  those  in  the  United  States.  In  some  cases,  we  may  not  be  able  to  obtain  patent  protection  for  certain
technology outside the United States. In addition, the laws of some foreign countries do not protect intellectual property
rights to the same extent as federal and state laws in the United States, even in jurisdictions where we do pursue patent
protection. Consequently, we may not be able to prevent third parties from practicing our inventions in all countries outside
the United States, even in jurisdictions where we do pursue patent protection or from selling or importing products made
using our inventions in and into the United States or other jurisdictions.

Many companies have encountered significant problems in protecting and defending intellectual property rights in foreign
jurisdictions. The legal systems of certain countries, particularly certain developing countries, do not favor the enforcement
of patents and other intellectual property protection, which could make it difficult for us to stop the infringement of our
patents,  if  pursued  and  obtained,  or  marketing  of  competing  products  in  violation  of  our  proprietary  rights  generally.
Proceedings to enforce our patent rights in foreign jurisdictions could result in substantial costs and divert our efforts and
attention from other aspects of our business, could put our patents at risk of being invalidated or interpreted narrowly and
our patent applications at risk of not issuing and could provoke third parties to assert claims against us. We may not prevail
in any lawsuits that we initiate and the damages or other remedies awarded, if any, may not be commercially meaningful.
Accordingly,  our  efforts  to  enforce  our  intellectual  property  rights  around  the  world  may  be  inadequate  to  obtain  a
significant commercial advantage from the intellectual property that we develop or license.

Reliance  on  third  parties  requires  us  to  share  our  proprietary  information,  which  increases  the  possibility  that  such
information will be misappropriated or disclosed.

Because  we  rely  on  third  parties  to  develop  and  manufacture  etripamil  and  any  future  product  candidates,  or  if  we
collaborate with third parties for the development or commercialization of etripamil or any future product candidates, we
must, at times, share proprietary information with them. We seek to protect our proprietary technology in part by entering
into  confidentiality  agreements  and,  if  applicable,  material  transfer  agreements,  consulting  agreements  or  other  similar
agreements with our advisors, employees, third-party contractors and consultants prior to beginning research or disclosing
proprietary information. These agreements typically limit the rights of the third parties to use or disclose our confidential
information. Despite the contractual provisions employed when working with third parties, the need to share confidential
information increases the risk that such information become known by our competitors, is inadvertently incorporated into
the technology of others, or is disclosed or used in violation of these agreements. Given that our proprietary position is

76

Table of Contents

based, in part, on our know-how, a competitor’s discovery of our know-how or other unauthorized use or disclosure could
have an adverse effect on our business and results of operations.

In  addition,  these  agreements  typically  restrict  the  ability  of  our  advisors,  employees,  third-party  contractors  and
consultants to publish data potentially relating to our know-how. Despite our efforts to protect our know-how, we may not
be  able  to  prevent  the  unauthorized  disclosure  or  use  of  our  technical  know-how  by  the  parties  to  these  agreements.
Moreover,  we  cannot  guarantee  that  we  have  entered  into  such  agreements  with  each  party  that  may  have  or  have  had
access  to  our  confidential  information  or  proprietary  technology  and  processes.  Monitoring  unauthorized  uses  and
disclosures is difficult, and we do not know whether the steps we have taken to protect our proprietary technologies will be
effective. If any of the collaborators, scientific advisors, employees, contractors and consultants who are parties to these
agreements breaches or violates the terms of any of these agreements, we may not have adequate remedies for any such
breach or violation. Moreover, if confidential information that is licensed or disclosed to us by our partners, collaborators,
or others is inadvertently disclosed or subject to a breach or violation, we may be exposed to liability to the owner of that
confidential information. Enforcing a claim that a third-party illegally obtained and is using our proprietary information,
like patent litigation, is expensive and time consuming, and the outcome is unpredictable. In addition, courts outside the
United States are sometimes less willing to protect proprietary information.

Any trademarks we may obtain may be infringed or successfully challenged, resulting in harm to our business.

We expect to rely on trademarks as one means to distinguish any of our product candidates that are approved for marketing
from the products of our competitors. We have not yet selected trademarks for etripamil and have not yet begun the process
of applying to register trademarks for etripamil or any other product candidate. Once we select trademarks and apply to
register them, our trademark applications may not be approved. Third parties may oppose our trademark applications or
otherwise challenge our use of the trademarks. In the event that our trademarks are successfully challenged, we could be
forced to rebrand our products, which could result in loss of brand recognition and could require us to devote resources to
advertising  and  marketing  new  brands.  Our  competitors  may  infringe  our  trademarks,  and  we  may  not  have  adequate
resources to enforce our trademarks.

In addition, any proprietary name we propose to use with etripamil or any future product candidate in the United States
must be approved by the FDA, regardless of whether we have registered it, or applied to register it, as a trademark. The
FDA typically conducts a review of proposed product names, including an evaluation of the potential for confusion with
other product names. If the FDA objects to any of our proposed proprietary product names, we may be required to expend
significant  additional  resources  in  an  effort  to  identify  a  suitable  proprietary  product  name  that  would  qualify  under
applicable trademark laws, not infringe the existing rights of third parties and be acceptable to the FDA.

If  we  are  unable  to  protect  the  confidentiality  of  our  proprietary  information,  our  business  and  competitive  position
would be harmed.

In  addition  to  seeking  patent  and  trademark  protection  for  etripamil  and  any  future  product  candidate,  we  also  rely  on
unpatented  know-how,  technology  and  other  proprietary  information,  to  maintain  our  competitive  position.  We  seek  to
protect  our  proprietary  information,  in  part,  by  entering  into  non-disclosure  and  confidentiality  agreements  with  parties
who  have  access  to  them,  such  as  our  employees,  corporate  collaborators,  outside  scientific  collaborators,  contract
manufacturers,  consultants,  advisors  and  other  third  parties.  We  also  enter  into  confidentiality  and  invention  or  patent
assignment  agreements  with  our  employees  and  consultants.  Despite  these  efforts,  any  of  these  parties  may  breach  the
agreements  and  disclose  our  proprietary  information.  Monitoring  unauthorized  uses  and  disclosures  of  our  intellectual
property  is  difficult,  and  we  do  not  know  whether  the  steps  we  have  taken  to  protect  our  intellectual  property  will  be
effective. In addition, we may not be able to obtain adequate remedies for any such breaches. Enforcing a claim that a party
illegally disclosed or misappropriated proprietary information is difficult, expensive and time consuming, and the outcome
is unpredictable. In addition, some courts inside and outside the United States are less willing or unwilling to protect trade
secrets.

77

Table of Contents

Moreover, our competitors may independently develop knowledge, methods and know-how equivalent to our proprietary
information. Competitors could purchase our products and replicate some or all of the competitive advantages we derive
from  our  development  efforts  for  technologies  on  which  we  do  not  have  patent  protection.  If  any  of  our  proprietary
information were to be lawfully obtained or independently developed by a competitor, we would have no right to prevent
them, or those to whom they communicate it, from using that technology or information to compete with us. If any of our
proprietary  information  were  to  be  disclosed  to  or  independently  developed  by  a  competitor,  our  competitive  position
would be harmed.

We  also  seek  to  preserve  the  integrity  and  confidentiality  of  our  data  and  other  confidential  information  by  maintaining
physical security of our premises and physical and electronic security of our information technology systems. While we
have  confidence  in  these  individuals,  organizations  and  systems,  agreements  or  security  measures  may  be  breached  and
detecting  the  disclosure  or  misappropriation  of  confidential  information  and  enforcing  a  claim  that  a  party  illegally
disclosed  or  misappropriated  confidential  information  is  difficult,  expensive  and  time-consuming,  and  the  outcome  is
unpredictable.  Further,  we  may  not  be  able  to  obtain  adequate  remedies  for  any  breach.  In  addition,  our  confidential
information may otherwise become known or be independently discovered by competitors, in which case we would have
no right to prevent them, or those to whom they communicate it, from using that technology or information to compete
with us.

Risks Related to Our Business Operations, Employee Matters and Managing Growth

Our  future  success  depends  on  our  ability  to  retain  key  executives  and  to  attract,  retain  and  motivate  qualified
personnel.

We are highly dependent on our President and Chief Executive Officer, Joseph Oliveto, our Chief Medical Officer, Francis
Plat,  our  Chief  Commercial  Officer,  Lorenz  Muller  and  our  Chief  Financial  Officer,  Amit  Hasija.  Each  of  them  may
currently terminate their employment with us at any time. The loss of the services of any of these persons could impede the
achievement of our research, development and commercialization objectives. We do not currently maintain “key person”
life  insurance  on  the  lives  of  our  executives  or  any  of  our  employees  other  than  on  our  President  and  Chief  Executive
Officer, Joseph Oliveto.

Recruiting  and  retaining  qualified  scientific  and  clinical  personnel  and,  if  we  progress  the  development  of  any  of  our
product candidates, commercialization, manufacturing and sales and marketing personnel, will be critical to our success.
The loss of the services of our executive officers or other key employees could impede the achievement of our research,
development  and  commercialization  objectives  and  seriously  harm  our  ability  to  successfully  implement  our  business
strategy. Furthermore, replacing executive officers and key employees may be difficult and may take an extended period of
time  because  of  the  limited  number  of  individuals  in  our  industry  with  the  breadth  of  skills  and  experience  required  to
successfully develop, gain regulatory approval of and commercialize our product candidates. Competition to hire from this
limited  pool  is  intense,  and  we  may  be  unable  to  hire,  train,  retain  or  motivate  these  key  personnel  on  acceptable  terms
given  the  competition  among  numerous  pharmaceutical  and  biotechnology  companies  for  similar  personnel.  We  also
experience  competition  for  the  hiring  of  scientific  and  clinical  personnel  from  universities  and  research  institutions.  In
addition,  we  rely  on  consultants  and  advisors,  including  scientific  and  clinical  advisors,  to  assist  us  in  formulating  our
research  and  development  and  commercialization  strategy.  Our  consultants  and  advisors  may  have  commitments  under
consulting or advisory contracts with other entities that may limit their availability to us. If we are unable to continue to
attract and retain high-quality personnel, our ability to pursue our growth strategy will be limited.

We expect to expand our organization, and we may experience difficulties in managing this growth, which could disrupt
our operations.

As of December 31, 2021, we had 29 full-time employees. As the clinical development of etripamil progresses and as we
expand  our  pipeline,  we  may  experience  significant  growth  in  the  number  of  our  employees  and  the  scope  of  our
operations, particularly in the areas of research, drug development, regulatory affairs and, if etripamil or any future product
candidates receives marketing approval, sales, marketing and distribution. To manage any future growth, we will be

78

Table of Contents

required to continue to implement and improve our managerial, operational and financial systems, expand our facilities and
continue  to  recruit  and  train  additional  qualified  personnel.  Due  to  our  limited  financial  resources  and  the  limited
experience of our management team in managing a company with growth, we may not be able to effectively manage any
expansion of our operations or recruit and train additional qualified personnel. Any expansion of our operations may lead
to significant costs and may divert our management and business development resources. Any inability to manage growth
could delay the execution of our business plans or disrupt our operations.

Our  internal  computer  systems,  or  those  of  our  collaborators  or  other  contractors  or  consultants,  may  fail  or  suffer
security breaches, which could result in a significant disruption of our product development programs and our ability to
operate our business effectively.

Our internal computer systems and those of our current and any future collaborators and other contractors or consultants
are  vulnerable  to  damage  from  computer  viruses,  unauthorized  access,  natural  disasters,  terrorism,  war  and
telecommunication and electrical failures. Cyber-attacks are increasing in their frequency, sophistication, and intensity, and
have become increasingly difficult to detect. Cyber-attacks could include the deployment of harmful malware, ransomware,
denial-of-service attacks, social engineering, and other means to affect service reliability and threaten the confidentiality,
integrity,  and  availability  of  information.  Cyber-attacks  also  could  include  phishing  attempts  or  e-mail  fraud  to  cause
payments or information to be transmitted to an unintended recipient.

While we have not experienced any significant system failure, accident or security breach to date, if such an event were to
occur  and  cause  interruptions  in  our  operations,  it  could  result  in  a  disruption  of  our  development  programs  and  our
business operations, whether due to a loss of our trade secrets or other proprietary information or other similar disruptions.
For example, the loss of clinical trial data from completed or future clinical trials by us or our CROs could result in delays
in our regulatory approval efforts and significantly increase our costs to recover or reproduce the data. Additionally, any
such  event  that  leads  to  unauthorized  access,  use  or  disclosure  of  personal  information,  including  personal  information
regarding our patients or employees, could harm our reputation, cause us not to comply with federal and/or state breach
notification laws and foreign law equivalents and otherwise subject us to liability under laws and regulations that protect
the privacy and security of personal information. Security breaches and other inappropriate access can be difficult to detect,
and any delay in identifying them may lead to increased harm of the type described above. While we have implemented
security measures to protect our information technology systems and infrastructure, such measures may not prevent service
interruptions or security breaches that could adversely affect our business and to the extent that any disruption or security
breach  were  to  result  in  a  loss  of,  or  damage  to,  our  data  or  applications,  or  inappropriate  disclosure  of  confidential  or
proprietary  information,  we  could  incur  liability,  our  competitive  position  could  be  harmed  and  the  further  development
and commercialization of our product candidates could be delayed.

If  we  fail  to  comply  with  European  data  protection  laws,  including  the  European  Union  General  Data  Protection
Regulation  2016/679,  or  GDPR,  when  appropriate,  and  any  other  existing  or  future  data  protection  regulations,  our
business, financial condition, results of operations and prospects may be materially adversely affected.

We anticipate seeking regulatory approval for, and commercialize, etripamil for the treatment of PSVT in Europe. We may
also elect to do so for future product candidates. We are conducting clinical trial activities in Europe, which will subject us
to European data protection laws, including the GDPR. The GDPR establishes requirements applicable to the processing of
personal  data  (i.e.,  data  which  identifies  an  individual  or  from  which  an  individual  is  identifiable).    The  GDPR  creates
significant and complex compliance burdens for companies such as: limiting permitted processing of personal data to only
that  which  is  necessary  for  specified,  explicit  and  legitimate  purposes;  requiring  the  establishment  a  legal  basis  for
processing personal data; expressly confirming that ‘pseudonymized’ or key-coded data constitutes personal data to which
the  GDPR  applies;  creating  obligations  for  controllers  and  processors  to  appoint  data  protection  officers  in  certain
circumstances;  increasing  transparency  obligations  to  data  subjects  for  controllers  (including  presentation  of  certain
information in a concise, intelligible and easily accessible form about how their personal data is used and their rights vis-à-
vis  that  data  and  its  use);  introducing  the  obligation  to  carry  out  so-called  data  protection  impact  assessments  in  certain
circumstances;  establishing  limitations  on  collection  and  retention  of  personal  data  through  ‘data  minimization’  and
‘storage limitation’ principles; establishing obligations to implement ‘privacy by design’; introducing obligations to honor
increased rights for data subjects (such as rights for individuals to be ‘forgotten,’ rights to data portability, rights to object

79

Table of Contents

etc.  in  certain  circumstances);  formalizing  a  heightened  and  codified  standard  of  data  subject  consent;  establishing
obligations  to  implement  certain  technical  and  organizational  safeguards  to  protect  the  security  and  confidentiality  of
personal  data;  introducing  obligations  to  agree  to  certain  specific  contractual  terms  and  to  take  certain  measures  when
engaging  third-party  processors  and  joint  controllers;  introducing  the  obligation  to  provide  notice  of  certain  significant
personal data breaches to the relevant supervisory authority(ies) and affected individuals; and mandating the appointment
of  representatives  in  the  United  Kingdom  and/or  European  Union  in  certain  circumstances.  The  processing  of  “special
category  personal  data”,  such  as  health  information,  may  also  impose  heightened  compliance  burdens  under  the  GDPR.
 The GDPR has robust regulatory enforcement and penalties for noncompliance, including fines of up to €20 million or 4%
of global annual revenue of any noncompliant company for the preceding financial year, whichever is higher. In addition to
administrative  fines,  a  wide  variety  of  other  potential  enforcement  powers  are  available  to  competent  supervisory
authorities in respect of potential and suspected violations of the GDPR, including extensive audit and inspection rights,
and powers to order temporary or permanent bans on all or some processing of personal data carried out by noncompliant
actors. The GDPR also confers a private right of action on data subjects and consumer associations to lodge complaints
with supervisory authorities, seek judicial remedies, and obtain compensation for damages resulting from violations of the
GDPR. There may be circumstances under which a failure to comply with GDPR, or the exercise of individual rights under
the GDPR, would limit our ability to utilize clinical trial data collected on certain subjects. The GDPR will likely impose
additional  responsibility  and  liability  in  relation  to  our  processing  of  personal  data.  This  may  be  onerous  and  materially
adversely affect our business, financial condition, results of operations and prospects.

A particular issue presented by the GDPR is the restriction on transfers of personal data from Europe to the United States
and most other countries unless the parties to the transfer have implemented specific safeguards to protect the transferred
personal  data.  One  of  the  primary  safeguards  allowing  U.S.  companies  to  import  personal  data  from  Europe  is  the
European Commission’s Standard Contractual Clauses and we have relied on Standard Contractual Clauses to comply with
the  GDPR’s  restrictions  on  transfer  of  personal  data  out  of  Europe.    However,  in  July  2020  the  Court  of  Justice  of  the
European  Union,  or  CJEU,  in  a  case  known  colloquially  as  “Schrems  II”  raised  questions  about  whether  the  Standard
Contractual  Clauses  can  lawfully  be  used  for  personal  data  transfers  from  Europe  to  the  United  States  or  other  third
countries  that  are  not  the  subject  of  an  adequacy  decision  of  the  European  Commission.  While  the  CJEU  upheld  the
adequacy of the Standard Contractual Clauses in principle in Schrems II, it made clear that reliance on those Clauses alone
may not necessarily be sufficient in all circumstances. Use of the Standard Contractual Clauses must now be assessed on a
case-by-case  basis  taking  into  account  the  legal  regime  applicable  in  the  destination  country,  in  particular  regarding
applicable  surveillance  laws  and  relevant  rights  of  individuals  with  respect  to  the  transferred  data.  In  the  context  of  any
given  transfer,  where  the  legal  regime  applicable  in  the  destination  country  may  or  does  conflict  with  the  intended
operation of the Standard Contractual Clauses and/or applicable European law, the decision in Schrems II and subsequent
draft guidance from the European Data Protection Board, or EDPB, would require the parties to that transfer to implement
certain supplementary technical, organizational and/or contractual measures to rely on the Standard Contractual Clauses as
a  compliant  ‘transfer  mechanism.’  However,  the  aforementioned  draft  guidance  from  the  EDPB  on  such  supplementary
technical, organizational and/or contractual measures appears to conclude that no combination of such measures could be
sufficient to allow effective reliance on the Standard Contractual Clauses in the context of transfers of personal data ‘in the
clear’ to recipients in countries where the power granted to public authorities to access the transferred data goes beyond
that  which  is  ‘necessary  and  proportionate  in  a  democratic  society’  –  which  may,  following  the  CJEU’s  conclusions  in
Schrems II on relevant powers of United States public authorities and commentary in that draft EDPB guidance, include
the  United  States  in  certain  circumstances  (e.g.,  where  Section  702  of  the  US  Foreign  Intelligence  Surveillance  Act
applies).  At present, there are few, if any, viable alternatives to the Standard Contractual Clauses. As such, if we are unable
to  implement  a  valid  solution  for  personal  data  transfers  from  Europe,  including,  we  will  face  increased  exposure  to
regulatory  actions,  substantial  fines  and  injunctions  against  processing  personal  data  from  Europe.  Inability  to  import
personal data from Europe may also: restrict our activities in Europe; limit our ability to collaborate with partners as well
as  other  service  providers,  contractors  and  other  companies  subject  to  European  data  protection  laws;  and  require  us  to
increase  our  data  processing  capabilities  in  Europe  at  significant  expense.  Restrictions  on  our  ability  to  import  personal
data  from  Europe  could  therefore  impact  our  clinical  trial  activities  in  Europe  and  limit  our  ability  to  collaborate  with
CROs and other third parties subject to European data protection laws. Additionally, other countries outside of Europe have
enacted or are considering enacting similar cross-border data transfer restrictions and laws requiring local data residency,
which could increase the cost and complexity of delivering our services and operating our business. The type of challenges
we face in

80

Table of Contents

Europe  will  likely  also  arise  in  other  jurisdictions  that  adopt  laws  similar  in  construction  to  the  GDPR  or  regulatory
frameworks of equivalent complexity.

Our  employees,  principal  investigators,  consultants  and  commercial  partners  may  engage  in  misconduct  or  other
improper activities, including non-compliance with regulatory standards and requirements and insider trading.

We  are  exposed  to  the  risk  of  fraud  or  other  misconduct  by  our  employees,  principal  investigators,  consultants  and
commercial partners. Misconduct by these parties could include intentional failures to comply with FDA regulations or the
regulations  applicable  in  other  jurisdictions,  provide  accurate  information  to  the  FDA  and  other  regulatory  authorities,
comply with healthcare fraud and abuse laws and regulations in the United States and abroad, report financial information
or data accurately or disclose unauthorized activities to us. In particular, sales, marketing and business arrangements in the
healthcare industry are subject to extensive laws and regulations intended to prevent fraud, misconduct, kickbacks, self-
dealing and other abusive practices. These laws and regulations restrict or prohibit a wide range of pricing, discounting,
marketing  and  promotion,  sales  commission,  customer  incentive  programs  and  other  business  arrangements.  Such
misconduct also could involve the improper use of information obtained in the course of clinical trials or interactions with
the  FDA  or  other  regulatory  authorities,  which  could  result  in  regulatory  sanctions  and  cause  serious  harm  to  our
reputation. It is not always possible to identify and deter employee misconduct, and the precautions we take to detect and
prevent this activity may not be effective in controlling unknown or unmanaged risks or losses or in protecting us from
government investigations or other actions or lawsuits stemming from a failure to comply with these laws or regulations. If
any such actions are instituted against us and we are not successful in defending ourselves or asserting our rights, those
actions could result in significant civil, criminal and administrative penalties, damages, fines, disgorgement, imprisonment,
exclusion  from  participating  in  government  funded  healthcare  programs,  such  as  Medicare  and  Medicaid,  additional
reporting  requirements  and  oversight  if  we  become  subject  to  a  corporate  integrity  agreement  or  similar  agreement  to
resolve  allegations  of  non-compliance  with  these  laws,  contractual  damages,  reputational  harm  and  the  curtailment  or
restructuring of our operations, any of which could have a negative impact on our business, financial condition, results of
operations and prospects.

Our  current  or  future  acquisitions  or  strategic  collaborations  could  increase  our  capital  requirements,  dilute  our
shareholders, cause us to incur debt or assume contingent liabilities and subject us to other risks.

We  actively  search  for  and  continually  evaluate  various  acquisition  and  strategic  collaboration  opportunities,  including
licensing or acquiring complementary drugs, intellectual property rights, technologies or businesses, as deemed appropriate
to carry out our business plan. Our collaborations, including any future acquisitions or strategic partnerships, may entail
numerous risks, including:

•

•

•

•

•

•

increased operating expenses and cash requirements;

the assumption of additional indebtedness or contingent liabilities;

assimilation  of  operations,  intellectual  property  and  drugs  of  an  acquired  company,  including  difficulties
associated with integrating new personnel;

the diversion of our management’s attention from our existing drug programs and initiatives in pursuing such
a strategic partnership, merger or acquisition;

retention  of  key  employees,  the  loss  of  key  personnel,  and  uncertainties  in  our  ability  to  maintain  key
business relationships;

risks and uncertainties associated with the other party to such a transaction, including the prospects of that
party and their existing drugs or product candidates and regulatory approvals; and

81

Table of Contents

•

our inability to generate revenue from acquired technology and/or drugs sufficient to meet our objectives in
undertaking the acquisition or even to offset the associated acquisition and maintenance costs.

In addition, in connection with our current or future acquisitions or strategic partnerships, we may issue dilutive securities,
assume or incur debt obligations, incur large one-time expenses and acquire intangible assets that could result in significant
future  amortization  expense.  Moreover,  we  may  not  be  able  to  locate  suitable  future  acquisition  opportunities,  and  this
inability could impair our ability to grow or obtain access to technology or drugs that may be important to the development
of our business.

Risks Related to Ownership of Our Common Shares

The market price of our common shares has been and may continue to be volatile and fluctuate substantially, and you
could lose all or part of your investment.

The  market  price  of  our  common  shares  has  been  and  may  continue  to  be  highly  volatile  and  could  be  subject  to  wide
fluctuations in price in response to various factors, many of which are beyond our control. Since our initial public offering
which occurred in May 2019, through March 21, 2022, the price of our common shares has ranged from $1.70 per share to
$27.15  per  share.  The  stock  market  in  general  and  the  market  for  biopharmaceutical  and  pharmaceutical  companies  in
particular,  has  experienced  extreme  volatility  that  has  often  been  unrelated  to  the  operating  performance  of  particular
companies. As a result of this volatility, you may not be able to sell your common shares at or above the price paid for the
shares. In addition to the factors discussed in this “Risk Factors” section and elsewhere in this Annual Report on Form 10-
K, the market price for our common shares may be influenced by the following:

•

•

•

•

•

•

•

•

•

•

•

•

•

the commencement, enrollment or results of our planned or future clinical trials of etripamil and any future
product candidates or those of our competitors;

the success of competitive drugs or therapies;

regulatory or legal developments in the United States and other countries;

the success of competitive products or technologies;

developments or disputes concerning patent applications, issued patents or other proprietary rights;

the recruitment or departure of key personnel;

the level of expenses related to etripamil and any future product candidates or clinical development programs;

the results of our efforts to discover, develop, acquire or in-license additional product candidates;

actual or anticipated changes in estimates as to financial results, development timelines or recommendations
by securities analysts;

our inability to obtain or delays in obtaining adequate drug supply for any approved drug or inability to do so
at acceptable prices;

disputes  or  other  developments  relating  to  proprietary  rights,  including  patents,  litigation  matters  and  our
ability to obtain patent protection for our technologies;

significant lawsuits, including patent or shareholder litigation;

variations in our financial results or those of companies that are perceived to be similar to us;

82

Table of Contents

•

changes in the structure of healthcare payment systems, including coverage and adequate reimbursement for
any approved drug;

• market conditions in the pharmaceutical and biotechnology sectors;

•

•

general economic, political, and market conditions , including deteriorating market conditions due to investor
concerns  regarding  inflation  and  Russian  hostilities  in  Ukraine  and  overall  fluctuations  in  the  financial
markets in the United States and abroad; and

investors’ general perception of us and our business.

These and other market and industry factors may cause the market price and demand for our common shares to fluctuate
substantially, regardless of our actual operating performance, which may limit or prevent investors from selling their shares
at  or  above  the  price  paid  for  the  shares  and  may  otherwise  negatively  affect  the  liquidity  of  our  common  shares.  In
addition, the stock market in general, and biopharmaceutical companies in particular, have experienced extreme price and
volume fluctuations that have often been unrelated or disproportionate to the operating performance of these companies.

Some  companies  that  have  experienced  volatility  in  the  trading  price  of  their  shares  have  been  the  subject  of  securities
class action litigation. Any lawsuit to which we are a party, with or without merit, may result in an unfavorable judgment.
We  also  may  decide  to  settle  lawsuits  on  unfavorable  terms.  Any  such  negative  outcome  could  result  in  payments  of
substantial  damages  or  fines,  damage  to  our  reputation  or  adverse  changes  to  our  business  practices.  Defending  against
litigation  is  costly  and  time-consuming,  and  could  divert  our  management’s  attention  and  our  resources.  Furthermore,
during the course of litigation, there could be negative public announcements of the results of hearings, motions or other
interim proceedings or developments, which could have a negative effect on the market price of our common shares.

Geopolitical instability outside of the U.S. may adversely impact the U.S. and global economies.

At the end of 2021 and into 2022, tensions between the U.S. and Russia escalated when Russia amassed large numbers of
military  ground  forces  and  support  personnel  on  the  Ukraine-Russia  border  and  in  February  2022,  Russia  initiated  a
military conflict across Ukraine. In response, NATO has deployed additional military forces to Eastern Europe, including to
Lithuania  and  Romania,  and  Australia,  Britain,  the  European  Union,  Japan,  Switzerland,  Taiwan,  the  U.S.  and  other
countries announced punishing sanctions against Russia. The Russo-Ukranian conflict and any retaliatory measures taken
by the U.S. and NATO could threaten global security and result in further regional conflict and otherwise have a lasting
impact on regional and global economies. Although we do not have patients or clinical sites in Ukraine or Russia, we could
experience an adverse affect our business and the price of our common stock.  

Our  common  shares  are  thinly  traded  and  our  shareholders  may  be  unable  to  sell  their  shares  quickly  or  at  market
price.

Although we have had periods of high volume daily trading in our common shares, generally our shares are thinly traded.
As  a  consequence  of  this  lack  of  liquidity,  the  trading  of  relatively  small  quantities  of  shares  by  our  shareholders  may
disproportionately  influence  the  price  of  those  shares  in  either  direction.  The  price  for  our  shares  could,  for  example,
decline significantly in the event that a large number of our common shares are sold on the market without commensurate
demand, as compared to a seasoned issuer that could better absorb those sales without adverse impact on its share price.

Concentration  of  ownership  of  our  common  shares  among  our  existing  executive  officers,  directors  and  principal
shareholders may prevent new investors from influencing significant corporate decisions.

Based upon our common shares outstanding as of December 31, 2021, our executive officers, directors and shareholders
who  owned  more  than  5%  of  our  outstanding  common  shares,  in  the  aggregate,  beneficially  owned  shares  representing
65.2% of our outstanding common shares. If our executive officers, directors and shareholders who owned more than 5%
of our outstanding common shares acted together, they may be able to significantly influence all matters requiring

83

Table of Contents

shareholder approval, including the election and removal of directors and approval of any merger, consolidation or sale of
all or substantially all of our assets. The concentration of voting power and transfer restrictions could delay or prevent an
acquisition of our company on terms that other shareholders may desire or result in the management of our company in
ways with which other shareholders disagree.

If  research  analysts  do  not  publish  research  or  reports,  or  publish  unfavorable  research  or  reports,  about  us,  our
business or our market, our share price and trading volume could decline.

The trading market for our common shares will be influenced by the research and reports that industry or financial analysts
publish about us or our business. Equity research analysts may discontinue research coverage of our common shares, and
such lack of research coverage may adversely affect the market price of our common shares. We do not have any control
over the analysts or the content and opinions included in their reports. The price of our shares could decline if one or more
equity research analysts downgrade our shares or issue other unfavorable commentary or research about us. If one or more
equity  research  analysts  ceases  coverage  of  us  or  fails  to  publish  reports  on  us  regularly,  demand  for  our  shares  could
decrease, which in turn could cause the trading price or trading volume of our common shares to decline.

Because  we  do  not  anticipate  paying  any  cash  dividends  on  our  share  capital  in  the  foreseeable  future,  capital
appreciation, if any, will be your sole source of gain.

You should not rely on an investment in our common shares to provide dividend income. We have never declared or paid
cash dividends on our share capital. We currently intend to retain all of our future earnings, if any, to finance the growth
and development of our business. In addition, the terms of any future debt agreements or preferred equity may preclude us
from paying dividends. As a result, capital appreciation, if any, of our common shares will be your sole source of gain for
the foreseeable future. Investors seeking cash dividends should not purchase our common shares.

We have broad discretion in the use of our cash and cash equivalents and may use them in ways in which you do not
agree or in ways that do not increase the value of your investment.

Our management has broad discretion in the application of our cash and cash equivalents and could spend these funds in
ways  that  do  not  improve  our  results  of  operations  or  enhance  the  value  of  our  common  shares.  The  failure  by  our
management  to  apply  these  funds  effectively  could  result  in  financial  losses  that  could  have  a  negative  impact  on  our
business, cause the price of our common shares to decline and delay the development of our product candidates. Pending
their use, we may invest our cash and cash equivalents, in a manner that does not produce income or that loses value.

If we are a passive foreign investment company, there could be adverse U.S. federal income tax consequences to U.S.
Holders (as defined below).

Based on the nature and composition of our income, assets, activities and market capitalization for our taxable year ending
December 31, 2021, we believe that we may have been classified as a passive foreign investment company, or PFIC, for
our taxable year ending December 31, 2021. Based on the expected nature and composition of our income and assets for
our taxable year ending December 31, 2022, we expect that we may be classified as a PFIC for our taxable year ending
December 31, 2022. If we are a PFIC for the current taxable year, or any subsequent taxable years, we intend to annually
furnish U.S. Holders, upon request, a “PFIC Annual Information Statement,” with the information required to allow U.S.
Holders to make a “qualified electing fund” election, or “QEF Election” for United States federal income tax purposes. No
assurances regarding our PFIC status can be provided for any past, current or future taxable years. The determination of
whether  we  are  a  PFIC  is  a  fact-intensive  determination  made  on  an  annual  basis  and  the  applicable  law  is  subject  to
varying  interpretation.  In  particular,  the  characterization  of  our  assets  as  active  or  passive  may  depend  in  part  on  our
current and intended future business plans, which are subject to change. In addition, the total value of our assets for PFIC
testing  purposes  may  be  determined  in  part  by  reference  to  the  market  price  of  our  common  shares  from  time  to  time,
which may fluctuate considerably. As a result, our PFIC status may change from year to year. Under the income test, our
status  as  a  PFIC  depends  on  the  composition  of  our  income  which  will  depend  on  the  transactions  we  enter  into  in  the
future and our

84

Table of Contents

corporate structure. The composition of our income and assets is also affected by how, and how quickly, we spend the cash
we raise in any offering.

If we are a PFIC, U.S. Holders may be subject to adverse U.S. federal income tax consequences, such as ineligibility for
any preferential tax rates for individuals on capital gains or on actual or deemed dividends, interest charges on certain taxes
treated as deferred, and additional reporting requirements under U.S. federal income tax laws and regulations.

A “U.S. Holder” is a holder of our common shares who, for U.S. federal income tax purposes, is: (i) an individual who is a
citizen or resident of the United States; (ii) a corporation, or another entity taxable as a corporation, created or organized in
or under the laws of the United States, any state therein or the District of Columbia; (iii) an estate the income of which is
subject to U.S. federal income taxation regardless of its source; or (iv) a trust if (1) a U.S. court is able to exercise primary
supervision  over  the  administration  of  the  trust  and  one  or  more  U.S.  persons  have  authority  to  control  all  substantial
decisions  of  the  trust  or  (2)  the  trust  has  a  valid  election  to  be  treated  as  a  U.S.  person  under  applicable  U.S.Treasury
Regulations.

If a U.S. Holder is treated as owning at least 10% of our common shares, such holder may be subject to adverse U.S.
federal income tax consequences.

If a U.S. Holder is treated as owning (directly, indirectly or constructively) at least 10% of the value or voting power of our
common shares, such U.S. Holder may be treated as a “United States shareholder” with respect to each “controlled foreign
corporation”  in  our  group  (if  any).  Because  our  group  includes  at  least  one  U.S.  subsidiary  (Milestone  Pharmaceuticals
USA Inc.), if we were to form or acquire any non-U.S. subsidiaries in the future, they may be treated as controlled foreign
corporations.  A  United  States  shareholder  of  a  controlled  foreign  corporation  may  be  required  to  annually  report  and
include  in  its  U.S.  taxable  income  its  pro  rata  share  of  “Subpart  F  income,”  “global  intangible  low-taxed  income”  and
investments  in  U.S.  property  by  that  controlled  foreign  corporation,  regardless  of  whether  that  controlled  foreign
corporation, or we, make any distributions. An individual that is a United States shareholder with respect to a controlled
foreign corporation generally would not be allowed certain tax deductions or foreign tax credits that would be allowed to a
United  States  shareholder  that  is  a  U.S.  corporation.  We  cannot  provide  any  assurances  that  we  will  assist  investors  in
determining  whether  any  non-U.S.  subsidiaries  that  we  may  form  or  acquire  in  the  future  will  be  treated  as  controlled
foreign corporations or whether any such investor would be treated as a United States shareholder with respect to any of
such  controlled  foreign  corporations.  Further,  we  cannot  provide  any  assurances  that  we  will  furnish  to  any  investor
information  that  may  be  necessary  to  comply  with  the  reporting  and  tax  paying  obligations  discussed  above.  Failure  to
comply with these reporting obligations may subject a U.S. Holder to significant monetary penalties and may extend the
statute  of  limitations  with  respect  to  its  U.S.  federal  income  tax  return  for  the  year  for  which  reporting  was  due.  U.S.
Holders  should  consult  their  tax  advisors  regarding  the  potential  application  of  these  rules  to  their  investment  in  our
common shares.

Future changes to tax laws could materially adversely affect our company and reduce net returns to our shareholders.

Our  tax  treatment  is  subject  to  the  enactment  of,  or  changes  in,  tax  laws,  regulations  and  treaties,  or  the  interpretation
thereof, tax policy initiatives and reforms under consideration and the practices of tax authorities in jurisdictions in which
we operate, including those related to the Organization for Economic Co-Operation and Development’s, or OECD, Base
Erosion  and  Profit  Shifting,  or  BEPS,  Project,  the  European  Commission’s  state  aid  investigations  and  other  initiatives.
Such changes may include (but are not limited to) the taxation of operating income, investment income, dividends received
or (in the specific context of withholding tax) dividends paid. We are unable to predict what tax reform may be proposed or
enacted  in  the  future  or  what  effect  such  changes  would  have  on  our  business,  but  such  changes,  to  the  extent  they  are
brought into tax legislation, regulations, policies or practices, could affect our financial position and overall or effective tax
rates  in  the  future  in  countries  where  we  have  operations,  reduce  post-tax  returns  to  our  shareholders,  and  increase  the
complexity, burden and cost of tax compliance.

For  example,  the  Tax  Act  enacted  many  significant  changes  to  the  U.S.  tax  laws.  Future  guidance  from  the  Internal
Revenue Service and other tax authorities with respect to the Tax Act may affect us, and certain aspects of the Tax Act
could be repealed or modified in future legislation. For example, the CARES Act modified certain provisions of the Tax

85

Table of Contents

Act. In addition, it is uncertain if and to what extent various states will conform to the Tax Act, the CARES Act or any
newly enacted federal tax legislation. Changes in corporate tax rates, the realization of net deferred tax assets relating to
our  operations,  the  taxation  of  foreign  earnings,  and  the  deductibility  of  expenses  under  the  Tax  Act  or  future  reform
legislation could have a material impact on the value of our deferred tax assets, could result in significant one-time charges,
and could increase our future U.S. tax expense. We urge you to consult with your legal and tax advisors with respect to this
legislation and the potential tax consequences of investing in or holding our common shares.

Tax  authorities  may  disagree  with  our  positions  and  conclusions  regarding  certain  tax  positions,  resulting  in
unanticipated costs, taxes or non-realization of expected benefits.

A  tax  authority  may  disagree  with  tax  positions  that  we  have  taken,  which  could  result  in  increased  tax  liabilities.  For
example, the Canadian Revenue Agency, the U.S. Internal Revenue Service or another tax authority could challenge our
allocation  of  income  by  tax  jurisdiction  and  the  amounts  paid  between  our  affiliated  companies  pursuant  to  our
intercompany arrangements and transfer pricing policies, including amounts paid with respect to our intellectual property
development. Similarly, a tax authority could assert that we are subject to tax in a jurisdiction where we believe we have
not established a taxable connection, often referred to as a “permanent establishment” under international tax treaties, and
such an assertion, if successful, could increase our expected tax liability in one or more jurisdictions. A tax authority may
take the position that material income tax liabilities, interest and penalties are payable by us, in which case, we expect that
we might contest such assessment. Contesting such an assessment may be lengthy and costly and if we were unsuccessful
in disputing the assessment, the result could increase our anticipated effective tax rate.

We  are  an  “emerging  growth  company,”  and  the  reduced  disclosure  requirements  applicable  to  emerging  growth
companies may make our common shares less attractive to investors.

We are an “emerging growth company,” or EGC, as defined in the Jumpstart Our Business Startups Act of 2012, or the
JOBS Act, and we intend to take advantage of some of the exemptions from reporting requirements that are applicable to
other public companies that are not emerging growth companies, including:

•

•

•

•

not  being  required  to  comply  with  the  auditor  attestation  requirements  in  the  assessment  of  our  internal
control over financial reporting;

not being required to comply with any requirement that may be adopted by the Public Company Accounting
Oversight  Board  regarding  mandatory  audit  firm  rotation  or  a  supplement  to  the  auditor’s  report  providing
additional information about the audit and the financial statements;

reduced disclosure obligations regarding executive compensation; and

not being required to hold a nonbinding advisory vote on executive compensation and shareholder approval
of any golden parachute payments not previously approved.

We currently take advantage of some or all of these reporting exemptions and may continue to until we are no longer an
EGC. We will remain an EGC until the earlier of (i) December 31, 2024, (ii) the last day of the fiscal year in which we
have total annual gross revenue of at least $1.07 billion, (iii) the last day of the first fiscal year in which we are deemed to
be  a  large  accelerated  filer,  which  means  the  market  value  of  our  common  shares  that  is  held  by  non-affiliates  exceeds
$700 million as of the prior June 30th, and (iv) the date on which we have issued more than $1.0 billion in non-convertible
debt during the prior three-year period. We cannot predict whether investors will find our common shares less attractive
because we will rely on these exemptions. If some investors find our common shares less attractive as a result, there may
be a less active trading market for our common shares and our share price may be more volatile.

In addition, under Section 107(b) of the JOBS Act, EGCs can delay adopting new or revised accounting standards until
such time as those standards apply to private companies. We have irrevocably elected not to avail ourselves of this

86

Table of Contents

exemption  from  new  or  revised  accounting  standards  and,  therefore,  we  will  be  subject  to  the  same  new  or  revised
accounting standards as other public companies that are not EGCs.

We are incurring, and expect to continue to incur additional costs as a result of operating as a public company, and our
management will be required to devote substantial time to new compliance initiatives.

As a public company, and particularly after we are no longer an EGC, we are incurring, and expect to continue to incur,
significant legal, accounting and other expenses. In addition, the Sarbanes-Oxley Act of 2002, or the Sarbanes-Oxley Act,
and rules subsequently implemented by the SEC and The Nasdaq Stock Market LLC have imposed various requirements
on public companies, including establishment and maintenance of effective disclosure and financial controls and corporate
governance  practices.  Our  management  and  other  personnel  need  to  devote  a  substantial  amount  of  time  to  these
compliance initiatives. Moreover, these rules and regulations have increased, and will continue to increase, our legal and
financial compliance costs and make some activities more time-consuming and costly.

While  we  remain  an  EGC,  we  are  not  be  required  to  include  an  attestation  report  on  internal  control  over  financial
reporting issued by our independent registered public accounting firm. However, pursuant to Section 404 of the Sarbanes
Oxley  Act,  or  Section  404,  in  the  future  we  will  be  required  to  furnish  an  attestation  on  internal  control  over  financial
reporting issued by our independent registered public accounting firm. To achieve compliance with Section 404, we will be
engaged in additional internal processes to document and evaluate our internal control over financial reporting, which will
be both costly and challenging. In this regard, we will need to continue to dedicate internal resources, potentially engage
outside consultants and adopt a detailed work plan to assess and document the adequacy of internal control over financial
reporting, continue steps to improve control processes as appropriate, validate through testing that controls are functioning
as  documented  and  implement  a  continuous  reporting  and  improvement  process  for  internal  control  over  financial
reporting.  Despite  our  efforts,  our  independent  registered  public  accounting  firm  may  determine  we  have  a  material
weakness  or  significant  deficiency  in  our  internal  control  over  financial  reporting  once  such  firm  begin  its  Section  404
reviews in the future, there is a risk that neither we nor our independent registered public accounting firm will be able to
conclude  within  the  prescribed  timeframe  that  our  internal  control  over  financial  reporting  is  effective  as  required  by
Section 404. This could result in an adverse reaction in the financial markets due to a loss of confidence in the reliability of
our consolidated financial statements.

Because we are a Canadian company, it may be difficult to serve legal process or enforce judgments against us.

We are a domestic filer in the United States; however, we are incorporated and have our corporate headquarters in Canada.
In  addition,  while  many  of  our  directors  and  officers  reside  in  the  United  States,  several  of  them  reside  outside  of  the
United States. Accordingly, service of process upon us may be difficult to obtain within the United States. Furthermore,
because  substantially  all  of  our  assets  are  located  outside  the  United  States,  any  judgment  obtained  in  the  United  States
against  us,  including  one  predicated  on  the  civil  liability  provisions  of  the  U.S.  federal  securities  laws,  may  not  be
collectible within the United States. Therefore, it may not be possible to enforce those actions against us.

In addition, it may be difficult to assert U.S. securities law claims in original actions instituted in Canada. Canadian courts
may refuse to hear a claim based on an alleged violation of U.S. securities laws against us or these persons on the grounds
that Canada is not the most appropriate forum in which to bring such a claim. Even if a Canadian court agrees to hear a
claim, it may determine that Canadian law and not U.S. law is applicable to the claim. If U.S. law is found to be applicable,
the content of applicable U.S. law must be proved as a fact, which can be a time-consuming and costly process. Certain
matters of procedure will also be governed by Canadian law. Furthermore, it may not be possible to subject foreign persons
or entities to the jurisdiction of the courts in Canada. Similarly, to the extent that our assets are located in Canada, investors
may  have  difficulty  collecting  from  us  any  judgments  obtained  in  the  U.S.  courts  and  predicated  on  the  civil  liability
provisions of U.S. securities provisions.

87

Table of Contents

We are governed by the corporate laws of Québec, which in some cases have a different effect on shareholders than the
corporate laws of Delaware.

We are governed by the Business Corporations Act (Québec), or the QBCA, and other relevant laws, which may affect the
rights of shareholders differently than those of a company governed by the laws of a U.S. jurisdiction, and may, together
with our charter documents, have the effect of delaying, deferring or discouraging another party from acquiring control of
us by means of a tender offer, a proxy contest or otherwise, or may affect the price an acquiring party would be willing to
offer  in  such  an  instance.  The  material  differences  between  the  QBCA  and  Delaware  General  Corporation  Law,  or  the
DGCL,  that  may  have  the  greatest  such  effect  include  but  are  not  limited  to  the  following:  (i)  for  material  corporate
transactions  (such  as  mergers  and  amalgamations,  other  extraordinary  corporate  transactions  or  amendments  to  our
articles),  the  QBCA  generally  requires  a  two-thirds  majority  vote  by  shareholders,  whereas  the  DGCL  generally  only
requires a majority vote; and (ii) under the QBCA, a holder of 5% or more of our common shares can requisition a special
meeting of shareholders, whereas such right does not exist under the DGCL.

Our  bylaws  and  certain  Canadian  legislation  contain  provisions  that  may  have  the  effect  of  delaying  or  preventing
certain change in control transactions or shareholder proposals.

Certain provisions of our bylaws and certain Canadian legislation, together or separately, could discourage or delay certain
change in control transactions or shareholder proposals.

Our bylaws contain provisions that establish certain advance notice procedures for nomination of candidates for election as
directors  at  shareholders’  meetings.  The  BCA  requires  that  any  shareholder  proposal  that  includes  nominations  for  the
election of directors must be signed by one or more holders of shares representing in the aggregate not less than 5% of the
shares  or  5%  of  the  shares  of  a  class  or  series  of  shares  of  the  corporation  entitled  to  vote  at  the  meeting  to  which  the
proposal is to be presented.

The Investment Canada Act requires that a non-Canadian must file an application for review with the Minister responsible
for  the  Investment  Canada  Act  and  obtain  approval  of  the  Minister  prior  to  acquiring  control  of  a  “Canadian  business”
within  the  meaning  of  the  Investment  Canada  Act,  where  prescribed  financial  thresholds  are  exceeded.  Furthermore,
limitations on the ability to acquire and hold our common shares may be imposed by the Competition Act (Canada). This
legislation  permits  the  Commissioner  of  Competition,  or  Commissioner,  to  review  any  acquisition  or  establishment,
directly or indirectly, including through the acquisition of shares, of control over or of a significant interest in our company.
Otherwise,  there  are  no  limitations  either  under  the  laws  of  Canada  or  Quebec,  or  in  our  articles  on  the  rights  of  non-
Canadians to hold or vote our common shares.

Any  of  these  provisions  may  discourage  a  potential  acquirer  from  proposing  or  completing  a  transaction  that  may  have
otherwise presented a premium to our shareholders.

ITEM 1B.  UNRESOLVED STAFF COMMENTS.

None.

ITEM 2.     PROPERTIES.

Our headquarters is currently located in Montréal (Québec), Canada and consists of 7,700 square feet of leased office space
under  a  lease  that  expires  in  November  2025.  We  also  have  a  U.S.  subsidiary  based  in  Charlotte,  North  Carolina.  We
believe that our facilities are adequate to meet our current needs and that additional space can be obtained on commercially
reasonable terms as needed.

88

Table of Contents

ITEM 3.     LEGAL PROCEEDINGS.

From time to time, we may become involved in legal proceedings arising in the ordinary course of our business. We are not
currently a party to any material legal proceedings, and we are not aware of any pending or threatened legal proceeding
against us that we believe could have an adverse effect on our business, operating results or financial condition.

ITEM 4.     MINE SAFETY DISCLOSURES.

Not applicable.

89

Table of Contents

PART II

ITEM  5.          MARKET  FOR  REGISTRANT’S  COMMON  EQUITY,  RELATED  STOCKHOLDER  MATTERS

AND ISSUER PURCHASES OF EQUITY SECURITIES.

MARKET INFORMATION

Our common shares began trading on The Nasdaq Global Select Market on May 9, 2019. Our common shares trade under
the symbol “MIST”. Prior to the commencement of trading on the Nasdaq Global Select Market on May 9, 2019, there was
no public market for our common shares.

HOLDERS OF RECORD

As of December 31, 2021, there were 16 holders of record of our common shares, including Cede & Co., a nominee for
The Depository Trust Company, or DTC, which holds shares of our common shares on behalf of an indeterminate number
of beneficial owners. All of the common shares held by brokerage firms, banks and other financial institutions as nominees
for beneficial owners are deposited into participant accounts at DTC, and are considered to be held of record by Cede &
Co. as one shareholder. Because many of our shares are held by brokers and other institutions on behalf of shareholders, we
are unable to estimate the total number of shareholders represented by these record holders.

DIVIDEND POLICY

We have never declared or paid any cash dividends on our capital stock and do not anticipate paying any cash dividends in
the foreseeable future. Payment of cash dividends, if any, in the future will be at the discretion of our board of directors and
will depend on then-existing conditions, including our financial condition, operating results, contractual restrictions, capital
requirements, business prospects and other factors our board of directors may deem relevant.

Recent Sales of Unregistered Securities

None.

Purchase of Equity Securities by the Issuer and Affiliated Purchasers

None.

Securities Authorized for Issuance Under Equity Compensation Plans

Information  about  securities  authorized  for  issuance  under  our  equity  compensation  plan  is  incorporated  herein  by
reference to Item 12 of Part III of this Annual Report on Form 10-K.

ITEM 6.     SELECTED FINANCIAL DATA.

Not Applicable.

90

Table of Contents

ITEM 7.     MANAGEMENT’S DISCUSSION AND ANALYSIS OF FINANCIAL CONDITION AND RESULTS

OF OPERATIONS.

You should read the following discussion and analysis of our financial condition and results of operations together with our
consolidated  financial  statements  and  related  notes  included  elsewhere  in  this  Annual  Report  on  Form  10-K.  This
discussion contains forward-looking statements based upon current expectations that involve risks and uncertainties. Our
actual  results  may  differ  materially  from  those  anticipated  in  these  forward-looking  statements  as  a  result  of  various
factors, including those discussed in “Risk Factors” and in other parts of this Annual Report on Form 10-K.

Overview

We  are  a  biopharmaceutical  company  focused  on  the  development  and  commercialization  of  innovative  cardiovascular
medicines.  Our  lead  product  candidate  etripamil  is  a  novel,  potent  and  short-acting  calcium  channel  blocker  that  we
designed as a rapid-onset nasal spray to be self-administered by patients. We are developing etripamil for the treatment of
specific  arrhythmias  with  a  lead  indication  to  treat  paroxysmal  supraventricular  tachycardia,  or  PSVT,  with  subsequent
indications to treat atrial fibrillation and rapid ventricular rate, or AFib-RVR, and other cardiovascular indications.

Etripamil - Pivotal Clinical Program in PSVT

PSVT is a rapid heart rate condition characterized by episodes of supraventricular tachycardia, or SVT, that start and stop
without warning. Episodes of SVT are often experienced by patients with symptoms including palpitations, sweating, chest
pressure or pain, shortness of breath, sudden onset of fatigue, lightheadedness or dizziness, fainting and anxiety. Calcium
channel blockers have long been approved for the treatment of PSVT as well as other cardiac conditions. Calcium channel
blockers available in oral form are frequently used prophylactically to control the frequency and duration of future episodes
of  SVT.  For  treatment  of  episodes  of  SVT,  approved  calcium  channel  blockers  are  administered  intravenously  under
medical  supervision,  usually  in  the  emergency  department.  The  combination  of  convenient  nasal-spray  delivery,  rapid-
onset and short duration of action of etripamil has the potential to shift the current treatment paradigm for episodes of SVT
away from the burdensome and costly emergency department setting. If approved, we believe that etripamil will be the first
self-administered therapy for the rapid termination of episodes of SVT wherever and whenever they occur.

Our late-stage etripamil clinical program for the treatment of PSVT is currently executing on two ongoing Phase 3 safety
and efficacy trials, RAPID and NODE-303. The RAPID study is our ongoing pivotal Phase 3 safety and efficacy trial. This
study enrolled its first patient in November 2020 and topline data is expected in mid-second half 2022. NODE-303 is an
open-label global safety trial enrolling patients to collect safety data that when combined with the safety data from the rest
of the program will form the safety dataset to be evaluated by the FDA and other regulatory agencies to form the basis for
marketing approval. We have also completed our first Phase 3 safety and efficacy trial of etripamil, NODE-301, and its
open-label safety extension trial, NODE-302. In addition to our PSVT clinical program, we began enrollment of patients in
a Phase 2 proof-of-concept clinical trial titled ReVeRA in the first quarter of 2021 to evaluate the potential effectiveness of
etripamil to reduce ventricular rate during AFib-RVR episodes.

In March 2020, we reported topline results of the NODE-301 pivotal trial of etripamil for the treatment of PSVT, which is a
placebo-controlled Phase 3 safety and efficacy trial. NODE-301, which enrolled a total of 431 patients across 65 sites in the
United States and Canada, did not meet its primary endpoint of time to conversion of SVT to sinus rhythm compared to
placebo over the five hour period in which patients wore a cardiac monitor following study drug administration.

In  July  2020,  we  announced  that  we  received  guidance  from  the  U.S.  Food  and  Drug  Administration,  or  FDA,  on  our
proposal to alter the size and design of our ongoing RAPID trial as well as the overall program based on the data from the
NODE-301  trial.    The  FDA  indicated  that  the  two  trials,  the  RAPID  trial  and  the  completed  NODE-301  trial,  could
potentially fulfill the efficacy requirement for our planned NDA for etripamil in patients with PSVT.

91

Table of Contents

Under an updated statistical analysis plan, or SAP, the primary efficacy endpoint for both the RAPID and NODE-301 trials
will be defined as time to conversion over the first 30 minutes, with a target p-value of less than 0.05 for each trial. This
endpoint  supports  the  desire  of  patients  to  rapidly  address  their  PSVT  symptoms  during  an  episode  and  ideally  avoid
visiting the emergency department. Later and earlier time points will also be assessed as part of secondary analyses to fully
characterize the efficacy profile of etripamil.

When employing the updated SAP retrospectively to the NODE-301 data, results in 54% of etripamil patients vs. 35% of
placebo patients converted within 30 minutes (HR 1.87, p=0.02). Applying the same primary endpoint to the RAPID study,
powering the study at 90% and using alpha of 0.05 to detect a 19% difference of etripamil versus placebo in 30 minute time
to conversion that was observed in the NODE-301 study results in the size of 180 confirmed PSVT events.

The  RAPID  study,  is  designed  very  similarly  to  NODE-301  however,  will  introduce  a  new  treatment  regimen  to  the
program.  Based  on  discussions  with  the  FDA  regarding  maximizing  the  treatment  effect  of  etripamil,  the  RAPID  trial
allows for repeat administration of study drug (either 70 mg of etripamil or placebo) for patients who have not experienced
symptom  relief  within  ten  minutes  of  the  first  study  drug  administration.  This  repeat  dose  regimen,  which  is  similar  to
current  PSVT  treatment  practices  in  the  emergency  department  setting,  is  tailored  to  the  pharmacokinetic  profile  of
etripamil  to  deliver  increased  exposure  over  approximately  the  first  30  minutes  following  initial  administration.  We
believe  that  the  repeat  administration  could  benefit  a  broader  group  of  patients,  including  those  with  more  persistent
episodes.

In  the  NODE-301  study,  32%  of  etripamil  patients  and  14%  of  placebo  patients  converted  to  sinus  rhythm  within  10
minutes. The FDA agreed that the single and repeat administrations of etripamil could be pooled and compared to placebo
for the primary analysis, resulting in no increase in the sample size.  

Etripamil - Safety Studies in PSVT

NODE-302 is our Phase 3 open-label safety extension of the NODE-301 trial. Patients who completed NODE-301 could
enroll in NODE-302 and receive up to an additional 11 doses of etripamil. NODE-302 is a multi-center, open label study
designed to evaluate the safety of etripamil nasal spray when self-administered by patients without medical supervision for
spontaneous  episodes  of  SVT  in  an  outpatient  setting.  Eligibility  was  also  contingent  on  satisfying  all  inclusion  and
exclusion criteria, including not experiencing a serious adverse event related to the study drug or the study procedure that
precludes the self-administration of etripamil. We completed NODE-302 in late 2020 with a data set of 245 episodes with
105  patients  dosed  at  least  once  out  of  169  patients  enrolled.  Trial  results  will  contribute  to  the  etripamil  NDA  safety
database.

NODE-303 is a Phase 3, multi-center, open-label safety trial, evaluating the safety of etripamil when self-administered
without medical supervision, and evaluating the treatment safety and efficacy of etripamil on multiple SVT episodes.
The study initiated with the etripamil 70 mg single dose regimen and the 70 mg repeat dose regimen was introduced
into the trial starting in the second half of 2021 following FDA acceptance of the protocol change.  The trial is designed
to add to the safety data from the remainder of the development program, including both the NODE-301 and RAPID
trials, in order to fulfill the safety data set needed for NDA filing. Our plan is to ascertain the final sizing of the trial
following future discussions with the FDA and other regulatory authorities.

We are conducting patient access programs to provide further access to etripamil to patients who have participated in the
clinical development registration trials to treat future SVT episodes. These programs are tailored to meet the regulatory
requirements in the territories in which the clinical sites are located.

92

Table of Contents

Etripamil: Atrial Fibrillation and Rapid Ventricular Rate

As with PSVT, calcium channel blockers are also approved for use in intravenous form for the treatment of some episodes
of atrial fibrillation in which patients experience rapid ventricular rates. We began enrollment in a Phase 2 proof-of-concept
clinical  trial,  titled  ReVeRA,  in  the  first  quarter  of  2021  to  evaluate  the  ability  of  etripamil  to  reduce  ventricular  rate  in
AFib-RVR episodes. The Phase 2 double blind, placebo controlled, proof-of-concept, which will be conducted in Canada
in  collaboration  with  the  Montreal  Heart  Institute  and  other  research  centers,  is  expected  to  enroll  approximately  50
patients  randomized  1:1  to  receive  either  70  mg  of  etripamil  nasal  spray  or  placebo.  The  primary  endpoint  will  assess
reduction in ventricular rate, with key secondary endpoints including the time to achieve the maximum reduction in rate
and the duration of the effect. The trial is to be conducted in the hospital or emergency department setting under medical
supervision.

Operations Overview

Since  the  commencement  of  our  operations  in  2003,  we  have  devoted  substantially  all  of  our  resources  to  performing
research  and  development  activities  in  support  of  our  product  development  efforts,  hiring  personnel,  raising  capital  to
support and expand such activities, providing general and administrative support for these operations and, more recently
preparing  for  commercialization.  We  operate  our  business  using  a  significant  outsourcing  model.   As  such,  our  team  is
composed  of  a  relatively  smaller  core  of  employees  who  direct  a  significantly  larger  number  of  team  members  who  are
outsourced in the forms of vendors and consultants to enable execution of our operational plans. We do not currently have
any products approved for sale, and we continue to incur significant research and development and general administrative
expenses related to our operations.

Since  inception,  we  have  incurred  significant  operating  losses.  For  the  years  ended  December  31,  2021  and  2020,  we
recorded  net  losses  of  $42.9  million  and  $50.0  million,  respectively.  As  of  December  31,  2021,  we  had  an  accumulated
deficit of $206.3 million. We expect to continue to incur significant losses for the foreseeable future. We anticipate that a
substantial portion of our capital resources and efforts in the foreseeable future will be focused on completing the necessary
development  activities  required  for  obtaining  regulatory  approval  and  preparing  for  potential  commercialization  of  our
product candidates. We had $114.1 million of cash and cash equivalents at December 31, 2021.

We expect to continue to incur significant expenses and increasing operating losses for at least the next several years. Our
net  losses  may  fluctuate  significantly  from  period  to  period,  depending  on  the  timing  of  our  planned  clinical  trials  and
expenditures on other research and development activities. We expect our expenses will increase substantially over time as
we:

● continue our ongoing and planned development of etripamil, including our Phase 3 clinical trials of etripamil for

the treatment of PSVT and our Phase 2 clinical trial of etripamil for the treatment of AFib-RVR;

● seek  marketing  approvals  for  etripamil  for  the  treatment  of  PSVT,  AFib-RVR  and  other  cardiovascular

indications;

● establish a sales, marketing, manufacturing and distribution capability, either directly or indirectly through third
parties, to commercialize etripamil or any future product candidate for which we may obtain marketing approval;

● build  a  portfolio  of  product  candidates  through  development,  or  the  acquisition  or  in-license  of  drugs,  product

candidates or technologies;

● initiate preclinical studies and clinical trials for etripamil for any additional indications we may pursue, including
the clinical trials for the treatment of atrial fibrillation and rapid ventricular rate as well as other areas of unmet
medical need, and for any additional product candidates that we may pursue in the future;

93

Table of Contents

● maintain, protect and expand our intellectual property portfolio;

● hire additional clinical, regulatory and scientific personnel;

● add  operational,  financial  and  management  information  systems  and  personnel,  including  personnel  to  support

our product development and planned future commercialization efforts; and

● incur additional legal, accounting, insurance and other expenses associated with operating as a public company.

Recent Developments

On  February  15,  2022,  the  Company  announced  the  appointment  of  David  Bharucha,  M.D.,  Ph.D.,  as  Chief  Medical
Officer. Dr. Bharucha is a cardiac electrophysiologist who brings to Milestone over thirty years of global drug development
and clinical experience across a range of therapeutic areas, with a focus on cardiovascular medicine. He replaces Francis
Plat,  M.D.,  who  transitioned  to  Chief  Scientific  Officer  of  the  Company  and,  following  the  completion  of  the  Phase  3
RAPID trial in the second half of 2022, will transition further to serve in an advisory capacity.

COVID-19 Business Update

The periods of reduced global economic activity and volatility, the overall disruption of global healthcare systems and the
other risks and uncertainties associated with the pandemic could have a material adverse effect on our business, financial
condition, results of operations and growth prospects.  Our global workforce is utilizing a hybrid remote and office based
model and this adjustment may adversely impact our business (see below for discussion on Clinical Development impacts).
In  addition,  working  at  home  policies  could  increase  cybersecurity  risk  and  communication  disruptions.    The  ongoing
pandemic has resulted in many state, local and foreign governments implementing, and continually making adjustments to,
restrictions as the spread and severity of the COVID-19 virus has impacted their territories, including as it relates to newer
strains such as the Delta and Omicron variants.  We continue to closely monitor the pandemic as we evolve our business
continuity plans and response strategy.

Clinical Development

With respect to clinical development, we have taken measures to maintain patient safety and trial continuity and to preserve
study integrity.  For our clinical development programs, we have experienced disruptions or delays in our ability to initiate
trial sites and enroll and assess patients, and such disruptions or delays may continue. The COVID-19 pandemic continues
to  impact  patient  enrollment  rates  in  all  of  our  clinical  studies.  While  COVID-19  resurgences  around  the  world  impact
different geographies and clinical sites to varying degrees and at different times, the PSVT clinical program average overall
enrollment  rate  has  stabilized  in  2021.  During  the  first  three  quarters  of  2021,  the  COVID-19  pandemic  delayed  the
initiation  of  many  proposed  RAPID  clinical  trial  sites  as  some  health  care  institutions  prioritized  their  resources  for
pandemic related activities with some precluding the initiation of new clinical trials or conduct of existing trials.  It also
delayed the initiation of enrollment for our ReVeRA trial of etripamil for AFib-RVR performed in the acute care hospital
setting  in  Quebec,  Canada,  due  to  closures  of  clinical  sites  as  well  as  to  the  increased  stress  that  COVID-19  places  on
Emergency  Departments  logistics  and  staff.    Given  the  uncertainty  and  differing  and  evolving  restrictions  applicable  to
clinical trial sites and participants, additional disruptions and delays are possible. We will continue to monitor the impact of
COVID-19 on our planned clinical sites and patient enrollment activities.  We could also see an impact on the ability to
supply  study  drug,  report  trial  results,  or  interact  with  regulators,  ethics  committees  or  other  important  agencies  due  to
limitations in regulatory authority employee resources or otherwise.  In addition, we rely on contract research organizations
or  other  third  parties  to  assist  us  with  clinical  trials,  and  we  cannot  guarantee  that  they  will  continue  to  perform  their
contractual duties in a timely and satisfactory manner as a result of the COVID-19 pandemic.  If the COVID-19 pandemic
continues and persists for an extended period of time, and if phased reopening’s stall or are limited due to continued spread
of  COVID-19,  including  variants,  we  could  experience  further  significant  disruptions  to  our  clinical  development
timelines, which would adversely affect our business, financial condition, results of operations and growth prospects.

94

Table of Contents

Other Financial and Corporate Impacts

While we expect the COVID-19 pandemic to continue to affect our business operations and financial results, the extent of
the impact on our clinical development and regulatory efforts, our corporate development objectives and the value of and
market for our common shares, will depend on future developments that are highly uncertain and cannot be predicted with
confidence at this time, such as the ultimate duration of the pandemic, travel restrictions, business closure requirements in
the United States, Canada, Europe and other countries, the timing and unpredictability of achieving widespread vaccination
rates, the effectiveness of any vaccines against new variants, and the timing of the return of the global economy to pre-
pandemic  levels.  In  addition,  we  may  be  impacted  by  general  economic,  political,  and  market  conditions,  including
deteriorating market conditions due to investor concerns regarding inflation and Russian hostilities in Ukraine and overall
fluctuations in the financial markets in the United States and abroad.

Components of Results of Operations

Revenues

We have not generated any revenues from product sales to date and we do not expect to generate revenues from product
sales in the near future. Our revenues for the current year are from the license and collaboration agreement with Ji Xing
and are comprised of a non-refundable upfront cash payment received on June 22, 2021. For additional information about
our Revenue,  see “Note 2— Summary of Significant Accounting Policies, and Note 3 - Revenue.”

Research and Development Expenses

Research  and  development  expenses  consist  primarily  of  salaries  and  fees  paid  to  external  service  providers  and  also
include  personnel  costs,  including  share-based  compensation  expense  and  other  related  compensation  expenses.  We
expense research and development costs in the periods in which they are incurred. Costs for certain development activities
are recognized based on an evaluation of the progress to completion of specific tasks using information and data provided
to us by our vendors, collaborators and third-party service providers.

To  date,  substantially  all  of  our  research  and  development  expenses  have  been  related  to  the  preclinical  and  clinical
development of etripamil. As we advance etripamil or other product candidates for other indications, we expect to allocate
our direct external research and development costs across each of the indications or product candidates. Further, while we
expect our research and development costs for the development of etripamil in atrial fibrillation with rapid ventricular rate
to  increase  for  initiation  of  the  ReVeRA  clinical  trial  as  we  continue  to  expand  this  trial,  we  expect  our  research  and
development  expenses  related  to  the  development  of  etripamil  for  PSVT  to  remain  a  very  large  majority  of  our  total
research and development expenses.

We expect our research and development expenses to increase as we continue the development of etripamil and prepare to
pursue  regulatory  approval.  The  process  of  conducting  the  necessary  clinical  research  to  obtain  regulatory  approval  is
costly  and  time-consuming  and  is  subject  to  uncertainties  and  delays,  including  as  a  result  of  the  ongoing  COVID-19
pandemic. As a result of the uncertainties discussed above, we are unable to determine the duration and completion costs of
our research and development projects or when and to what extent we will generate revenue from the commercialization
and sale of our product candidates, if at all.

We  recognize  the  benefit  of  Canadian  research  and  development  tax  credits  as  a  reduction  of  research  and  development
costs for fully refundable investment tax credits.

95

Table of Contents

General and Administrative Expenses

General and administrative expenses include personnel and related compensation costs, expenses for outside professional
services, lease expense, insurance expense and other general administrative expenses. Personnel costs consist of salaries,
bonuses,  benefits,  related  payroll  taxes  and  share-based  compensation.  Outside  professional  services  consist  of  legal,
accounting and audit services and other consulting fees.

We expect to continue to incur expenses as a public company, including expenses related to compliance with the rules and
regulations of the Securities and Exchange Commission, or SEC, and those of any national securities exchange on which
our  securities  are  traded,  additional  insurance  expenses,  investor  relations  activities,  and  other  administrative  and
professional services.

Commercial Expenses

Commercial expenses consist primarily of personnel and related compensation costs, market and health economic research,
and market development activities for PSVT and, to a lesser extent, AFib-RVR. The focus of these expenses is three-fold:
first, we want to leverage rigorous primary and secondary research to fully understand our target disease states from the
perspective  of  the  patient,  healthcare  provider,  and  payer;  second,  we  want  to  understand  and  document  the  burden  of
disease posed by PSVT and AFib-RVR from an epidemiology, healthcare resource use, and cost perspective; and third, we
want  to  engage  our  target  patient,  physician,  and  payer  stakeholders  with  evidence-based  and  compliant  educational
materials that serve to increase the awareness and understanding of the impact of PSVT and AFib-RVR on patients and the
overall healthcare system.

Starting  approximately  six  months  to  one  year  before  we  file  our  new  drug  application,  or  NDA  with  the  FDA,  we
anticipate our commercial expenses will increase substantially as we invest in the infrastructure, personnel, and operational
expenses required to launch our first product in the United States, if approved.

Interest Income

Interest income primarily consists of interest income from our cash equivalents and short-term investments.

Results of Operations

Comparison of the Years Ended December 31, 2021 and 2020

(in thousands)

Revenue

Operating expenses

Research and development, net of tax credits
General and administrative
Commercial

Total operating expenses

Loss from operations
Interest income, net
Loss before income taxes
Income tax benefit
Net loss

Year ended December 31, 

2021

2020

$ Change      % Change

$  15,000

 — $  15,000  

100.0%

38,671
  12,399
7,003
 58,073
   (43,073)
 220
 (42,853)

 —  

34,488
10,285
5,937
 50,710
 (50,710)
 726
 (49,984)
 17

$  (42,853) $  (49,967) $

 4,183  
 2,114  
 1,066  
 7,363  
 7,637  
 (506) 
 7,131  
 (17) 
 7,114  

12.1%
20.6%
18.0%
14.5%
(15.1)%
(69.7)%
(14.3)%
(100.0)%
(14.2)%

96

 
    
    
 
 
 
 
 
 
 
 
 
 
 
 
 
Table of Contents

Revenue

We  generated  revenue  of  $15  million  from  upfront  payments  under  the  License  Agreement  during  the  year  ended
December 31, 2021.

Research and Development Expenses

The following table shows our research and development expenses by type of activity for the periods indicated.

Year ended December 31, 

(in thousands)
Clinical
Drug manufacturing and formulation
Regulatory and other costs
Less: R&D tax credits
Total R&D expenses

2021
$  30,984
 5,691
 2,454
 (458)
$  38,671

2020
$  28,098
 4,580
 2,183
 (373)
$  34,488

$ Change     % Change
10.3%
$
24.3%
12.4%
22.8%
12.1%

 2,886  
 1,111  
 271  
 (85) 
 4,183  

$

Research and development expenses increased by $4.2 million, or 12.1% for the year ended December 31, 2021 compared
to the year ended December 31, 2020. Clinical trial expense increased by $2.9 million mainly due to an increase of $1.5
million in clinical personnel related costs, higher clinical consulting fees and CRO costs due to advancing RAPID Phase 3
efficacy  and  safety  trials  in  etripamil  for  the  treatment  of  PSVT  along  with  an  increase  in  non-cash  compensation  costs
related to share-based compensation expense.

General and Administrative

General and administrative expenses increased by $2.1 million, or 20.6% for the year ended December 31, 2021 compared
to the year ended December 31, 2020. The primary contributor to the increase was due to the increase of personnel related
costs  for  general  and  administrative  expenses  of    $1.4  million.  This  comprises  $1.0  million  non-cash  compensation  cost
increase compared to prior year related to share-based compensation expense mainly due to high stock option valuation in
2020 and $0.4 million primarily due to the reversal of temporary salary implemented in June 2020.

Commercial

Commercial expenses increased by $1.1 million, or 18.0%, for the year ended December 31, 2021, compared to the same
period in 2020. The increase is due to marketing and personnel related costs, mainly resulting from an increase in non-cash
compensation costs related to share-based compensation expense.

Interest Income, net

Interest income, net, was $0.2 million and $0.7 million for the year ended December 31, 2021 and 2020, respectively.  The
reduction in interest income was due to lower interest rates earned on investments in 2021 when compared to 2020.

Liquidity and Capital Resources

Sources of Liquidity

We have incurred operating losses and experienced negative operating cash flows since our inception, and we anticipate
continuing to incur losses for at least the next several years. As of December 31, 2021, we had cash and cash equivalents
$114.1 million and an accumulated deficit of $206.3 million.

97

    
    
 
 
 
 
 
 
 
 
 
Table of Contents

On  May  15,  2021,  pursuant  to  the  License  Agreement,  we  and  affiliates  of  RTW  Investments,  LP,  (RTW),  or  the
Purchasers,  entered  into  a  securities  purchase  agreement  pursuant  to  which  we  issued  to  the  Purchasers,  in  a  private
placement, pre-funded warrants to purchase up to an aggregate of 910,746 of our common shares at a purchase price of
$5.48 per pre-funded warrant, or the Private Placement. The gross proceeds to us from the Private Placement, excluding
proceeds from the exercise price of the warrants, were approximately $5.0 million.

On  July  29,  2020,  we  entered  into  an  Open  Market  Sale  Agreement℠,  or  the  Sales  Agreement,  with  Jefferies  LLC,  or
Jefferies, with respect to an at-the-market offering program, or the ATM Program, under which we may issue and sell our
common shares having an aggregate offering price of up to $50 million through Jefferies as our sales agent or principal.
The common shares to be sold under the Sales Agreement, if any, will be offered and sold pursuant to our shelf registration
statement on Form S-3 (File No. 333-239318), which was declared effective by the Securities and Exchange Commission
on July 6, 2020. We have not sold shares under the ATM program as of the date of this filing.

We have evaluated whether material uncertainties exist relating to clinical trials, the COVID-19 pandemic and the impact
on market conditions. The COVID-19 pandemic has had an impact on our business, operations and clinical development
timelines.  Government  orders  and  restrictions  in  order  to  control  the  spread  of  the  disease  have  impacted  patient
recruitment, enrollment and follow-up visits at clinical sites. At the date of the publication of our annual report, it is not
possible  to  reliably  estimate  the  length  and  severity  of  these  developments.  We  expect  that  our  current  operating  plan,
existing cash and cash equivalents and access to financing sources to be sufficient to fund our operations and determined
that there are no events or conditions that may cast substantial doubt on our ability to continue as a going concern for at
least the next 12 months from the date of this filing. Based on our cash and cash equivalents as of December 31, 2021,
including the upfront payment from Ji Xing and proceeds from the equity investment from the Purchasers, we expect to be
able to support our ongoing operations into mid-2023.

Funding Requirements

We  use  our  cash  primarily  to  fund  research  and  development  expenditures.  We  expect  our  research  and  development
expenses to increase as we continue the development of etripamil and prepare to pursue regulatory approval. We expect to
incur an increase in general and administrative expenses, and an increase in expenses related to commercial activities in
2022  as  we  focus  our  efforts  on  the  clinical  pathway  and  potential  commercialization  of  etripamil.  We  expect  to  incur
increasing operating losses for the foreseeable future as we continue the clinical development of our product candidate. At
this time, due to the inherently unpredictable nature of clinical development, we cannot reasonably estimate the costs we
will incur and the timelines that will be required to complete development, obtain marketing approval, and commercialize
etripamil or any future product candidates, if at all. For the same reasons, we are also unable to predict when, if ever, we
will generate revenue from product sales or whether, or when, if ever, we may achieve profitability. Clinical and preclinical
development timelines, the probability of success, and development costs can differ materially from expectations.

In  addition,  we  have  exclusive  development  and  commercialization  rights  for  etripamil  for  all  indications  that  we  may
pursue and as such have the potential to license development and or commercialization rights for etripamil to a potential
partner.  We  plan  to  establish  commercialization  and  marketing  capabilities  using  a  direct  sales  force  to  commercialize
etripamil  in  the  United  States.  Outside  of  the  United  States,  we  are  considering  commercialization  strategies  that  may
include  collaborations  with  other  companies.  We  have  recently  entered  into  such  agreement  Ji  Xing,  which  is  futher
discussed below.

On  May  15,  2021,  we  entered  into  the  License  Agreement  with  Ji  Xing,  which  is  an  entity  affiliated  with  RTW
Investments, LP, (RTW) a beneficial owner of approximately 14.4% of the Company’s common shares. Under the License
Agreement,  we  granted  Ji  Xing  exclusive  development  and  commercialization  rights  to  any  pharmaceutical  product  that
uses  a  device  to  deliver  the  Company’s  proprietary  calcium  channel  blocker  known  as  etripamil  by  nasal  spray  for  all
prophylactic and therapeutic uses in humans in the following territories: People’s Republic of China, including mainland
China, Hong Kong Special Administrative Region, Macau Special Administrative Region, and Taiwan (the Territory). Ji
Xing  will  be  responsible  for  development  and  regulatory  activities  in  the  Territory,  and  we  will  remain  responsible  for
certain  manufacturing  activities  in  the  Territory,  subject  to  the  supply  agreement  subsequently  entered  into  by  us  and  Ji
Xing  as  contemplated  by  the  License  Agreement  (the  Supply  Agreement).    We  received  a  non-refundable  upfront  cash
payment of

98

Table of Contents

$15 million and the right to future payments of up to $107.5 million in total development and sales milestone payments. In
addition, we are entitled to receive tiered royalty payments ranging from a percentage in the low double digits to the high
double digits of Net Sales (as defined in the License Agreement) of all products sold in the Territory.

For other new product candidates, our efforts are focused on licensing development and/or commercialization rights from
potential partners.  In the case of either in-licensing or out-licensing, we cannot forecast when such arrangements will be
secured, if at all, and to what degree such arrangements would affect our development and commercialization plans and
capital requirements.

The timing and amount of our operating expenditures will depend largely on:

● the  timing,  progress  and  results  of  our  ongoing  and  planned  clinical  trials  and  other  development  activities  of

etripamil in PSVT, AFib-RVR and in other cardiovascular indications;

● the scope, progress, results and costs of preclinical development, laboratory testing and clinical trials of etripamil

for additional indications or any future product candidates that we may pursue;

● our ability to establish collaborations on favorable terms, if at all;

● the  ability  of  vendors  and  third-party  service  providers  to  accurately  forecast  expenses  and  deliver  on

expectations;

● the costs, timing and outcome of regulatory review of etripamil and any future product candidates;

● the costs and timing of future commercialization activities, including product manufacturing, marketing, sales and

distribution, for etripamil and any future product candidates for which we receive marketing approval;

● the revenue, if any, received from commercial sales of etripamil and any future product candidates for which we

receive marketing approval;

● the  costs  and  timing  of  preparing,  filing  and  prosecuting  patent  applications,  maintaining  and  enforcing  our

intellectual property rights and defending any intellectual property-related claims; and

● the extent to which we acquire or in-license other product candidates and technologies.

Until such time, if ever, as we can generate substantial revenue from product sales, we expect to fund our operations and
capital funding needs through equity and/or debt financing. We may also consider entering into collaboration arrangements
or  selectively  partnering  for  clinical  development  and  commercialization.  The  sale  of  additional  equity  would  result  in
additional dilution to our shareholders. The incurrence of debt financing would result in debt service obligations and the
instruments  governing  such  debt  could  provide  for  operating  and  financing  covenants  that  restrict  our  operations  or  our
ability  to  incur  additional  indebtedness  or  pay  dividends,  among  other  items.  In  addition,  the  COVID-19  pandemic  has
resulted  in  periods  of  reduced  global  economic  activity  and  volatility.  If  the  disruption  contributes  to  future  periods  of
disruption of the global financial markets, we could experience an inability to access additional capital, which could in the
future negatively affect our operations. If we are not able to secure adequate additional funding, we may be forced to make
reductions  in  spending,  extend  payment  terms  with  suppliers,  liquidate  assets  where  possible,  and/or  suspend  or  curtail
planned programs. Any of these actions could materially and adversely affect our business, financial condition and results
of operations.

99

Table of Contents

Cash Flows

The following table summarizes our cash flows for the periods indicated:

(in thousands)
Net cash (used in) provided by:

Operating activities
Investing activities
Financing activities

Net increase (decrease) in cash and cash equivalents during the period

Operating Activities

2021

Year ended December 31, 
$ Change

2020

 % Change

$  (33,224) $  (50,732)
 (70,000)
 73,224
$  41,831   $  (47,508)

 70,000
 5,055

 17,508  
 140,000  
 (68,169) 
 89,339  

34.5%
200.0%
93.1%

Net cash used in operating activities during the year ended December 31, 2021 was $33.2 million, which consisted of a net
loss of $42.9 million and a net change of $2.3 million in our operating assets and liabilities, in addition to non-cash charges
of $7.4 million related to share-based compensation and depreciation expenses.

Net cash used in operating activities during the year ended December 31, 2020 was $50.7 million, which consisted of a net
loss of $50.0 million and a net change of $5.7 million in our operating assets and liabilities offset by non-cash charges of
$5.0 million related to share-based compensation and depreciation expenses.

Investing Activities

In the year ended December 31, 2021, we redeemed $85.0 million of short-term investments and we acquired $15.0 million
of short-term investments. In the year ended December 30, 2020, we redeemed $20.0 million of short-term investments and
we acquired $90.0 million of short-term investments.

Financing Activities

In the year ended December 31, 2021, our financing activities provided $5.0 million, consisting of net proceeds from the
Private Placement and a de minimis amount of proceeds from the exercise of share options. In the year ended December
31,  2020,  our  financing  activities  provided  $73.2  million,  consisting  of  net  proceeds  of  $24.9  million  from  the  Private
Placement, $23.2 million from the pre-funded warrants in a public offering, $24.8 million from the pre-funded warrants
and proceeds of $0.3 million from the exercise of share options.

Contractual Obligations

We  enter  into  contracts  in  the  normal  course  of  business  with  clinical  research  organizations,  or  CROs,  contract
manufacturing organizations, or CMOs, and other third parties for clinical trials, preclinical research studies and testing and
manufacturing services. These contracts are generally cancelable at our option with various notice requirements as defined
in the contract. Payments due upon cancellation consist of payments for services provided or expenses incurred, including
noncancelable  obligations  of  our  service  providers,  up  to  and  through  the  date  of  cancellation.  These  payments  are  not
included as the amount and timing of these payments are not known.

Critical Accounting Estimates

Our management’s discussion and analysis of our financial condition and results of operations is based on our consolidated
financial  statements  as  at  December  31,  2021,  which  have  been  prepared  in  accordance  with  United  States  generally
accepted accounting principles, or U.S. GAAP and on a basis consistent with those accounting principles followed by us.
The preparation of these consolidated financial statements requires our management to make judgments and estimates that
affect the reported amounts of assets and liabilities and the disclosure of contingent assets and liabilities at the date of the

100

    
Table of Contents

financial  statements,  as  well  as  the  reported  revenue  generated  and  expenses  incurred  during  the  reporting  periods.  Our
estimates  are  based  on  our  historical  experience  and  on  various  other  factors  that  we  believe  are  reasonable  under  the
circumstances, the results of which form the basis for making judgments about the carrying value of assets and liabilities
that are not readily apparent from other sources. Significant estimates and judgments include, but are not limited to:

● Estimates of the percentage of work completed of the total work over the life of the individual trial in
accordance with agreements established with CROs, CMOs and clinical trial sites which in turn impact
the research & development expenses.

● Estimate of the grant date fair value share options granted to employees, consultants and direct, and the

resulting share-based compensation expense, using the Black-Scholes option-pricing model.

Accordingly, actual results may differ from these judgments and estimates under different assumptions or conditions and
any such differences may be material. We believe that the accounting policies discussed below are critical to understanding
our  historical  and  future  performance,  as  these  policies  relate  to  the  more  significant  areas  involving  management’s
judgments and estimates.

a) Research & Development Expenses — Accruals

Research and development costs are charged against income in the period of expenditure. Our research and development
costs consist primarily of salaries and fees paid to CROs and to CMO.

Clinical trial expenses include direct costs associated with CROs, direct CMO costs for the formulation and packaging of
clinical trial material, as well as investigator and patient-related costs at sites at which our trials are being conducted. Direct
costs associated with our CROs and CMOs are generally payable on a time-and-materials basis, or when milestones are
achieved. The invoicing from clinical trial sites can lag several months. We record expenses for our clinical trial activities
performed by third parties based upon estimates of the percentage of work completed of the total work over the life of the
individual trial in accordance with agreements established with CROs and clinical trial sites. We determine the estimates
through discussions with internal clinical personnel, CROs and CMOs as to the progress or stage of completion of trials or
services  and  the  agreed-upon  fee  to  be  paid  for  such  services  based  on  facts  and  circumstances  known  to  us  as  of  each
consolidated balance sheet date. The actual costs and timing of clinical trials are highly uncertain, subject to risks and may
change  depending  upon  a  number  of  factors,  including  our  clinical  development  plan.  If  the  actual  timing  of  the
performance of services of the level of effort varies from the estimate, we will adjust the accrual accordingly. Adjustments
to  prior  period  estimates  have  not  been  material.  We  recognize  the  benefit  of  Canadian  research  and  development  tax
credits as a reduction of research and development costs for fully refundable investment tax credits and as a reduction of
income taxes for investment tax credits that can only be claimed against income taxes payable when there is reasonable
assurance that the claim will be recovered.

b) Share-Based Compensation

We  recognize  compensation  costs  related  to  share  options  granted  to  employees,  consultants  and  directors  based  on  the
estimated fair value of the awards on the date of grant. We estimate the grant date fair value, and the resulting share-based
compensation  expense,  using  the  Black-Scholes  option-pricing  model.  This  Black-Scholes  option  pricing  model  uses
various  inputs  to  measure  fair  value,  including  estimated  fair  value  of  our  underlying  common  shares  at  the  grant  date,
expected  term,  estimated  volatility,  risk-free  interest  rate  and  expected  dividend  yields  of  our  common  shares.  The
estimated volatility creates a critical estimate because we have not been a public company long enough to demonstrate our
own historical volatility. The grant date fair value of the share-based awards is recognized on a straight-line basis over the
requisite service periods, which are generally the vesting period of the respective awards. Forfeitures are accounted for as
they occur.

101

Table of Contents

The  following  table  summarizes,  by  grant  date,  the  number  of  underlying  common  shares  and  the  associated  per-share
exercise price, which was the fair value per share as determined by our board of directors on the applicable grant date, for
share options granted during the years ended December 31, 2020 and 2021:

Number of
Common Shares
Subject to

Exercise
Price Per
    Options Granted     Common Share     Grant Date     

Estimated
Fair Value
per Common
Share at

January 6, 2020
January 23, 2020
February 10, 2020
June 5, 2020
June 26, 2020
June 29, 2020
October 1, 2020
March 1, 2021
March 24, 2021
April 26, 2021
June 14, 2021
August 30, 2021
September 13, 2021
October 1, 2021
November 1, 2021

 13,000
 748,400
 3,760
 690,500
 11,000
 7,800
 60,000
 70,000
 1,793,950
 11,300
 180,000
 7,300
 2,650
 8,050
 64,000

$
$
$
$
$
$
$
$
$
$
$
$
$
$
$

17.000
21.480
21.730
3.740
3.850
3.830
7.100
7.510
6.260
5.910
5.540
6.070
5.650
5.640
5.700

$
$
$
$
$
$
$
$
$
$
$
$
$
$
$

17.000
21.480
21.730
3.740
3.850
3.830
7.100
7.510
6.260
5.910
5.540
6.070
5.650
5.640
5.700

Estimated
Per-Share
Fair Value
of Options
11.948
15.248
15.390
2.610
2.680
2.740
5.200
5.672
4.758
4.490
3.958
4.606
4.287
4.282
4.314

$
$
$
$
$
$
$
$
$
$
$
$
$
$
$

The intrinsic value of all outstanding options as of December 31, 2021 was $11.7 million, based on the fair value of our
common shares of $6.55 per share at December 31, 2021, of which $9.8 million related to vested options and $1.9 million
related to unvested options.

Recent Accounting Pronouncements

Refer to Note 2, “Summary of Significant Accounting Policies,” in the accompanying notes to our consolidated financial
statements for a discussion of recent accounting pronouncements.

Emerging Growth Company Status

The Jumpstart Our Business Startups Act of 2012 permits an “emerging growth company” such as us to take advantage of
an  extended  transition  period  to  comply  with  new  or  revised  accounting  standards  applicable  to  public  companies  until
those  standards  would  otherwise  apply  to  private  companies.  We  have  irrevocably  elected  to  “opt  out”  of  this  provision
and,  as  a  result,  we  comply  with  new  or  revised  accounting  standards  when  they  are  required  to  be  adopted  by  public
companies that are not emerging growth companies.

102

Table of Contents

ITEM 7A.     QUANTITATIVE AND QUALITATIVE DISCLOSURES ABOUT MARKET RISK.

Quantitative and Qualitative Disclosures about Market Risk

We are exposed to market risks in the ordinary course of our business. These risks primarily relate to interest rate risks. We
had cash and cash equivalents of $114.1 million and $142.3 million as of December 31, 2021 and 2020, respectively, which
consist  primarily  of  bank  deposits  and  guaranteed  investment  certificates.  The  primary  objective  of  our  investment
activities is to preserve principal and liquidity while maximizing income without significantly increasing risk. We do not
enter into investments for trading or speculative purposes. Due to the short-term nature of our investment portfolio, we do
not believe an immediate 10% increase or decrease in interest rates would have a material effect on the fair market value of
our portfolio, and accordingly we do not expect our operating results or cash flows to be materially affected by a sudden
change in market interest rates.

We undertake certain transactions in Canadian dollars and as such are subject to risk due to fluctuations in exchange rates.
Canadian dollar denominated payables are paid at the converted rate as due. We do not use derivative instruments to hedge
exposure  to  foreign  exchange  rate  risk  due  to  the  low  volume  of  transactions  denominated  in  foreign  currencies.  At
December  31,  2021  and  2020,  our  net  monetary  exposure  denominated  in  Canadian  dollars  was  $1.1  million  and
$0.2 million, respectively.

Our operating results and financial position are reported in U.S. dollars in our financial statements. The fluctuation of the
Canadian dollar in relation to the U.S. dollar might, consequently, have an impact upon our loss and may also affect the
value  of  our  assets  and  the  amount  of  shareholders’  equity.  We  do  not  believe  that  inflation  and  changing  prices  had  a
significant impact on our results of operations for any periods presented herein.

103

Table of Contents

ITEM 8.     FINANCIAL STATEMENTS

INDEX TO CONSOLIDATED FINANCIAL STATEMENTS

Report of Independent Registered Public Accounting Firm (PCAOB ID: 271)
Consolidated Balance Sheets
Consolidated Statements of Loss
Consolidated Statements of Shareholders’ Equity
Consolidated Statements of Cash Flows
Notes to Consolidated Financial Statements

105
106
107
108
109
110

104

Table of Contents

Report of Independent Registered Public Accounting Firm

To the Shareholders and Board of Directors of Milestone Pharmaceuticals Inc.

Opinion on the Financial Statements

We  have  audited  the  accompanying  consolidated  balance  sheets  of  Milestone  Pharmaceuticals  Inc.  and  its  subsidiary
(together,  the  “Company”)  as  of  December  31,  2021  and  2020,  and  the  related  consolidated  Statements  of  Loss,  and
shareholders’  equity  for  each  of  the  years  then  ended,  including  the  related  notes  (collectively  referred  to  as  the
“consolidated financial  statements”).  In  our  opinion,  the  consolidated  financial  statements  present  fairly,  in  all  material
respects, the financial position of the Company as of December 31, 2021 and 2020, and the results of its operations and its
cash flows for the years then ended in  conformity  with  accounting  principles  generally  accepted  in  the  United  States  of
America.  

Basis for Opinion

These  consolidated  financial  statements  are  the  responsibility  of  the  Company’s  management.  Our  responsibility  is  to
express an opinion on the Company’s consolidated financial statements based on our audits. We are a public accounting
firm  registered  with  the  Public  Company  Accounting  Oversight  Board  (United  States)  (PCAOB)  and  are  required  to  be
independent with respect to the Company in accordance with the U.S. federal securities laws and the applicable rules and
regulations of the Securities and Exchange Commission and the PCAOB.

We conducted our audits of these consolidated financial statements in accordance with the standards of the PCAOB. Those
standards  require  that  we  plan  and  perform  the  audit  to  obtain  reasonable  assurance  about  whether  the  consolidated
financial statements are free of material misstatement, whether due to error or fraud. The Company is not required to have,
nor  were  we  engaged  to  perform,  an  audit  of  its  internal  control  over  financial  reporting.  As  part  of  our  audits  we  are
required  to  obtain  an  understanding  of  internal  control  over  financial  reporting  but  not  for  the  purpose  of  expressing  an
opinion on the effectiveness of the Company’s internal control over financial reporting. Accordingly, we express no such
opinion.

Our  audits  included  performing  procedures  to  assess  the  risks  of  material  misstatement  of  the  consolidated  financial
statements, whether due to error or fraud, and performing procedures that respond to those risks. Such procedures included
examining, on a test basis, evidence regarding the amounts and disclosures in the consolidated financial statements. Our
audits also included evaluating the accounting principles used and significant estimates made by management, as well as
evaluating the overall presentation of the consolidated financial statements. We believe that our audits provide a reasonable
basis for our opinion.

/s/PricewaterhouseCoopers LLP
Montreal, Canada
March 24, 2022

We have served as the Company's auditor since 2016

105

Table of Contents

Milestone Pharmaceuticals Inc.
Consolidated Balance Sheets
(in thousands of US dollars, except share data)

Assets

Current assets

Cash and cash equivalents
Short-term investments
Research and development tax credits receivable
Prepaid expenses
Other receivables  

Total current assets
Operating lease assets
Property and equipment
Total assets

Liabilities, and Shareholders' Equity

Current liabilities

Accounts payable and accrued liabilities
Operating lease liabilities

Total current liabilities
Operating lease liabilities (net of current portion)
Total liabilities
Commitments and contingencies (Note 13)

Shareholders’ Equity
Common shares, no par value, unlimited shares authorized 29,897,559 shares issued and
outstanding as of December 31, 2021, 29,827,997 shares issued and outstanding as of
December 31, 2020
Pre-funded warrants - 12,327,780 issued and outstanding as of December 31, 2021 and
11,417,034 as of December 31, 2020
Additional paid-in capital
Cumulative translation adjustment
Accumulated deficit

Total shareholders’ equity

Total liabilities and shareholders’ equity

December 31, 2021     

December 31, 2020

$

$

$

$

$

$

114,141  

—
356  
4,299  
127  
118,923  

711
215  
119,849  

6,551  
224  
6,775  
474  
7,249  

251,901  

52,941
15,711  
(1,634) 
(206,319) 

112,600  

$

119,849  

$

72,310
70,000
725
5,428
223
148,686
980
308
149,974

5,914
245
6,159
696
6,855

251,682

48,007
8,530
(1,634)
(163,466)

143,119

149,974

The accompanying notes are an integral part of these consolidated financial statements.

106

    
   
  
   
  
   
  
   
  
   
  
Table of Contents

Milestone Pharmaceuticals Inc.
Consolidated Statements of Loss
(in thousands of US dollars, except share and per share data)

Revenue

Operating expenses
Research and development, net of tax credits
General and administrative
Commercial

Loss from operations

Interest income, net

Loss before income taxes

Income tax benefit

Net loss

Weighted average number of shares and pre-funded warrants outstanding, basic and diluted

Net loss per share, basic and diluted

The accompanying notes are an integral part of these consolidated financial statements.

107

Year ended December 31, 
2020

2021

$

15,000  

$

—

38,671  
12,399  
7,003  

34,488
10,285
5,937

(43,073) 

(50,710)

220  

726

(42,853)

(49,984)

—  

17

(42,853) 

$

(49,967)

41,833,861

29,344,993

(1.02) 

$

(1.70)

$

$

                                                                                                                                                                        
   
   
 
Table of Contents

Balance as of December 31, 2019
Transactions during 2020
Net loss
Exercise of stock options
Share-based compensation
Pre-funded warrants - Private
Placement
Public Offering
Balance as of December 31, 2020

Balance as of December 31, 2020
Transactions during 2021
Net loss
Exercise of stock options
Private Placement
Share-based compensation
Balance as of December 31, 2021

Milestone Pharmaceuticals Inc.
Consolidated Statements of Shareholders’ Equity
(in thousands of US dollars, except share data)

Common Shares

Pre-funded warrants

Number
of shares      Amount

24,505,748

$

226,245

Number

of warrants     Amount     

Additional
paid-in
capital
3,805

Cumulative
translation
adjustment     
(1,634)
$

Accumulated
deficit
(113,499)

$

Total
$ 114,917

— $

—
520
—

— $

—
—
—

—
24,917
251,682

6,655,131
4,761,903
11,417,034

251,682

11,417,034

—
219
—
—
251,901

—
—
910,746
—
12,327,780

$

$

$

$

$

$

—
226,352
—

—
5,095,897
29,827,997

29,827,997

—
69,562
—
—
29,897,559

—
—
—

24,771
23,236
48,007

48,007

—
—
4,934
—
52,941

—
(220)
4,945

—
—
8,530

8,530

$

$

—
(98)
—
7,279
$ 15,711

$

$

$

—
—
—

—
—
(1,634)

(1,634)

—
—
—
—
(1,634)

$

$

$

(49,967)
—
—

(49,967)
300
4,945

—
—
(163,466)

24,771
48,153
$ 143,119

(163,466)

$ 143,119

(42,853)
—
—
—
(206,319)

(42,853)
121
4,934
7,279
$ 112,600

The accompanying notes are an integral part of these consolidated financial statements.

108

    
    
    
    
Table of Contents

Milestone Pharmaceuticals Inc.
Consolidated Statements of Cash Flows
(in thousands of US dollars)

Cash flows used in operating activities
Net loss
Adjustments to reconcile net loss to net cash used in operating activities:

Depreciation of property and equipment
Share-based compensation expense
Changes in operating assets and liabilities:

Other receivables  
Research and development tax credits receivable
Prepaid expenses
Operating lease assets and liabilities
Accounts payable and accrued liabilities

Net cash used in operating activities

Cash provided by (used in) investing activities
Acquisition of short-term investments
Redemption of short-term investments

Net cash provided by (used in) investing activities

Cash provided by financing activities
Proceeds from exercise of options
Net proceeds from issuance of common shares in a public offering, net of issuance cost
Net proceeds from issuance of pre-funded warrants in a public offering, net of issuance cost
Proceeds from issuance of pre-funded warrants, net of issuance cost

Cash provided by financing activities

Net increase (decrease) in cash and cash equivalents

Cash and cash equivalents – Beginning of year

Cash and cash equivalents – End of year

The accompanying notes are an integral part of these consolidated financial statements.

109

Year ended December 31, 
2020
2021

$

(42,853)

$

(49,967)

93
7,279

96
369
1,129
26
637

97
4,945

35
(147)
(3,583)
(29)
(2,083)

(33,224)

(50,732)

(15,000)
85,000

70,000

121
—
—
4,934

5,055

41,831

72,310

$

114,141

$

(90,000)
20,000

(70,000)

300
24,917
23,236
24,771

73,224

(47,508)

119,818

72,310

    
Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

1 Organization and Nature of Operations

Milestone  Pharmaceuticals  Inc.  (Milestone  or  the  Company)  is  a  biopharmaceutical  company  incorporated  under  the
Business  Corporations  Act  of  Québec.  Milestone  is  focused  on  the  development  and  commercialization  of  innovative
cardiovascular  medicines.  Milestone’s  lead  product  candidate,  etripamil,  is  a  novel,  potent  short-acting  calcium  channel
blocker that the Company designed and is developing as a rapid-onset nasal spray to be  -administered by patients. The
Company  is  developing  etripamil  to  treat  paroxysmal  supraventricular  tachycardia,  atrial  fibrillation,  and  other
cardiovascular indications.

2 Summary of Significant Accounting Policies

a)  Basis of consolidation

The consolidated financial statements include the accounts of the Company and Milestone Pharmaceuticals USA, Inc. All
intercompany transactions and balances have been eliminated.

b)  Basis of Presentation and Use of Accounting Estimates

These consolidated financial statements of the Company have been presented in United States dollars (USD) and have been
prepared  in  accordance  with  accounting  principles  generally  accepted  in  the  United  States  of  America  (U.S.  GAAP),
including  the  applicable  rules  and  regulations  of  the  Securities  and  Exchange  Commission  (SEC)  regarding  financial
reporting.

The  preparation  of  consolidated  financial  statements  in  conformity  with  US  GAAP  requires  the  Company  to  make
estimates and judgments that affect certain reported amounts of assets and liabilities and disclosure of contingent assets and
liabilities at the date of the consolidated financial statements and the reported amounts of revenue and expenses during the
period. The Company bases its estimates and assumptions on current facts, historical experience and various other factors
that it believes are reasonable under the circumstances, to determine the carrying values of assets and liabilities that are not
readily apparent from other sources. Significant estimates and judgments include, but are not limited to,

● Estimates of the percentage of work completed of the total work over the life of the individual trial in
accordance with agreements established with CROs, CMOs and clinical trial sites which in turn impact
the research & development expenses.

● Estimate of the grant date fair value share options granted to employees, consultants and direct, and the

resulting share-based compensation expense, using the Black-Scholes option-pricing model.

110

Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

The  ongoing  COVID-19  pandemic  has  had  an  impact  on  the  Company’s  business,  operations  and  clinical  development
timelines. The pandemic has resulted in many state, local and foreign governments implementing, and making adjustments
to, various orders and restrictions in order to control the spread of the disease, which have impacted patient recruitment,
enrollment and follow-up visits at clinical sites The Company will continue to evaluate the COVID-19 pandemic impact on
the development timelines of its clinical programs. Estimates and assumptions about future events and their effects cannot
be  determined  with  certainty  and  therefore  require  the  exercise  of  judgment.  As  of  the  date  of  issuance  of  these
consolidated financial statements, the Company is not aware of any specific event or circumstance that would require the
Company  to  update  its  estimates,  assumptions  and  judgments.  These  estimates  may  change  as  new  events  occur  and
additional  information  is  obtained  and  are  recognized  in  the  consolidated  financial  statements  as  soon  as  they  become
known.  Actual  results  could  differ  from  those  estimates  and  any  such  differences  may  be  material  to  the  Company’s
consolidated financial statements.

c) Segment Information

The Company manages its operations as a single operating segment for the purposes of assessing performance and making
operating decisions while focusing on the development and commercialization of innovative cardiovascular medicines.

d) Revenue Recognition

Collaborative Arrangements

The Company considers the nature and contractual terms of arrangements and assesses whether an arrangement involves a
joint  operating  activity  pursuant  to  which  the  Company  is  an  active  participant  and  is  exposed  to  significant  risks  and
rewards  dependent  on  the  commercial  success  of  the  activity.  If  the  Company  is  an  active  participant  and  is  exposed  to
significant  risks  and  rewards  dependent  on  the  commercial  success  of  the  activity,  the  Company  accounts  for  such  an
arrangement  as  a  collaborative  arrangement  under  Accounting  Standards  Codification  (ASC)  808,  Collaborative
Arrangements (ASC 808), which  requires that certain transactions between the Company and collaborators be recorded in
its consolidated statements of comprehensive loss on either a gross basis or net basis, depending on the characteristics of
the collaborative relationship, and requires enhanced disclosure of collaborative relationships. The Company evaluates its
collaboration agreements for proper classification in its consolidated statements of comprehensive loss based on the nature
of the underlying activity. If payments to and from collaborative partners are not within the scope of other authoritative
accounting literature, the consolidated statements of loss classification for the payments is based on a reasonable, rational
analogy to authoritative accounting literature that is applied in a consistent manner. If the Company concludes that it has a
customer  relationship  with  one  of  its  collaborators,  the  Company  follows  the  guidance  in  Accounting  Standards
Codification (ASC) Topic 606, Revenue From Contracts With Customers (ASC 606).

Revenue from Contracts with Customers

In accordance with ASC 606, revenue is recognized when a customer obtains control of promised goods or services. The
amount of revenue recognized reflects the consideration to which the Company expects to be entitled in exchange for these
goods and services. To achieve this core principle, the Company applies the following five steps: 1) identify the customer
contract; 2) identify the contract’s performance obligations; 3) determine the transaction price; 4) allocate the transaction
price  to  the  performance  obligations;  and  5)  recognize  revenue  when  or  as  a  performance  obligation  is  satisfied.  The
Company evaluates all promised goods and services within a customer contract and determines which of such goods and
services  are  separate  performance  obligations.  This  evaluation  includes  an  assessment  of  whether  the  good  or  service  is
capable  of  being  distinct  and  whether  the  good  or  service  is  separable  from  other  promises  in  the  contract.  In  assessing
whether promised goods or services in licensing arrangements are distinct, the Company considers factors such as the stage
of  development  of  the  underlying  intellectual  property  and  the  capabilities  of  the  customer  to  develop  the  intellectual
property  on  their  own  or  whether  the  required  expertise  is  readily  available.  Licensing  arrangements  are  analyzed  to
determine whether the promised goods or services, which often include licenses, research and development services and
governance  committee  services,  are  distinct  or  whether  they  must  be  accounted  for  as  part  of  a  combined  performance
obligation. If the license is considered not to be distinct, the license would then be combined with other promised goods

111

Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

or  services  as  a  combined  performance  obligation.  If  the  Company  is  involved  in  a  governance  committee,  it  assesses
whether  its  involvement  constitutes  a  separate  performance  obligation.  When  governance  committee  services  are
determined to be separate performance obligations, the Company determines the fair value to be allocated to this promised
service. Certain contracts contain optional and additional items, which are considered marketing offers and are accounted
for as separate contracts with the customer if such option is elected by the customer, unless the option provides a material
right  which  would  not  be  provided  without  entering  into  the  contract.  An  option  that  is  considered  a  material  right  is
accounted  for  as  a  separate  performance  obligation.  The  transaction  price  is  determined  based  on  the  consideration  to
which  the  Company  will  be  entitled  in  exchange  for  transferring  goods  and  services  to  the  customer.  A  contract  may
contain variable consideration, including potential payments for both milestone and research and development services. For
certain potential milestone payments, the Company estimates the amount of variable consideration by using the most likely
amount method. In making this assessment, the Company evaluates factors such as the clinical, regulatory, commercial and
other risks that must be overcome to achieve the milestone. Each reporting period the Company re-evaluates the probability
of achievement of such variable consideration and any related constraints. Milestone will include variable consideration,
without constraint, in the transaction price to the extent it is probable that a significant reversal in the amount of cumulative
revenue recognized will not occur when the uncertainty associated with the variable consideration is subsequently resolved.

If the contract contains a single performance obligation, the entire transaction price is allocated to the single performance
obligation. Contracts that contain multiple performance obligations require an allocation of the transaction price among the
performance obligations on a relative standalone selling price basis unless a portion of the transaction price is variable and
meets the criteria to be allocated entirely to a performance obligation or to a distinct good or service that forms part of a
single performance obligation.

The Company allocates the transaction price based on the estimated standalone selling price of the underlying performance
obligations  or  in  the  case  of  certain  variable  consideration  to  one  or  more  performance  obligations.  The  Company  must
develop  assumptions  that  require  judgment  to  determine  the  stand-alone  selling  price  for  each  performance  obligation
identified  in  the  contract.  The  Company  utilizes  key  assumptions  to  determine  the  stand-alone  selling  price,  which  may
include other comparable transactions, pricing considered in negotiating the transaction and the estimated costs to complete
the respective performance obligation. Certain variable consideration is allocated specifically to one or more performance
obligations  in  a  contract  when  the  terms  of  the  variable  consideration  relate  to  the  satisfaction  of  the  performance
obligation and the resulting amounts allocated to each performance obligation are consistent with the amount the Company
would expect to receive for each performance obligation.

When  a  performance  obligation  is  satisfied,  revenue  is  recognized  for  the  amount  of  the  transaction  price,  excluding
estimates  of  variable  consideration  that  are  constrained,  that  is  allocated  to  that  performance  obligation  on  a  relative
standalone  selling  price  basis.  Significant  management  judgment  is  required  in  determining  the  level  of  effort  required
under an arrangement and the period over which the Company is expected to complete its performance obligations under
an arrangement.

For performance obligations consisting of licenses and other promises, the Company utilizes judgment to assess the nature
of the combined performance obligation to determine whether the combined performance obligation is satisfied over time
or at a point in time and, if over time, the appropriate method of measuring progress for purposes of recognizing revenue
from  non-  refundable,  up-front  fees.  The  Company  evaluates  the  measure  of  progress  each  reporting  period  and,  if
necessary, adjusts the measure of performance and related revenue recognition. If the license to the Company’s intellectual
property is determined to be distinct from the other performance obligations identified in the arrangement, the Company
will recognize revenue from non-refundable, up-front fees allocated to the license at the point in time when the license is
transferred to the customer and the customer is able to use and benefit from the license.

e) Cash and Cash Equivalents

Cash and cash equivalents consist of cash and highly liquid investments that are readily convertible into cash with original
maturities of three months or less at acquisition date.

112

Table of Contents

f) Short Term Investments

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

Short  term  investments  are  classified  as  held-to-maturity,  are  initially  recognized  at  fair  value  and  are  subsequently
accounted  for  at  amortized  cost.  They  are  comprised  of  guaranteed  investment  certificates  with  a  maturity  greater  than
90 days but less than one year and, as such, are classified as current assets.

g) Concentration of Credit Risk

Financial instruments which potentially subject the Company to concentration of credit risk consist primarily of cash and
cash  equivalents  and  investment  securities  classified  as  held  to  maturity.  The  Company  maintains  deposits  in  financial
institutions. Management believes that the Company is not exposed to significant credit risk due to the financial position of
the depository institutions in which those deposits are held. Additionally, the Company has adopted an investment policy
that includes guidelines relative to credit quality, diversification of maturities and liquidity.

h) Currency Risk

The Company is exposed to currency risk due to financial instruments denominated in foreign currencies. The Company is
exposed to the Canadian dollar currency risk and does not enter into arrangements to hedge its currency risk exposure.

i) Property and Equipment

Property and equipment is stated at historical cost less accumulated amortization. Expenditures for maintenance and repairs
are  recorded  to  expense  as  incurred.  The  Company  reviews  its  property  and  equipment  whenever  events  or  changes  in
circumstances indicate that the carrying value of certain assets might not be recoverable and recognizes an impairment loss
when it is probable that an asset’s realizable value is less than the carrying value. To date, no such impairment losses have
been recorded. Amortization is calculated using the straight-line method over the following estimated useful lives of the
assets:

Computer hardware and software
Office equipment
Furniture and fixtures
Leasehold improvements

j) Leases

    3 years
  5 years
  5 years
  over the lease-term

At the inception of an arrangement, the Company determines whether the arrangement is or contains a lease based on the
unique facts and circumstances present in the arrangement. Leases with a term greater than one year are recognized on the
balance  sheet  as  right-of-use  assets  and  short-term  and  long-term  lease  liabilities,  as  applicable.  The  Company  does  not
have financing leases.

Operating lease liabilities and their corresponding right-of-use assets are initially recorded based on the present value of
lease payments over the expected remaining lease term. Right-out-use assets are subsequently accounted for as long-lived
assets, including evaluating for indicators of impairment. Certain adjustments to the right-of-use asset may be required for
items such as incentives received. The interest rate implicit in lease contracts is typically not readily determinable. As a
result,  the  Company  utilizes  its  incremental  borrowing  rate  to  discount  lease  payments,  which  reflects  the  fixed  rate  at
which the Company could borrow on a collateralized basis the amount of the lease payments in the same currency, for a
similar  term,  in  a  similar  economic  environment.  Prospectively,  the  Company  will  adjust  the  right-of-use  assets  for
straight-line  rent  expense  or  any  incentives  received  and  remeasure  the  lease  liability  at  the  net  present  value  using  the
same incremental borrowing rate that was in effect as of the lease commencement or transition date.

113

Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

The  Company  has  elected  not  to  recognize  leases  with  an  original  term  of  one  year  or  less  on  the  balance  sheet.  The
Company typically only includes an initial lease term in its assessment of a lease arrangement. Options to renew a lease are
not included in the Company’s assessment unless there is reasonable certainty that the Company will renew.

k) Pre-funded Warrants

Pre-funded warrants allow the holder to pay little or no consideration to receive the shares upon exercise of the warrant.
The pre-funded warrants do not meet the definition of a derivative under ASC 815 because their fair value at issuance is
equal to the fair value of the shares underlying the warrant. As such, they have the characteristics of a prepaid forward sale
of equity. As a result, the pre-funded warrants are accounted for as equity instruments.

l) Share Issuance Costs

Share issuance costs applicable to the issuance of equity instruments are recorded as a reduction of the financing equity
proceeds.

m) Research and Development and Investment Tax Credits

Research  and  development  costs  are  charged  to  expense  as  costs  are  incurred  in  performing  research  and  development
activities. The Company’s research and development costs consist primarily of salaries and fees paid to contract research
organizations (CROs) and to contract manufacturing organizations (CMOs).

Clinical trial expenses include direct costs associated with CROs, direct CMO costs for the formulation and packaging of
clinical  trial  material,  as  well  as  investigator  and  patient  related  costs  at  sites  at  which  the  Company’s  trials  are  being
conducted.  Direct  costs  associated  with  the  Company’s  CROs  and  CMOs  are  generally  payable  on  a  time  and  materials
basis,  or  when  milestones  are  achieved.  The  invoicing  from  clinical  trial  sites  can  lag  several  months.  The  Company
records expenses for its clinical trial activities performed by third parties based upon estimates of the percentage of work
completed of the total work over the life of the individual study in accordance with agreements established with CROs and
clinical trial sites. The Company determines the estimates through discussions with internal clinical personnel, CROs and
CMOs as to the progress or stage of completion of trials or services and the agreed upon fee to be paid for such services
based on facts and circumstances known to the Company as of each consolidated balance sheet date. The actual costs and
timing  of  clinical  trials  are  highly  uncertain,  subject  of  risks  and  may  change  depending  upon  a  number  of  factors,
including the Company’s clinical development plan. If the actual timing of the performance of services of the level of effort
varies from the estimate, the Company will adjust the accrual accordingly.

The  Company  recognizes  the  benefit  of  Canadian  research  and  development  tax  credits  as  a  reduction  of  research  and
development costs for fully refundable investment tax credits and as a reduction of income taxes for investment tax credits
that can only be claimed against income taxes payable when there is reasonable assurance that the claim will be recovered.

n) Income Taxes

The  provision  for  income  taxes  is  computed  using  the  liability  method.  Under  this  method,  deferred  tax  assets  and
liabilities are determined based on differences between financial reporting and tax bases of assets and liabilities. Deferred
tax  assets  and  liabilities  are  measured  using  enacted  tax  rates  and  laws  that  will  be  in  effect  when  the  differences  are
expected to reverse. A valuation allowance is recorded to reduce the carrying amount of deferred income tax assets until
when it is more likely than not that these assets will be realized. Tax benefits related to tax positions not deemed to meet
the “more-likely-than-not” threshold are not permitted to be recognized in the consolidated financial statements.

o) Foreign Currency Translation and Transactions

The functional currency of the Company is the US dollar. Accordingly, transactions denominated in currencies other than
the functional currency are measured and recorded in the functional currency at the exchange rate in effect on the date of

114

Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

the transactions. At each consolidated balance sheet date, monetary assets and liabilities denominated in currencies other
than  the  functional  currency  are  remeasured  using  the  exchange  rate  in  effect  at  that  date.  Non-monetary  assets  and
liabilities  and  revenue  and  expense  items  denominated  in  foreign  currencies  are  translated  into  the  functional  currency
using the exchange rate prevailing at the dates of the respective transactions. Any gains or losses arising on remeasurement
are included in the consolidated statement of operations.

p) Share Based Compensation

The  Company  has  a  share  based  compensation  plan  which  is  described  in  detail  in  note  8  and  records  all  share-based
payments,  including  grants  of  employee  share  options,  at  their  fair  values.  The  fair  value  of  share  options  granted  to
employees  and  non-employees  is  estimated  at  the  date  of  grant  using  the  Black-Scholes  option  pricing  model.  The
Company recognizes share based compensation expense over the requisite service period of the individual grants, which
equals the vesting period, using the straight-line method. Forfeitures, if any, are recorded as they occur. Any consideration
paid by employees on exercising share options and the corresponding portion previously credited to contributed surplus are
credited  to  share  capital.  The  Black-Scholes  option  pricing  model  used  by  the  Company  to  calculate  option  values  was
developed to estimate fair value.

The Company approved an employee share purchase plan in April 2019, which became effective on May 8, 2019 and is
described  in  note  8.  The  plan  provides  a  means  by  which  eligible  employees  of  the  Company  and  certain  designated
companies may be given an opportunity to purchase common shares. The plan permits the Company to grant a series of
purchase rights to eligible employees under an employee stock purchase plan.

q) Recently Adopted Accounting Pronouncements

The Company has considered recent accounting pronouncements and concluded that they are either not applicable to the
business  or  that  the  effect  is  not  expected  to  be  material  to  the  consolidated  financial  statements  as  a  result  of  future
adoption.

r) Significant Risks and Uncertainties

The ongoing COVID-19 pandemic has had an impact on our business, operations and clinical development timelines. The
pandemic has resulted in many state, local and foreign governments implementing various orders and restrictions in order
to control the spread of the disease which has impacted patient recruitment, enrollment and follow-up visits at clinical sites
In  light  of  the  ongoing  pandemic,  the  Company  has  implemented  business  continuity  plans  designed  to  address  and
mitigate the impact of the COVID-19 pandemic on its business.  The Company anticipates that the COVID-19 pandemic
will continue to have an impact on the development timelines for its clinical programs.  The extent to which the COVID-19
pandemic  continues  to  impact  its  business,  its  clinical  development  and  regulatory  efforts,  its  corporate  development
objectives  and  the  value  of  and  market  for  its  common  shares  will  depend  on  future  developments  that  remain  highly
uncertain  and  cannot  be  predicted  with  confidence  at  this  time,  such  as  the  ultimate  duration  of  the  pandemic,  travel
restrictions,  business  closure  requirements  in  the  U.S.,  Europe  and  other  countries,  the  timing  and  unpredictability  of
achieving widespread vaccination rates, the effectiveness of any vaccines against new variants, and the timing of the return
of the global economy to pre-pandemic levels.  The global economic slowdown, the overall disruption of global healthcare
systems  and  the  other  risks  and  uncertainties  associated  with  the  pandemic  could  have  a  material  adverse  effect  on  the
Company’s business, financial condition, results of operations and growth prospects.

In addition, the Company is subject to other challenges and risks specific to its business and its ability to execute on its
strategy,  as  well  as  risks  and  uncertainties  common  to  companies  in  the  pharmaceutical  industry,  including,  without
limitation,  risks  and  uncertainties  associated  with:  obtaining  regulatory  approval  of  its  product  candidate;  delays  or
problems in the supply of its study drug or failure to comply with manufacturing regulations; identifying, acquiring or in-
licensing product candidates; pharmaceutical product development and the inherent uncertainty of clinical success; and the
challenges  of  protecting  and  enhancing  its  intellectual  property  rights;  and  complying  with  applicable  regulatory
requirements.  

115

Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

Further,  the  Company  may  be  impacted  by  general  economic,  political,  and  market  conditions,  including  deteriorating
market conditions due to investor concerns regarding inflation and Russian hostilities in Ukraine and overall fluctuations in
the financial markets in the U.S. and abroad.

s) Sources of Liquidity and Funding Requirements

The  Company  has  incurred  operating  losses  and  experienced  negative  operating  cash  flows  since  its  inception  and
anticipates to continue to incur losses for at least the next several years. As of December 31, 2021, the Company had cash
and cash equivalents of $114.1 million and an accumulated deficit of $206.3 million.

The Company believes that its cash and cash equivalents as of December 31, 2021 are sufficient for the Company to fund
planned operations for at least one year from the issuance date of these consolidated financial statements. The Company
has  historically  financed  its  operations  primarily  through    the  sale  of  equity  securities  and,  to  a  lesser  extent  from  cash
received  pursuant  to  its  license  agreement.  To  date,  the  Company  has  not  generated  any  revenue  from  product  sales.
Management expects operating losses and negative cash flows from operations to continue for the foreseeable future. The
Company currently plans to raise additional funding as required based on the status of its clinical trials and projected cash
flows.  There  can  be  no  assurance  that,  in  the  event  the  Company  requires  additional  financing,  such  financing  will  be
available  at  terms  acceptable  to  the  Company,  if  at  all.  Failure  to  generate  sufficient  cash  flows  from  operations,  raise
additional capital and reduce discretionary spending should additional capital not become available could have a material
adverse effect on the Company’s ability to achieve its business objectives.

3     Revenue

General

To  date,  the  Company  has  not  generated  revenue  from  product  sales.  During  the  year  ended  December  31,  2021,  the
Company recognized revenue of $15 million, in the form of a non-refundable upfront cash payment in connection with the
License Agreement.

On May 15, 2021, the Company entered into the License Agreement with Ji Xing, which is an entity affiliated with RTW
Investments, LP, (RTW) a beneficial owner of approximately 14% of the Company’s common shares. Under the License
Agreement,  the  Company  granted  Ji  Xing  exclusive  development  and  commercialization  rights  to  any  pharmaceutical
product that uses a device to deliver the Company’s proprietary calcium channel blocker known as etripamil by nasal spray
for  all  prophylactic  and  therapeutic  uses  in  humans  in  the  following  territories:  People’s  Republic  of  China,  including
mainland  China,  Hong  Kong  Special  Administrative  Region,  Macau  Special  Administrative  Region,  and  Taiwan  (the
Territory).  Ji  Xing  will  be  responsible  for  development  and  regulatory  activities  in  the  Territory,  and  the  Company  will
remain  responsible  for  certain  manufacturing  activities  in  the  Territory,  subject  to  the  supply  agreement  subsequently
entered  into  by  the  Company  and  Ji  Xing  as  contemplated  by  the  License  Agreement  (the  Supply  Agreement).    The
Company received a non-refundable upfront cash payment of $15 million (see note 3) and the right to future payments of
up to $107.5 million in total development and sales milestone payments. In addition, the Company is entitled to receive
tiered  royalty  payments  ranging  from  a  percentage  in  the  low  double  digits  to  the  high  double  digits  of  Net  Sales  (as
defined in the License Agreement) of all products sold in the Territory.

Strategic Partnerships

Ji Xing

Pursuant to the License Agreement, the Company granted Ji Xing exclusive development and commercialization rights to
any  pharmaceutical  product  that  uses  a  device  to  deliver  the  Company’s  proprietary  calcium  channel  blocker  known  as
etripamil by nasal spray for all prophylactic and therapeutic uses in humans in the Territory.

116

Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

Ji  Xing  will  be  responsible  for  development  and  regulatory  activities  in  the  Territory,  and  the  Company  will  remain
responsible for certain manufacturing activities in the Territory, subject to the Supply Agreement.

The  Company  received  a  non-refundable  upfront  cash  payment  consisting  of  $15  million,  and  the  right  to  receive  up  to
$107.5 million in future milestone payments and royalties on any sales of etripamil in the Territory.

Management  evaluated  all  of  the  promised  goods  or  services  within  the  contract  and  determined  that  such  goods  and
services  were  separate  performance  obligations.  The  Company  determined  that  the  license  granted  was  a  separate
performance obligation as Ji Xing can benefit from the license granted on its own after the transfer of the license, as it does
not require any significant development, regulatory or commercialization activities from Milestone. Ji Xing is responsible
for all development, regulatory and commercialization activities in the Territory, including the performance of clinical trials
necessary for regulatory approval, and is responsible for all such related costs. Supply of the product can be provided by
another  entity,  as  the  Company  currently  uses  a  CMO  for  the  production  of  etripamil  without  subsequent  significant
modification or customization by the Company, therefore the Company determined the obligation to supply product is a
separate and distinct obligation. The Company concluded that the obligation for participation on the various governance
committees  was  distinct  as  the  services  could  be  performed  by  an  outside  party,  however  it  was  determined  to  be
immaterial after estimating the stand alone cost compared to the License Agreement as a whole.  As a result, the Company
concluded there were two material and distinct performance obligations to account for under ASC 606 at the inception of
the License Agreement.

The Company determined that the transaction price consists of the $15 million non-refundable upfront cash payment and
the  constrained  variable  consideration  of  the  development  milestone  payments.  As  the  development  milestones  are
contingent  on  occurrences  out  of  the  direct  control  of  the  Company,  the  estimate  of  the  variable  consideration  is  $0.
 Variable constraint does not apply to sales- or usage-based royalties derived from the licensing of Intellectual property;
rather, consideration from such royalties is only recognized as revenue at the later of when the performance obligation is
satisfied or when the uncertainty is resolved (e.g., when subsequent sales or usage occurs), therefore the sales and royalty
milestones are not included in the transaction price. The Company will re-evaluate the transaction price at the end of each
reporting period and as uncertain events are resolved, or other changes in circumstances occur, adjust its estimate of the
transaction  price  if  necessary.  For  the  year  ended  December  31,  2021,  the  Company  has  recognized  the  non-refundable
upfront payment as collaboration revenue, for the reasons described in the preceding paragraph.  

Concurrent with the License Agreement, Ji Xing acquired $5 million of pre-funded warrants (see note 8). The Company
considered whether this equity investment should be evaluated  as part of the transaction price, and concluded that as the
fair value of the company’s common shares on a per share basis was equal to the fair value of the pre-funded warrants at
the date of the investment, there was no premium or discount on the shares that should be allocated and included in the
transaction  price.  The  Company  accounted  for  the  issuance  of  pre-funded  warrants  as  equity  and  included  in  basic  and
diluted loss per share in the accompanying financial statements. See note 8 for additional details.

For any future subsequent purchases of product pursuant to the Supply Agreement, each order will be accounted for as a
separate purchase and the order price will be allocated to the products based on the standalone selling price of the products.
Under this methodology, the order price will be allocated to the single performance obligation to supply the products. As
the  Company  has  not  previously  licensed  a  product  for  a  territory,  the  residual  approach  was  used    by    deducting  the
estimated  stand-alone  selling  price  of  the  other  obligations  from  the  total  transaction  price  to  determine  the  stand-alone
selling price of the remaining goods and services, which consisted of the transfer of intellectual property pursuant to the
license. Therefore, the remaining transaction price of $15 million was allocated to the technology transfer and recognized
at a point in time when the technology has been transferred.  The technology transfer was completed on June 22, 2021, and
the $15 million was recognized at that point in time as revenue in the related statement of comprehensive loss.  

117

Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

4 Short-term Investments

The Company had no short-term investments as at December 31, 2021.  For the year ended December 31, 2020, the short-
term  investments  were  comprised  of  term  deposits  issued  in  US  currency,  earning  interest  between  0.30%  and  0.86%,
maturing  between  January  29,  2021  and  August  16,  2021.  These  short-term  investments  were  in  scope  of  ASC  320,
Investments - Debt Securities. The short-term investments maturity is greater than 90 days but less than one year, and they
were classified as held to maturity, recorded as current assets and were accounted for at amortized cost.

5 Leases

On  June  3,  2019,  the  Company  entered  into  a  new  lease  arrangement  for  a  three-year  term  for  its  office  located  in
Charlotte, NC. The Company recognized the operating lease right-of-use asset and operating lease liabilities at the lease
commencement date on September 10, 2019. The interest rate implicit in lease contracts is not readily determinable and the
Company  does  not  have  a  public  credit  rating  and  carries  no  debt.    As  such,  several  factors  were  considered  in  the
determination of the Company’s incremental borrowing rate used in determining the present value of lease payments.  The
Company’s examined credit ratings for similar companies, assumed equivalency between the Canadian and U.S. markets
for  collateralized  debt  and  used  rates  over  the  36-month  period.  This  resulted  in  an  incremental  borrowing  rate  of  8%.
Lease  expenses  are  recognized  on  a  straight-line  basis  over  the  lease  term,  which  is  accomplished  by  increasing  the
amortization of the right-of-use asset as interest expense on the lease liability declines over the lease term. The company
was  not  reasonably  certain  of  renewing  the  lease  following  the  initial  term  and  recognized  the  right-of-use  asset  and
operating lease liabilities over the 36-month period ending September 30, 2022.

On July 1, 2020, the Company entered into an arrangement for the lease renewal for its headquarters located in Ville Saint-
Laurent,  Quebec.  The  5-year  lease  term  is  from  December  1,  2020  expiring  on  November  30,  2025.  The  Company
revalued the operating lease right-of-use asset and operating lease liabilities at the effective lease arrangement date of July
1, 2020. The Company’s examined credit ratings for similar companies, assumed equivalency between the Canadian and
U.S.  markets  for  collateralized  debt  and  used  rates  for  the  remaining  lease  term  of  65  months.    This  resulted  in  an
incremental borrowing rate of 5.26%. Lease expenses are recognized on a straight-line basis over the lease term, which is
accomplished by increasing the amortization of the right-of-use asset as interest expense on the lease liability declines over
the  lease  term.  The  Company  is  not  reasonably  certain  of  renewing  the  lease  following  the  current  renewal  option  and
recognized the right-of-use asset and operating lease liabilities to November 30, 2025.

The Company's two operating office leases right-of-use assets as at December 31 were as follows:

Opening balance
Right-of-use adjustment renewal on July 1, 2020
Amortization of right-of-use asset
Closing balance

2021

2020

980
—
(269)
711

$

$

524
735
(279)
980

     $

$

Operating  lease  expenses  of  $314  and  $318  are  included  in  general  and  administrative  operating  expenses  in  the
consolidated statement loss and comprehensive loss, and within operating activities in the statement of cash flows for the
year ended December 31, 2021 and 2020, respectively and are comprised of two operating lease right-of-use assets and one
operating lease of less than 12 months.

118

    
Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

The following table summarizes the future minimum lease payments of right-of-use assets operating lease as at December
31, 2021:

January 1, 2022 to December 31, 2022
January 1, 2023 to December 31, 2023
January 1, 2024 to December 31, 2024
January 1, 2025 to November 30, 2025

Less interest

6 Property and equipment

Property and equipment consist of the following at December 31:

Computer hardware and software
Office equipment
Leasehold improvements
Total
Less accumulated depreciation
Property and equipment, net

    $

$

243
176
176
160
755
(68)
687

2021

2020

$

$

$

22
406
26
454
(239)
215

$

$

$

22
406
26
454
(146)
308

During the year ended December 31, 2021 and December 31, 2020, the Company did not record any write off. For the year
ended December 31, 2021 and 2020, amortization expense was $93 and $97, respectively and was included in research and
development expense.

7 Accounts payable and accrued liabilities

Accounts payable and accrued liabilities comprised the following as of December 31:

Trade accounts payable
Accrued compensation and benefits payable
Accrued research and development liabilities
Other accrued liabilities

8 Shareholders’ Equity

Authorized Share Capital

2021

2020

  $

  $

4,384
1,458
272
437
6,551

$

$

4,641
957
152
164
5,914

The Company has authorized and issued common shares, voting and participating, without par value, of which unlimited
shares were authorized and 29,897,559 shares were issued and outstanding as of December 31, 2021.

As of December 31, 2021, there were 827,187 common shares available for issuance under the Employee Stock Purchase
Plans and no common shares have been issued under such plan.

119

    
    
 
 
 
 
 
 
    
    
 
 
 
Table of Contents

Shelf Registration

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

On  November  12,  2021,  the  company  entered  into  an  agreement  and  the  company  may  sell  any  combination  of  the
securities described in this prospectus in one or more offerings up to a total aggregate offering price of $250,000,000.

Pre-funded Warrants – Private Placement

On May 15, 2021, the Company entered into a securities purchase agreement to sell and issue in a private placement pre-
funded warrants to purchase up to 910,746 of the Company’s common shares, at a purchase price of $5.48 per pre-funded
warrant pursuant to the License Agreement for aggregate net proceeds of $5.0 million (the Private Placement).  The Private
Placement closed on May 21, 2021. Each pre-funded warrant is exercisable for one of the Company’s common shares at an
exercise  price  of  $0.01  per  share,  has  no  expiration  date,  and  is  immediately  exercisable,  subject  to  certain  beneficial
ownership limitations. The pre-funded warrants are classified and accounted for as equity.

On July 23, 2020, the Company entered into a securities purchase agreement to sell and issue in a private placement pre-
funded warrants of 6,655,131 of the Company’s common shares, at a purchase price of $3.7465 per pre-funded warrant for
aggregate net proceeds of $24.8 million (the Private Placement).  The Private Placement closed on July 24, 2020. Each pre-
funded  warrant  is  exercisable  for  one  of  the  Company’s  common  shares  at  an  exercise  price  of  $0.01  per  share,  has  no
expiration  date,  and  is  immediately  exercisable,  subject  to  certain  beneficial  ownership  limitations.  The  pre-funded
warrants are classified and accounted for as equity.  

Open Market Sale Agreement

On July 29, 2020, the Company entered into an Open Market Sale Agreement℠ with respect to an at-the-market offering
program (ATM Program) under which the Company may issue and sell its common shares having an aggregate offering
price of up to $50 million. The Company has not sold shares under the ATM program as of the date of this filing.

Pre-funded Warrants and Common Shares – Public Offering

On October 22, 2020, the Company issued (i) 5,095,897 common shares, without par value, at a price to the public of $5.25
per share, and (ii) pre-funded warrants to purchase 4,761,903 common shares at an exercise price equal to $0.01 per share,
at a price to the public of $5.24 per common share underlying the pre-funded warrants (the Offering).  The net proceeds to
the Company from the Offering were $48.2 million. The pre-funded warrants are classified and accounted for as equity.  

Additional Paid-in Capital

Opening balance
Share-based compensation expense
Exercise of stock options
Closing balance

2021

2020

$

$

8,530  
7,279  
(98) 
15,711  

$

$

3,805
4,945
(220)
8,530

120

 
    
Table of Contents

9   Share Based Compensation

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

Under the Company’s 2019 Equity Incentive Plan (the 2019 Plan) and the Company’s Stock Option Plan (the 2011 Plan),
unless  otherwise  decided  by  the  Board  of  Directors,  options  vest  and  are  exercisable  as  follows:  25%  vest  and  are
exercisable on the one year anniversary of the grant date and one thirty-sixth (1/36th) of the remaining options vest and are
exercisable each month thereafter, such that options are vested in full on four-year anniversary of the grant date.

On November 10th, 2021, the Company established an 2021 Inducement Plan under Nasdaq Marketplace Rules through
the granting of awards. This 2021 Inducement Plan is intended to help the Company provide an inducement material for
certain individuals to enter into employment with the Company, incentives for such persons to exert maximum efforts for
the success of the Company and provide a means by which employees may benefit from increases in value of the common
shares. There were no options granted under the 2021 Inducement Plan for the year ended December 31 2021.

On January 1, 2021, the number of the Company’s common shares reserved for issuance under the 2019 Plan increased by
1,193,119 common shares. In addition, 72,186 options have been forfeited under the 2011 Plan after adoption of the 2019
Plan  and  became  available  for  issuance  under  the  2019  Plan.  As  of  December  31,  2021,  there  were  4,596,021  shares
available for issuance under the 2019 Plan, of which 827,187 shares were available for future grants.

The total outstanding and exercisable options from the 2011 Plan and 2019 Plan as of December 31 were as follows:

2021

2020

Number
of shares

     2019 Plan    

2011 Plan    

Total

Weighted
average
exercise
price

Number
of shares

    2019 Plan     2011 Plan     Total

Weighted
average
exercise
price

Outstanding at beginning of year -
2011 Plan
Outstanding at beginning of year -
2019 Plan
Granted - 2019 Plan
Exercised - 2011 Plan
Exercised - 2019 Plan
Forfeited - 2011 Plan
Forfeited - 2019 Plan
Cancelled - 2011 Plan
Cancelled - 2019 Plan
Expired - 2011 Plan
Outstanding at end of period
Outstanding at end of period -
Weighted average exercise price
Exercisable at end of period
Exercisable at end of period -
Weighted average exercise price

—

2,080,087

2,080,087

$

2.15  

—

2,364,526

2,364,526

$

2.15

1,706,190
2,137,250
—
(19,000)
—
(63,303)
—
(11,303)
—
3,749,834

— 1,706,190
— 2,137,250
(50,562)
(19,000)
(8,812)
(63,303)
(23,029)
(11,303)
(1,713)
5,745,805

(50,562)
—
(8,812)
—
(23,029)
—
(1,713)
1,995,971

$

9.52
1,094,316

  $

11.48

$

$

2.07
1,795,332

2.01

2,889,648

13.55
6.22
0.98
3.74
9.42  
8.64
9.42
9.22  
0.70
6.93  

220,140
1,534,460
—
—
—
(45,413)

—
220,140
— 1,534,460
—
—
(226,352)
(226,352)
(58,087)
(58,087)
(45,413)
—

(2,997)

—

(2,997)

1,706,190

2,080,087

3,786,277

$

13.55
268,164

5.60

  $

8.23

$

$

2.15
1,536,895

2.02

1,805,059

20.78
12.68
—
1.23
5.94
18.53

21.48

7.29

2.94

$

$

$

$

The weighted average remaining contractual life was 7.81 and 7.86 years for outstanding options as of December 31, 2021
and 2020, respectively. The weighted average remaining contractual life was 6.80 and 6.91 years for vested options, as of
December 31, 2021 and 2020, respectively.

121

   
   
 
 
 
Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

There was $15,324 and $13,012 total unrecognized compensation cost related to non-vested share options as of December
31,  2021  and  2020,  respectively.  The  share  options  are  expected  to  be  recognized  over  a  remaining  weighted  average
vesting period of 2.42 years and 2.67 years as of December 31, 2021 and 2020, respectively.

The non-vested options as of December 31 were as follows:

2021

Number
of options

Weighted
average

Number
of options

2020

     2019 Plan 2011 Plan     Total

    fair value         2019 Plan 2011 Plan      Total

Weighted
average
    fair value

Non-vested share options at beginning of
year - 2011 Plan
Non-vested share options at beginning of
year - 2019 Plan
Granted - 2019 Plan
Vested, outstanding 2011 Plan
Vested, outstanding 2019 Plan
Forfeited - 2011 Plan
Forfeited - 2019 Plan
Non-vested share options at end of period  
Non-vested share options at end of period
- Weighted average fair value

$

— 543,192

543,192   $

1.81  

— 1,152,300

1,152,300   $

1.88

1,438,026
2,137,250

— 1,438,026   $
— 2,137,250

— (333,741)
—
(8,812)
—
200,639

(856,455)
—
(63,303)
2,655,518

(333,741) 
(856,455)
(8,812) 
(63,303)
2,856,157   $

10.28
4.70
1.65  
8.69
6.66  
6.28
6.08  

218,975
1,534,460

— (551,026)
—
(58,082)
—
543,192

(269,996)
—
(45,413)
1,438,026

—
— 1,534,460

218,975   $ 14.44
8.98
1.70
5.80
4.32
13.03
7.96

(551,026) 
(269,996)
(58,082) 
(45,413)
1,981,218   $

6.40 $

1.86

$

10.28 $

1.81

Options  granted  are  valued  using  the  Black-Scholes  option  pricing  model.  Amortization  of  the  fair  value  of  the  options
over vesting years has been expensed and credited to additional paid-in capital in shareholders’ equity.

The following table summarizes information with respect to share options outstanding as of December 31, 2021:

Exercise price
$0.84-$1.00
$1.01-$2.00
$2.01-$4.00
$4.01-$10.00
$15.01-$20.00
$20.01-$22.45
Total

Options outstanding
     Weighted     
average
remaining
contractual
life (years)
2.36
5.61
7.64
9.20
7.82
8.00
7.81

$
$
$
$
$
$
$

Number
of options
73,629
1,202,193
1,321,374
2,221,317
80,380
846,912
5,745,805  

Weighted
average
exercise
price

0.89  
1.48  
3.20  
6.32  
17.20  
21.65  
6.93  

Options exercisable
     Weighted     
average
remaining
contractual
life (years)
2.36
5.57
7.61
8.69
7.81
7.99
6.80

$
$
$
$
$
$
$

Number
of options

73,629  
1,120,697  
1,066,458  
157,524  
50,592  
420,748  
2,889,648  

Weighted
average
exercise
price

0.89
1.47
3.18
6.86
17.24
21.67
5.60

The intrinsic value of all outstanding options as of December 31, 2021 was $11.7 million, based on the fair value of our
common shares of $6.55 per share at December 31, 2021, of which $9.8 million related to vested options and $1.9 million
related to unvested options.

122

 
 
 
 
 
 
 
    
    
 
 
 
 
 
 
Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

The  fair  value  of  share-based  payment  transaction  is  measured  using  Black-Scholes  valuation  model.  This  model  also
requires  assumptions,  including  expected  option  life,  volatility,  risk-free  interest  rate  and  dividend  yield,  which  greatly
affect the calculated values:

Exercise price
Share price
Volatility
Risk-free interest rate
Expected life
Dividend

2021

2020

$
$

6.22  
6.22  

$
$

93 %  
1.05 %  

12.68
12.68

85 %
1.03 %

6.01 years  

5.88 years

0 %  

0 %

Expected volatility is determined using comparable companies for which the information is publicly available. The risk-
free interest rate is determined based on the U.S. sovereign rates benchmark in effect at the time of grant with a remaining
term  equal  to  the  expected  life  of  the  option.  Expected  option  life  is  determined  based  on  the  simplified  method  as  the
Company does not have sufficient historical exercise data to provide a reasonable basis upon which to estimate expected
term. The simplified method is an average of the contractual term of the options and its ordinary vesting period. Dividend
yield is based on the share option’s exercise price and expected annual dividend rate at the time of grant.

The Company recognized share-based compensation expense as follows for the year ended December 31:

Administration
Research and development
Commercial activities

10 Net loss per share

2021

2020

$

$

3,011   $
3,046  
1,222  
7,279   $

2,007
2,055
883
4,945

Basic and diluted net loss per common share is determined by dividing net loss applicable to common shareholders by the
weighted  average  number  of  common  shares  and  pre-funded  warrants  outstanding  during  the  period.  Share-based
compensation shares have been excluded from the calculation because their effects would be anti-dilutive. Therefore, the
weighted average number of shares used to calculate both basic and diluted loss per share are the same.

The following potentially dilutive securities have been excluded from the computation of diluted weighted average shares
outstanding as of December 31, 2021 and 2020, as they would be anti-dilutive:

Share options

2021
5,745,805  

2020
3,786,277

Amounts in the table above reflect the common share equivalents of the noted instruments.

123

    
 
 
 
 
 
    
    
    
    
 
Table of Contents

11 Income taxes

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

A  reconciliation  between  tax  expense  and  the  product  of  accounting  income  multiplied  by  the  basic  income  tax  rate  for
the years ended December 31, 2021 and 2020 is as follows:

Loss before income taxes
Basic income tax rate
Computed income tax recovery
Effect on income tax rate resulting from

Accounting charges not deductible for tax purposes
Non‑deductible share‑based compensation
Share issue costs
Tax benefits of current period losses and other tax assets
Valuation allowance for prior year adjustment
Other

2021
(42,853)$ $
26.19 %  

2020
(49,984)

26.33 %

(11,221) 

(13,161)

18  
1,929  
15
9,536  
(276)
(1)

7
1,310
(984)
12,715
108
(12)

Income tax expense recovery reported in the consolidated statements of loss and comprehensive
loss

$

— $

(17)

The  Company  has  incurred  Canadian  federal  and  provincial  net  operating  losses  (NOLs)  from  inception.  As  of
December  31,  2021,  the  Company  has  NOL  carry-forwards  of  approximately  $149,012  and  $146,652,  respectively,  for
Canadian federal and Québec purposes, available to reduce future taxable income, which expire beginning in 2027 through
2041. The Company also has scientific research and experimental development expenditures of approximately $18,051 and
$22,185,  respectively,  for  Canadian  federal  and  Québec  income  tax  purposes,  which  have  not  been  deducted.  These
expenditures  are  available  to  reduce  future  taxable  income  and  have  an  unlimited  carry-forward  period.  Research  and
development tax credits and expenditures are subject to verification by the tax authorities, and, accordingly, these amounts
may vary.

The Company has incurred NOLs for U.S. tax purposes. As of December 31, 2021, the Company has carry-forwards of
approximately $26,347 related to U.S. NOLs that may be carried forward indefinitely and are available to reduce future
taxable income.

Deferred  income  taxes  reflect  the  net  tax  effects  of  temporary  differences  between  the  carrying  amounts  of  assets  and
liabilities for financial reporting purposes and the amounts used for income tax purposes. The net deferred tax assets have
not been recognized in these financial statements because the criteria for recognition of these assets were not met.

124

    
    
 
 
 
 
 
 
 
 
 
Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

The Company’s deferred tax assets consist of the following for the years ended December 31, 2021 and 2020:

Net operating loss carry‑forwards
Tax basis of property and equipment in excess of carrying values
Federal SR&ED investment tax credits
Taxation of federal SR&ED investment tax credits
Research and development expenditures
Financing costs
Change in tax rates
Others
Total gross deferred tax assets
Valuation allowance
Net deferred tax assets

2021
45,756
103
709
(108)
5,259
1,726
51
26
53,522
(53,522)
—

2020

36,951
100
496
(132)
3,929
2,583
25
34
43,986
(43,986)
—

The Company files income tax returns in Canada and in the United States. The Company is subject to Canada Revenue
Agency and Revenu Québec examination for fiscal years 2016 to 2021 due to unexpired statute of limitation periods and is
subject to US Federal and state income tax examination for fiscal years 2018 to 2021.

12 Government assistance

The Company incurred research and development expenditures that are eligible for investment tax credits. The investment
tax credits recorded are based on management’s estimates of amounts expected to be recovered and are subject to audit by
the  taxation  authorities.  These  amounts  (expressed  in  thousands  of  US  dollars)  have  been  recorded  as  a  reduction  of
research  and  development  expenditures  the  year  ended  December  31,  2021  and  2020  for  an  amount  of  $458  and  $373,
respectively.

13 Commitments

In  the  normal  course  of  business,  the  Company  enters  into  contracts  with  clinical  research  organizations,  drug
manufacturers and other vendors for preclinical and clinical research studies, research and development supplies and other
services and products for operating purposes. These contracts generally provide for termination on notice, and therefore are
cancellable contracts. Therefore, as at December 31, 2021 there are no contractual commitments, except for office leases
(see note 5).

14 Currency risk

The  Company  is  exposed  to  the  financial  risk  related  to  the  fluctuation  of  foreign  exchange  rates  and  the  degree  of
volatility  of  those  rates.  The  foreign  currency  risk  is  limited  to  the  portion  of  the  Company’s  business  transactions
denominated in currency other than US dollars. The following table provides an indication of the Company’s exposure to
the Canadian dollar, which is expressed in US dollars as of December 31:

Cash
Other receivables  
Operating lease assets
Accounts payable and accrued liabilities
Operating lease liabilities

Net financial position exposure

2021

2020

$

$

2,049
106
605
998
622
1,140

$

$

426
—
—
675
—
249

The Company does not enter into arrangements to hedge its currency risk exposure.

125

    
 
 
 
 
 
 
 
 
 
    
    
Table of Contents

Milestone Pharmaceuticals Inc.
Notes to Consolidated Financial Statements
(in thousands of US dollars, except share and per share data)

15 Fair value of financial instruments

Pursuant  to  the  accounting  guidance  for  fair  value  measurement  and  its  subsequent  updates,  fair  value  is  defined  as  the
price  that  would  be  received  to  sell  an  asset  or  paid  to  transfer  a  liability  (i.e.  the  exit  price)  in  an  orderly  transaction
between market participants at the measurement date. The accounting guidance establishes a hierarchy for inputs used in
measuring fair value that minimizes the use of unobservable inputs by requiring the use of observable market data when
available. Observable inputs are inputs that market participants would use in pricing the asset or liability based on active
market data. Unobservable inputs are inputs that reflect the assumptions market participants would use in pricing the asset
or liability based on the best information available in the circumstances.

The fair value hierarchy is broken down into the three input levels summarized below:

Level 1— Valuations are based on quoted prices in active markets for identical assets or liabilities and readily accessible by

the Company at the reporting date.

Level 2— Valuations based on inputs other than the quoted prices in active markets that are observable either directly or

indirectly in active markets.

Level 3— Valuations based on unobservable inputs in which there is little or no market data, which requires the Company

to develop its own assumptions.

The Company’s fair value hierarchy for all its financial assets (by major security type measured at fair value on a recurring
basis)  for  the  year  ended  December  31,  2021  is  nil,  as  there  was  no  financial  instruments  measured  at  fair  value  on  a
recurring  basis  as  of  that  date.  For  the  year  ended  December  31,  2020,  the  Company  held  a  Guaranteed  investment
certificate at Level 1 with a fair value of $70 million.

126

Table of Contents

ITEM  9.          CHANGES  IN  AND  DISAGREEMENTS  WITH  ACCOUNTANTS  ON  ACCOUNTING  AND

FINANCIAL DISCLOSURE.

None.

ITEM 9A.    CONTROLS AND PROCEDURES.

Evaluation of Disclosure Controls and Procedures

We  maintain  disclosure  controls  and  procedures,  as  defined  in  Rules  13a-15(e)  and  15d-15(e)  under  the  Securities
Exchange  Act  of  1934  (the  Exchange  Act)  that  are  designed  to  ensure  that  information  required  to  be  disclosed  in  our
periodic  and  current  reports  that  we  file  with  the  SEC  is  recorded,  processed,  summarized  and  reported  within  the  time
periods  specified  in  the  SEC’s  rules  and  forms,  and  that  such  information  is  accumulated  and  communicated  to  our
management,  including  our  principal  executive  officer  and  principal  financial  officer,  as  appropriate,  to  allow  timely
decisions regarding required disclosure. In designing and evaluating the disclosure controls and procedures, management
recognizes that any controls and procedures, no matter how well designed and operated, can provide only reasonable and
not absolute assurance of achieving the desired control objectives. In reaching a reasonable level of assurance, management
necessarily is required to apply its judgment in evaluating the cost-benefit relationship of possible controls and procedures.
In  addition,  the  design  of  any  system  of  controls  also  is  based  in  part  upon  certain  assumptions  about  the  likelihood  of
future events, and there can be no assurance that any design will succeed in achieving its stated goals under all potential
future conditions; over time, control may become inadequate because of changes in conditions, or the degree of compliance
with  policies  or  procedures  may  deteriorate.  Because  of  the  inherent  limitations  in  a  cost-effective  control  system,
misstatements due to error or fraud may occur and not be detected.

We carried out an evaluation, under the supervision and with the participation of our management, including our principal
executive officer and principal financial officer, of the effectiveness of the design and operation of our disclosure controls
and  procedures,  as  defined  in  Rules  13a-15(e)  and  15d-15(e)  under  the  Exchange  Act.  Based  on  this  evaluation,  our
principal  executive  officer  and  principal  financial  officer  concluded  that  our  disclosure  controls  and  procedures  were
effective at the reasonable assurance level as of December 31, 2021.

Management’s Report on Internal Control Over Financial Reporting

Our management is responsible for establishing and maintaining adequate internal control over financial reporting as such
term is defined in Rules 13a-15(f) and 15-d-15(f) of the Exchange Act. Internal control over financial reporting is a process
designed under the supervision and with the participation of our management, including our principal executive officer and
principal  financial  officer,  to  provide  reasonable  assurance  regarding  the  reliability  of  financial  reporting  and  the
preparation of financial statements for external purposes in accordance with accounting principles generally accepted in the
United States of America.

As  of  December  31,  2021,  management  assessed  and  management  concluded  the  effectiveness  of  internal  control  over
financial reporting using the criteria set forth by the Committee of Sponsoring Organizations of the Treadway Commission
in  Internal  Control  –  2013  Integrated  Framework  (2013  Framework).  Based  on  this  assessment,  management  concluded
that our internal control over financial reporting was effective as of December 31, 2021.

This Annual Report on Form 10-K does not include an attestation report of our independent registered public accounting
firm due to a transition period established by the JOBS Act for smaller reporting companies.

Inherent Limitations of Internal Controls

Our  management,  including  our  principal  executive  officer  and  principal  financial  officer,  does  not  expect  that  our
disclosure controls and procedures or our internal controls will prevent all errors and all fraud. A control system, no matter
how well conceived and operated, can provide only reasonable, not absolute, assurance that the objectives of the control
system are met. Because of the inherent limitations in all control systems, no evaluation of controls can provide absolute
assurance that all control issues and instances of fraud, if any, within the company have been detected. These inherent

127

Table of Contents

limitations include the realities that judgments in decision-making can be faulty, and that breakdowns can occur because of
a simple error or mistake. Additionally, controls can be circumvented by the individual acts of some persons, by collusion
of two or more people, or by management override of the control. The design of any system of controls also is based in part
upon certain assumptions about the likelihood of future events, and there can be no assurance that any design will succeed
in achieving its stated goals under all potential future conditions. Over time, controls may become inadequate because of
changes in conditions, or the degree of compliance with the policies or procedures may deteriorate. Because of the inherent
limitations in a cost-effective control system, misstatements due to error or fraud may occur and not be detected.

Changes in Internal Control Over Financial Reporting

During the year ended December 31, 2021, there have been no changes in our internal control over financial reporting, as
such term is defined in Rules 13a-15(f) and 15d-15(f) promulgated under the Exchange Act, that have materially affected,
or are reasonably likely to materially affect, our internal control over financial reporting.

ITEM 9B.     OTHER INFORMATION.

None.

ITEM 9C.     DISCLOSURE REGARDING FOREIGN JURISDICTIONS THAT PREVENT INSPECTIONS.

Not applicable.

PART III

ITEM 10. DIRECTORS, EXECUTIVE OFFICERS AND CORPORATE GOVERNANCE

The information required by this item is incorporated by reference to our Proxy Statement for our 2022 Annual General
Meeting  of  Shareholders  to  be  filed  with  the  SEC  within  120  days  after  the  end  of  the  fiscal  year  ended  December  31,
2021.

As part of our system of corporate governance, our board of directors has adopted a code of business conduct and ethics.
The  code  applies  to  all  of  our  employees,  officers  (including  our  principal  executive  officer,  principal  financial  officer,
principal accounting officer or controller, or persons performing similar functions), agents and representatives, including
our independent directors and consultants, who are not employees of ours, with regard to their Company-related activities.
Our code of business conduct and ethics is available on our website at www.milestonepharma.com. We intend to post on
this section of our website any amendment to our code of business conduct and ethics, as well as any waivers of our code
of business conduct and ethics, that are required to be disclosed by the rules of the SEC or the Nasdaq Stock Market.

ITEM 11.    EXECUTIVE COMPENSATION.

The information required by this item is incorporated by reference to our Proxy Statement for our 2022 Annual Meeting of
Shareholders to be filed with the SEC within 120 days after the end of the fiscal year ended December 31, 2021.

ITEM  12.  SECURITY  OWNERSHIP  OF  CERTAIN  BENEFICIAL  OWNERS  AND  MANAGEMENT  AND

RELATED STOCKHOLDER MATTERS.

The information required by this item is incorporated by reference to our Proxy Statement for our 2022 Annual Meeting of
Shareholders to be filed with the SEC within 120 days after the end of the fiscal year ended December 31, 2021.

128

Table of Contents

ITEM  13. 

  CERTAIN  RELATIONSHIPS  AND  RELATED  TRANSACTIONS,  AND  DIRECTOR

INDEPENDENCE.

The information required by this item is incorporated by reference to our Proxy Statement for our 2022 Annual General
Meeting  of  Shareholders  to  be  filed  with  the  SEC  within  120  days  after  the  end  of  the  fiscal  year  ended  December  31,
2021.

ITEM 14.    PRINCIPAL ACCOUNTANT FEES AND SERVICES.

The information required by this item is incorporated by reference to our Proxy Statement for our 2022 Annual General
Meeting  of  Shareholders  to  be  filed  with  the  SEC  within  120  days  after  the  end  of  the  fiscal  year  ended  December  31,
2021.

129

 
Table of Contents

PART IV

ITEM 15.    EXHIBITS, FINANCIAL STATEMENT SCHEDULES.

(a)(1) Financial Statements

See  Index  to  Consolidated  Financial  Statements  on  page  103  of  this  Annual  Report  on  Form  10-K,  which  is

incorporated into this item by reference.
(a)(2) Financial Statement Schedules

All financial statement schedules are omitted because they are not applicable or the required information is shown

in the financial statements or notes thereto.
(b) Exhibits

The following list of exhibits includes exhibits submitted with this Annual Report on Form 10-K as filed with the

SEC and others incorporated by reference to other filings.

EXHIBIT
NUMBER DESCRIPTION
3.1

3.2

4.1

4.2

4.3

4.4

4.5

10.1+

10.2+

10.3+

10.4+

10.5+

10.6+

Amended  Articles  of  Incorporation  (incorporated  herein  by  reference  to  Exhibit  3.1  to  the  Registrant’s
Current Report on Form 8-K (File No. 001-38899), filed with the SEC on May 15, 2019).
Amended and Restated Bylaws (incorporated herein by reference to Exhibit 3.2 to the Registrant’s Current
Report on Form 8-K (File No. 001-38899), filed with the SEC on May 15, 2019).
Form of Common Share Certificate (incorporated herein by reference to Exhibit 4.1 to Amendment No. 1 to
the Registrant’s Registration Statement on Form S-1 (File No. 333-230846), filed with the SEC on April 29,
2019).
Form of Pre-Funded Warrant to Purchase Common Shares (incorporated herein by reference to Exhibit 4.1
to the Registrant’s Current Report on Form 8-K (File No. 001-38899), filed with the SEC on July 23, 2020.
Form  of  Pre-Funded  Warrant  (incorporated  herein  by  reference  to  Exhibit  4.1  to  the  Registrant’s  Current
Report on Form 8-K (File No. 001-38899), filed with the SEC on October 26, 2020.
Third Amended and Restated Registration Rights Agreement, by and among the Company and certain of its
shareholders,  dated  October  15,  2018  (incorporated  herein  by  reference  to  Exhibit  4.2  to  the  Registrant’s
Registration Statement on Form S-1 (File No. 333-230846), filed with the SEC on April 12, 2019).
Description  of  Securities  Registered  pursuant  to  Section  12  of  the  Securities  Exchange  Act  of  1934,  as
amended
Third  Amended  and  Restated  Stock  Option  Plan  (incorporated  herein  by  reference  to  Exhibit  10.1  to  the
Registrant’s  Registration  Statement  on  Form  S-1  (File  No.  333-230846),  filed  with  the  SEC  on  April  12,
2019).
Form of Award and Grant Notices under the Third Amended and Restated Stock Option Plan (incorporated
herein by reference to Exhibit 10.2 to the Registrant’s Registration Statement on Form S-1 (File No. 333-
230846), filed with the SEC on April 12, 2019).
2019 Equity Incentive Plan (incorporated herein by reference to Exhibit 4.8 to the Registrant’s Registration
Statement on Form S-8 (File No. 333-231347), filed with the SEC on May 9, 2019).
Form of U.S. Stock Option Grant Notice and Stock Option Agreement under the 2019 Equity Incentive Plan
(incorporated  herein  by  reference  to  Exhibit  10.4  to  Amendment  No.  1  to  the  Registrant’s  Registration
Statement on Form S-1 (File No. 333-230846), filed with the SEC on April 29, 2019).
Form  of  U.S.  Restricted  Stock  Unit  Grant  Notice  and  Restricted  Stock  Unit  Award  Agreement  under  the
2019 Equity Incentive Plan (incorporated herein by reference to Exhibit 10.5 to Amendment No. 1 to the
Registrant’s  Registration  Statement  on  Form  S-1  (File  No.  333-230846),  filed  with  the  SEC  on  April  29,
2019).
Form of Canadian Stock Option Grant Notice and Option Agreement under the 2019 Equity Incentive Plan
(incorporated  herein  by  reference  to  Exhibit  10.6  to  Amendment  No.  1  to  the  Registrant’s  Registration
Statement on Form S-1 (File No. 333-230846), filed with the SEC on April 29, 2019).

130

Table of Contents

10.7+

10.8+

10.9+

10.10+

10.11+

10.12+

10.13+

10.14+

10.15+

10.16+

10.17*

23.1
24.1
31.1

31.2

32.1˄

101.INS
101.SCH
101.CAL
101.DEF
101.LAB

Form of Canadian Restricted Stock Unit Grant Notice and Restricted Stock Unit Award Agreement under
the 2019 Equity Incentive Plan (incorporated herein by reference to Exhibit 10.7 to Amendment No. 1 to the
Registrant’s  Registration  Statement  on  Form  S-1  (File  No.  333-230846),  filed  with  the  SEC  on  April  29,
2019).
2019 Employee Share Purchase Plan (incorporated herein by reference to Exhibit 4.13 to the Registrant’s
Registration Statement on Form S-8 (File No. 333-231347), filed with the SEC on May 9, 2019).
Amended  and  Restated  Employment  Agreement  between  Joseph  Oliveto  and  Milestone  Pharmaceuticals
USA,  Inc.  (incorporated  herein  by  reference  to  Exhibit  10.9  to  Amendment  No.  1  to  the  Registrant’s
Registration  Statement  on  Form  S-1  (File  No.  333-230846),  filed  with  the  SEC  on  April  29,  2019),  as
amended by First Amendment to Amended and Restated Employment Agreement between Joseph Oliveto
and Milestone Pharmaceuticals USA, Inc. (incorporated herein by reference to Exhibit 10.1 to  Registrant’s
Current Report on Form 8-K (File No. 001-38899), filed with the SEC on June 8, 2020).
Employment  Agreement  between  Amit  Hasija  and  Milestone  Pharmaceuticals  USA,  Inc.  (incorporated
herein by reference to Exhibit 10.1 to the Registrant’s Current Report on Form 8-K (File No. 001-38899),
filed  with  the  SEC  on  September  9,  2019),  as  amended  by  First  Amendment  to  Employment  Agreement
between  Amit  Hasija  and  Milestone  Pharmaceuticals  USA,  Inc.  (incorporated  herein  by  reference  to
Exhibit 10.2 to  Registrant’s Current Report on Form 8-K (File No. 001-38899), filed with the SEC on June
8, 2020).
Amended and Restated Employment Agreement between Francis Plat and Milestone Pharmaceuticals Inc.
(incorporated  herein  by  reference  to  Exhibit  10.11  to  Amendment  No.  1  to  the  Registrant’s  Registration
Statement  on  Form  S-1  (File  No.  333-230846),  filed  with  the  SEC  on  April  29,  2019),  as  amended  by
Amending  Agreement  between  Francis  Plat  and  Milestone  Pharmaceuticals  Inc.  (incorporated  herein  by
reference to Exhibit 10.3 to the Registrant’s Current Report on Form 8-K (File No. 001-38899), filed with
the SEC on June 8, 2020).
Employment  Agreement,  dated  February  15,  2022  between  David  Bharucha,  M.D.,  Ph.D.  and  Milestone
Pharmaceuticals  USA,  Inc.  (incorporated  herein  by  reference  to  Exhibit  10.1  to  the  Registrant’s  Current
Report on Form 8-K (File No. 001-38899), filed with the SEC on February 16, 2022).
Securities Purchase Agreement dated July 22, 2020 (incorporated herein by reference to Exhibit 10.1 to the
Registrant’s Current Report on Form 8-K (File No. 001-38899), filed with the SEC on July 23, 2020).
Open Market Sale AgreementSM, dated July 29, 2020, by and between Milestone Pharmaceuticals Inc. and
Jefferies LLC 2020 (incorporated herein by reference to Exhibit 10.1 to the Registrant’s Current Report on
Form 8-K (File No. 001-38899), filed with the SEC on July 29, 2020).
Form  of  Indemnity  Agreement  (incorporated  herein  by  reference  to  Exhibit  10.14  to  the  Registrant’s
Registration Statement on Form S-1 (File No. 333-230846), filed with the SEC on April 12, 2019).

Amended  and  Restated  Employment  Agreement  between  Lorenz  Muller  and  Milestone  Pharmaceuticals
USA,  Inc.  (incorporated  herein  by  reference  to  Exhibit  10.12  to  Amendment  No.  1  to  the  Registrant’s
Registration Statement on Form S-1 (File No. 333-230846), filed with the SEC on April 29, 2019).
License and Collaboration Agreement by and among the Company and Ji Xing Pharmaceuticals, Limited,
dated May 15, 2021 (incorporated herein by reference to Exhibit 10.1 to the Registrant’s Quarterly Report
on Form 10-Q (File No. 001-38899), filed with the SEC on August 11, 2021.
Consent of PricewaterhouseCoopers LLP, an Independent Registered Public Accounting Firm.
Power of Attorney (included on the signature page to this registration statement).
Certification of Principal Executive Officer pursuant to Rules 13a-14(a) and 15d-14(a) promulgated under
the Securities Exchange Act of 1934, as adopted pursuant to Section 302 of the Sarbanes-Oxley Act of 2002
Certification  of  Principal  Financial  Officer  pursuant  to  Rules  13a-14(a)  and  15d-14(a)  promulgated  under
the Securities Exchange Act of 1934, as adopted pursuant to section 302 of the Sarbanes-Oxley Act of 2002
Certification of Principal Executive Officer and Principal Financial Officer pursuant to Rules 13a-14(b) and
15d-14(b) promulgated under the Securities Exchange Act of 1934 and 18 U.S.C. Section 1350, as adopted
pursuant to section 906 of The Sarbanes-Oxley Act of 2002
Inline XBRL Instance Document
Inline XBRL Taxonomy Extension Schema Document
Inline XBRL Taxonomy Extension Calculation Linkbase Document
Inline XBRL Taxonomy Extension Definition Linkbase Document
Inline XBRL Taxonomy Extension Label Linkbase Document

131

Table of Contents

101.PRE
104

Inline XBRL Taxonomy Extension Presentation Linkbase Document
Cover  Page  Interactive  Data  File  (formatted  as  inline  XBRL  with  applicable  taxonomy  extension
information contained in Exhibit 101)

*

+

Certain portions of this exhibit have been omitted pursuant to Item 601(b)(10) of Regulation S-K. The Registrant
hereby undertakes to furnish to the SEC, upon request, copies of any such instruments.

Indicates a management contract or compensatory plan

˄     
These  certifications  are  being  furnished  solely  to  accompany  this  Annual  Report  pursuant  to  18  U.S.C.  Section
1350, and are not being filed for purposes of Section 18 of the Securities Exchange Act of 1934, as amended, and are not to
be incorporated by reference into any filing of the Registrant, whether made before or after the date hereof, regardless of
any general incorporation language in such filing.

ITEM 16.    FORM 10-K SUMMARY

Not applicable

132

Table of Contents

SIGNATURES

Pursuant to the requirements of Section 13 or 15(d) of the Securities Exchange Act of 1934, the Company has duly caused
this report to be signed on its behalf by the undersigned, thereunto duly authorized.

Dated: March 24, 2022

Milestone Pharmaceuticals Inc.

/s/ Joseph Oliveto
Joseph Oliveto
Chief Executive Officer

POWER OF ATTORNEY
KNOW ALL BY THESE PRESENTS, that each person whose signature appears below constitutes and appoints Joseph
Oliveto and Amit Hasija, and each of them, as his or her true and lawful attorneys-in-fact and agents, each with the full
power of substitution, for him or her and in his or her name, place or stead, in any and all capacities, to sign any and all
amendments  to  this  report,  with  exhibits  thereto  and  other  documents  in  connection  therewith,  with  the  Securities  and
Exchange Commission, granting unto said attorneys-in-fact and agents, and each of them, full power and authority to do
and  perform  each  and  every  act  and  thing  requisite  and  necessary  to  be  done  in  and  about  the  premises,  as  fully  to  all
intents and purposes as he or she might or could do in person, hereby ratifying and confirming all that said attorneys-in-fact
and agents, or their, his substitute or substitutes, may lawfully do or cause to be done by virtue hereof.

Pursuant to the requirements of the Securities Exchange Act of 1934, this report has been signed below by the following
persons on behalf of the Company and in the capacities indicated on the 24th of  March 2022.

/s/ Joseph Oliveto
Joseph Oliveto

/s/ Amit Hasija
Amit Hasija

/s/ Robert J. Wills
Robert Wills

/s/ Michael Tomsicek
Michael Tomsicek

/s/ Paul Truex
Paul Truex

/s/ Debra K. Liebert
Debra K. Liebert

/s/ Richard Pasternak
Richard Pasternak

/s/ Lisa M. Giles
Lisa M. Giles

    Chief Executive Officer

(principal executive officer)

Chief Financial Officer
(principal financial officer and principle accounting officer)

Chairman of the Board

Director

Director

Director

Director

Director

133

DESCRIPTION OF THE REGISTRANT'S SECURITIES
REGISTERED PURSUANT TO SECTION 12 OF THE
SECURITIES EXCHANGE ACT OF 1934

Exhibit 4.5

The following description sets forth certain material terms and provisions of the securities of Milestone Pharmaceuticals Inc.
(the “Company”) that are registered under Section 12 of the Securities Exchange Act of 1934, as amended. The following
description of our securities is intended as a summary only and is qualified in its entirety by reference to our articles of
incorporation and amendments thereto and our bylaws, each of which are filed as exhibits to the Annual Report on Form 10-
K of which this description is a part, and to the applicable provisions of the Business Corporations Act (Québec) (BCA).

General

Our authorized share capital consists of an unlimited number of common shares, no par value per share, and an unlimited
number of preferred shares, no par value per share, which are issuable in one or more series.

Common Shares

Voting Rights

Under our articles of incorporation, the holders of common shares are entitled to one vote for each share held at any
meeting of our shareholders.

Dividends

Subject to the prior rights of holders of our preferred shares, if applicable, the holders of common shares are entitled to
receive dividends as and when declared by our board of directors. We have never declared or paid cash dividends on our
share capital, and we do not currently intend to pay any cash dividends on our share capital in the foreseeable future. We
currently intend to retain all available funds and any future earnings, if any, to fund the development and expansion of our
business. Any future determination related to dividend policy will be made at the discretion of our board of directors, subject
to applicable laws, and will depend upon, among other factors, our results of operations, financial condition, contractual
restrictions and capital requirements. In addition, our ability to pay cash dividends on our share capital in the future may be
limited by the terms of any future debt or preferred securities we issue or any credit facilities we enter into.

Liquidation

Subject to the prior payment to holders of our preferred shares, if any, in the event of our liquidation, dissolution or winding-
up or other distribution of our assets among our shareholders, the holders of common shares are entitled to share pro rata in
the distribution of the balance of our assets.

Rights and Preferences

The holders of common shares have no preemptive, conversion rights or other subscription rights. There are no redemption
or sinking fund provisions applicable to our common shares. There is no provision in our articles of incorporation requiring
the holders of common shares to contribute additional capital or permitting or restricting the issuance of additional securities
or any other material restrictions. The rights, preferences and privileges of the holders of common shares may be subject to,
and adversely affected by, the rights of the holders of any series of preferred shares that we may designate in the future.

Preferred Shares

We do not have any preferred shares outstanding. Under our articles of incorporation, we are authorized to issue, without
shareholder approval, an unlimited number of preferred shares, issuable in one or more series, and, subject to the
provisions of the BCA, having such designations, rights, privileges, restrictions and conditions, including dividend and voting
rights, as our board of directors may determine, and such rights and privileges, including dividend and voting rights, may be
superior to those of the common shares. The issuance of preferred shares, while providing flexibility in connection with
possible acquisitions and other corporate purposes, could, among other things, have the effect of delaying, deferring or
preventing a change in control of our company and might adversely affect the market price of our common shares and the
voting and other rights of the holders of common shares. We have no current plans to issue any preferred shares.

Registration Rights

Holders of certain of the common shares issued upon the conversion of our preferred shares in connection with our initial
public offering on May 13, 2019 are entitled to certain rights with respect to registration of any securities held by such
investors, as well as any under the Securities Act. These shares are referred to as registrable securities. The holders of
these registrable securities possess registration rights pursuant to the terms of our third amended and restated registration
rights agreement and are described below. The registration of common shares pursuant to the exercise of the registration
rights described below would enable the holders to trade these shares without restriction under the Securities Act when the
applicable registration statement is declared effective. We will pay the registration expenses, other than underwriting
discounts, selling commissions and share transfer taxes for the shares registered pursuant to the demand, piggyback and
Form S-3 registrations described below. Expenses relating to underwriting discounts, selling commissions and share transfer
taxes for the shares registered will be borne by us and the participating holders in proportion to the number of common
shares sold by each, or, as between the participating holders, as such participating holders may otherwise agree.

Generally, in an underwritten offering, the managing underwriter, if any, has the right, subject to specified conditions, to limit
the number of shares the holders may include. The demand, piggyback and Form S-3 registration rights described below will
expire upon the earliest of (i) the occurrence of certain mergers or consolidations of the company, (ii) the date on which the
shares that are the subject to the agreement are publicly sold, or if they may be publicly sold: (x) pursuant to Rule 144 of the
Securities Act and (y) Section 2.5 of Regulation 45-102 respecting Resale of Securities, as adopted by the Canadian
Securities Administrators, and (iii) five years after the completion of our initial public offering.

Demand Registration Rights

Certain holders of the common shares issued upon conversion of our preferred shares are entitled to certain demand
registration rights. These demand rights permit holders of at least 25% of the registrable securities then outstanding, on not
more than two occasions, to request that we register all or a portion of their shares, subject to certain specified exceptions,
pursuant to either the Securities Act, Regulation 41-101 respecting General Prospectus Requirements, as adopted by
Canadian Securities Administrators or both.

Piggyback Registration Rights

Holders of certain of the common shares issued upon conversion of our preferred shares are entitled to include their shares
of registrable securities in any registration statement we file in the event that we propose to register any of our securities
under the Securities Act in an offering, either for our own account or for the account of other security holders, subject to
specified conditions and limitations.

S-3 Registration Rights

Holders of certain of the common shares issued upon conversion of our preferred shares are entitled to certain Form S-3
registration rights. The holders of at least 25% of the registrable securities then outstanding may, on not more than two
occasions within any 12-month period, request that we register all or a portion of their shares on Form S-3 or a form under
the Canada-United States Multijurisdictional Disclosure System, or the MJDS, if we are qualified to file a registration
statement on Form S-3 or the MJDS, as applicable, subject to specified exceptions. Such request for registration on Form S-
3 must cover securities with an aggregate offering price which equals or exceeds$10.0 million. The right to have such shares
registered on Form S-3 is further subject to other specified conditions and limitations.

Indemnification

The third amended and restated registration rights agreement contains customary cross-indemnification provisions, pursuant
to which we are obligated to indemnify the selling shareholders in the event of material misstatements or omissions in the
registration statement attributable to us, and they are obligated to indemnify us for material misstatements or omissions in
the registration statement attributable to them.

Transfer Agent and Registrar

Our transfer agent and registrar for our common shares is Computershare Investor Services Inc., with an address of
1500 Robert-Bourassa Boulevard, 7th Floor, Montréal, Quebec H3A 3S8.

Nasdaq Global Market Listing

Our common shares are listed on The Nasdaq Global Market under the trading symbol "MIST."

Advance Notice Procedures and Shareholder Proposals

Under the BCA, shareholders may make proposals for matters to be considered at the annual general meeting of
shareholders. Such proposals must be sent to us in advance of any proposed meeting by delivering a timely written notice in
proper form to our registered office in accordance with the requirements of the BCA. The notice must include information on
the business the shareholder intends to bring before the meeting.

In addition, our bylaws require that shareholders provide us with advance notice of their intention to nominate any persons,
other than those nominated by management, for election to our board of directors at a meeting of shareholders.

These provisions could have the effect of delaying the nomination of certain persons for director that are favored by the
holders of a majority of our outstanding voting securities.

Exhibit 23.1

CONSENT OF INDEPENDENT REGISTERED PUBLIC ACCOUNTING FIRM

We hereby consent to the incorporation by reference in the Registration Statements on Form S-8 (Nos. 333-231347, 333-236971
and 333-254838) of Milestone Pharmaceuticals Inc. of our report dated March 24, 2022 relating to the consolidated financial
statements, which appears in this Form 10-K.

/s/ PricewaterhouseCoopers LLP 
Montréal, Québec, Canada

March 24, 2022

 
 
Exhibit 31.1

CERTIFICATION PURSUANT TO
RULES 13a-14(a) AND 15d-14(a) UNDER THE SECURITIES EXCHANGE ACT OF 1934,
AS ADOPTED PURSUANT TO SECTION 302 OF THE SARBANES-OXLEY ACT OF 2002

I, Joseph Oliveto, certify that:

1.           I have reviewed this Annual Report on Form 10-K of Milestone Pharmaceuticals Inc.;

2.           Based on my knowledge, this report does not contain any untrue statement of a material fact or omit to state a

material fact necessary to make the statements made, in light of the circumstances under which such statements
were made, not misleading with respect to the period covered by this report;

3.           Based on my knowledge, the financial statements, and other financial information included in this report, fairly

present in all material respects the financial condition, results of operations and cash flows of the registrant as of,
and for, the periods presented in this report;

4.           The registrant’s other certifying officer(s) and I are responsible for establishing and maintaining disclosure

controls and procedures (as defined in Exchange Act Rules 13a-15(e) and 15d-15(e)) and internal control over
financial reporting (as defined in Exchange Act Rules 13a-15(f) and 15d-15(f)) for the registrant and have:

(a)          Designed such disclosure controls and procedures, or caused such disclosure controls and procedures to

be designed under our supervision, to ensure that material information relating to the registrant, including
its consolidated subsidiaries, is made known to us by others within those entities, particularly during the
period in which this report is being prepared;

(b)          Designed such internal control over financial reporting, or caused such internal control over financial

reporting to be designed under our supervision, to provide reasonable assurance regarding the reliability
of financial reporting and the preparation of financial statements for external purposes in accordance with
generally accepted accounting principles;

(c)          Evaluated the effectiveness of the registrant’s disclosure controls and procedures and presented in this

report our conclusions about the effectiveness of the disclosure controls and procedures, as of the end of
the period covered by this report based on such evaluation; and

(d)          Disclosed in this report any change in the registrant’s internal control over financial reporting that

occurred during the registrant’s most recent fiscal quarter (the registrant’s fourth fiscal quarter in the case
of an annual report) that has materially affected, or is reasonably likely to materially affect, the
registrant’s internal control over financial reporting; and

5.            The registrant’s other certifying officer(s) and I have disclosed, based on our most recent evaluation of internal
control over financial reporting, to the registrant’s auditors and the audit committee of the registrant’s board of
directors (or persons performing the equivalent functions):

(a)          All significant deficiencies and material weaknesses in the design or operation of internal control over

financial reporting which are reasonably likely to adversely affect the registrant’s ability to record,
process, summarize and report financial information; and

(b)          Any fraud, whether or not material, that involves management or other employees who have a significant

role in the registrant’s internal control over financial reporting.

Date: March 24, 2022

/s/ Joseph Oliveto
Joseph Oliveto
President and Chief Executive Officer
(Principal Executive Officer)

Exhibit 31.2

CERTIFICATION PURSUANT TO
RULES 13a-14(a) AND 15d-14(a) UNDER THE SECURITIES EXCHANGE ACT OF 1934,
AS ADOPTED PURSUANT TO SECTION 302 OF THE SARBANES-OXLEY ACT OF 2002

I, Amit Hasija, certify that:

1.           I have reviewed this Annual Report on Form 10-K of Milestone Pharmaceuticals Inc.;

2.           Based on my knowledge, this report does not contain any untrue statement of a material fact or omit to state a

material fact necessary to make the statements made, in light of the circumstances under which such statements
were made, not misleading with respect to the period covered by this report;

3.           Based on my knowledge, the financial statements, and other financial information included in this report, fairly

present in all material respects the financial condition, results of operations and cash flows of the registrant as of,
and for, the periods presented in this report;

4.           The registrant’s other certifying officer(s) and I are responsible for establishing and maintaining disclosure

controls and procedures (as defined in Exchange Act Rules 13a-15(e) and 15d-15(e)) and internal control over
financial reporting (as defined in Exchange Act Rules 13a-15(f) and 15d-15(f)) for the registrant and have:

(a)          Designed such disclosure controls and procedures, or caused such disclosure controls and procedures to

be designed under our supervision, to ensure that material information relating to the registrant, including
its consolidated subsidiaries, is made known to us by others within those entities, particularly during the
period in which this report is being prepared;

(b)          Designed such internal control over financial reporting, or caused such internal control over financial

reporting to be designed under our supervision, to provide reasonable assurance regarding the reliability
of financial reporting and the preparation of financial statements for external purposes in accordance with
generally accepted accounting principles;

(c)          Evaluated the effectiveness of the registrant’s disclosure controls and procedures and presented in this

report our conclusions about the effectiveness of the disclosure controls and procedures, as of the end of
the period covered by this report based on such evaluation; and

(d)          Disclosed in this report any change in the registrant’s internal control over financial reporting that

occurred during the registrant’s most recent fiscal quarter (the registrant’s fourth fiscal quarter in the case
of an annual report) that has materially affected, or is reasonably likely to materially affect, the
registrant’s internal control over financial reporting; and

5.            The registrant’s other certifying officer(s) and I have disclosed, based on our most recent evaluation of internal
control over financial reporting, to the registrant’s auditors and the audit committee of the registrant’s board of
directors (or persons performing the equivalent functions):

(a)          All significant deficiencies and material weaknesses in the design or operation of internal control over

financial reporting which are reasonably likely to adversely affect the registrant’s ability to record,
process, summarize and report financial information; and

(b)          Any fraud, whether or not material, that involves management or other employees who have a significant

role in the registrant’s internal control over financial reporting.

Date: March 24, 2022

/s/ Amit Hasija
Amit Hasija
Chief Financial Officer
(Principal Financial and Accounting Officer)

CERTIFICATION PURSUANT TO
18 U.S.C. SECTION 1350, AS ADOPTED PURSUANT TO
SECTION 906 OF THE SARBANES-OXLEY ACT OF 2002

Exhibit 32.1

Pursuant to the requirement set forth in Rule 13a-14(b) of the Securities Exchange Act of 1934, as amended, (the
“Exchange Act”) and Section 1350 of Chapter 63 of Title 18 of the United States Code (18 U.S.C. §1350), Joseph Oliveto,
Chief Executive Officer of Milestone Pharmaceuticals Inc. (the “Company”), and Amit Hasija, Chief Financial Officer of
the Company, each hereby certifies that, to the best of his or her knowledge:

1.            The Company’s Annual Report on Form 10-K for the period ended December 31, 2021, to which this

Certification is attached as Exhibit 32.1 (the “Periodic Report”), fully complies with the requirements of
Section 13(a) or Section 15(d) of the Exchange Act; and

2.            The information contained in the Periodic Report fairly presents, in all material respects, the financial condition

and results of operations of the Company.

Dated: March 24, 2022

/s/ Joseph Oliveto
Joseph Oliveto
Chief Executive Officer
(Principal Executive Officer)

/s/ Amit Hasija
Amit Hasija
Chief Financial Officer
(Principal Financial and Accounting Officer)