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Mirati Therapeutics

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FY2016 Annual Report · Mirati Therapeutics
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2016 Annual Report

Dear Shareholders, 

At Mirati, our overriding mission and motivation is to improve and extend the lives of patients with 

cancer. Our precision approach to drug development, expertly targeting drivers of cancer to identify

those patients most likely to benefit from treatment, leverages the best of our exceptionally experienced 

team. We employ multiple methods to address the complexities of cancer, including patient selection 

based on genetic screening, immuno-oncology drug combinations with strong scientific rationale, and 

the exploration of novel oncology targets such as KRAS. In 2016, we achieved several important 

clinical and corporate goals, setting us on a path for greater success. With the completion of a $66.8 

million public offering in January 2017, we are well-positioned to deliver key clinical data across the 

breadth of our programs in 2017.  

Single Agent Programs

Our single agent clinical programs are focused on select populations of patients with a variety of solid 

tumors but with a primary focus on patients with non-small cell lung cancer (NSCLC), which accounts

for 80% to 85% of all lung cancer diagnoses. There remains a significant unmet need and commercial

opportunity for novel targeted agents that improve patient outcomes.  

Glesatinib selectively kills tumor cells with genetic alterations in MET. We have observed promising 

TT

activity in the ongoing Phase 1b and Phase 2 AMETHYST NSCLC clinical trials in genetically selected 

patients which was reported in January 2017. In 13 NSCLC patients with MET Exon 14 deletion, a 

T

tumor regression rate of 85% and a response rate of 46% including confirmed and unconfirmed 

responses were observed. 

We are focused on continuing to enroll patients into the AMETHYST clinical trial and expect to provide

an update on our progress in the second half of 2017.     

Our sitravatinib program is enrolling patients in a Phase 1b expansion clinical trial with a primary focus

on the treatment of NSCLC patients with RET fusions, CHR4q12 amplicons and 

T

CBL mutations. The

early Phase 1b data in patients with RET fusions have demonstrated that sitravatinib is well-tolerated. 

T

Further, sitravatinib has demonstrated a tumor regression rate of 100% in 4 patients including an

unconfirmed and another confirmed partial response. We plan to provide an update on this clinical trial

in the third quarter of 2017.  

Immuno-oncology Combinations

Immunotherapies such as PD-1/PD-L1 (checkpoint) inhibitors harness the body’s immune response to 

destroy cancer cells. While this approach represents an exciting opportunity to address difficult tumors

such as NSCLC, there remains a large unmet need for the majority of patients who do not respond to

these therapies. Mirati has two Phase 2 immuno-oncology combination programs that are intended to

enhance the effectiveness of checkpoint inhibitors via scientifically validated mechanisms that augment 

the immune response to cancer. 

Our first immuno-oncology program is a Phase 2 clinical trial evaluating the combination of sitravatinib 

with nivolumab, an approved checkpoint inhibitor, in patients with NSCLC. Sitravatinib is a potent 

inhibitor of the TAM (Tyro, Axl, Mer) and split (KDR, KIT) tyrosine kinase families. Preclinical data 

have demonstrated that simultaneous inhibition of the TAM and split kinase families reduces the

negative impact of immune suppressive cells while improving immune supportive cells that promote the

body’s anti-tumor response. Based upon these positive immunomodulatory properties, sitravatinib may 

enhance the efficacy of checkpoint inhibitor therapy in NSCLC. We expect to provide initial clinical 

results from this trial in the second half of 2017.  

Our second immuno-oncology program is a Phase 2 clinical trial being conducted in collaboration with 

MedImmune/Astra Zeneca in NSCLC patients that combines mocetinostat, our selective Class I & IV 

HDAC inhibitor, with durvalumab, a checkpoint inhibitor being developed by AstraZeneca. Preclinical

data have shown that mocetinostat stimulates the immune responsiveness of both tumor cells and local 

immune cells, which may improve the effectiveness of checkpoint inhibitors like durvalumab. We

expect to provide an update from this clinical trial in mid-2017.    

Late Phase Discovery Programs

Lastly, we are enthusiastic about the progress in our preclinical pipeline, which is focused on 

genomically-informed precision medicine. We have made exciting progress with our KRAS inhibitor 

program, where we have produced potent and selective compounds that have demonstrated significant 

tumor regression in preclinical animal models. Mutations in the KRAS protein are found in many 

cancers and are thought to be responsible for driving a variety of cancers including NSCLC and 

colorectal cancer. However, KRAS has historically proven to be a very difficult drug target. Based upon 

our early success, we believe that our KRAS program represents a remarkable opportunity to develop a 

first-in-class therapy that will target one of the most commonly mutated cancer genes which could 

benefit 10-15% of NSCLC patients and 5% of colorectal cancer patients. We anticipate that we will

select a drug candidate from our KRAS program in the second half of 2017 and begin the preclinical 

process of preparing for an IND submission. In addition, in December 2016, we selected a clinical 

candidate for our LSD1 program, a compound with potential best-in-class properties for the treatment of 

small cell lung cancer and acute myeloid leukemia. This molecule is in preclinical development with and 

IND anticipated by the end of 2017. 

In closing, we expect 2017 to be a significant year for Mirati with important milestones across our 

development pipeline. We remain grateful to our employees, board members, shareholders, and 

especially the patients and clinical investigators, for their support as we execute on our mission of 

making a difference in the lives of those affected by cancer. We look forward to updating our progress

throughout the coming year. 

Sincerely,  

Charles M. Baum, MD, Ph.D.

President and Chief Executive Officer 

Mirati Therapeutics, Inc. 9393 Towne Centre Drive, Suite 200, San Diego, CA 92121

[THIS PAGE INTENTIONALLY LEFT BLANK]

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

        (Mark one) 

(cid:58) ANNUAL REPORT UNDER SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934.

(cid:133) TRANSITION REPORT UNDER SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934.

For the fiscal year ended December 31, 2016; or

For the transition period from                      to 

Commission file number: 1-15803

____________________________________________________ 
MIRATI THERAPEUTICS, INC.
(Exact Name of Registrant as Specified in Its Charter) 
_____________________________________________________ 

Delaware 
(State or other jurisdiction of 
incorporation or organization)

9393 Towne Centre Drive Suite 200, San Diego, California 
(Address of principal executive offices)

46-2693615
(IRS Employer
Identification No.)

92121 
(Zip Code)

Registrant’s telephone number: (858) 332-3410 
Securities registered pursuant to Section 12(b) of the Act:

Title of Each Class 

Name of Each Exchange on Which Registered

Common Stock, Par value $0.001 per share 

The NASDAQ Stock Market LLC 

Securities registered pursuant to Section 12(g) of the Act:   None

Indicate by check mark if the registrant is a well-known seasoned issuer, as defined in Rule 405 of the Securities Act.    Yes (cid:133)    No  (cid:58)

Indicate by check mark if the registrant is not required to file reports pursuant to Section 13 or Section 15(d) of the Act.  

ff

 Yes  (cid:133)    No  (cid:58)

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  (cid:58)    No  (cid:133)
Indicate by check mark whether the registrant has submitted electronically and posted on its corporate Web site, if any, every Interactive Data 
File required to be submitted and posted 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  (cid:58)    No  (cid:133)
Indicate by check mark if disclosure of delinquent filers pursuant to Item 405 of Regulation S-K is not contained herein, and will not be
contained, to the best of registrant’s knowledge, in definitive proxy or information statements incorporated by reference in Part III of this
Form 10-K or any amendment to this Form 10-K.  (cid:133)
Indicate by check mark whether the registrant is a large accelerated filer, an accelerated filer, a non-accelerated filer, or a smaller reporting 
company. See the definitions of “large accelerated filer,” “accelerated filer” and “smaller reporting company” in Rule 12b-2 of the Exchange 
Act. (Check one):

uu

aa

a

f

Large accelerated filer 

(cid:133)(cid:3)

Accelerated filer 

Non-accelerated filer 

(cid:133)(Do not check if a smaller reporting company)

Smaller reporting company 

Indicate by check mark whether the registrant is a shell company (as defined in Rule 12b-2 of the Act).    Yes  (cid:133)    No  (cid:58)

(cid:58)

(cid:133)(cid:3)

The  aggregate  market  value  of  common  stock  held  by  non-affiliates  (based  on  the  closing  price  on  the  last  business  day  of  the 
registrant’s  most  recently  completed  second  fiscal  quarter  as  reported  on  the  NASDAQ  Capital  Market)  was  $77  million.  All  executive 
officers and directors of the registrant and all persons filing a Schedule 13D or Schedule 13G with the Securities and Exchange Commission 
in  respect  to  registrant’s  common  stock  have  been  deemed,  solely  for  the  purpose  of  the  foregoing  calculation,  to  be  “affiliates”  of  the 
registrant.

uu

As of March 3, 2017, the registrant had 24,939,797 shares of common stock outstanding. 

DOCUMENTS INCORPORATED BY REFERENCE

Certain information required to be disclosed in Part III of this report is incorporated by reference from the registrant’s definitive Proxy 
Statement for the 2017 Annual Meeting of Stockholders, which will be held on May 17, 2017 and which proxy statement will be filed not 
later than 120 days after the end of the fiscal year covered by this report. 

ii

 
 
 
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Table of Contents

PART I

Item 1.

Business

Item 1A. Risk Factors

Item 1B. Unresolved Staff Comments

Item 2.

Item 3.

Item 4.

Properties

Legal Proceedings

Mine Safety Disclosures

PART II

Item 5.

Item 6.

Market for Registrant’s Common Equity, Related Stockholder Matters and Issuer Purchases of Equity
Securities
Selected Consolidated Financial Data

Item 7.
Item 7A. Quantitative and Qualitative Disclosures About Market Risk

Management’s Discussion and Analysis of Financial Condition and Results of Operations

Item 8.

Item 9.

Financial Statements and Supplementary Data

Changes in and Disagreements With Accountants on Accounting and Financial Disclosure

Item 9A. Controls and Procedures

Item 9B. Other Information

Item 10. Directors, Executive Officers and Corporate Governance

Item 11.

Executive Compensation

PART III

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

Item 15.

Exhibits and Financial Statement Schedules

SIGNATURES

PART IV

Page

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22

42

42

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43

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56

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56

56

57

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1

 
Forward-Looking Statements

PART I

This Annual Report on Form 10-K (the "Annual Report") may contain “forward-looking statements” within the meaning 
of the federal securities laws made pursuant to the safe harbor provisions of the Private Securities Litigation Reform Act of 1995. 
Our actual results could differ materially from those anticipated in these forward-looking statements as a result of various factors, 
including those set forth under Part I, Item 1A, “Risk Factors” in this Annual Report. Except as required by law, we assume no 
obligation to update these forward-looking statements, whether as a result of new information, future events or otherwise. These 
statements, which represent our current expectations or beliefs concerning various future events, may contain words such as “may,” 
“will,”  “expect,”  “anticipate,”  “intend,”  “plan,”  “believe,”  “estimate”  or  other  words  indicating  future  results,  though  not  all 
forward-looking statements necessarily contain these identifying words. Such statements may include, but are not limited to, 
statements concerning the following:

·                  the initiation, cost, timing, progress and results of our research and development activities, preclinical studies and 

future clinical trials;

·                  our ability to obtain and maintain regulatory approval for our product candidates, and any related restrictions, 

limitations, and/or warnings in the label of any approved product candidate;

·                  our ability to obtain funding for our operations;

·                  our plans to research, develop and commercialize our future product candidates;

·                  our strategic partners’ decisions relating to development and commercialization of product candidates;

·                  our ability to attract collaborators with development, regulatory and commercialization expertise;

·                  our ability to obtain and maintain intellectual property protection for our future product candidates;

·                  the size and growth potential of the markets for our future product candidates, and our ability to serve those 

markets;

·                  our ability to successfully commercialize our future product candidates;

·                  the rate and degree of market acceptance of our future product candidates;

·                  our ability to develop sales and marketing capabilities, whether alone or with potential future collaborators;

·                  regulatory developments in the United States and foreign countries;

·                  the performance of our third-party suppliers and manufacturers;

·                  the success of competing therapies that are or become available;

·                  our expectations regarding the time during which we will be an emerging growth company under the Jumpstart 

Our Business Startups Act of 2012 ("the JOBS Act");

·                  the loss of key scientific or management personnel; and

·                  our future financial results, capital requirements and need for additional financing.

2

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
  
References  in  this Annual  Report  on  Form 10-K  to  "we",  "our",  "us",  "Mirati"  or  "the  Company"  refer  to  Mirati 

Therapeutics, Inc. and its subsidiaries.

Item 1.     Business

Overview

BUSINESS

Mirati Therapeutics, Inc. is a clinical-stage biopharmaceutical company focused on developing a pipeline of oncology 
products including candidates intended to treat specific genetic and epigenetic drivers of cancer in selected subsets of cancer 
patients with unmet needs. Additionally, we are evaluating our product candidates in combination with checkpoint inhibitors (anti-
PD-1 and PD-L1) to determine whether they will enhance the efficacy of those agents in patients with non-small cell lung cancer 
("NSCLC") and other solid tumors.  We believe that an increased understanding of the genomic factors that drive tumor cell growth 
can lead to the development of cancer drugs that target these genomic factors, resulting in increased efficacy while reducing side 
effects. 

Our clinical pipeline consists of three product candidates: glesatinib, sitravatinib and mocetinostat. Both glesatinib and 
sitravatinib are orally-bioavailable, spectrum-selective kinase inhibitors with distinct target profiles that are in development for 
the treatment of patients with NSCLC and other solid tumors. Glesatinib is in Phase 2 clinical development, and targets the MET 
and Axl receptor tyrosine kinase families ("RTKs"). Sitravatinib is in Phase 1b clinical development and targets genetic alterations 
in RET gene rearrangements, CHR4q12 amplifications, CBL mutations and AXL alterations. We are also evaluating sitravatinib 
in a multi-arm Phase 2 clinical trial to determine its ability to enhance the clinical efficacy of nivolumab, a checkpoint inhibitor 
approved for the treatment of patients with a variety of solid tumors including NSCLC and metastatic Renal Cell Carcinoma 
(“RCC”). Our third candidate is mocetinostat, an orally-bioavailable, Class 1 selective histone deacetylase ("HDAC") inhibitor. 
Mocetinostat is in Phase 1b/2 clinical development in combination with durvalumab, MedImmune Limited’s ("MedImmune") 
anti-PD-L1 immune checkpoint inhibitor, for the treatment of patients with NSCLC. 

Our novel kinase inhibitors, glesatinib and sitravatinib, are intended to treat specific mutations that drive the growth of 
cancer or are implicated in cancer drug resistance or pathogenic processes such as tumor angiogenesis. Sitravatinib is a potent 
inhibitor  of  the Tyro, Axl,  Mer  ("TAM")  family  of  kinases  which  we  believe  may  lead  to  enhanced  anti-tumor  immunity  in 
combination with immune checkpoint inhibitors by changing the tumor microenvironment from a tolerogenic to an immunogenic 
state and increasing anti-tumor immune response by reducing T-cell and macrophage suppressor effects. Our HDAC inhibitor, 
mocetinostat, acts through important epigenetic mechanisms, the effects of which could potentially enhance the efficacy of immune 
checkpoint inhibitors when used in combination.  

Two candidates are in pre-clinical development. The first is a highly-potent and potentially best-in-class LSD1 inhibitor 
with potential for rapid clinical proof-of-concept in small cell lung cancer ("SCLC") or acute myeloid leukemia ("AML"). An 
investigational new drug ("IND") submission is planned for this compound in late 2017. Additionally, a mutant-selective KRAS 
inhibitor program is advancing to candidate selection phase and prototype inhibitors have demonstrated marked tumor regression 
in KRAS mutant tumor models, with an IND candidate selection anticipated by the end of 2017. We plan to identify additional 
drug development opportunities by leveraging our deep scientific understanding of molecular drug targets and mechanisms of 
resistance and potentially in-licensing or internally discovering promising, early-stage novel drug candidates.

Our three clinical stage product candidates are further described below:

•  Glesatinib is an orally-bioavailable, potent, small molecule kinase inhibitor of MET and Axl RTKs. Glesatinib is in 

clinical development for the treatment of solid tumors, with an initial focus on NSCLC.  

We presently have two ongoing clinical trials of glesatinib: a single-arm Phase 2 clinical trial for the treatment of NSCLC 
patients with genetic alterations of MET and a Phase 1b clinical trial in patients with genetic alterations of MET and Axl 
in NSCLC and other solid tumors.

On January 5, 2017, we provided a clinical update focused on our experience with a spray dried dispersion (“SDD”) 
formulation of glesatinib that was implemented in the ongoing Phase 1b and Phase 2 clinical trials in May 2016.  We 
announced that patients from both Phase 1b and Phase 2 trials were assessed as of December 2, 2016 to evaluate the 
impact of the SDD formulation (n=41) as compared to the prior soft gel formulation (n=50). Adverse event-related (“AE-
related”) dose reductions occurred in 17% (7/41) of patients treated with the SDD formulation, versus 46% (23/50) of 
patients treated with the prior soft gel formulation.  In patients who were transitioned to the SDD formulation during 

3

 
 
 
 
   
their therapy (n=12), AE-related dose reductions took place in 8% (1/12) of patients versus 33% (4/12) of patients treated 
with the soft gel formulation.

In an initial evaluation of 24 genetically-selected patients treated with the SDD formulation: 11 patients were in the Phase 
2  MET  Exon  14  deletion  mutation  cohort,  of  whom  eight  were  evaluable;  eight  patients  were  in  the  Phase  2  MET 
amplification cohort, all of whom were evaluable; and five patients were in the Phase 1b trial with MET Exon 14 deletion 
mutations, who had clinical characteristics and genetic driver alterations identical to the entry criteria in the ongoing 
Phase 2 trial, all of whom were evaluable.

In MET Exon 14 deletion patients treated with the SDD formulation across both the Phase 1b and Phase 2 trials, glesatinib 
demonstrated promising activity. In the Phase 2 trial, one confirmed partial response (“PR”) and two unconfirmed PRs 
out of the eight evaluable patients were observed. As of December 2, 2016, one unconfirmed PR remained on study 
awaiting a confirmatory scan. Tumor reduction was observed in six of eight evaluable patients. In the Phase 1b trial, three 
confirmed PRs out of five evaluable patients were observed.  Tumor reduction was observed in all five patients. Overall, 
data in these 13 patients reflected an objective response rate (“ORR”) of 46% across the Phase 1b and Phase 2 patient 
populations, including confirmed and unconfirmed responses. Tumor reduction was observed in 11 of 13 patients. As of 
December 2, 2016, the longest duration of a patient on study was more than 55 weeks and the patient remained on study.

In MET amplification patients treated with the SDD formulation, glesatinib also demonstrated clinical benefit. In the 
Phase 2 trial, two unconfirmed PRs out of eight evaluable patients were observed.  Neither of the unconfirmed responses 
remains on study.  Tumor reduction was observed in six of eight evaluable patients. As of December 2, 2016, the longest 
duration of a patient on study was more than 24 weeks and the patient remained on study.

The Company expects to provide an additional update on the glesatinib program in the second half of 2017. 

• 

Sitravatinib is an orally-bioavailable, potent, small molecule spectrum-selective kinase inhibitor in clinical development 
for the treatment of solid tumors with an emphasis on genetic alterations involving RET gene rearrangements, CHR4q12 
amplifications, CBL mutations and AXL alterations. Sitravatinib is being evaluated in a Phase 1b expansion clinical trial 
designed to evaluate its safety and efficacy in multiple pre-specified cohorts of cancer patients with these genetic mutations.

On January 5, 2017 we provided a clinical update of the ongoing Phase 1b clinical trial. As of a data cut-off of December 
9, 2016, a total of six NSCLC patients with RET gene rearrangements had been enrolled, four of whom were evaluable. 
Of the four evaluable patients, one patient with a KIF5B-RET gene rearrangement demonstrated a confirmed PR and one 
patient with a DSP RET gene rearrangement had achieved an unconfirmed PR on initial scan, representing a 50% ORR, 
including confirmed and unconfirmed responses. As of December 9, 2016, both patients remained on study. A third patient 
with RET gene rearrangements demonstrated tumor reduction of 29%, representing stable disease. Tumor reduction was 
observed in all four patients. As of December 9, 2016, the longest duration of a patient on study was more than 46 weeks 
and the patient remained on study. The Phase 1b trial is also enrolling NSCLC patients with CBL mutations, CHR4q12 
amplification and AXL alterations. As of the data cut-off date, no patients with these genetic mutations were evaluable.   
The Company expects to provide an update on efficacy data in the third quarter of 2017.

Sitravatinib is also being evaluated in combination with nivolumab, a checkpoint inhibitor approved for the treatment of 
patients with a variety of solid tumors including NSCLC and metastatic RCC. Pre-clinical data indicate sitravatinib is an 
exceptionally potent inhibitor of the TAM and split (KDR, KIT, PDGFRA) family tyrosine kinases which regulate multiple 
stages  in  the  cancer  immunity  cycle  and  are  thought  to  enhance  anti-tumor  immunity  by  improving  the  efficacy  of 
checkpoint inhibitors (anti PD-1/PD-L1). Enrollment of this multicenter Phase 2 clinical trial in patients with NSCLC 
commenced in November 2016. The Company expects to provide initials results from this combination trial in the third 
quarter of 2017.

•  Mocetinostat is  an  orally  administered  spectrum-selective  Class  1  HDAC  inhibitor.  Preclinical  data  suggests  that 
mocetinostat has the potential to enhance anti-tumor efficacy when combined with immunotherapy by increasing HLA 
expression and tumor immunogenicity, depleting regulatory T-cells and myeloid-derived suppressor cells and increasing 
tumor PD-L1 expression. A Phase 1b/2 clinical trial combining mocetinostat and durvalumab, MedImmune’s monoclonal 
antibody inhibiting PD-L1, continues to enroll patients with advanced solid tumors and NSCLC. The Company expects 
to provide an additional update on the mocetinostat program mid-year 2017.

4

 
Our Strategy

Our goal is to be a leading developer of cancer therapies. We are currently focused on therapies targeted for genetically 
selected  patient  populations  as  well  as  combinations  of  these  targeted  therapies  with  immune  checkpoint  inhibitors. The  key 
components of our strategy include:

•  Develop a pipeline of targeted cancer therapies.  We believe that an increased understanding of the genomic factors that 
drive tumor cell growth will lead to the development of cancer drugs with increased efficacy while reducing side effects. 
We are leveraging the prior successful experience of certain members of our management team in the development and 
approval of multiple oncology and targeted oncology drugs (e.g. Temodar, Sutent, Inlyta, Xalkori, and Ibrance) to develop 
targeted cancer therapies to address unmet needs in specific cancer populations. Our clinical pipeline is comprised of 
two novel kinase inhibitors that target specific mutations that drive cancer cell growth and an HDAC inhibitor which is 
one of the most advanced epigenetic therapies in development. We plan to identify additional targets by leveraging our 
deep scientific understanding of molecular drug targets and mechanisms of resistance through internal drug discovery 
activities or potentially in-licensing promising, early-stage novel drug candidates.

•  Employ efficient and flexible approaches to accelerate clinical development.  Based on the prior extensive experience 
of certain members of our management team in oncology drug development, which includes the successful registration 
of several products, we take an adaptive approach to our clinical trials so that we use the information from the ongoing 
trials to increase our likelihood of success. We will pursue indications and select specific patient populations in which 
activity of our product candidates can be assessed in small proof of concept ("POC") clinical trials potentially leading to 
accelerated clinical development. When designing clinical trials, we structure our clinical development approach to test 
multiple clinical hypotheses in a single trial and design trials with the flexibility to adapt quickly and accelerate once a 
signal of clinical benefit is observed. We believe our approach may increase the likelihood of seeing results early in 
clinical trials with fewer patients, reducing our clinical development risk and development costs and allowing us to 
potentially accelerate the development of our product pipeline.

•  Advance our two lead kinase inhibitors. We have two internally discovered novel kinase inhibitors in development: 
glesatinib and sitravatinib. These product candidates target pathways of high scientific interest, including MET, AXL, 
RET, CHR4q12 and CBL. These pathways are believed to be drivers of tumor growth and to be responsible for the 
development of tumor resistance to several anti-cancer treatments. Glesatinib is in Phase 2 development and sitravatinib 
is currently in a Phase 1b dose expansion clinical trial and a Phase 2 clinical trial in combination with nivolumab.

•  Advance mocetinostat, our HDAC inhibitor. HDAC inhibitors modulate epigenetic events by their potent inhibition of 
histone  deacetylation. This  class  of  agents  has  been  shown  to  be  effective,  as  single  agents,  in  treating  hematologic 
malignancies, as evidenced by the approvals of Istodax, Zolinza, Beleodaq and Farydak. A growing body of evidence 
indicates that Class I HDAC inhibitors like mocetinostat have effects directly on tumor cells as well as on immune cells 
(regulatory T cells ("T-regs") and Myeloid-derived Suppressor Cells ("MDSCs")) that may enhance the efficacy of immune 
checkpoint inhibitors such as nivolumab, pemrolizumab, durvalumab and others. We have completed several clinical 
trials with mocetinostat in more than 400 patients which have provided valuable information on the pharmacokinetic, 
pharmacodynamic  and  safety  profile  of  the  drug.  We  are  currently  evaluating  mocetinostat  in  combination  with 
MedImmune’s immune checkpoint inhibitor durvalumab in NSCLC since we believe that is the most promising indication 
and will create the greatest benefit for the largest number of patients. 

•  Advance  our  pre-clinical  development  programs.    We  maintain  an  active  discovery  research  function  focused  on 
identifying molecules to target novel pathways in the treatment of cancer. We have developed two candidates internally 
including an LSD1 inhibitor, for which we expect to file an IND by late 2017 with an initial focus on AML and SCLC, 
and a mutant-selective KRAS inhibitor that is entering the preclinical candidate selection phase.  

•  Leverage partnerships to develop our product candidates and companion diagnostics. We plan to collaborate with third 
parties and partner certain rights to our product candidates as a means to accelerate their broader clinical development 
and maximize their therapeutic and market potential. We plan to retain certain key development and commercialization 
rights in our partnerships. We believe that retaining this strategic flexibility will enable us to maximize shareholder value. 
For example, we have entered into collaboration agreements, including with Foundation Medicine, Inc. and Guardant 
Health, Inc. to explore development of their platforms as companion diagnostics for glesatinib and to leverage their 
commercial testing platforms to enable enrollment in our clinical trials that are treating genetically selected patients.

5

Product Candidates

The following chart depicts the current state of our oncology development programs:

PRODUCT
CANDIDATE
Glesatinib

INDICATION
Solid Tumors

TARGETS
MET, Axl

COMMERCIAL
RIGHTS
Mirati: Global

Sitravatinib

Solid Tumors

Mocetinostat

Solid Tumors

RET,
CHR4q12,
CBL, Axl

HDACs
Class I and IV

Mirati: Global

Taiho: Certain Asian 
Territories
Mirati: All Other 
Territories

Our Targeted Kinase Programs

STAGE OF DEVELOPMENT
- Single-arm, single-agent Phase 2 clinical trial 
in patients with NSCLC ongoing. 

- Phase 1b clinical trial in patients with NSCLC 
and other solid tumors ongoing.
- Single-agent Phase 1b dose expansion clinical 
trial ongoing. 
-  Phase  2  clinical  trial  combination  with 
nivolumab in NSCLC ongoing

- Phase 2 clinical trial evaluating the combination 
of mocetinostat with durvalumab in patients with 
NSCLC ongoing.

Specific genes or pathways that are inappropriately activated in certain types of cancer cells and not in normal tissue are 
called driver mutations. Targeted therapies selectively inhibit these driver mutations. RTKs are a family of kinases involved in the 
transmission of signals that regulate intercellular processes, including those that control cell growth and cell division. RTKs may 
be inappropriately activated in cancerous tissues resulting in uncontrolled tumor cell growth. Aberrant kinase function, caused by 
genetic mutations, gene amplification, or over-expression, underlies many cancer cell processes, making the kinome an important 
source for therapeutic targets in oncology. Discoveries of specific drivers of disease have led to the development of targeted 
therapies, or the tailoring of therapies to a particular tumor or disease profile. In some cases, these therapies have proven to be 
more efficacious while having fewer side effects than traditional non-targeted therapies, such as chemotherapy, which kill healthy 
cells along with cancer cells. Examples of successful development of oral targeted kinase inhibitors include Novartis AG’s Gleevec, 
a  BCR-ABL  kinase  inhibitor  for  the  treatment  of  Philadelphia  chromosome  positive  chronic  myelogenous  leukemia;  and 
GlaxoSmithKline’s Tykerb, a HER2 kinase inhibitor for the treatment of a subset of breast cancer patients over-expressing the 
HER2 kinase. Further examples of oral targeted kinase inhibitors include Pfizer’s Xalkori and Bosulif and Bristol-Myers Squibb’s 
Sprycel. We believe that therapies targeting specific genetic abnormalities in subsets of cancer patients identified through companion 
diagnostic tests will result in streamlined clinical trials and improved patient outcomes and will be increasingly important in the 
continued evolution of the treatment of cancer.

We believe that by selecting patients whose tumors have genetic mutations and alterations in the pathways that are critical 
for tumor growth and that may be potently inhibited by our drugs, we will increase the potential for clinical benefit. A greater 
clinical benefit in selected patients would increase the likelihood of demonstrating clinical benefit earlier in development, potentially 
in Phase 1, which may allow us to move rapidly into registration trials. As a part of our ongoing development activities, we are 
using commercial diagnostic assays as well as assays developed internally for early clinical trials. We are working with external 
diagnostic providers to develop validated companion diagnostics for later stage clinical use and for potential registration to ensure 
that the diagnostic is widely available for commercial use upon approval. In December of 2015 we announced collaborations with 
Foundation Medicine, Inc., and Guardant Health, Inc. to explore development of their platforms as companion diagnostics for 
glesatinib and to leverage their commercial testing platforms to enable enrollment in our clinical trials that are treating genetically 
selected patients.

6

 
The clinical and commercial success of leading small molecule kinase inhibitors demonstrates the potential of new targeted 

treatments for cancer. The following table lists retail sales figures for selected small molecule kinase inhibitors. 

2015 Worldwide Retail Sales Figures of Selected Small Molecule Kinase Inhibitors

Brand Name
Gleevec
Tarceva
Sutent
Nexavar
Sprycel
Tykerb
Zelboraf
Xalkori

_____________________
(1)  Source: Evaluate Pharma.

2015 Worldwide 
Sales(1) (in millions)
4,658
$
1,227
$
1,120
$
990
$
1,620
$
236
$
218
$
488
$

Our kinase inhibitor programs in clinical development, glesatinib and sitravatinib, are kinase inhibitors with distinct target 
profiles. These new molecular entities are in development for the treatment of patients with NSCLC and other solid tumors that 
exhibit the genetic mutations and alterations of interest. Glesatinib and sitravatinib were developed internally and we own all 
global rights.

Glesatinib - A Multi Targeted Kinase Inhibitor for Solid Tumors

Glesatinib Overview

Glesatinib is an orally-bioavailable, potent, small molecule kinase inhibitor of MET and Axl. We are currently focused 
on our ongoing single-arm Phase 2 clinical trial for the treatment of NSCLC patients with genetic alterations of MET and a Phase 
1b clinical trial in patients with genetic alterations of MET and AXL in NSCLC and other solid tumors.   Based on a meeting with 
the U.S. Food and Drug Administration ("FDA"), if we observe a response rate in the Phase 2 trial of glesatinib that is significantly 
better than the response rate for currently approved second line therapy, we believe the trial could potentially serve as a registration 
enabling trial and qualify for submission for accelerated approval under U.S. Code of Federal Regulations 21 CFR Part 314, 
Subpart H (Accelerated Approval of New Drugs for Serious or Life-Threatening Illnesses).

Our development strategy for glesatinib is based on our understanding of the compound’s target inhibition profile and, 
accordingly, our focus for this program is NSCLC, although we intend to also explore other solid tumors where genetic alterations 
in MET or AXL are also known to be present. We intend to undertake patient selection using a targeted next generation sequencing 
assay to identify patients with certain genetic mutations or alterations of MET or AXL that result in oncogenic activation and are 
implicated as drivers of tumor progression.

Glesatinib Market Overview

The National Cancer Institute ("NCI") estimates that in 2016, approximately 224,000 patients in the United States ("U.S.") 
were diagnosed with lung cancer and 158,000 died due to the disease. Approximately 85% of lung cancers are NSCLCs. The 
potential oncogenic mutations of MET and AXL that we are targeting may exist in up to 6% of NSCLC cases. At present, the 
prevalence of the genetic alterations of MET and AXL is less well characterized in other solid tumors, however, they are known 
to occur in other solid tumors and we are exploring those additional indications. Although other tumor types may respond to 
treatment with glesatinib, NSCLC, HNSCC and gastroesophageal cancers are of particular relevance to demonstrate the clinical 
activity of glesatinib. 

Approximately 15% of NSCLC cases have activating EGFR mutations, equating to approximately 28,000 patients each 
year in the United States. Although tyrosine kinase inhibitors that target EGFR have demonstrated efficacy in treating patients 
with EGFR mutations, tumors eventually become resistant to therapy. Resistance to EGFR therapy is mediated through mutation 
and/or overexpression of alternative targets and pathways, including MET and Axl in approximately 70% of resistant tumors, or 
approximately 20,000 patients annually in the United States.

7

 
 
 
 
Glesatinib Background

Glesatinib is a small molecule, spectrum-selective kinase inhibitor that potently inhibits MET and Axl. These targets 
have been shown to play key roles in tumor development, tumor cell survival, therapeutic resistance and blood vessel formation, 
or angiogenesis. Glesatinib is selective for these two targets at clinically achievable dose levels and shows minimal activity against 
a panel of over 300 other kinases. We believe this profile provides the following potential advantages for glesatinib:

• 

• 

• 

• 

therapeutic action against specific mutations and genetic alterations of MET;

therapeutic action against a novel target like Axl;

high specificity reduces the risk of side effects from off-target activity; and

the selection of specific patients whose tumors exhibit genetic alterations of MET or AXL that may be drivers of tumor 
growth provides an opportunity to demonstrate single agent clinical responses of glesatinib.

The MET receptor is a member of the RTK protein family that is found on the cell’s surface and which plays a key role 
in the growth, survival and metastasis of various types of cancers, when not properly regulated. The MET target has generated 
significant scientific and pharmaceutical interest because of its direct involvement in tumor cell survival and angiogenesis. MET 
expression is elevated in several major tumor types including NSCLC, gastric cancer, RCC and HCC and is associated with poor 
prognosis. MET activation may also be associated with resistance to EGFR inhibitors such as Tarceva, Iressa and Erbitux. In 
tumors with EGFR mutation or activation, the activation or genetic alteration of MET is implicated as an escape mechanism 
leading  to  EGFR-inhibitor  resistance.  Inhibition  of  MET  may  result  in  clinical  benefit  by  blocking  the  MET-driven  escape 
mechanism used by some tumor cells when treated with other targeted inhibitors of the EGFR, such as Tarceva or Iressa.

The profile of glesatinib and our clinical development strategy is clearly distinguished from MET antibody antagonists 
(such as MetMab) that inhibit the MET pathway signaling primarily by preventing the binding of HGF to MET.  The inhibition 
of the catalytic activity of MET via small molecule strategies like glesatinib, as opposed to inhibition of ligand binding by MET 
antibody antagonists, is an important differentiated strategy in disease settings in which MET is activated by ligand-independent 
mechanisms including activating mutations, gene amplification, and/or extreme overexpression. Our primary focus in clinical 
development is on patients with NSCLC or other solid tumors exhibiting driver mutations in the MET and AXL pathways. These 
driver mutations result in constitutive activation of the MET or Axl receptors so they become independent of normally tightly 
regulated growth factor signaling. In the case of MET, genetic alterations can result in the activation of MET-dependent signaling 
independent  of  binding  to  HGF.  Therefore,  patients  with  these  driver  mutations  would  not  be  responsive  to  MET  antibody 
antagonists that inhibit HGF binding, but are more likely to respond to glesatinib, which inhibits signaling irrespective of growth 
factor binding. Finally, in preclinical studies glesatinib has demonstrated inhibition of tumor cells which express mutant forms of 
MET that may be important mechanisms of resistance that appear to be greater than other known small molecule inhibitors of 
MET.  Recent glesatinib data has indicated that glesatinib also potently inhibits certain mutant variants of MET (i.e., D1228N and 
Y1230C/H) that have recently been implicated in acquired resistance to other MET inhibitors including crizotinib and capmatinib.  
This data indicates that glesatinib may be able to be utilized as a differentiated MET inhibitor in patients exhibiting these mutations 
and may have utility in treating selected patients that become resistant to other classes of MET inhibitors.  

Glesatinib is distinguished from many other small molecule inhibitors of MET due in part to its potent activity against 
Axl, which provides an opportunity against tumors driven by Axl such as NSCLC tumors that exhibit a translocation of AXL that 
drives tumor growth, thereby increasing the likelihood that these tumors will respond to glesatinib. Further, MET and Axl are 
either overexpressed or genetically altered, or both, in tumors that are resistant to EGFR inhibitors such as Tarceva, Iressa and 
Erbitux. It is estimated that MET is overexpressed in approximately half of EGFR-resistant tumors, and amplified in 5-20% of 
EGFR-resistant  tumors.  It  is  estimated  that Axl  is  overexpressed  in  approximately  20-30%  of  EGFR-resistant  tumors.  The 
simultaneous inhibition of both MET and Axl pathways may be required for clinical efficacy in patients developing resistance to 
EGFR inhibitors or for the prevention of resistance by combining glesatinib with an EGFR inhibitor as first line treatment. 

Axl is also an RTK, and its expression has been shown to correlate with clinical-stage and lymph node status in NSCLC. 
Axl can be dysregulated in certain cancers through increased protein expression or gene rearrangement, resulting in abnormal 
tumor growth and tumor cell survival. Axl has also been linked to resistance to EGFR inhibitors such as Tarceva and Erbitux. Axl 
is also expressed in other tumor types and may be a clinically significant driver in RCC, ovarian, pancreatic and other tumors.

8

Glesatinib Clinical Trials

Multiple  Phase 1  clinical  trials  conducted  with  glesatinib  show  evidence  of  clinical  activity  as  monotherapy  and  in 
combination trials. Glesatinib doses have resulted in exposures consistent with greater than 90% inhibition of MET mutations, 
MET amplifications and Axl gene rearrangements. Dosing is ongoing in the Phase 1b expansion study which is enrolling patients 
selected for specific genetic mutations and alterations of MET and AXL.

The original IND for glesatinib was filed in December 2007 and became effective in January 2008. To date, approximately 
350 patients have been administered glesatinib in multiple clinical trials in a variety of solid tumor types. Glesatinib has been 
generally well tolerated at all doses and schedules tested to date, both as monotherapy and in combination with either Taxotere or 
Tarceva.

The most frequent treatment-related adverse events observed in prior clinical studies with glesatinib were diarrhea, fatigue 
and nausea. Other than as noted below, all of these trials were conducted with prior formulations of glesatinib that are no longer 
actively being developed. In addition, none of those prior trials were conducted in patient populations that were selected for genetic 
alterations or mutations in MET and AXL that we expect are the most likely to respond to treatment with glesatinib, which is our 
current development focus.

The historical glesatinib clinical trials are set forth in the following table.

CLINICAL TRIALS EVALUATING GLESATINIB 

Phase 1 Clinical Trial

Single Agent Dose Escalation, 21 day cycle

Phase 1b Clinical Trial

Single  Agent  Expansion  Cohort  in  patients  with 
genetic alterations of MET and Axl in NSCLC and 
other solid tumors, 21 day cycle

Completed  (trial  amended  and  continuing  as 
described  under  Phase  1b  dose  expansion 
clinical trial below)
Ongoing

Phase 1/2 Clinical Trial Combination with Erlotinib or Docetaxel in patients 

Completed

Phase 2 Clinical Trial

with advanced NSCLC, 21 day cycle
Single Agent Phase 2 clinical trial in patients with 
genetic alterations of MET in NSCLC, 21 day cycle

Ongoing

The  maximum  tolerated  dose  (“MTD”)  of  glesatinib  spray  dried  dispersion  formulation  was  established  as  750mg 
administered orally twice-daily on a 21 day continuous cycle. The observed dose limiting toxicities included one patient who 
experienced grade 3 fatigue and one patient that experienced grade 3 diarrhea. Clinical pharmacokinetic and pharmacodynamic 
data and nonclinical projections for glesatinib at the MTD indicate glesatinib plasma levels consistent with MET and Axl inhibition.  

Glesatinib Developmental Initiatives and Objectives

In December 2015, we initiated a single agent Phase 2 clinical trial in patients with genetic alterations of MET in NSCLC. 
Enrollment in the Phase 2 clinical trial is ongoing. Refer to the Overview section for the most recent update on the status of this 
clinical trial. We are also exploring other solid tumors that also have the genetic mutations and alterations of interest. 

We believe that by selecting patients whose tumors have genetic mutations and alterations that are implicated as oncogenic 
drivers and that are potently inhibited by glesatinib we may increase the likelihood of seeing clinical activity earlier in clinical 
development. We are using commercially available diagnostic assays as well as assays developed internally for early clinical use. 
We are developing companion diagnostics in collaboration with diagnostic platform providers including Foundation Medicine, 
Inc. and Guardant Health, that we plan to use in the current Phase 2 clinical trial, later stage trials and for commercialization, if 
approved.

Sitravatinib - A Novel Multi Targeted Kinase Inhibitor for Solid Tumors

Sitravatinib  is  an  orally-bioavailable,  potent,  small  molecule  multi-targeted  kinase  inhibitor.  Sitravatinib  is  a  potent 
inhibitor of closely related RTKs including RET, CHR4q12, CBL and AXL. Sitravatinib has demonstrated oral bioavailability in 
preclinical studies, inhibited target-dependent tumor cell growth and survival, and demonstrated broad spectrum antitumor activity 
in preclinical cancer models including tumor regression in tumor models exhibiting genetic alteration of sitravatinib RTK targets.

9

We are focusing our development efforts on solid tumors in which genetic mutations and alterations of RET, CHR4q12, 
CBL and AXL are implicated as oncogenic drivers with an initial focus on NSCLC. We are also exploring novel patient selection 
strategies and are targeting patients with CHR4q12 amplicons, CBL inactivating mutations and AXL alterations that may be treatable 
with sitravatinib. Genetic alterations consisting of RET gene rearrangements, CHR4q12 amplifications, CBL mutations and AXL 
alterations account for up to 5.5% of NSCLC patient cases annually in the U.S. We also plan to evaluate other tumor types for 
which the RTK targets of sitravatinib may suggest activity. The MTD of sitravatinib is 150mg administered once a day, orally on 
a continuous schedule. Sitravatinib is being evaluated in a Phase 1b expansion clinical trial designed to evaluate its safety and 
efficacy in multiple pre-specified cohorts of cancer patients with genetic mutations involving sitravatinib targets, including a cohort 
of NSCLC patients with RET gene rearrangements. Refer to the Overview section for the most recent update on the status of this 
clinical trial.

Sitravatinib is a potent inhibitor of the TAM family of kinases which we believe may lead to enhanced anti-tumor immunity 
by changing the tumor microenvironment from a tolerogenic to an immunogenic state and increasing anti-tumor immune response 
by reducing T-cell and macrophage suppressor effects. Sitravatinib is also being evaluated in combination with nivolumab, a 
checkpoint inhibitor approved for the treatment of patients with NSCLC in a Phase 2 clinical trial in patients with NSCLC.  

Mocetinostat - A Spectrum-Selective Oral HDAC Inhibitor 

Mocetinostat Overview

Mocetinostat is an orally administered, spectrum-selective Class 1 HDAC inhibitor.   By virtue of its specificity for Class 
1 HDACs, mocetinostat showed a favorable effect on the immune system in preclinical studies. By increasing PD-L1, costimulatory 
molecules,  and  HLA  antigens  on  tumor  cells,  we  believe  that  mocetinostat  may  enhance  the  immune  response  to  tumors. 
Mocetinostat may also have a favorable effect on the immune system by decreasing T-regs and MDSCs. We believe that, overall, 
these  effects  on  the  immune  system  have  the  potential  to  enhance  the  efficacy  of  checkpoint  inhibitors.  We  are  evaluating 
mocetinostat in combination with durvalumab, MedImmune’s monoclonal antibody inhibiting PD-L1 in a Phase 1b/2 clinical trial 
which continues to enroll patients with advanced solid tumors and NSCLC.  

    The epigenetic mechanisms of HDAC inhibitors have demonstrated efficacy in hematologic malignancies and have 
been approved as single agents. In addition, HDAC inhibition by agents like mocetinostat may be complementary with other 
epigenetic mechanisms. Epigenetics is the regulation of gene expression and resulting cellular phenotypes through mechanisms 
other  than  primary  DNA  sequence  alterations. The  epigenetic  regulation  of  gene  expression  involves  the  regulation  of  DNA 
methylation and modification of certain histones via modulation of acetylation or methylation of specific amino acid residues. 
Epigenetic pathways can become dysregulated during cancer progression through a variety of mechanisms, including the genetic 
alteration of molecules that participate in DNA methylation and histone modification.

Mocetinostat Market Overview

The potential of HDAC inhibitors for the treatment of certain cancers has been validated by the approval of Zolinza, 

Istodax and Beleodaq for the treatment of T-cell lymphoma and Farydak for multiple myeloma.

Our  current  focus  for  mocetinostat  is  on  the  treatment  of  patients  with  NSCLC  in  combination  with  durvalumab, 
MedImmune’s immune checkpoint inhibitor. We believe that the combination has the potential to address all patients with NSCLC.  
In the United States alone, the estimated annual incidence of NSCLC is approximately 190,000. 

10

Mocetinostat Background

Histones are protein components of the structural architecture of DNA known as chromatin (chromatin is the material 
that chromosomes are made of, and is comprised of DNA and histone proteins). Local gene expression activity can be controlled 
through epigenetic mechanisms by inducing changes in chromatin conformation through chemical modifications of histones. 
Acetylated histones are associated with a more open configuration of chromatin that is receptive to gene expression signals. In 
contrast, decreases in histone acetylation result in a more compact structure where gene expression is restricted or suppressed. 
Tumor suppressor genes serve to regulate cell growth and cell death, but during oncogenesis these tumor suppressor genes may 
become silenced due to HDAC-dependent decreases in histone acetylation leading to unrestricted growth of tumor cells. HDACs 
are a family of 11 enzymes (the individual HDAC enzymes are referred to as isoforms) that appear to act as a master regulator of 
the expression of genes. HDAC inhibitors modulate inappropriate deacetylation of histones to restore normal acetylation patterns 
as well as tumor suppressor gene expression. Inhibition of HDACs may result in multiple anti-cancer effects such as (1) the 
inhibition of cancer cell proliferation, (2) the induction of apoptosis (cell death) of cancer cells, (3) improved cell cycle regulation,
(4) the induction of tumor suppressor genes, and (5) re-establishing normal histone acetylation activity in cells where mutations 
or alterations may cause a loss of normal function.

We believe that a key differentiating feature of mocetinostat is its spectrum of activity, targeting HDAC isoforms 1, 2, 3 
and 11 which are categorized as Class I (1,2,3) and Class IV (11) HDACs. We believe that these isoforms, and particularly isoforms 
1 and 2, are the most relevant HDAC isoforms in cancer therapy and are also the isoforms most potently inhibited by mocetinostat. 
Compared to other HDAC inhibitors that have a broader spectrum of activity, the profile of mocetinostat may allow us to inhibit 
the targets relevant to cancer more potently and thereby potentially demonstrate improved clinical efficacy and reduced side effects. 
Furthermore,  the  selectivity  of  mocetinostat  for  Class  I  HDACs  and  the  lack  of  activity  against  Class  II  HDACs  may  have 
complimentary effects on tumor cells and the immune system that would enhance the activity of checkpoint inhibitors and potentially 
expand the utility of checkpoint inhibition to the majority of patients with solid tumors who fail to respond to single agent checkpoint 
inhibitor therapy.

Mocetinostat Clinical Development

The first IND for mocetinostat was submitted in December 2003 and became effective in January 2004. Our current focus 
for mocetinostat is on the treatment of patients with NSCLC in combination with durvalumab and we initiated a clinical trial 
evaluating this combination approach in patients with NSCLC in the second quarter of 2016.

To date, we have evaluated mocetinostat as a monotherapy and in combination with other anticancer agents in more than 
400 patients in Phase 1 and Phase 2 clinical trials with various malignancies, including myelodysplastic syndromes ("MDS"), 
hodgkin's lymphoma ("HL"), non-hodgkin's lymphoma ("NHL") including DLBCL or FL, acute myeloid leukemia ("AML"), 
chronic lymphocytic leukemia and chronic myelogenous leukemia, as well as advanced solid tumors. Through these trials, the 
safety and tolerability of mocetinostat as a single agent and in combination has been well characterized. The clinical trials showed 
activity as a single agent in HL and NHL and in combination with azacitidine in MDS and AML. 

We have completed several clinical trials with mocetinostat which enrolled more than 400 patients with a variety of 
advanced malignancies and we completed Phase 2 clinical trials in bladder cancer and NHL. To date we have not seen a level of 
activity or response to single agent mocetinostat that justifies continuing development in those indications. As a result, at the 
present time we do not expect to undertake further clinical trials with mocetinostat as a single agent in bladder cancer, NHL or 
MDS.

Intellectual Property

Patents and Proprietary Technology

Our goal is to obtain, maintain and enforce patent protection wherever appropriate for our product candidates, formulations, 
processes, methods and any other proprietary technologies and operate without infringing on the proprietary rights of other parties, 
both in the United States and in other countries. Our practice is to actively seek to obtain, where appropriate, intellectual property 
protection for our current product candidates and any future product candidates, proprietary information and proprietary technology 
through a combination of patents, protection of proprietary know-how and trade secrets, and contractual arrangements, both in 
the United States and abroad. However, patent protection may not afford us with complete protection against competitors who 
seek to circumvent our patents. We also depend upon the skills, knowledge, experience and know-how of our management and 
research and development personnel as well as that of our advisors, consultants and other contractors. To help protect our proprietary 
know-how that is not patentable, we seek to put in place appropriate internal policies for the management of confidential information, 
and require all of our employees, consultants, advisors and other contractors to enter into confidentiality agreements that prohibit 
11

 
the disclosure of confidential information and which require disclosure and assignment or licensure to us of the ideas, developments, 
discoveries and inventions important to our business.

We typically file for patents in the United States with counterparts in certain countries in Europe and certain key market 
countries in the rest of the world, thereby covering the major pharmaceutical markets. As of December 31, 2016, we own or co-
own U.S. patents and patent applications and their foreign counterparts, including 32 issued U.S. patents as reflected in the following 
table:

Granted and Pending U.S. Patents

Program
Small Molecule Kinase Inhibitors
HDAC
TOTAL

Granted
(United
States)

Pending
(United
States)

15
17
32

—
1
1

Small Molecule Kinase Inhibitors - (15 granted U.S. patents)

As of December 31, 2016, we have fifteen issued patents in the United States covering kinase inhibitor compounds, 
including glesatinib and sitravatinib, and methods of use of these compounds. Of these issued patents, one covers multiple series 
of  kinase  inhibitors  and  protects  glesatinib  generically. Another  issued  patent,  which  expires  no  earlier  than  2026,  protects  a 
selection of compounds including glesatinib, as well as methods of inhibiting VEGF and HGF receptor signaling, and methods 
of treating angiogenesis-mediated cell proliferative disease or inhibiting solid tumor growth. Two issued patents cover processes 
of manufacturing kinase inhibitors such as glesatinib and sitravatinib, and synthetic intermediates required for the production of 
these inhibitors. Exclusivity arising from our issued patents for glesatinib extends to at least 2026, including our patents covering 
the specific composition of matter of glesatinib, and the generic class of compounds to which glesatinib belongs expires 2025, 
prior to legal or regulatory extensions, including any patent term extension, that may be available under the Hatch Waxman Act. 
Another four issued patents cover several distinct classes of kinase inhibitor compounds. Such coverage includes specific claims 
to sitravatinib, generic coverage of the class of compounds to which sitravatinib belongs, as well as patents covering methods of 
use of such compounds. Exclusivity arising from our patent protection for sitravatinib extends to at least 2029, prior to legal or 
regulatory extensions, including any patent term extension that may be available under the Hatch Waxman Act.

HDAC Program - (17 granted U.S. patents; 1 pending U.S. patent application)

Our  patent  estate  for  our  HDAC  program  covers  multiple  series  of  HDAC  inhibitors,  including  mocetinostat. As  of 
December 31, 2016, this group of patents includes 15 issued patents and 1 pending patent applications in the United States protecting 
composition of matter and method of use. Two of the 15 issued patents cover mocetinostat generically and specifically. Exclusivity 
for mocetinostat extends to 2022 prior to legal or regulatory extensions, including any patent term extension that may be available 
under the Hatch Waxman Act.

In aggregate, these U.S. patents and patent applications cover the following inventions: novel HDAC inhibitors, including 
mocetinostat  (eleven  issued  patents  and  one  patent  application),  methods  of  inhibiting  HDACs,  methods  for  treating  cell 
proliferative  disease  or  cancer,  specific  methods  for  treating  colon,  lung  and  pancreatic  cancers,  and  methods  for  treating 
polyglutamine expansion diseases such as Huntington’s disease. Two issued patents claim pharmaceutical compositions comprising 
a specific HDAC inhibitor and methods of use inhibiting HDACs for treating neurodegenerative disorders.

Licensing Agreements

We may enter into license or sub-license agreements when we believe such license is required to pursue a specific program.

Competition

Competitors in Oncology - Small Molecule Kinase Inhibitors

A  large  number  of  kinase  inhibitors  are  currently  in  clinical  trials,  with  many  more  in  the  early  research  stage. 

Biotechnology and pharmaceutical companies are also developing monoclonal antibodies to kinase targets and their ligands.

12

Our  glesatinib  program  is  characterized  by  potential  advantages  including:  a  unique  kinase  spectrum  including  the 
emerging RTK target Axl; potent inhibition of MET driver mutations which are not inhibited by other small molecule inhibitors 
due to a different mode of binding to the MET molecule; a lack of activity against over 300 off-target kinases, supporting a favorable 
safety  profile;  and  excellent  tolerability  to  date  in  combination  with  other  anti-cancer  agents  (including  chemotherapy),  thus 
optimizing the potential for combination therapy approaches.

Companies with MET inhibitors believed to be in late preclinical or clinical development include, but are not limited to: 
AbbVie, Inc., AstraZeneca PLC, Celldex Therapeutics Inc., Eli Lilly, Inc., Exelixis Inc., GlaxoSmithKline PLC, Ignyta, Inc., Incyte 
Corporation, Merck KGaA, NantPharma LLC, Novartis AG, Pfizer Inc.,Sanofi S. A., Sorrento Therapeutics, Inc., and Symphogen 
A/S.

Companies with Axl inhibitors in late preclinical or clinical development include, but are not limited to, Aravive Biologics, 
Inc., Astellas Pharma Inc., BergenBio AS, BioAtla LLC, Exelixis, Inc., Ignyta, Inc., GlaxoSmithKline PLC, Ono Pharmaceutical 
Co. Ltd., Les Laboratoires Servier, and Tolero, Inc.

Companies with RET inhibitors believed to be in late preclinical or clinical development include, but are not limited to, 

Blueprint Medicines, Inc., Ignyta, Inc., and Loxo Oncology, Inc.  

Competitors in Oncology - HDAC

We believe that a key differentiating feature of mocetinostat is its spectrum of activity covering only isoforms 1, 2, 3 and 
11, which are the most relevant HDAC isoforms in human cancers. Other companies that are developing spectrum-selective HDAC 
inhibitors include, but are not limited to, Acetylon Pharmaceuticals, Inc., Chroma Therapeutics Ltd., Huya Bioscience International, 
Shenzen Chipscreen Biosciences Ltd. and Syndax Pharmaceuticals Inc.

Companies with Pan-HDAC inhibitors, which are HDAC inhibitors that have an effect across a broader range of HDAC 
isoforms and are therefore not as selective as molecules like mocetinostat, include but are not limited to: Celgene Corporation, 
Curis Inc., MEI Pharma Inc., Merck & Co Inc., Novartis, Pharmacyclics Inc. and others. We expect that these and other companies 
may continue to pursue research and development in relation to HDAC inhibitors. We continue to monitor these and other companies 
in order to be aware of any third party products and/or intellectual property rights relevant to our products.

Competitors in Oncology - General 

In addition to companies that have HDAC inhibitors or kinase inhibitors addressing our targets of interest, our competition 
also includes hundreds of private and publicly traded companies that operate in the area of oncology but have therapeutics with 
different mechanisms of action. The oncology market in general is highly competitive, with over 1,000 molecules currently in 
clinical  development.  Other  important  competitors,  in  addition  to  those  mentioned  above,  are  small  and  large  biotechnology 
companies,  including,  but  not  limited  to, Amgen,  Inc.  and  Gilead  Sciences  Inc.,  and  specialty  and  regional  pharmaceutical 
companies  and  multinational  pharmaceutical  companies,  including  but  not  limited  to Astellas  Pharma Inc.,  Bayer-Schering 
Pharmaceutical,  Boehringer  Ingelheim  AG,  Bristol-Myers  Squibb,  Eisai Co. Ltd.,  Eli  Lilly  and  Company,  F. Hoffmann-
LaRoche Ltd., GlaxoSmithKline, Johnson & Johnson, Merck KGaA, Novartis AG, Taiho and Takeda Pharmaceutical Co.

Many companies have filed, and continue to file, patent applications which may or could affect our program if and when 
they issue, either because they protect a product that may compete with our product candidates, or because they protect intellectual 
property rights that are necessary for us to develop and commercialize our product candidates. These companies include, but are 
not limited to: Bristol-Myers Squibb, Compugen Limited, Exelixis, GlaxoSmithKline, Novartis and Pfizer. Since this area is 
competitive and of strong interest to pharmaceutical and biotechnology companies, we expect that these and other companies will 
continue to publish and file patent applications in this space in the future, as well as pursuing research and development programs 
in this area. We continue to monitor these and other companies in order to be aware of any third party products and/or intellectual 
property rights relevant to our product candidates.

Manufacturing

We do not own or operate manufacturing facilities for the production of any of our product candidates, nor do we plan 
to develop our own manufacturing operations in the foreseeable future. We currently depend on third-party contract manufacturers 
for all of our required raw materials and finished products for our preclinical and clinical trials.

Manufacturers of our products are required to comply with applicable FDA manufacturing requirements contained in the 
FDA's  Current  Good  Manufacturing  Practices  (“cGMP”)  regulations.  cGMP  regulations  require,  among  other  things,  quality 
13

control  and  quality  assurance  as  well  as  corresponding  maintenance  of  records  and  documentation.  Pharmaceutical  product 
manufacturers and other entities involved in the manufacture and distribution of approved pharmaceutical products are required 
to register their establishments with the FDA and certain state agencies, and are subject to periodic unannounced inspections by 
the FDA and certain state agencies for compliance with cGMP and other laws. Accordingly, manufacturers must continue to expend 
time, money, and effort in the area of production and quality control to maintain cGMP compliance. Discovery of problems with 
a product after approval may result in restrictions on a product, manufacturer or holder of an approved new drug applications 
("NDA"), including withdrawal of the product from the market. In addition, changes to the manufacturing process generally require 
prior FDA approval before being implemented.

Government Regulation

The Regulatory Process for Drug Development

The production and manufacture of our product candidates and our research and development activities are subject to 
regulation by various governmental authorities around the world. In the United States, drug products are subject to regulation by 
the FDA. There are other comparable agencies in Europe and other parts of the world. Regulations govern, among other things, 
the research, development, testing, manufacture, quality control, approval, labeling, packaging, storage, record-keeping, promotion, 
advertising,  distribution,  post-approval  monitoring  and  reporting,  marketing  and  export  and  import  of  products. Applicable 
legislation requires licensing of manufacturing and contract research facilities, carefully controlled research and testing of products, 
governmental review and/or approval of results prior to marketing therapeutic products. Additionally, adherence to good laboratory 
practices (“GLP”) and good clinical practices (“GCP”) during nonclinical and clinical testing and cGMP during production is 
required. 

U.S. Pharmaceutical Product Development Process

In the United States, the FDA regulates pharmaceutical products under the Federal Food, Drug and Cosmetic Act and 
implementing regulations. Pharmaceutical products are also subject to other federal, state and local statutes and regulations. The 
process of obtaining regulatory approvals and the subsequent compliance with appropriate federal, state, local and foreign statutes 
and regulations require the expenditure of substantial time and financial resources. Failure to comply with the applicable U.S. 
requirements at any time during the product development process, approval process or after approval, may subject an applicant 
to administrative or judicial sanctions. FDA sanctions could include refusal to approve pending applications, withdrawal of an 
approval, a clinical hold, warning 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. Any agency or judicial 
enforcement action could have a material adverse effect on us.

The process required by the FDA before a pharmaceutical product may be marketed in the United States generally includes 

the following:

• 

• 

• 

• 

• 

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

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

performance of adequate and well-controlled human clinical trials in accordance with GCP standards and regulations 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 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; and 

• 

FDA review and approval of the NDA.

The FDA monitors the progress of trials conducted in the U.S. under an IND and may, at its discretion, re-evaluate, alter, 
suspend or terminate testing based on the data accumulated to that point and the FDA’s risk/benefit assessment with regard to the 
patients enrolled in the trial. The FDA may also place a hold on one or more clinical trials conducted under an IND for a drug if 
deems warranted. Furthermore, even after regulatory approval of an NDA is obtained, under certain circumstances, such as later 
discovery of previously unknown problems, the FDA can withdraw approval or subject the drug to additional restrictions.

14

Preclinical Studies:   Preclinical studies include laboratory evaluations of product chemistry, toxicity and formulation, 
as well as animal studies to evaluate efficacy and activity, toxic effects, pharmacokinetics and metabolism of the pharmaceutical 
product candidate and to provide evidence of the safety, bioavailability and activity of the pharmaceutical product candidate in 
animals. Most of these studies must be performed according to GLP.

Clinical Trials:    Clinical trials involve the administration of the pharmaceutical product candidate to healthy volunteers 
or patients under the supervision of qualified investigators, generally physicians not employed by the sponsor. Clinical trials must 
be conducted in accordance with the FDA's GCP requirements. Further, each clinical trial must be reviewed and approved by an 
independent institutional review board (“IRB”), or ethics committee at or servicing each institution at which the clinical trial will 
be conducted. An IRB or ethics committee is charged with protecting the welfare and rights of trial participants and considers 
such items as whether the risks to individuals participating in the clinical trials are minimized and are reasonable in relation to 
anticipated benefits. The IRB or ethics committee also approves the informed consent form that must be provided to each clinical 
trial subject or his or her legal representative and must monitor the clinical trial until completed.

Clinical trials in the U.S. typically are conducted in sequential phases: Phases 1, 2, 3 and post-approval clinical trials, 
sometimes referred to as Phase 4 clinical trials. The phases may overlap. The FDA may require that we suspend clinical trials at 
any time on various grounds.

Phase 1 Clinical Trials:    Phase 1 clinical trials are generally conducted on a small number of healthy human subjects 
to evaluate the drug's activity, schedule and dose, absorption, metabolism, distribution, excretion and other drug effects. However, 
in the case of life-threatening diseases, such as cancer, the initial Phase 1 testing may be done in patients with the disease. These 
trials typically take longer to complete and may provide insights into drug activity. Follow-on Phase 1b clinical trials may also 
evaluate efficacy with respect to trial participants.

Phase 2 Clinical Trials:    Phase 2 clinical trials are carried out on a relatively small number of patients (generally up to 
several hundred) in a specific indication. The pharmaceutical product is evaluated to preliminarily assess efficacy, to identify 
possible adverse effects and safety risks, and to determine optimal dose, regimens, pharmacokinetics, pharmacodynamics and 
dose response relationships. Multiple Phase 2 clinical trials may be conducted to obtain information prior to beginning Phase 3 
clinical trials.

Phase 3 Clinical Trials:    Phase 3 clinical trials involve tests on a much larger population of patients (several hundred 
to several thousand patients) suffering from the targeted condition or disease. These trials are undertaken to confirm proof of 
concept  and further evaluate dosage, clinical efficacy and safety and are intended to establish the overall risk/benefit ratio of the 
product and provide an adequate basis for product labeling. Generally, two adequate and well-controlled Phase 3 clinical trials 
are required by the FDA for approval of an NDA or foreign authorities for approval of marketing applications.

Post-Approval Clinical Trials:    Phase 4 clinical trials or other post-approval commitments may be conducted after initial 
marketing approval. These studies are used to gain additional experience from the treatment of patients in the intended therapeutic 
indication and may be required by the FDA as a condition of approval.  Additional studies and follow-up may be conducted to 
document a clinical benefit where drugs are approved under accelerated approval regulations and based on surrogate endpoints. 
In clinical trials, surrogate endpoints are alternative measurements of the symptoms of a disease or condition that are substituted 
for measurements of observable clinical symptoms. Failure to timely conduct of Phase 4 clinical trials and follow-up could result 
in withdrawal of approval for products approved under accelerated approval regulations.

Progress reports detailing the results of the clinical trial must be submitted at least annually to the FDA, and written IND 
safety reports must be submitted to the FDA and the investigators for serious and unexpected adverse events or for any finding 
from tests in laboratory animals that suggests a significant risk for human subjects. Phase 1, Phase 2 and Phase 3 clinical trials 
may not be completed successfully within any specified period, if at all. The FDA or the sponsor or, if used, its data safety and 
monitoring board may suspend a clinical trial at any time on various grounds, including a finding that the research subjects or 
patients are being exposed to an unacceptable health risk. Similarly, an IRB or ethics committee 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 or ethics committee's 
requirements or if the pharmaceutical product has been associated with unexpected serious harm to patients.

Concurrent with clinical trials, companies usually complete additional animal studies and must also develop additional 
information  about  the  chemistry  and  physical  characteristics  of  the  pharmaceutical  product,  as  well  as  finalize  a  process  for 
manufacturing the product in commercial quantities in accordance with GMP requirements. The manufacturing process must be 
capable of consistently producing quality batches of the pharmaceutical product candidate and, among other things, must develop 
methods for testing the identity, strength, quality and purity of the final pharmaceutical product. Additionally, appropriate packaging 
15

must be selected and tested and stability studies must be conducted to demonstrate that the pharmaceutical product candidate does 
not undergo unacceptable deterioration over its shelf life.

U.S. Pharmaceutical Review and Approval Process

Upon completion of pivotal Phase 3 clinical studies, the sponsor assembles all the product development, preclinical and 
clinical data along with descriptions of the manufacturing process, analytical tests conducted on the chemistry of the pharmaceutical 
product, proposed labeling and other relevant information, and submits it to the FDA as part of an NDA. If accepted by the FDA 
as substantially complete to permit substantive review, the submission or application is then reviewed for approval to market the 
product. This process takes eight months to one year to complete, but in some cases may take longer. At the end of the review 
period the FDA may issue a Complete Response Letter, refusing to approve an NDA if the applicable regulatory criteria are not 
satisfied or requiring additional clinical data or other data and information. Even if such data and information is submitted, the 
FDA may ultimately decide that the NDA does not satisfy the criteria for approval. If a product receives regulatory approval, the 
approval may be significantly limited to specific diseases and dosages or the indications for use may otherwise be limited, which 
could  restrict  the  commercial  value  of  the  product.  Further,  the  FDA  may  require  that  certain  contraindications,  warnings  or 
precautions be included in the product labeling.

Accelerated Approval

Accelerated Approval is a program that is intended to make promising products for life threatening diseases available on 
the basis of evidence of effect on a surrogate endpoint that is reasonably likely to predict clinical benefit, taking into account the 
severity, rarity or prevalence of the condition and the availability or lack of alternative treatments. Approvals of this kind typically 
include requirements for appropriate post-approval Phase 4 clinical trials to validate the surrogate endpoint or otherwise confirm 
the effect of the clinical endpoint. 

Post-Approval Requirements

Any pharmaceutical products for which we receive FDA approvals are subject to continuing regulation by the FDA, 
including, among other things, record-keeping requirements, reporting of adverse experiences with the product, providing the 
FDA  with  updated  safety  and  efficacy  information,  product  sampling  and  distribution  requirements,  complying  with  certain 
electronic records and signature requirements and complying with FDA promotion and advertising requirements, which include, 
among others, standards for direct-to-consumer advertising, promoting pharmaceutical products for uses or in patient populations 
that are not described in the pharmaceutical product's approved labeling (known as "off-label use"), industry-sponsored scientific 
and educational activities and promotional activities involving the internet. Failure to comply with FDA requirements can have 
negative  consequences,  including  adverse  publicity,  enforcement  letters  from  the  FDA,  mandated  corrective  advertising  or 
communications with doctors and civil or criminal penalties.

The FDA also may require post-marketing testing, known as Phase 4 testing, risk evaluation and mitigation strategies 
and surveillance to monitor the effects of an approved product or place conditions on an approval that could restrict the distribution 
or use of the product.

FDA Regulation of Companion Diagnostics

As part of our clinical development plans, we are exploring the use of companion diagnostics to identify patients most 
likely to respond to our product candidates. Companion diagnostics are classified as medical devices under the Federal Food, 
Drug, and Cosmetic Act in the United States. In the United States, the FDA regulates the medical device design and development, 
preclinical and clinical testing, premarket clearance or approval, registration and listing, manufacturing, labeling, storage, reporting, 
recordkeeping, advertising and promotion, export and import, sales and distribution, and post-market surveillance of medical 
devices. Unless an exemption applies, companion diagnostics require marketing clearance or approval from the FDA prior to 
commercial distribution. The two primary types of FDA marketing authorization applicable to a medical device are premarket 
notification, also called 510(k) clearance, and premarket approval ("PMA"). 

The FDA previously has required in vitro companion diagnostics intended to select the patients who will respond to the 
cancer treatment to obtain a PMA simultaneously with approval of the drug. Based on the draft guidance, and the FDA's past 
treatment of companion diagnostics, we believe that the FDA will require a PMA for one or more companion diagnostics to identify 
patient populations suitable for our product candidates. The review of these companion diagnostics in conjunction with the review 
of our product candidates involves coordination of review by the FDA's Center for Drug Evaluation and Research and by the 
FDA's Center for Devices and Radiological Health.

16

Pharmaceutical Coverage, Pricing and Reimbursement

In the United States and markets in other countries, sales of any products for which we receive regulatory approval for 
commercial sale will depend in part on the availability of coverage and adequate reimbursement from third-party payors, including 
government authorities, managed care providers, private health insurers and other organizations. In the United States, private 
health insurers and other third-party payors often provide reimbursement for products and services based on the level at which 
the government (through the Medicare or Medicaid programs) provides reimbursement for such products and services. Third-
party payors are increasingly examining the medical necessity and cost-effectiveness of medical products and services in addition 
to their safety and efficacy and, accordingly, significant uncertainty exists as to the coverage and reimbursement status of newly 
approved therapeutics. In particular, in the United States, the European Union 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 
medical products and services, particularly for new and innovative products and therapies, which often has resulted in average 
selling prices that are 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 European Union will put additional pressure on 
product pricing, reimbursement and utilization, which may adversely affect our future product sales and results of operations. 
These pressures can arise from rules and practices of managed care groups, judicial decisions and governmental laws and regulations 
related to Medicare, Medicaid and healthcare reform, pharmaceutical reimbursement policies and pricing in general. As a result, 
coverage and adequate third-party reimbursement may not be available for our product candidates to enable us realize an appropriate 
return on our investment in research and product development.

The market for our product candidates for which we may receive regulatory approval will depend significantly on access 
to third-party payors' drug formularies, or lists of medications for which third-party payors provide coverage and reimbursement. 
The  industry  competition  to  be  included  in  such  formularies  often  leads  to  downward  pricing  pressures  on  pharmaceutical 
companies. Also, third-party payors may refuse to include a particular branded drug in their formularies or may otherwise restrict 
patient access to a branded drug when a less costly generic equivalent or other alternative is available. In addition, because each 
third-party payor individually approves coverage and reimbursement levels, obtaining coverage and adequate reimbursement is 
a time-consuming and costly process. We would be required to provide scientific and clinical support for the use of any product 
to each third-party payor separately with no assurance that approval would be obtained, and we may need to conduct expensive 
pharmacoeconomic studies in order to demonstrate the cost-effectiveness of our products. This process could delay the market 
acceptance of any of our product candidates for which we may receive approval and could have a negative effect on our future 
revenue and operating results. We cannot be certain that our product candidates will be considered cost-effective. If we are unable 
to obtain coverage and adequate payment levels for our product candidates from third-party payors, physicians may limit how 
much or under what circumstances they will prescribe or administer them and patients may decline to purchase them. This in turn 
could affect our ability to successfully commercialize our products and impact our profitability, results of operations, financial 
condition, and future success.

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 products. Whether or not we obtain FDA approval for a product, 
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 product 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.

Other Healthcare Laws and Compliance Requirements

Several other types of state and federal laws restrict certain marketing practices in the pharmaceutical industry. These 
laws, which generally will not be applicable to us or our product candidates unless and until we obtain FDA marketing approval 
for any of our product candidates, include state and federal anti-kickback, fraud and abuse, false claims, physician payment, 
sunshine, patient protection and affordable care, privacy and security laws and regulations regarding providing drug samples. 

We may in the future be subject to the Foreign Corrupt Practices Act of 1997 (“FCPA”). The FCPA and other similar 
anti-bribery laws in other jurisdictions, such as the U.K. Bribery Act, generally prohibit companies and their intermediaries from 
providing money or anything of value to officials of foreign governments, foreign political parties, or international organizations 
with the intent to obtain or retain business or seek a business advantage. A determination that our operations or activities are not, 

17

 
 
or were not, in compliance with United States or foreign laws or regulations could result in the imposition of substantial fines, 
interruptions of business, loss of supplier, vendor or other third-party relationships, termination of necessary licenses and permits 
and other legal or equitable sanctions. 

Other Laws 

In addition to the above, we are subject to a variety of financial disclosure and securities trading regulations as a public 
company in the U.S., including laws relating to the oversight activities of the SEC and the regulations of The NASDAQ Stock 
Exchange, on which our shares are traded. We are also subject to various laws, regulations and recommendations relating to safe 
working conditions, laboratory practices and the experimental use of animals.

Employees

As of December 31, 2016, we had 52 employees located in our offices in San Diego. We also utilize the services of 
consultants  on  a  regular  basis.  32  employees  are  engaged  in  research  and  development  activities  and  20  are  in  general  and 
administrative functions. 

Corporate Information

We were incorporated under the laws of the State of Delaware on April 29, 2013 as Mirati Therapeutics, Inc.  Our website 
address is www.mirati.com. Our website and the information contained on, or that can be accessed through, the website will not 
be deemed to be incorporated by reference in, and are not considered part of, this Annual Report on Form 
Our Annual 
Reports on Form 
and amendments to reports filed or 
furnished pursuant to Section 13(a) and 15(d) of the Securities Exchange Act of 1934, as amended, are available free of charge 
on the Investors portion of our web site at www.mirati.com as soon as reasonably practical after we electronically file such material 
with, or furnish it to, the Securities and Exchange Commission ("SEC").

Quarterly Reports on Form 

Current Reports on Form 

Executive Officers and Directors

The following table sets forth information about our executive officers, directors and key employee as of December 31, 2016.

Name
Charles M. Baum, M.D., Ph.D.
Isan Chen, M.D.
Chris LeMasters
James Christensen, Ph.D.
Jamie A. Donadio
Rodney W. Lappe, Ph.D.(3)
Michael Grey(1)(3)
Henry J. Fuchs, M.D.(2)(3)
Craig Johnson(1)(2)
Bruce L.A. Carter, Ph.D.(1)(2)

Age
58
54
50
48
41
62
64
59
55
73

Position
President and Chief Executive Officer, Director
Executive Vice President and Chief Medical and Development Officer
Executive Vice President and Chief Business Officer
Senior Vice President and Chief Scientific Officer
Senior Vice President and Chief Financial Officer
Chairman of the Board
Director
Director
Director
Director

_____________________________________________

(1)  Member of the Audit Committee.
(2)  Member of the Compensation Committee.
(3)  Member of the Nominating and Corporate Governance Committee.

18

Executive Officers

Charles M. Baum, M.D., Ph.D. has served as our President and Chief Executive Officer and member of our Board of 
Directors since November 2012. From June 2003 to September 2012, he was at Pfizer as Senior Vice President for Biotherapeutic 
Clinical Research within Pfizer's Worldwide Research & Development division and as Vice President and Head of Oncology 
Development  and  Chief  Medical  Officer  for  Pfizer's  Biotherapeutics  and  Bioinnovation  Center.  From  2000  to  2003,  he  was 
responsible for the development of several oncology compounds at Schering-Plough Corporation (acquired by Merck). His career 
has included academic and hospital positions at Stanford University and Emory University, as well as positions of increasing 
responsibility within the pharmaceutical industry at SyStemix, Inc. (acquired by Novartis AG), G.D. Searle & Company (acquired 
by Pfizer), Schering-Plough Corporation (acquired by Merck) and Pfizer. Dr. Baum currently serves on the board of directors of 
Array BioPharma.  Dr. Baum received his M.D. and Ph.D. (Immunology) degrees from Washington University School of Medicine 
in St. Louis, Missouri and completed his post-doctoral training at Stanford University. 

Dr. Baum's experience in the pharmaceutical industry provides our Board of Directors with subject matter expertise. In 
addition, through his position as President and Chief Executive Officer of the Company and Chief Medical Officer for Pfizer's 
Biotherapeutics and Bioinnovation Center, Dr. Baum has acquired the operational expertise, which we believe qualifies him to 
serve on our Board of Directors.

Isan Chen, M.D. has served as our Executive Vice President and Chief Medical and Development Officer since September 
2013. Dr. Chen is board certified in Internal medicine, hematology and medical oncology with more than 15 years of experience 
in oncology and clinical trials from first-in-humans through global registrational studies. He has experience in oncology clinical 
development and interactions with regulatory agencies in the United States and Europe. He was most recently the Chief Medical 
Officer of Aragon Pharmaceuticals, which was acquired by Johnson & Johnson in July of 2013. At Aragon Pharmaceuticals, 
Dr. Chen was responsible for the clinical development strategy of all the company's programs, including prostate and breast cancer. 
Prior to Aragon Pharmaceuticals, Dr. Chen served as Vice President of tumor strategy in the oncology business unit at Pfizer. In 
addition he was the clinical lead for Sutent, a multiple kinase inhibitor, for the treatment of RCC, an indication in which the drug 
secured FDA approval in 2006. He was also the clinical lead for the Phase 1 studies of crizotinib and CDK 4/6 inhibitor palbociclib. 
Dr. Chen completed his hematology/oncology fellowship at University of California, San Diego. Before joining Pfizer, Dr. Chen 
practiced medicine as a staff physician at City of Hope Medical Center and later as an assistant professor at the University of 
Texas, M.D. Anderson Cancer Center.

James Christensen, Ph.D. has served as our Senior Vice President, and Chief Scientific Officer since January 2014 and 
served as our Vice President, Research from June 2013 through January 2014. Prior to joining us, he held various positions at 
Pfizer from 2003 to 2013, the most recent of which was Senior Director of Oncology Precision Medicine in the Oncology Research 
Unit. Dr. Christensen joined Pfizer in 2003 and his responsibilities there included leading nonclinical research efforts for oncology 
programs including sunitinib malate research activities and leading the nonclinical and translational biology efforts for other 
research and development programs including crizotinib. Dr. Christensen participated as a member of the Cancer Research or 
Oncology Research Unit leadership team from 2005 to 2013. Prior to 2003, Dr. Christensen was a Group Leader on the Preclinical 
Research and Exploratory Development team at SUGEN, Inc., which was acquired by Pharmacia Corporation, now owned by 
Pfizer. Dr. Christensen began his career in 1998 at Warner Lambert, now owned by Pfizer, with research focus in RTK biology 
and RTK pathway biomarker development in the oncology therapeutic area. Dr. Christensen participates on the editorial boards 
for Cancer Research and Molecular Cancer Therapeutics. Dr. Christensen received a Ph.D. in molecular pharmacology from North 
Carolina State University with dissertation research directed toward characterization of mechanisms of apoptosis dysregulation 
during the process of carcinogenesis.

Jamie A. Donadio has served as our Senior Vice President, Finance and Chief Financial Officer since March 2016 and 
Vice President, Finance from March 2013 through March 2016. Prior to joining us, Mr. Donadio was at Amylin Pharmaceuticals 
from April 2001 through January 2013. From November 2011 to January 2013, Mr. Donadio served as Senior Director of Finance 
at Amylin. From December 2010 to November 2011, he served as Director of Corporate Financial Planning and Analysis at Amylin. 
From March 2007 to December 2010 he served as Director of SEC Reporting and from April 2001 to March 2007 he held various 
corporate  accounting  roles  at Amylin.  From  December  2000  to April  2001,  Mr. Donadio  was  senior  accountant  at  Novatel 
Wireless, Inc. From August 1997 to December 2000, Mr. Donadio was with Ernst & Young LLP, last serving as an audit senior. 
Mr. Donadio  holds  a  B.S.  in Accounting  from  Babson  College  and  is  a  certified  public  accountant  (inactive)  in  the  State  of 
California.

Chris LeMasters has served as our Executive Vice President and Chief Business Officer since September 2016. Prior to 
joining Mirati, Mr. LeMasters served as the Chief Executive Officer of Promosome, a privately held biotherapeutics and biosimilars 
company  from  August  2015  to  September  2016. Previously,  Mr.  LeMasters  held  senior  management  positions  at  several 
biotherapeutics companies, most recently as co-founder and chief business officer of Tragara Pharmaceuticals, a clinical-stage 
19

 
 
 
 
 
 
cancer therapeutics company, a position he held from January 2007 to August 2015. Mr. LeMasters also served as Co-Founder 
and Chief Business Officer of Cabrellis Pharmaceuticals, Inc. from May 2006 to December 2007, where he negotiated its acquisition 
by Pharmion Corporation for $104 million, and as Vice President, Corporate Development of Conforma Therapeutics from April 
2004 to May 2006, where he negotiated its acquisition by Biogen IDEC for $250 million. From July 1998 to April 2004, Mr. 
LeMasters worked in the Corporate Business Development group at Eli Lilly & Company and was responsible for the successful 
negotiation of numerous partnerships and licenses across a range of therapeutic areas. Earlier in his career, he was a management 
consultant with Coopers & Lybrand Consulting and an operational auditor with Owens Corning. Mr. LeMasters currently serves 
as a board member of Aarden Pharmaceuticals, where he is also a co-founder, and as a board member of the Hoosier Cancer 
Research Network, a clinical research organization and as a board member of Promosome.

Non-Employee Directors

Henry J. Fuchs, M.D. has served as a member of our Board of Directors since February 2012. Dr. Fuchs has served as 
the President of Worldwide Research & Development at BioMarin Pharmaceutical Inc since September 2016 and as the Executive 
Vice President and Chief Medical Officer from March 2009 to August 2016. From September 2005 to December 2008, Dr. Fuchs 
was Executive Vice President and Chief Medical Officer of Onyx Pharmaceuticals, Inc. From 1996 to 2005, Dr. Fuchs served in 
multiple roles of increasing responsibility at Ardea Biosciences, Inc., first as Vice President, Clinical Affairs, then as President 
and Chief Operating Officer, and finally as Chief Executive Officer. From 1987 to 1996, Dr. Fuchs held various positions at 
Genentech Inc. Dr. Fuchs serves on the Board of Directors of Genomics Health, Inc. and was on the Board of Directors of Ardea 
Biosciences, Inc. from 1996 until its acquisition by AstraZeneca PLC in 2012. Dr. Fuchs received a B.A. in Biochemical Sciences 
from Harvard University, and an M.D. from George Washington University. 

We believe that Dr. Fuchs' experience as an executive and his breadth of knowledge and valuable understanding of the 

pharmaceutical industry qualify him to serve on our Board of Directors.

Michael Grey has served as a member of our Board of Directors since November 2014. Mr. Grey currently serves as 
Executive Chairman of Amplyx Pharmaceuticals as well as Chief Executive Officer and Chairman of Reneo Pharmaceuticals. Mr. 
Grey also serves as a Venture Partner with Pappas Ventures, a life sciences venture capital firm, since January 2010. He recently 
served as President and Chief Executive Officer of Lumena Pharmaceuticals, Inc., a privately-held biotechnology company before 
it was acquired by Shire. Between January and September 2009, he served as President and Chief Executive Officer of Auspex 
Pharmaceuticals, Inc., a private biotechnology company. From January 2005 until its acquisition in August 2008, Mr. Grey was 
President and Chief Executive Officer of SGX Pharmaceuticals, Inc., a public biotechnology company, where he previously served 
as President from June 2003 to January 2005 and as Chief Business Officer from April 2001 until June 2003. Prior to joining SGX 
Pharmaceuticals, Inc., Mr. Grey acted as President, Chief Executive Officer and Board member of Trega Biosciences, Inc., a 
biotechnology company. From November 1994 to August 1998, Mr. Grey was the President of BioChem Therapeutic, Inc., the 
pharmaceutical operating division of BioChem Pharma, Inc. During 1994, Mr. Grey served as President and Chief Operating 
Officer for Ansan, Inc., a pharmaceutical company. From 1974 to 1993, he served in various roles with Glaxo, Inc. and Glaxo 
Holdings, plc, culminating in the position of Vice President, Corporate Development. Mr. Grey is currently a director of BioMarin 
Pharmaceutical, Inc. and Horizon Pharma, plc, public pharmaceutical companies and Balance Therapeutics, Inc. and Biothera 
Pharmaceutical, Inc., privately held healthcare companies. Mr. Grey previously served on the board of directors of two public 
companies during the past five years: IDM Pharma, Inc. from 1999 to 2009 and Achillion Pharmaceuticals, Inc. from 2001 to 
2010. He received a B.Sc. in chemistry from the University of Nottingham, United Kingdom.

We believe that based on Mr. Grey's experience as an executive in the biopharmaceutical industry and his breadth of 

knowledge and valuable understanding of the pharmaceutical industry qualify him to serve on our Board of Directors.

Craig Johnson has served as a member of our Board of Directors since September 2013. Mr. Johnson serves on the boards 
of directors for several life science companies.  He is currently a director for Heron Therapeutics, Inc., a NASDAQ-listed specialty 
pharmaceutical company, a position he has held since January 2014, as well as for La Jolla Pharmaceutical Company, a NASDAQ-
listed biopharmaceutical company, a position he has held since October 2013. Mr. Johnson also serves as a director of GenomeDx 
Biosciences, a privately held biotechnology company, a position he has held since October 2015. Mr. Johnson also served as a 
past director of Adamis Pharmaceuticals Corporation, a NASDAQ-listed biopharmaceutical company, from 2011 to 2014, as well 
as Ardea Biosciences, Inc., a NASDAQ-listed biotechnology company, from 2008 until its sale to AstraZeneca PLC in June 2012. 
From 2011 to 2012 he was Chief Financial Officer of PURE Bioscience, Inc., and from 2010 to 2011 he was Senior Vice President 
and  Chief  Financial  Officer  of  NovaDel  Pharma  Inc.  Mr.  Johnson  served  as  Vice  President  and  Chief  Financial  Officer  of 
TorreyPines Therapeutics, Inc. from 2004 until its sale to Raptor Pharmaceuticals Corp. in 2009, and then as Vice President of a 
wholly-owned subsidiary of Raptor Pharmaceutical Corp. from 2009 to 2010. He held several positions, including Chief Financial 
Officer and Senior Vice President of Operations, at MitoKor, Inc. from 1994 to 2004. Prior to 1994, Mr. Johnson held senior 

20

 
 
 
 
 
financial positions with several early-stage technology companies, and also practiced as a Certified Public Accountant with Price 
Waterhouse. Mr. Johnson received his B.B.A. in accounting from the University of Michigan-Dearborn.

We believe Mr. Johnson's leadership and experience and skills in accounting and finance qualify him to serve on our 

Board of Directors.

Rodney Lappe, Ph.D. has served as a member of our Board of Directors since June 2012 and as Chairman of the Board 
since July 2013. Since January 2012, Dr. Lappe has served as the Senior Vice President of Tavistock Life Sciences, a private 
investment firm. From January 2004 to December 2011, Dr. Lappe was Group Senior Vice President, Pfizer Worldwide Research 
and Development and Chief Scientific Officer for CovX in San Diego, California. Dr. Lappe joined Pfizer with the CovX acquisition 
in 2008. From 2000 to 2002, Dr. Lappe served as Vice President for cardiovascular and metabolic diseases at Pharmacia. He was 
also site leader for Pharmacia in St. Louis. Prior to joining Pharmacia, he held positions of increasing responsibility with Wyeth, 
Rorer Central Research, CIBA Geigy and Searle Pharmaceuticals. Dr. Lappe received his B.A. from Blackburn College and his 
Ph.D. in Pharmacology from Indiana University.

We believe Dr. Lappe's extensive experience managing pharmaceutical and biotech companies bring important strategic 

insight and qualifies him to serve on our Board of Directors.

Bruce L.A. Carter, Ph.D. has served as a member of our Board of Directors since September 2016. Dr. Carter currently 
serves as a director of Dr. Reddy’s Laboratories Limited, Enanta Pharmaceuticals, Inc. and Xencor, Inc. Dr. Carter is an affiliate 
Professor in the Department of Biotechnology at the University of Washington, Seattle Washington, a position he has held since 
1986. Dr. Carter served on the board for QLT, Inc. from 2006 to 2012. Dr. Carter served as Executive Chairman of Immune Design 
Corp. a privately-held biotechnology company from 2009 to 2011, and he served as a director from 2000 to 2009. From 1998 to 
2009, Dr. Carter served as President and Chief Executive Officer of  ZymoGenetics, Inc., a publicly-held biotechnology company, 
and as its Chairman of the Board from 2005 until it was acquired by Bristol-Myers Squibb in October 2010. From 1994 to 1998 
Dr. Carter was the Chief Scientific Officer of Novo Nordisk, a publicly-held pharmaceutical company. Previously, he held positions 
in research at Zymogenetics and G.D. Searle & Co. Ltd. Dr. Carter received a B.Sc. with Honors in Botany from the University 
of Nottingham, England, and a Ph.D. in Microbiology from Queen Elizabeth College, University of London.

We believe that Dr. Carter's experience as an executive and his breadth of knowledge and valuable understanding of the 

pharmaceutical industry qualify him to serve on our Board of Directors.

21

 
 
 
 
 
Item 1A.     Risk Factors

RISK FACTORS

Except for the historical information contained herein, this annual report on Form 10-K and the information incorporated 
by reference herein contains forward-looking statements that involve risks and uncertainties. These statements include projections 
about our accounting and finances, plans and objectives for the future, future operating and economic performance and other 
statements regarding future performance. These statements are not guarantees of future performance or events. Our actual results 
may differ materially from those discussed here. Factors that could cause or contribute to such differences are described in the 
following  section  as  well  as  those  discussed  in  Part II,  Item 7  entitled  "Management's  Discussion  and Analysis  of  Financial 
Condition and Results of Operations," and elsewhere throughout this report and in any other documents incorporated by reference 
herein. There may be additional risks that we do not presently know of or that we currently believe are immaterial which could 
also impair our business and financial position. We disclaim any obligation to update any forward-looking statement.

Risks Relating to Our Financial Position and Capital Requirements

We will require additional financing and may be unable to raise sufficient capital, which could lead us to delay, reduce 

or abandon development programs or commercialization.

Our operations have consumed substantial amounts of cash since inception. Our research and development expenses 
were $68.5 million, $49.0 million, and $26.1 million for the years ended December 31, 2016, 2015 and 2014, respectively. In 2015 
we completed two public offerings of our common stock that generated net proceeds of $143.3 million and in January 2017 we 
completed a public offering of our common stock and pre-funded common stock warrants that generated net proceeds of $66.8 
million. We will require substantial additional capital to pursue additional clinical development for our lead clinical programs, 
including  conducting  late-stage  clinical  trials,  manufacturing  clinical  supplies  and  potentially  developing  other  assets  in  our 
pipeline, and, if we are successful, to commercialize any of our current product candidates. If the U.S. Food and Drug Administration 
("FDA") or any foreign regulatory agency, such as the European Medicines Agency ("EMA") requires that we perform studies or 
trials in addition to those that we currently anticipate with respect to the development of our product candidates, or repeat studies 
or trials, our expenses would further increase beyond what we currently expect. Any delay resulting from such further or repeat 
studies or trials could also result in the need for additional financing. We may not be able to adequately finance our development 
programs, which could limit our ability to move our programs forward in a timely and satisfactory manner or require us to abandon 
the programs, any of which would harm our business, financial condition and results of operations. Because successful development 
of  our  product  candidates  is  uncertain,  we  are  unable  to  estimate  the  actual  funds  we  will  require  to  complete  research  and 
development and commercialize our product candidates.

If we are unable to obtain funding from equity offerings or debt financings on a timely basis, we may be required to 
(1) seek collaborators for one or more of our product candidates at an earlier stage than otherwise would be desirable or on terms 
that are less favorable than might otherwise be available; (2) relinquish or license on unfavorable terms our rights to technologies 
or product candidates that we otherwise would seek to develop or commercialize ourselves; or (3) significantly curtail one or more 
of our research or development programs or cease operations altogether.

We are a clinical-stage company with no approved products and no historical product revenue. Consequently, we 

expect that our financial and operating results will vary significantly from period to period.

We are a clinical-stage company that has incurred losses since its inception and expect to continue to incur substantial 
losses  in  the  foreseeable  future.  Biopharmaceutical  product  development  is  a  highly  speculative  undertaking  and  involves  a 
substantial degree of uncertainty.

Our actual financial condition and operating results have varied significantly in the past and are expected to continue to 
fluctuate significantly from quarter-to-quarter or year-to-year due to a variety of factors, many of which are beyond our control. 
Factors relating to our business that may contribute to these fluctuations include:

• 

• 

• 

• 

the success of our clinical trials through all phases of clinical development;

delays in the commencement, enrollment and timing of clinical trials;

our  ability  to  secure  and  maintain  collaborations,  licensing  or  other  arrangements  for  the  future  development  and/or 
commercialization of our product candidates, as well as the terms of those arrangements;

our ability to obtain, as well as the timeliness of obtaining, additional funding to develop our product candidates;

22

 
 
 
 
 
• 

• 

• 

• 

• 

• 

• 

• 

• 

• 

• 

• 

• 

the results of clinical trials or marketing applications for product candidates that may compete with our product candidates;

competition from existing products or new products that may receive marketing approval;

potential side effects of our product candidates that could delay or prevent approval or cause an approved drug to be taken 
off the market;

any delays in regulatory review and approval of our clinical development plans or product candidates;

our ability to identify and develop additional product candidates;

the ability of patients or healthcare providers to obtain coverage or sufficient reimbursement for our products;

our ability, and the ability of third parties such as Clinical Research Organizations ("CROs") to adhere to clinical study 
and other regulatory requirements;

the ability of third-party manufacturers to manufacture our product candidates and key ingredients needed to conduct 
clinical trials and, if approved, successfully commercialize our products;

the costs to us, and our ability as well as the ability of any third-party collaborators, to obtain, maintain and protect our 
intellectual property rights;

costs related to and outcomes of potential intellectual property litigation;

our ability to adequately support future growth;

our ability to attract and retain key personnel to manage our business effectively; and

our ability to build our finance infrastructure and, to the extent required, improve our accounting systems and controls.

Accordingly, the likelihood of our success must be evaluated in light of many potential challenges and variables associated 
with a clinical-stage company, many of which are outside of our control, and past operating or financial results should not be relied 
on as an indication of future results. Fluctuations in our operating and financial results could cause our share price to decline. It 
is possible that in some future periods, our operating results will be above or below the expectations of securities analysts or 
investors, which could also cause our share price to decline.

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

for the foreseeable future. We have never generated any revenue from product sales and may never be profitable.

We have derived limited revenue from our research and licensing agreements which has not been sufficient to cover the 
substantial expenses we have incurred in our efforts to develop our product candidates. Consequently, we have accumulated net 
losses since inception in 1995. Our net loss for the years ended December 31, 2016, 2015, and 2014 were $83.1 million, $64.5 
million, and $43.7 million respectively. As of December 31, 2016, we had an accumulated deficit of $389.8 million. Our prior 
losses, combined with expected future losses, have had and will continue to have an adverse effect on our stockholders' equity 
and working capital. Such losses are expected to increase in the future as we continue the development of our product candidates 
and seek regulatory approval and commercialization for our product candidates. We are unable to predict the extent of any future 
losses or when we will become profitable, if ever. Even if we do achieve profitability, we may not be able to sustain or increase 
profitability on an ongoing basis.

We do not anticipate generating revenue from sales of products for the foreseeable future, if ever. If any of our product 
candidates fail in clinical trials or do not gain regulatory approval, or if any of our product candidates, if approved, fail to achieve 
market acceptance, we may never become profitable. If one or more of our product candidates is approved for commercial sale 
and we retain commercial rights, we anticipate incurring significant costs associated with commercializing any such approved 
product candidate. Therefore, even if we are able to generate revenue from the sale of any approved product, we may never become 
profitable. Even if we achieve profitability in the future, we may not be able to sustain profitability in subsequent periods. Our 
ability to generate future revenue from product sales depends heavily on our success in:

• 

completing development and clinical trial programs for our product candidates;

23

 
 
• 

• 

• 

• 

• 

entering into collaboration and license agreements;

seeking and obtaining marketing approvals for any product candidates that successfully complete clinical trials;

establishing and maintaining supply and manufacturing relationships with third parties;

successfully commercializing any product candidates for which marketing approval is obtained; and

successfully establishing a sales force and marketing and distribution infrastructure.

Raising  additional  funds  through  debt  or  equity  financing  will  be  dilutive  and  raising  funds  through  licensing 

agreements may be dilutive, restrict operations or relinquish proprietary rights.

To the extent that additional capital is raised through the sale of equity or convertible debt securities, the issuance of those 
securities could result in substantial dilution for our current stockholders and the terms may include liquidation or other preferences 
that adversely affect the rights of our current stockholders. Existing stockholders may not agree with our financing plans or the 
terms of such financings. Moreover, the incurrence of debt financing could result in a substantial portion of our operating cash 
flow being dedicated to the payment of principal and interest on such indebtedness and could impose restrictions on our operations. 
In  addition,  if  we  raise  additional  funds  through  collaboration  and  licensing  arrangements,  it  may  be  necessary  to  relinquish 
potentially valuable rights to our products or proprietary technologies, or to grant licenses on terms that are not favorable to us. 
Additional funding may not be available to us on acceptable terms, or at all.

As a public company in the United States, we incur significant legal and financial compliance costs and we are subject 
to the Sarbanes-Oxley Act. We can provide no assurance that we will, at all times, in the future be able to report that our internal 
controls over financial reporting are effective.

Companies  that  file  reports  with  the  Securities  and  Exchange  Commission  ("SEC"),  including  us,  are  subject  to  the 
requirements of Section 404 of the Sarbanes-Oxley Act of 2002. Section 404 requires management to establish and maintain a 
system of internal control over financial reporting, and annual reports on Form 10-K filed under the Securities Exchange Act of 
1934, as amended ("the Exchange Act"), must contain a report from management assessing the effectiveness of a company’s 
internal control over financial reporting. Ensuring that we have adequate internal financial and accounting controls and procedures 
in place to produce accurate financial statements on a timely basis remains a costly and time-consuming effort that needs to be 
re-evaluated frequently. Failure on our part to have effective internal financial and accounting controls would cause our financial 
reporting to be unreliable, could have a material adverse effect on our business, operating results, and financial condition, and 
could cause our stock price to decline as a result.

As an “emerging growth company” (as defined in the JOBS Act), we are not required to comply with Section 404(b) which 
requires attestation from our external auditors on our internal control over financial reporting. We are subject to Section 404(a), 
which requires management to provide a report regarding the effectiveness of internal controls. We are required to review all of 
our control processes to align them to the Section 404 requirements. Failure to provide assurance that our financial controls are 
effective could lead to lack of confidence by investors which could cause our stock price to decline. When we are no longer an 
“emerging growth company” (as defined in the Exchange Act or the Securities Act of 1933, as amended (the "Securities Act"), 
our independent registered public accounting firm will be required to attest to the effectiveness of our internal control over financial 
reporting. The rules governing the standards that must be met for management to assess our internal control over financial reporting 
are complex and require significant documentation, testing and possible remediation.  To continue complying with the requirements 
of  being  a  reporting  company  under  the  Exchange Act,  we  may  need  to  further  upgrade  our  systems,  including  information 
technology,  implement  additional  financial  and  management  controls,  reporting  systems  and  procedures,  and  hire  additional 
accounting and finance staff.

In addition, our independent registered public accounting firm has never performed an evaluation of our internal control 
over financial reporting in accordance with the provisions of the Sarbanes-Oxley Act because no such evaluation has been required. 
Had our independent registered public accounting firm performed an evaluation of our internal control over financial reporting 
in accordance with the provisions of the Sarbanes-Oxley Act, significant deficiencies or material weaknesses may have been 
identified. If we identify any significant deficiencies or material weaknesses that may exist or are unable to successfully remediate 
any significant deficiency or material weakness in our internal control over financial reporting, the accuracy and timing of our 
financial reporting may be adversely affected, we may be unable to maintain compliance with securities law requirements regarding 
timely filing of periodic reports in addition to applicable stock exchange listing requirements, investors may lose confidence in 
our financial reporting, and our stock price may decline as a result.

24

 
Furthermore, shareholder activism, the current political environment and the current high level of government intervention 
and regulatory reform may lead to substantial new regulations and disclosure obligations, which may lead to additional compliance 
costs and impact the manner in which we operate our business in ways we cannot currently anticipate. Our management and other 
personnel will need to devote a substantial amount of time to these compliance initiatives. Moreover, any new regulations or 
disclosure obligations may increase our legal and financial compliance costs and will make some activities more time-consuming 
and costly.

We are an emerging growth company and we cannot be certain if the reduced disclosure requirements applicable to 

emerging growth companies will make our common stock less attractive to investors.

We are an emerging growth company. Under the JOBS Act, emerging growth companies 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 exemption from new or revised accounting standards and, therefore, will be subject to the same new or revised 
accounting standards as other public companies that are not emerging growth companies.

For as long as we continue to be an emerging growth company, we intend to take advantage of certain other exemptions 
from various reporting requirements that are applicable to other public companies including, but not limited to, reduced disclosure 
obligations regarding executive compensation in our periodic reports and proxy statements, exemptions from the requirements of 
holding a nonbinding advisory stockholder vote on executive compensation and any golden parachute payments not previously 
approved, exemption from the requirement of auditor attestation in the assessment of our internal control over financial reporting 
and exemption from any requirement that may be adopted by the Public Company Accounting Oversight Board. If we do continue 
to be an emerging growth company, the information that we provide stockholders may be different than what is available with 
respect to other public companies. We cannot predict if investors will find our common stock less attractive because we rely on 
these exemptions. If some investors find our common stock less attractive as a result, there may be a less-active trading market 
for our common stock and our stock price may be more volatile.

We will remain an emerging growth company until the earliest of (1) the end of the fiscal year in which the market value 
of our common stock that is held by non-affiliates exceeds $700 million as of the end of the second fiscal quarter, (2) the end of 
the fiscal year in which we have total annual gross revenue of $1 billion or more during such fiscal year, (3) the date on which we 
issue more than $1 billion in non-convertible debt in a three-year period, or (4) December 31, 2018.

Decreased disclosures in our SEC filings due to our status as an emerging growth company may make it harder for investors 

to analyze our results of operations and financial prospects.

Risks Relating to Our Business and Industry

Our research and development programs and product candidates are at an early stage of development. As a result, we 

are unable to predict if or when we will successfully develop or commercialize our product candidates.

Our clinical-stage product candidates as well as our other pipeline assets are at an early stage of development and will 
require significant further investment and regulatory approvals prior to commercialization. We currently have no product candidates 
beyond Phase 2 clinical trials. Glesatinib is currently in a Phase 2 clinical trial, mocetinostat is currently in a Phase1b/Phase 2 
combination clinical trial and sitravatinib is in Phase 1b and Phase 2 clinical trials. Each of our product candidates will require 
the selection of suitable patients for our clinical trials and additional clinical development, management of clinical, preclinical 
and  manufacturing  activities,  obtaining  regulatory  approval,  obtaining  manufacturing  supply,  building  of  a  commercial 
organization, substantial investment and significant marketing efforts before we generate any revenues from product sales. We 
are not permitted to market or promote any of our product candidates before we receive regulatory approval from the FDA or 
comparable foreign regulatory authorities, and we may never receive such regulatory approval for any of our product candidates. 
The treatment of cancer is a rapidly evolving field and will continue to evolve.  By such time, if ever, as we may receive necessary 
regulatory approvals for our product candidates, the standard of care for the treatment of cancers may have evolved such that it 
would be necessary to modify our plans for full approval and commercial acceptance of our products may be limited by a change 
in the standard of care. In addition, some of our product development programs contemplate the development of companion 
diagnostics. Companion diagnostics are subject to regulation as medical devices and we or our future collaborators may be required 
to obtain marketing approval for accompanying companion diagnostics before we may commercialize our product candidates.

Even if we obtain the required financing or establish a collaboration to enable us to conduct late-stage clinical development 
of our product candidates and pipeline assets, we cannot be certain that such clinical development would be successful, or that 
we will obtain regulatory approval or be able to successfully commercialize any of our product candidates and generate revenue. 
Success in preclinical testing and early clinical trials does not ensure that later clinical trials will be successful, and the clinical 
25

 
trial process may fail to demonstrate that our product candidates are safe and effective for their proposed uses. Any such failure 
could cause us to abandon further development of any one or more of our product candidates and may delay development of other 
product candidates. Product candidates in later stages of clinical trials may fail to show the desired safety and efficacy traits despite 
having progressed through preclinical studies and initial clinical trials. Any delay in, or termination of, our clinical trials will delay 
and  possibly  preclude  the  submission  of  any  new  drug  applications  ("NDAs")  with  the  FDA  and,  ultimately,  our  ability  to 
commercialize our product candidates and generate product revenue.

We have not previously submitted an NDA to the FDA, or similar drug approval filings to comparable foreign authorities, 
for any product candidate, and we cannot be certain that any of our product candidates will receive regulatory approval. Further, 
our product candidates may not receive regulatory approval even if they are successful in clinical trials. If we do not receive 
regulatory approvals for our product candidates, we may not be able to continue our operations. Even if we successfully obtain 
regulatory approvals to market one or more of our product candidates, our revenues will be dependent, in part, upon our or our 
future collaborators’ ability to obtain regulatory approval for the companion diagnostics to be used with our product candidates, 
if required, and upon the size of the markets in the territories for which we gain regulatory approval and have commercial rights. 
If the markets for patient subsets that we are targeting are not as significant as we estimate, we may not generate significant 
revenues from sales of such products, if approved.

All of our product candidates are subject to extensive regulation, which can be costly and time consuming, cause delays 

or prevent approval of such product candidates for commercialization.

The clinical development of product candidates is subject to extensive regulation by the FDA in the United States and by 
comparable regulatory authorities in foreign markets. Product development is a very lengthy and expensive process, and its outcome 
is inherently uncertain. The product development timeline can vary significantly based upon the product candidate’s novelty and 
complexity. Regulations are subject to change and regulatory agencies have significant discretion in the approval process.

Numerous statutes and regulations govern human testing and the manufacture and sale of human therapeutic products in 
the United States, Europe and other countries and regions where we intend to market our products. Such legislation and regulation 
bears upon, among other things, the approval of trial protocols and human testing, the approval of manufacturing facilities, safety 
of the product candidates, testing procedures and controlled research, review and approval of manufacturing, preclinical and 
clinical data prior to marketing approval including adherence to good manufacturing practices ("GMP") during production and 
storage as well as regulation of marketing activities including advertising and labeling.

In order to obtain regulatory approval for the commercial sale of any of our product candidates, we must demonstrate 
through preclinical studies and clinical trials that the potential product is safe and effective for use in humans for each target 
indication. The failure to adequately demonstrate the safety and efficacy of a product under development could delay or prevent 
regulatory approval of our product candidates.

No assurance can be given that current regulations relating to regulatory approval will not change or become more stringent 
in the United States or foreign markets. Regulatory agencies may also require that additional trials be run in order to provide 
additional information regarding the safety or efficacy of any drug candidates for which we seek regulatory approval. Moreover, 
any regulatory approval of a drug which is eventually obtained may entail limitations on the indicated uses for which that drug 
may be marketed. Furthermore, product approvals may be withdrawn or limited in some way if problems occur following initial 
marketing or if compliance with regulatory standards is not maintained. Regulatory agencies could become more risk averse to 
any side effects or set higher standards of safety and efficacy prior to reviewing or approving a product. This could result in a 
product not being approved. Any of the foregoing scenarios could materially harm the commercial prospects for our product 
candidates.

We may not be successful in establishing development and commercialization collaborations which could adversely 

affect, and potentially prohibit, our ability to develop our product candidates.

Because  developing  pharmaceutical  products,  conducting  clinical  trials,  obtaining  regulatory  approval,  establishing 
manufacturing capabilities and marketing approved products is expensive, we may seek to enter into collaborations with companies 
that have more resources and experience in order to continue to develop and commercialize our product candidates. We also may 
be required due to financial or scientific constraints to enter into additional collaboration agreements to research and/or to develop 
and commercialize our product candidates. The establishment and realization of such collaborations may be not be possible or 
may be problematic. There can be no assurance that we will be able to establish such additional collaborations on favorable terms, 
if at all, or that our current or future collaborative arrangements will be successful or maintained for any specific product candidate 
or indication. If we are unable to reach successful agreements with suitable collaboration partners for the ongoing development 
and commercialization of our product candidates, we may face increased costs, we may be forced to limit the scope and number 
26

of our product candidates we can commercially develop or the territories in which we commercialize such product candidates, 
and we may be unable to commercialize products or programs for which a suitable collaboration partner cannot be found. If we 
fail to achieve successful collaborations, our operating results and financial condition will be materially and adversely affected.

In addition, the terms of any collaboration agreements may place restrictions on our activities with respect to other products, 
including by limiting our ability to grant licenses or develop products with other third parties, or in different indications, diseases 
or geographical locations, or may place additional obligations on us with respect to development or commercialization of our 
product candidates. If we fail to comply with or breach any provision of a collaboration agreement, a collaborator may have the 
right to terminate, in whole or in part, such agreement or to seek damages.

Some of our collaboration agreements are complex and involve sharing or division of ownership of certain data, know-
how and intellectual property rights among the various parties. Accordingly, our collaborators could interpret certain provisions 
differently than we or our other collaborators which could lead to unexpected or inadvertent disputes with collaborators. In addition, 
these agreements might make additional collaborations, partnering or mergers and acquisitions difficult.

There is no assurance that a collaborator who is acquired by a third party would not attempt to change certain contract 
provisions that could negatively affect our collaboration. The acquiring company may also not accept the terms or assignment of 
our contracts and may seek to terminate the agreements. Any one of our collaborators could breach covenants, restrictions and/or 
sub-license agreement provisions leading us into disputes and potential breaches of our agreements with other partners.

If we or third parties are unable to successfully develop companion diagnostics for our product candidates, or experience 
significant delays in doing so, we may not achieve marketing approval or realize the full commercial potential of such product 
candidates.

A key part of our development strategy for each of glesatinib, sitravatinib and mocetinostat is to identify subsets of patients 
with  specific  types  of  tumors  that  express  specific  genetic  markers.  Identification  of  these  patients  will  require  the  use  and 
development of companion diagnostics. We expect that the FDA and comparable foreign regulatory authorities will require the 
regulatory approval of a companion diagnostic as a condition to approving our product candidates. We do not have experience or 
capabilities in developing or commercializing diagnostics and plan to rely in large part on third parties to perform these functions. 
We are developing companion diagnostics in collaboration with diagnostic platform providers including Foundation Medicine, 
Inc., Guardant Health and Qiagen Manchester Limited that we plan to use in the current Phase 2 trial of glesatinib, later stage 
trials and commercialization, if approved. We do not currently have any long-term arrangements in place with any third party to 
develop or commercialize companion diagnostics for sitravatinib and mocetinostat product candidates.

Companion diagnostics are subject to regulation by the FDA and comparable foreign regulatory authorities as medical 
devices  and  will  likely  require  separate  regulatory  approval  prior  to  commercialization.    If  we  or  third  parties  are  unable  to 
successfully develop companion diagnostics for our product candidates, or experience delays in doing so:

• 

• 

• 

the development of these product candidates may be delayed because it may be difficult to identify patients for enrollment 
in our clinical trials in a timely manner;

these product candidates may not receive marketing approval if their safe and effective use depends on a companion 
diagnostic; and

we may not realize the full commercial potential of these product candidates that receive marketing approval if, among 
other reasons, we are unable to appropriately identify patients or types of tumors with the specific genetic alterations 
targeted by these product candidates.

Even  if  our  product  candidates  and  any  associated  companion  diagnostics  are  approved  for  marketing,  the  need  for 
companion diagnostics may slow or limit adoption of our product candidates. Although we believe genetic testing is becoming 
more prevalent in the diagnosis and treatment of cancer, our product candidates may be perceived negatively compared to alternative 
treatments that do not require the use of companion diagnostics, either due to the additional cost of the companion diagnostic or 
the need to complete additional procedures to identify genetic markers prior to administering our product candidates.

If any of these events were to occur, our business and growth prospects would be harmed, possibly materially.

27

We  rely  upon  third-party  contractors  and  service  providers  for  the  execution  of  some  aspects  of  our  development 
programs. Failure of these collaborators to provide services of a suitable quality and within acceptable timeframes may cause 
the delay or failure of our development programs.

We  outsource  certain  functions,  tests  and  services  to  CROs,  medical  institutions  and  collaborators  and  outsource 
manufacturing to collaborators and/or contract manufacturers, and we rely on third parties for quality assurance, clinical monitoring, 
clinical data management and regulatory expertise. In particular, we rely on CROs to run our clinical trials on our behalf and 
contract manufacturers to manufacture our product candidates. There is no assurance that such individuals or organizations will 
be able to provide the functions, tests, drug supply or services as agreed upon or to acceptable quality standards, and we could 
suffer significant delays in the development of our products or processes.

In  some  cases,  there  may  be  only  one  or  few  providers  of  such  services,  including  clinical  data  management  and 
manufacturing services. In addition, the cost of such services could increase significantly over time. We rely on third parties as 
mentioned above to enroll qualified patients and conduct, supervise and monitor our clinical trials. Our reliance on these third 
parties and collaborators for clinical development activities reduces our control over these activities, but does not relieve us of 
our regulatory responsibilities, including ensuring that our clinical trials are conducted in accordance with good clinical practices 
("GCP") regulations and the investigational plan and protocols contained in the regulatory agency applications. In addition, these 
third parties may not complete activities on schedule or may not manufacture compounds under GMP conditions. Preclinical 
studies may not be performed or completed in accordance with good laboratory practices, or GLP, regulatory requirements or our 
trial design. If we or our CROs fail to comply with GCP regulations, the clinical data generated in our clinical trials may be deemed 
unreliable and the FDA, the EMA or comparable foreign regulatory authorities may require us to perform additional clinical trials 
before approving any marketing applications. If these third parties or collaborators do not successfully carry out their contractual 
duties  or  meet  expected  deadlines,  obtaining  regulatory  approval  for  manufacturing  and  commercialization  of  our  product 
candidates may be delayed or prevented. We rely substantially on third-party data managers for our clinical trial data. There is no 
assurance that these third parties will not make errors in the design, management or retention of our data or data systems. There 
is no assurance that these third parties will pass FDA or regulatory audits, which could delay or prohibit regulatory approval.

Our CROs may also have relationships with other commercial entities, including our competitors, for whom they may 
also be conducting clinical trials or other product development activities, which could harm our competitive position. If any of 
our relationships with these third-party CROs terminate, we may not be able to enter into arrangements with alternative CROs or 
to do so on commercially reasonable terms. Further, switching or adding additional CROs involves additional cost and requires 
management time and attention. In addition, there is a natural transition period when a new CRO commences work. As a result, 
delays may occur, which could materially impact our ability to meet our desired clinical development timelines. Though we 
carefully manage 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 material adverse impact on our business, financial condition and 
prospects.

The timelines of our clinical trials may be impacted by numerous factors and any delays may adversely affect our ability 

to execute our current business strategy.

Clinical testing is expensive, difficult to design and implement, can take many years to complete, and is uncertain as to 
outcome. We may experience delays in clinical trials at any stage of development and testing of our product candidates. Our 
planned clinical trials may not begin on time, have an effective design, enroll a sufficient number of subjects, or be completed on 
schedule, if at all.

Events which may result in a delay or unsuccessful completion of clinical trials include:

• 

• 

• 

• 

• 

• 

inability to raise funding necessary to initiate or continue a trial;

delays in obtaining regulatory approval to commence a trial;

delays in reaching agreement with the FDA on final trial design;

delays in recruiting patients with the specific genetic alterations we are targeting to participate in a trial;

imposition of a clinical hold following an inspection of our clinical trial operations or trial sites by the FDA or other 
regulatory authorities;

delays in reaching agreement on acceptable terms with prospective CROs and clinical trial sites;

28

• 

• 

• 

• 

• 

• 

delays in obtaining required institutional review board approval at each site;

delays in having subjects complete participation in a trial or return for post-treatment follow-up;

delays caused by subjects dropping out of a trial due to side effects or otherwise;

clinical sites dropping out of a trial to the detriment of enrollment;

time required to add new clinical sites; and

delays by our contract manufacturers to produce and deliver a sufficient supply of clinical trial materials.

For example, due to the targeted indications and patient populations we intend to focus on for development of our product 
candidates, the number of study sites and patient populations available to us may be limited, and therefore enrollment of suitable 
patients to participate in clinical trials for these product candidates may take longer than would be the case if we were pursuing 
broader indications or patient populations. In addition, some of our competitors are developing targeted oncology therapeutics for 
non-small cell lung cancer ("NSCLC") which could limit our ability to enroll patients and complete our planned clinical trials in 
a timely manner.

Furthermore, enrollment may depend on the availability of suitable companion diagnostics to identify genetic markers 

we are targeting and the capability and willingness of clinical sites to conduct genetic screening of potential patients.

If initiation or completion of any of our clinical trials for our product candidates are delayed for any of the above reasons 
or for other reasons, our development costs may increase, our approval process could be delayed, any periods after commercial 
launch and before expiration of patent protection may be reduced and our competitors may have more time to bring products to 
market before we do. Any of these events could impair the commercial potential of our product candidates and could have a 
material adverse effect on our business.

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

Undesirable side effects caused by our product candidates could cause us or regulatory authorities to interrupt, delay or 
halt clinical trials and could result in a more restrictive label or the delay or denial of regulatory approval by the FDA or other 
comparable foreign authorities. Results of our trials could reveal a high and unacceptable severity and prevalence of side effects. 
In such an event, our trials could be suspended or terminated and the FDA or comparable foreign regulatory authorities could 
order us to cease further development of or deny approval of our product candidates for any or all targeted indications. Treatment-
related side effects could affect patient recruitment or the ability of enrolled patients to complete the trial, or result in potential 
product liability claims. Any of these occurrences may harm our business, financial condition and prospects significantly. For 
example, in the glesatinib Phase 2 clinical trial, we recently introduced a new spray-dried dispersion ("SDD") formulation. We 
can make no assurances the SDD formulation will be well tolerated or that it will not cause previously unreported side effects.

Additionally,  if  one  or  more  of  our  product  candidates  receives  marketing  approval,  and  we  or  others  later  identify 
undesirable side effects caused by such products, a number of potentially significant negative consequences could result, including:

• 

• 

• 

• 

• 

regulatory authorities may withdraw approvals of such product;

regulatory authorities may require additional warnings on the product label;

we may be required to create a medication guide outlining the risks of such side effects for distribution to patients;

we could be sued and held liable for harm caused to patients; and

our reputation may suffer.

Any  of  these  events  could  prevent  us  from  achieving  or  maintaining  market  acceptance  of  any  product  candidate,  if 

approved, and could significantly harm our business, results of operations and prospects.

29

We are and continue to be subject to stringent government regulations concerning the clinical testing of our products. 

We will also continue to be subject to government regulation of any product that receives regulatory approval.

Numerous statutes and regulations govern human testing and the manufacture and sale of human therapeutic products in 
the United States and other countries where we intend to market our products. Such legislation and regulation bears upon, among 
other things, the approval of trial protocols and human testing, the approval of manufacturing facilities, testing procedures and 
controlled research, the review and approval of manufacturing, preclinical and clinical data prior to marketing approval, including 
adherence to GMP during production and storage, and marketing activities including advertising and labeling.

Clinical trials may be delayed or suspended at any time by us or by the FDA or other similar regulatory authorities if it is 
determined at any time that patients may be or are being exposed to unacceptable health risks, including the risk of death, or if 
compounds are not manufactured under acceptable GMP conditions or with acceptable quality. Current regulations relating to 
regulatory approval may change or become more stringent. The agencies may also require additional trials be run in order to 
provide additional information regarding the safety, efficacy or equivalency of any product candidate for which we seek regulatory 
approval.

Moreover, any regulatory approval of a drug which is eventually obtained may entail limitations on the indicated uses for 
which that drug may be marketed or on the conditions of approval, or contain requirements for potentially costly post-marketing 
testing, including Phase 4 clinical trials, and surveillance to monitor the safety and efficacy of the product candidate. In addition, 
if the FDA or a comparable foreign regulatory authority approves any of our product candidates, the manufacturing processes, 
labeling, packaging, distribution, adverse event reporting, storage, advertising, promotion and recordkeeping for the product will 
be subject to extensive and ongoing regulatory requirements. These requirements include submissions of safety and other post-
marketing information and reports, registration, as well as continued compliance with GMPs and GCPs for any clinical trials that 
we conduct post-approval. Furthermore, product approvals may be withdrawn or limited in some way if problems occur following 
initial marketing or if compliance with regulatory standards is not maintained. Similar restrictions are imposed in foreign markets. 
Regulatory agencies could become more risk averse to any side effects or set higher standards of safety and efficacy prior to 
reviewing or approving a product. This could result in a product not being approved.

If  we,  or  any  future  marketing  collaborators  or  contract  manufacturers,  fail  to  comply  with  applicable  regulatory 
requirements,  we  may  be  subject  to  sanctions  including  fines,  product  recalls  or  seizures  and  related  publicity  requirements, 
injunctions, total or partial suspension of production, civil penalties, suspension or withdrawals of previously granted regulatory 
approvals,  warning  or  untitled  letters,  refusal  to  approve  pending  applications  for  marketing  approval  of  new  products  or  of 
supplements to approved applications, import or export bans or restrictions, and criminal prosecution and penalties. Any of these 
penalties could delay or prevent the promotion, marketing or sale of our products and product candidates.

The FDA’s policies, and policies of comparable foreign regulatory authorities, 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 to adopt 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, which would adversely affect our business, 
prospects and ability to achieve or sustain profitability.

We have no experience in clinical or commercial manufacturing and depend on others for the production of our product 
candidates at suitable levels of quality and quantity. Any problems or delays in the manufacture of our products would have a 
negative impact on our ability to successfully execute our development and commercialization strategies.

We do not currently have nor do we plan to acquire the infrastructure or capability internally to manufacture our clinical 
drug supplies for use in the conduct of our clinical trials, and we lack the resources and the capability to manufacture any of our 
product candidates on a clinical or commercial scale. We rely on collaborators and/or third parties for development, scale-up, 
formulation, optimization, management of clinical trial and commercial scale manufacturing and commercialization. There are 
no  assurances  we  can  scale-up,  formulate  or  manufacture  any  product  candidate  in  sufficient  quantities  with  acceptable 
specifications for the conduct of our clinical trials or for the regulatory agencies to grant approval of such product candidate. We 
have not yet commercialized any products and have no commercial manufacturing experience. To be successful, our products 
must be properly formulated, scalable, stable and safely manufactured in clinical trial and commercial quantities in compliance 
with GMP and other regulatory requirements and at acceptable costs. Should any of our suppliers or our collaborators be unable 
to supply or be delayed in supplying us with sufficient supplies, no assurance can be given that we will be able to find alternative 
means of supply in a short period of time. Should such parties’ operations suffer a material adverse effect, the manufacturing of 
our products would also be adversely affected. Furthermore, key raw materials could become scarce or unavailable. There may 
be a limited number of third parties who can manufacture our products. We may not be able to meet specifications previously 
established for product candidates during scale-up and manufacturing.

30

Our reliance on third parties to manufacture our product candidates will expose us and our partners to risks including the 
following, any of which could delay or prevent the commercialization of our products, result in higher costs, or deprive us of 
potential product revenue:

• 

• 

• 

Contract  manufacturers  can  encounter  difficulties  in  achieving  the  scale-up,  optimization,  formulation,  or  volume 
production  of  a  compound  as  well  as  maintaining  quality  control  with  appropriate  quality  assurance. They  may  also 
experience shortages of qualified personnel. Contract manufacturers are required to undergo a satisfactory GMP inspection 
prior to regulatory approval and are obliged to operate in accordance with FDA, International Conference on Harmonisation 
of Technical Requirements for Registration of Pharmaceuticals for Human Use ("ICH"), European and other nationally 
mandated GMP regulations and/or guidelines governing manufacturing processes, stability testing, record keeping and 
quality  standards. A  failure  of  these  contract  manufacturers  to  follow  GMP  and  to  document  their  adherence  to  such 
practices or failure of an inspection by a regulatory agency may lead to significant delays in the availability of our product 
candidate materials for clinical study, leading to delays in our trials.

For each of our current product candidates we will initially rely on a limited number of contract manufacturers. Changing 
these  or  identifying  future  manufacturers  may  be  difficult.  Changing  manufacturers  requires  re-validation  of  the 
manufacturing processes and procedures in accordance with FDA, ICH, European and other mandated GMP regulations 
and/or guidelines. Such re-validation may be costly and time-consuming. It may be difficult or impossible for us to quickly 
find replacement manufacturers on acceptable terms, if at all.

Our contract manufacturers may not perform as agreed or may not remain in the contract manufacturing business for the 
time required to produce, store and distribute our products successfully.

The successful commercialization of our product candidates, if approved, will depend on achieving market acceptance 

and we may not be able to gain sufficient acceptance to generate significant revenue.

Even if our product candidates are successfully developed and receive regulatory approval, they may not gain market 
acceptance among physicians, patients, healthcare payors such as private insurers or governments and other funding parties and 
the medical community. The degree of market acceptance for any of our products will depend on a number of factors, including:

• 

• 

• 

• 

• 

• 

• 

demonstration of the clinical efficacy and safety of our products;

the prevalence and severity of any adverse side effects;

limitations or warnings contained in the product’s approved labeling;

cost-effectiveness and availability of acceptable pricing;

competitive product profile versus alternative treatment methods and the superiority of alternative treatment or 
therapeutics;

the effectiveness of marketing and distribution methods and support for the products; and

coverage and reimbursement policies of government and third-party payors to the extent that our products could receive 
regulatory approval but not be approved for coverage by or receive adequate reimbursement from government and quasi-
government agencies or other third-party payors.

Disease indications may be small subsets of a disease that could be parsed into smaller and smaller indications as different 
subsets of diseases are defined. This increasingly fine characterization of diseases could have negative consequences; including 
creating an approved indication that is so small as not to have a viable market for us. If future technology allows characterization 
of a disease in a way that is different from the characterization used for large pivotal studies, it may make those studies invalid or 
reduce their usefulness, and may require repeating all or a portion of the studies. Future technology may supply better prognostic 
ability which could reduce the portion of patients projected to need a new therapy. Even after being cleared by regulatory authorities, 
a product may later be shown to be unsafe or not to have its purported effect, thereby preventing its widespread use or requiring 
withdrawal from the market.

31

If we fail to obtain coverage and adequate reimbursement for our products, our revenue-generating ability will be 

diminished and there is no assurance that the anticipated market for our products will be sustained.

We believe that there will be many different applications for products successfully derived from our technologies and that 
the anticipated market for products under development will continue to expand. However, due to competition from existing or 
new products and the yet-to-be established commercial viability of our products, no assurance can be given that these beliefs will 
prove to be correct. Physicians, patients, formularies, payors or the medical community in general may not accept or utilize any 
products that we or our collaborative partners may develop. Other drugs may be approved during our clinical testing which could 
change the accepted treatments for the disease targeted and make our product candidates obsolete.

Our and our collaborators’ ability to commercialize our products successfully will depend, in part, on the extent to which 
coverage and adequate reimbursement for such products and related treatments will be available from governmental health payor 
programs at the federal and state levels, including Medicare and Medicaid, private health insurers, managed care plans and other 
organizations. No assurance can be given that third-party coverage and adequate reimbursement will be available that will allow 
us to maintain price levels sufficient for the realization of an appropriate return on our investment in product development.

Coverage and adequate reimbursement from governmental healthcare programs, such as Medicare and Medicaid, and 
private health insurers, managed care plans and other organizations is critical to new product acceptance. Coverage decisions may 
depend upon clinical and economic standards that disfavor new drug products when more established or lower cost therapeutic 
alternatives are already available or subsequently become available. Even if we obtain coverage for our product candidates, the 
resulting reimbursement payment rates might not be adequate or may require co-payments that patients find unacceptably high. 
Patients are unlikely to use our product candidates unless coverage is provided and reimbursement is adequate to cover a significant 
portion of the cost of our product candidates.

In the United States and in many other countries, pricing and/or profitability of some or all prescription pharmaceuticals 
and  biopharmaceuticals  are  subject  to  varying  degrees  of  government  control.  Outside  of  the  United  States,  the  successful 
commercialization of our products will depend largely on obtaining and maintaining government coverage, because in many 
countries patients are unlikely to use prescription drugs that are not covered by their government healthcare programs. Negotiating 
coverage and reimbursement with governmental authorities can delay commercialization by 12 months or more. Coverage and 
reimbursement policies may adversely affect our ability to sell our products on a profitable basis. In many international markets, 
governments control the prices of prescription pharmaceuticals, including through the implementation of reference pricing, price 
cuts, rebates, revenue-related taxes and profit control, and we expect prices of prescription pharmaceuticals to decline over the 
life of the product or as volumes increase. Healthcare reform and controls on healthcare spending may limit the price we charge 
for any products and the amounts thereof that we can sell. In particular, in the United States, the federal government and private 
insurers have changed and have considered ways to change, the manner in which healthcare services are provided. In March 2010, 
the Patient Protection and Affordable Care Act, as amended by the Health Care and Education Reconciliation Act (collectively, 
the "ACA"), became law in the United States. In January 2017, Congress voted to adopt a budget resolution for fiscal year 2017, 
the Budget Resolution, that authorizes the implementation of legislation that would repeal portions of the ACA. The Budget 
Resolution is not a law, however, it is widely viewed as the first step toward the passage of legislation that would repeal certain 
aspects of the ACA.  As a result, there is significant uncertainty regarding future healthcare reform and its impact on our operations. 
Moreover, in the United States, there has recently been significantly increased government enforcement and payor scrutiny relating 
to drug pricing and price increases. For example, there have been several recent U.S. Congressional inquiries and proposed bills 
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, and such measures, if enacted, could 
adversely impact the prices we or our future collaborators may charge for our products candidates, if commercialized.

In addition, other legislative changes have been proposed and adopted since the ACA was enacted. In August 2011, the 
Budget Control Act of 2011, among other things, created measures for spending reductions by Congress. A Joint Select Committee 
on Deficit Reduction, tasked with recommending a targeted deficit reduction of at least $1.2 trillion for the years 2013 through 
2021, was unable to reach required goals, thereby triggering the legislation’s automatic reduction to several government programs. 
These changes include aggregate reductions to Medicare payments to providers of up to 2% per fiscal year, which went into effect 
on April 1, 2013 and, as amended, will stay in effect through 2025 unless additional Congressional action is taken. In January 2013, 
President Obama signed into law the American Taxpayer Relief Act of 2012, which, among other things, further reduced Medicare 
payments to several types of providers and increased the statute of limitations period for the government to recover overpayments 
to providers from three to five years. Moreover, the Drug Supply Chain Security Act, enacted in 2013, imposes new obligations 
on manufacturers of pharmaceutical products related to product tracking and tracing. These new laws may result in additional 
reductions in Medicare and other healthcare funding, which could have a material adverse effect on our customers and accordingly, 
our financial operations.

32

 
We anticipate that the ACA, as well as alternative or replacement healthcare reform measures that may be adopted in the 
future, may result in more rigorous coverage criteria and additional downward pressure on the reimbursement we may receive for 
any approved product. Moreover, payment methodologies may be subject to changes in healthcare legislation and regulatory 
initiatives. 

In addition, levels of reimbursement may be impacted by other current and future legislation, regulation or reimbursement 
policies of third-party payors in a manner that may harm the demand and reimbursement available for our products, including for 
companion  diagnostics  for  our  products,  which  in  turn,  could  harm  our  future  product  pricing  and  sales. Any  reduction  in 
reimbursement from Medicare and other government programs may result in a similar reduction in payments from private payors. 
The implementation of cost containment measures or other healthcare reforms may prevent us from being able to generate revenue, 
attain profitability or commercialize our products.

Competition  in  our  targeted  market  area  is  intense  and  this  field  is  characterized  by  rapid  technological  change. 
Therefore  developments  by  competitors  may  substantially  alter  the  predicted  market  or  render  our  product  candidates 
uncompetitive.

There are hundreds of drugs in clinical development today in the area of oncology therapeutics. We have competitors both 
in the United States and internationally, including major multinational pharmaceutical companies, biotechnology companies and 
universities  and  other  research  institutions.  In  the  oncology  market,  our  major  competitors  include,  but  are  not  limited  to: 
AbbVie, Inc., AstraZeneca  PLC,  Exelixis  Inc.,  GlaxoSmithKline  PLC, Ignyta,  Inc.,  BergenBio,  Blueprint  Medicines,  Loxo 
Oncology, Syndax Pharmaceuticals Inc., Merck KGaA, NantPharma LLC, Novartis AG, Pfizer Inc. and Sanofi S. A. among others.

Many companies have filed, and continue to file, patent applications in oncology which may or could affect our programs. 
Some of these patent applications may have already been allowed or issued, and others may issue in the future. These companies 
include, but are not limited to: Bristol-Myers Squibb Company; Compugen Limited; Exelixis; GlaxoSmithKline PLC; Novartis; 
and Pfizer. Since this area is competitive and of strong interest to pharmaceutical and biotechnology companies, there will likely 
be additional patent applications filed, and additional patents granted, in the future, as well as additional research and development 
programs expected in the future.

In addition to companies that have HDAC inhibitors or kinase inhibitors addressing oncology indications, our competition 
also includes hundreds of private and publicly traded companies that operate in the area of oncology but have therapeutics with 
different mechanisms of action. The oncology market in general is highly competitive with over 1,000 molecules currently in 
clinical development.

Developments by others may render our products or technologies non-competitive or obsolete or we may not be able to 
keep pace with technological developments. Our competitors may have developed or may be developing technologies which may 
be the basis for competitive products. Some of these products may prove to be more effective and less costly than the products 
developed or being developed by us. Our competitors may obtain regulatory approval for their products more rapidly than we do 
which may change the standard of care in the indications we are targeting, rendering our technology or products non-competitive 
or obsolete. For example, with the recent approval of immunotherapy agents for the treatment of NSCLC and other cancers, the 
standard of care for the treatment of cancer is evolving and will continue to evolve which could require us to change the design 
and timelines for our registration trails and may limit the commercial acceptance of our products in the future. Others may develop 
treatments or cures superior to any therapy we are developing or will develop. Moreover, alternate, less toxic forms of medical 
treatment may be developed which may be competitive with our products.

Many of the organizations which could be considered to be our competitors have substantially more financial and technical 
resources,  more  extensive  discovery  research,  preclinical  research  and  development  capabilities  and  greater  manufacturing, 
marketing, distribution, production and human resources than we do. Many of our current or potential competitors have more 
experience than us in research, preclinical testing and clinical trials, drug commercialization, manufacturing and marketing, and 
in obtaining domestic and foreign regulatory approvals. In addition, failure, unacceptable toxicity, lack of sales or disappointing 
sales or other issues regarding competitors’ products or processes could have a material adverse effect on our product candidates, 
including our clinical candidates or our lead compounds. Established pharmaceutical companies may invest heavily to accelerate 
discovery and development of novel compounds or to in-license novel compounds that could make our product candidates less 
competitive. In addition, any new product that competes with an approved product must demonstrate compelling advantages in 
efficacy, convenience, tolerability and safety in order to overcome price competition and brand recognition and to be commercially 
successful. Accordingly, our competitors may succeed in obtaining patent protection, receiving FDA, EMA or other regulatory 
approval or discovering, developing and commercializing medicines before we do, which would have a material adverse impact 
on our business.

33

We will not be able to successfully commercialize our product candidates without establishing sales and marketing 

capabilities internally or through collaborators.

We  currently  have  no  sales  and  marketing  staff.  We  may  not  be  able  to  find  suitable  sales  and  marketing  staff  and 
collaborators for all of our product candidates. We have no prior experience in the marketing, sale and distribution of pharmaceutical 
products and there are significant risks involved in building and managing a sales organization, including our ability to hire, retain 
and incentivize qualified individuals, generate sufficient sales leads, provide adequate training to sales and marketing personnel, 
and effectively manage a geographically dispersed sales and marketing team. Any collaborators may not be adequate or successful 
or could terminate or materially reduce the effort they direct to our products. The development of a marketing and sales capability 
will require significant expenditures, management resources and time. The cost of establishing such a sales force may exceed any 
potential product revenue, or our marketing and sales efforts may be unsuccessful. If we are unable to develop an internal marketing 
and sales capability in a timely fashion, or at all, or if we are unable to enter into a marketing and sales arrangement with a third 
party on acceptable terms, we may be unable to successfully develop and seek regulatory approval for our product candidates and/
or effectively market and sell approved products, if any.

We are subject to competition for our skilled personnel and may experience challenges in identifying and retaining key 

personnel that could impair our ability to conduct our operations effectively.

Our future success depends on our ability to retain our executive officers and to attract, retain and motivate qualified 
personnel. If we are not successful in attracting and retaining highly qualified personnel, we may not be able to successfully 
implement our business strategy. Although we have not experienced problems attracting and retaining highly qualified personnel 
in the recent past, our industry has experienced a high rate of turnover of management personnel in recent years. Our ability to 
compete in the highly competitive biotechnology and pharmaceuticals industries depends upon our ability to attract and retain 
highly qualified managerial, scientific and medical personnel. We are highly dependent on our management, scientific and medical 
personnel, especially Charles M. Baum, M.D., Ph.D., our President and Chief Executive Officer, Isan Chen, M.D., our Executive 
Vice President and Chief Medical and Development Officer, James Christensen, Ph.D. our Chief Scientific Officer, Jamie A. 
Donadio, our Senior Vice President and Chief Financial Officer, and Chris LeMasters, our Executive Vice President and Chief 
Business Officer whose services are critical to the successful implementation of our product candidate acquisition, development 
and regulatory strategies, as well as the management of our financial operations. We are not aware of any present intention of any 
of these individuals to leave our Company. In order to induce valuable employees to continue their employment with us, we have 
provided stock options that vest over time. The value to employees of stock options that vest over time is significantly affected 
by movements in our stock price that are beyond our control, and may at any time be insufficient to counteract more lucrative 
offers from other companies.

Despite our efforts to retain valuable employees, members of our management, scientific and development teams may 
terminate their employment with us at any time, with or without notice. The loss of the services of any of our executive officers 
or other key employees and our inability to find suitable replacements could harm our business, financial condition and prospects. 
Our success also depends on our ability to continue to attract, retain and motivate highly skilled junior, mid-level and senior 
managers as well as junior, mid-level and senior scientific and medical personnel.

We may also experience growth in the number of our employees and the scope of our operations, especially in clinical 
development. This growth will place a significant strain on our management, operations and financial resources and we may have 
difficulty managing this future potential growth. No assurance can be provided that we will be able to attract new employees to 
assist in our growth. Many of the other pharmaceutical companies that we compete against for qualified personnel have greater 
financial and other resources, different risk profiles and a longer history in the industry than we do. We also may employ consultants 
or part-time and contract employees. There can be no assurance that these individuals are retainable. While we have been able to 
attract and retain skilled and experienced personnel and consultants in the past, no assurance can be given that we will be able to 
do so in the future.

Our current and future relationships with customers and third-party payors in the United States and elsewhere may be 
subject, directly or indirectly, to applicable anti-kickback, fraud and abuse, false claims, transparency, health information 
privacy and security and other healthcare laws and regulations, which could expose us to criminal sanctions, civil penalties, 
contractual damages, reputational harm, administrative burdens and diminished profits and future earnings.

As a pharmaceutical company, even though we do not and will not control referrals of healthcare services or bill directly 
to Medicare, Medicaid or other third-party payors, certain federal and state healthcare laws and regulations pertaining to fraud 
and abuse and patients’ rights are and will be applicable to our business. Our current and future arrangements with third-party 
payors and customers may expose us to broadly applicable fraud and abuse and other healthcare laws and regulations, including, 
without  limitation,  the  federal Anti-Kickback  Statute  and  the  federal  False  Claims Act,  which  may  constrain  the  business  or 
34

 
financial arrangements and relationships through which we sell, market and distribute any drugs for which we obtain marketing 
approval. In addition, we may be subject to transparency laws and patient privacy regulation by U.S. federal and state governments 
and by governments in foreign jurisdictions in which we conduct our business. The laws that may affect our ability to operate 
include:

• 

• 

• 

• 

• 

• 

the federal Anti-Kickback Statute, which prohibits, among other things, persons from knowingly and willfully soliciting, 
offering, receiving or providing remuneration, directly or indirectly, in cash or in kind, to induce or reward, or in return 
for, either the referral of an individual for, or the purchase, order or recommendation of, any good or service, for which 
payment may be made under federal and state healthcare programs, such as Medicare and Medicaid;

federal civil and criminal false claims laws and civil monetary penalty laws, including the federal False Claims Act, which 
impose criminal and civil penalties, including civil whistleblower or qui tam actions, against individuals or entities for 
knowingly  presenting,  or  causing  to  be  presented,  to  the  federal  government,  including  the  Medicare  and  Medicaid 
programs, claims for payment that are false or fraudulent or making a false statement to avoid, decrease or conceal an 
obligation to pay money to the federal government;

the federal Health Insurance Portability and Accountability Act of 1996 ("HIPAA"), which imposes criminal and civil 
liability for executing a scheme to defraud any healthcare benefit program or making false statements relating to healthcare 
matters;

HIPAA, as amended by the Health Information Technology for Economic and Clinical Health Act of 2009 ("HITECH"), 
and their respective implementing regulations, which impose obligations on covered healthcare providers, health plans, 
and healthcare clearinghouses, as well as their business associates that create, receive, maintain or transmit individually 
identifiable health information for or on behalf of a covered entity, with respect to safeguarding the privacy, security and 
transmission of individually identifiable health information;

the federal Open Payments program, which requires 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 CMS information related to “payments or other transfers of value” made to physicians, which is 
defined  to  include  doctors,  dentists,  optometrists,  podiatrists  and  chiropractors,  and  teaching  hospitals  and  applicable 
manufacturers and applicable group purchasing organizations to report annually to CMS ownership and investment interests 
held by the physicians and their immediate family members, and contains requirements for manufacturers to submit reports 
to CMS by the 90th day of each calendar year, and disclosure of such information to be made by CMS on a publicly 
available website; and

analogous state and foreign laws and regulations, such as state anti-kickback and false claims laws, which may apply to 
sales or marketing arrangements and claims involving healthcare items or services reimbursed by non-governmental third-
party payors, including private insurers; state and foreign 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 or otherwise restrict payments that may be made to healthcare providers; state and foreign 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; and state and foreign laws governing the privacy and security of health 
information in certain circumstances, many of which differ from each other in significant ways and often are not preempted 
by HIPAA, thus complicating compliance efforts.

Because of the breadth of these laws and the narrowness of available statutory and regulatory exceptions, it is possible 
that some of our business activities could be subject to challenge under one or more of such laws. To the extent that any of our 
product candidates is ultimately sold in countries other than the United States, we may be subject to similar laws and regulations 
in those countries. If we or our operations are found to be in violation of any of the laws described above or any other governmental 
regulations that apply to us, we may be subject to penalties, including civil and criminal penalties, damages, fines, imprisonment, 
exclusion from participation in government healthcare programs, and the curtailment or restructuring of our operations, any of 
which could have a material adverse effect on our business. If any of the physicians or other healthcare providers or entities with 
whom we expect to do business, including any of our collaborators, is found not to be in compliance with applicable laws, they 
may be subject to criminal, civil or administrative sanctions, including exclusion from participation in government healthcare 
programs, which could also materially affect our business.

35

We may become subject to the risk of product liability claims.

We face an inherent risk of product liability as a result of the clinical testing of our product candidates and will face an 
even greater risk if we commercialize any products. Human therapeutic products involve the risk of product liability claims and 
associated adverse publicity. Currently, the principal risks we face relate to patients in our clinical trials, who may suffer unintended 
consequences. Claims might be made by patients, healthcare providers, pharmaceutical companies or others. For example, we 
may be sued if any product we develop allegedly causes injury or is found to be otherwise unsuitable during product testing, 
manufacturing, marketing or sale. Any such product liability claims may include allegations of defects in manufacturing, defects 
in design, a failure to warn of dangers inherent in the product, negligence, strict liability and a breach of warranties. Claims could 
also be asserted under state consumer protection laws.  If we cannot successfully defend ourselves against product liability claims, 
we may incur substantial liabilities or be required to limit commercialization of our product candidates, if approved. Even successful 
defense would require significant financial and management resources. Regardless of the merits or eventual outcome, liability 
claims may result in:

• 

• 

decreased demand for our product candidates;

injury to our reputation;

•  withdrawal of clinical trial participants;

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• 

• 

• 

• 

• 

• 

initiation of investigations by regulators;

costs to defend the related litigation;

a diversion of management’s time and our resources;

substantial monetary awards to trial participants or patients;

product recalls, withdrawals or labeling, marketing or promotional restrictions;

loss of revenue from product sales; and

the inability to commercialize any of our product candidates, if approved.

We may not have or be able to obtain or maintain sufficient and affordable insurance coverage, and without sufficient 
coverage any claim brought against us could have a materially adverse effect on our business, financial condition or results of 
operations. We run clinical trials through investigators that could be negligent through no fault of our own and which could affect 
patients, cause potential liability claims against us and result in delayed or stopped clinical trials. We are required in many cases 
by contractual obligations to indemnify collaborators, partners, third-party contractors, clinical investigators and institutions. These 
indemnifications could result in a material impact due to product liability claims against us and/or these groups. We currently 
carry $10 million in product liability insurance, which we believe is appropriate for our clinical trials. Although we maintain such 
insurance, any claim that may be brought against us could result in a court judgment or settlement in an amount that is not covered, 
in whole or in part, by our insurance or that is in excess of the limits of our insurance coverage. Our insurance policies also have 
various exclusions, and we may be subject to a product liability claim for which we have no coverage. We will have to pay any 
amounts awarded by a court or negotiated in a settlement that exceed our coverage limitations or that are not covered by our 
insurance, and we may not have, or be able to obtain, sufficient capital to pay such amounts.

Our business involves the controlled use of hazardous materials and as such we are subject to environmental and 
occupational safety laws. Continued compliance with these laws may incur substantial costs and failure to maintain compliance 
could result in liability for damages that may exceed our resources.

Our preclinical research, manufacturing and development processes involve the controlled use of hazardous and radioactive 
materials. We are subject to federal, local and foreign laws and regulations governing the use, manufacture, storage, handling and 
disposal of such materials and certain waste products. Our operations involve the use of hazardous and flammable materials, 
including  chemicals  and  biological  materials.  Our  operations  also  produce  hazardous  waste  products. The  risk  of  accidental 
contamination or injury from these materials cannot be completely eliminated. In the event of such an accident, we could be held 
liable for any damages that result, and any such liability could exceed our resources. We may not be adequately insured against 
this type of liability. We may be required to incur significant costs to comply with environmental laws and regulations in the future, 
and our operations, business or assets may be materially adversely affected by current or future environmental laws or regulations.
36

We may have to dedicate resources to the settlement of litigation.

Securities legislation in the United States, Canada and other countries makes it relatively easy for stockholders to sue. 
This could lead to frivolous lawsuits which could take substantial time, money, resources and attention or force us to settle such 
claims rather than seek adequate judicial remedy or dismissal of such claims.

If we are required to defend patent infringement actions brought by third parties, or if we sue to protect our own patent 
rights or otherwise to protect our proprietary information and to prevent its disclosure, or if we are involved in other litigation, 
whether as a plaintiff or defendant, we may be required to pay substantial litigation costs and managerial attention may be diverted 
from business operations even if the outcome is in our favor. If we are required to defend our patents or trademarks against 
infringement by third parties, we may be required to pay substantial litigation costs and managerial attention and financial resources 
may be diverted from our research and development operations even if the outcome is in our favor.

We may be vulnerable to disruption, damage and financial obligation as a result of system failures.

Despite the implementation of security measures, any of the internal computer systems belonging to us, our collaborators 
or  our  third-party  service  providers  are  vulnerable  to  damage  from  computer  viruses,  unauthorized  access,  natural  disasters, 
terrorism, war and telecommunication and electrical failure. Any system failure, accident or security breach that causes interruptions 
in our own, in collaborators’ or in third-party service vendors’ operations could result in a material disruption of our drug discovery 
and development programs. In addition, we rely upon third-party contractors and service providers for the hosting, support and/
or maintenance of some aspects of our computer hardware, computer software and telecommunications systems.  Failure of those 
contractors and service providers to provide systems and services of a suitable quality and within acceptable timeframes may 
cause the delay or failure of our development programs, or loss of confidential or proprietary information. To the extent that any 
disruption or security breach results in a loss or damage to our data or applications, or inappropriate disclosure of confidential or 
proprietary information, we may incur liability, our drug discovery and development programs may be adversely affected and the 
further development of our product candidates may be delayed. Furthermore, we may incur additional costs to remedy the damages 
caused by these disruptions or security breaches.

Risks Relating to Our Intellectual Property

We may not obtain adequate protection for our product candidates through patents and other intellectual property 

rights and as such our competitive advantage in the marketplace may be compromised.

Our success depends, in part, on our ability to secure and protect our patents, trade secrets, trademarks and other intellectual 
property rights and to operate without infringing on the proprietary rights of others or having third parties circumvent the rights 
that we own or license. We have filed and are actively pursuing patent applications in the United States, Japan, Europe and other 
major markets via the Patent Cooperation Treaty or directly in countries of interest. The patent positions of healthcare companies, 
universities and biopharmaceutical companies, including ours, are uncertain and involve complex questions of law and fact for 
which important legal issues may remain unresolved. Therefore, there is no assurance that our pending patent applications will 
result in the issuance of patents or that we will develop additional proprietary products which are patentable. Moreover, patents 
issued or to be issued to us may not provide us with any competitive advantage. Further, if the patent applications we hold or in-
license with respect to our programs, product candidates and companion diagnostic fail to issue, if their breadth or strength of 
protection is threatened, or if they fail to provide meaningful exclusivity for our product candidates, it could dissuade companies 
from collaborating with us to develop product candidates, and threaten our ability to commercialize future products.

Our patents may be challenged by third parties at the United States Patent and Trademark Office ("USPTO"), comparable 
foreign patent offices, or in patent litigation. In addition, it is possible that third parties with products that are very similar to ours 
will circumvent our patents by means of alternate designs or processes or file applications or be granted patents that would block 
or hurt our efforts.

There are no assurances that our patent counsel, lawyers or advisors have given us correct advice or counsel. Opinions 
from such patent counsel or lawyers may not be correct or may be based on incomplete facts. We cannot be certain that we are 
the first to invent or first to file for patent protection for the inventions covered by pending patent applications and, if we are not, 
we may be subject to priority disputes. We may be required to disclaim part or all of the subject matter and/or term of certain 
patents or all of the subject matter and/or term of certain patent applications. There may be prior art of which we are not aware 
that may affect the validity or enforceability of a patent claim. There also may be prior art of which we are aware, but which we 
do not believe affects the validity or enforceability of one or more claims, which may, nonetheless, ultimately be found to affect 
the validity or enforceability of a claim. No assurance can be given that if challenged, our patents would be declared by the USPTO, 
comparable foreign patent offices or a court to be valid or enforceable or that even if found valid and enforceable, a competitor’s 
37

 
technology or product would be found by a court to infringe our patents. The possibility exists that others will develop products 
which have the same effect as our products on an independent basis which do not infringe our patents or other intellectual property 
rights, or will design around the claims of patents that we have had issued that cover our products. The steps we have taken to 
protect our intellectual property may not prevent the misappropriation of our proprietary information and technologies, particularly 
in foreign countries where laws or law enforcement practices may not protect proprietary rights to the same extent as in the United 
States, Europe or Japan. Unauthorized disclosure of our proprietary information could also harm our competitive position. We 
could also inadvertently use our collaborators’ data inappropriately which could lead to liability. We may file patent applications 
but have claims restricted or we may not be able to supply sufficient data to satisfy a patent office to support our claims and, as a 
result, may not obtain the original claims desired or we may receive restricted claims. Alternatively, it is possible that we may not 
receive any patent protection from an application.

Maintaining our patents and applications requires timely payment of fees and other associated costs in the countries of 
filing, and we could inadvertently abandon a patent or patent application (or trademark or trademark application) due to non-
payment of fees, or as a result of a failure to comply with filing deadlines or other requirements of the prosecution process, resulting 
in the loss of protection of certain intellectual property rights in a certain country. Alternatively, we, our collaborators or our patent 
counsel may take action resulting in a patent or patent application becoming abandoned which may not be able to be reinstated, 
or if reinstated, may suffer patent term adjustments. Any of these outcomes could hurt our ability to gain full patent protection for 
our products. Registered trademarks and/or applications for trademark registrations in the United States that belong to us are 
subject to similar risks as described above for patents and patent applications.

Many of our collaboration agreements are complex and may call for licensing or cross-licensing of potentially blocking 
patents, know-how or intellectual property. Due to the potential overlap of data, know-how and intellectual property rights there 
can be no assurance that one of our collaborators will not dispute our right to send data or know-how or other intellectual property 
rights to third parties and this may potentially lead to liability or termination of a program or litigation. There are no assurances 
that the actions of our collaborators would not lead to disputes or cause us to default with other collaborators. We cannot be certain 
that a collaborator will not challenge the validity of licensed patents.

We cannot be certain that any country’s patent and/or trademark office will not implement new rules which could affect 
how we draft, file, prosecute and/or maintain patents and patent applications, or that certain patent rights and/or trademark rights 
will be granted by governmental authorities in particular foreign countries. We cannot be certain that increasing costs for drafting, 
filing, prosecuting and maintaining patent applications and patents will not limit our ability to file for patent protection, or to 
prosecute applications through to grant. We may be forced to abandon or return the rights to specific patents due to a lack of 
financial resources. There is no assurance that we could enter into licensing arrangements at a reasonable cost, or develop or obtain 
alternative technology in respect of patents issued to third parties that incidentally cover our products. Any inability to secure such 
licenses or alternative technology could result in delays in the introduction of some of our products or even lead to prohibition of 
the development, manufacture or sale of certain products by us.

We may file applications for trademark registrations in connection with our product candidates in various jurisdictions, 
including the United States. No assurance can be given that any of our trademark applications will be registered in the United 
States  or  elsewhere,  or  that  the  use  of  any  registered  or  unregistered  trademarks  will  confer  a  competitive  advantage  in  the 
marketplace. Furthermore, even if we are successful in our trademark registrations, the FDA and regulatory authorities in other 
countries  have  their  own  process  for  drug  nomenclature  and  their  own  views  concerning  appropriate  proprietary  names.  No 
assurance can be given that the FDA or any other comparable regulatory authority will accept any of our trademarks or will not 
request reconsideration of one of our trademarks, for use in connection with our drug product candidates, whether currently or at 
some time in the future. The loss, abandonment, or cancellation of any of our trademarks or trademark applications could negatively 
affect the success of the product candidates to which they relate.

Moreover, some of our know-how and technology which is not patented or not patentable may constitute trade secrets. 
Therefore, we require our consultants, advisors and collaborators to enter into confidentiality agreements and our employees to 
enter into invention and non-disclosure agreements. However, no assurance can be given that such agreements will provide for a 
meaningful protection of our trade secrets, know-how or other proprietary information in the event of any unauthorized use or 
disclosure of information. Furthermore, we cannot provide assurance that any of our employees, consultants, contract personnel 
or collaborators, either accidentally or through willful misconduct, will not cause serious negative impact to our programs and/or 
our  strategy. All  of  our  employees  have  signed  confidentiality  agreements,  but  there  can  be  no  assurance  that  they  will  not 
inadvertently or through their misconduct give trade secrets away.

38

Third-party patents or intellectual property infringement claims may result in a reduction in the scope of our patent 
protection and competitive exclusivity with respect to our product candidates. Patent litigation, including defense against third-
party intellectual property claims, may result in us incurring substantial costs.

Patent applications which may relate to or affect our business may have been filed by others.  Such patent applications or 
patents resulting there from may conflict with our technologies, patents or patent applications, potentially reducing the scope or 
strength of our patent protection, and may ultimately be determined to limit or prohibit our freedom to operate with respect to our 
product candidates. Such events could cause us to stop or change the course of our research and development or modify our 
intellectual property strategies. We could also become involved in interference proceedings in connection with one or more of our 
patents or patent applications to determine priority of invention, or in post-grant opposition proceedings at the USPTO or comparable 
foreign patent offices. There can be no guarantees that an interference proceeding or defense of a post-grant opposition would be 
successful or that such an outcome would be upheld on appeal. An unfavorable outcome could require us to cease using the related 
technology or to attempt to license rights to it from the prevailing party. Our business could be harmed if the prevailing party does 
not offer us a license on commercially reasonable terms. Our defense of such interference proceedings may fail and, even if 
successful, may result in substantial costs and distract our management and other employees.

No assurance can be given that our patents, once issued, would be declared by a court to be valid or enforceable, or that 

we would not be found to infringe a competitor’s patent.

Third parties may assert that we are using their proprietary information without authorization. Third parties may also have 
or obtain patents and may claim that technologies licensed to or used by us infringe their patents. Because patent applications can 
take many years to issue, third parties may have currently pending patent applications which may later result in issued patents that 
our product candidates or companion diagnostic may infringe, or which such third parties claim are infringed by the use of our 
technologies. If any third-party patents are held by a court of competent jurisdiction to cover any aspect of our product candidates, 
including the formulation or method of use of such product candidate, the holders of any such patents may be able to block our 
ability to commercialize such product candidate unless we obtain a license under the applicable patents, or until such patents 
expire. In any such case, such a license may not be available on commercially reasonable terms or at all. We may attempt to 
invalidate a competitor’s patent or trademark. There is no assurance such action will ultimately be successful and, even if initially 
successful, it could be overturned upon appeal. In addition, any legal action that seeks damages or an injunction to stop us from 
carrying on our commercial activities relating to the affected technologies could subject us to monetary liability. Some of our 
competitors may be able to sustain the costs of complex patent litigation more effectively than we can because they have substantially 
greater resources.

Parties making claims against us for alleged infringement of their intellectual property rights may obtain injunctive or 
other equitable relief, which could effectively block our ability to further develop and commercialize one or more of our product 
candidates. Defense of these claims, regardless of their merit, would involve substantial litigation expense and would be a substantial 
diversion of employee resources from our business. In the event of a successful claim of infringement against us, we could be 
required to redesign our infringing products or obtain a license from such third party to continue developing and commercializing 
our products and technology. However, we may not be able to obtain any required license on commercially reasonable terms, or 
at all. Even if we are able to obtain a license, it may be non-exclusive, thereby giving our competitors access to the same technologies 
licensed to us. It may be impossible to redesign our products and technology, or it may require substantial time and expense, which 
could force us to cease commercialization of one or more of our product candidates, or some of our business operations, which 
could materially harm our business. In addition, in any such proceeding, we may be required to pay substantial damages, including 
treble damages and attorneys’ fees in the event we are found liable for willful infringement.

Our intellectual property may be infringed upon by a third party.

Third parties may infringe one or more of our issued patents or trademarks. We cannot predict if, when or where a third 
party may infringe one or more of our issued patents or trademarks. There is no assurance that we would be successful in a court 
of law to prove that a third party is infringing one or more of our issued patents. Even if we are successful in proving in a court 
of law that a third party is infringing one or more of our issued patents there can be no assurance that we would be successful in 
halting their infringing activities, for example, through a permanent injunction, or that we would be fully or even partially financially 
compensated for any harm to our business. We may be forced to enter into a license or other agreement with the infringing third 
party at terms less profitable or otherwise less commercially acceptable to us than if the license or agreement were negotiated 
under conditions between those of a willing licensee and a willing licensor. We may not become aware of a third party infringer 
within legal timeframes that would enable us to seek adequate compensation, or at all, thereby possibly losing the ability to be 
compensated for any harm to our business. Such a third-party may be operating in a foreign country where the infringer is difficult 
to locate, where we do not have issued patents and/or the patent laws may be more difficult to enforce. Some third-party infringers 
may  be  able  to  sustain  the  costs  of  complex  patent  infringement  litigation  more  effectively  than  we  can  because  they  have 
39

 
substantially greater resources. Any inability to stop third-party infringement could result in loss in market share of some of our 
products or even lead to a delay, reduction and/or inhibition of the development, manufacture or sale of certain products by us. 
There is no assurance that a product produced and sold by a third-party infringer would meet our or other regulatory standards or 
would be safe for use. Such third-party infringer products could irreparably harm the reputation of our products thereby resulting 
in substantial loss in market share and profits.

Third parties may seek to obtain approval of a generic version of approved products.  Defense against entry of a generic 
product may result in us incurring substantial costs and ultimate failure to prevail against approval of a generic product could 
result in a substantial loss of market share and profits.

Even if we are successful in obtaining regulatory approval to sell any of our product candidates in one or more countries, 
we cannot be certain that our patents and other intellectual property rights will ultimately prevent approval during the patent term 
of generic products developed and commercialized by third parties.  A generic manufacturer may seek approval of a generic version 
of any of our products in the United States by filing an Abbreviated New Drug Application ("ANDA"), with the FDA asserting 
that our patents are invalid and/or unenforceable to maintain market exclusivity for any of our products, if approved. We cannot 
predict if, or when, one or more generic manufacturers may attempt to seek regulatory approval for a generic version of any of 
our products, if approved. There is no assurance that we will ultimately be successful in a court of law to prevent entry of a generic 
version of any of our products during the applicable patent term and we may incur substantial costs defending our patents and 
intellectual property rights. An inability to stop a generic manufacturer from selling a generic version of our products could result 
in a substantial loss of market share and profits or even preclude the ability to continue to commercialize any of our products, if 
approved.

Risks Related to Our Shares of Common Stock

Our share price is volatile and may be influenced by numerous factors that are beyond our control.

A low share price and low market valuation may make it difficult to raise sufficient additional cash due to the significant 
dilution to current stockholders. Market prices for shares of biotechnology and biopharmaceutical companies such as ours are 
often volatile. Factors such as clinical and regulatory developments regarding our products or processes, developments regarding 
potential or future third-party collaborators, announcements of technological innovations, new commercial products, patents, the 
development of proprietary rights by us or by others or any litigation relating to these rights, regulatory actions, general conditions 
in the biotechnology and pharmaceutical industries, failure to meet analysts’ expectations, publications, financial results or public 
concern over the safety of biopharmaceutical and biotechnological products, economic conditions in the United States and other 
countries, terrorism and other factors could have a significant effect on the share price for our shares of common stock. Any setback 
or delay in the clinical development of our programs could result in a significant decrease in our share price. In recent years the 
stock of other biotechnology and biopharmaceutical companies has experienced extreme price fluctuations that have been unrelated 
to the operating performance of the affected companies. There can be no assurance that the market price of our shares of common 
stock will not experience significant fluctuations in the future, including fluctuations that are unrelated to our performance. These 
fluctuations may result due to macroeconomic and world events, national or local events, general perception of the biotechnology 
industry or to a lack of liquidity. In addition, other biotechnology companies' or our competitors’ programs could have positive 
or negative results that impact their stock prices and their results or experience stock price fluctuations that could have a positive 
or negative impact on our stock price, regardless whether such impact is direct or not.

Stockholders may not agree with our business, scientific, clinical and financial strategy, including additional dilutive 
financings, and may decide to sell their shares or vote against such proposals. Such actions could materially impact our stock 
price. In addition, portfolio managers of funds or large investors can change or change their view on us and decide to sell our 
shares. These actions could have a material impact on our stock price. In order to complete a financing, or for other business 
reasons, we may elect to consolidate our shares of common stock. Investors may not agree with these actions and may sell our 
shares. We may have little or no ability to impact or alter such decisions.

40

Our principal stockholders control the majority of our shares, and their actions may significantly influence matters 

submitted to our stockholders for approval and our share price.

Based on the information available to us as of December 31, 2016, our stockholders and their affiliates who owned more 
than 5% of our outstanding common stock collectively owned 40% of our outstanding common stock. Baker Bros. Advisors, L.L.C. 
("Baker Brothers") and Boxer Capital, LLC ("Boxer Capital") and their affiliates collectively own 29% of our outstanding common 
stock. In addition, in conjunction with certain financing transactions, we granted to Baker Brothers and Boxer Capital each the 
right to nominate a member of our Board of Directors and the right to appoint an observer on our Board of Directors. Collectively 
Baker Brothers and Boxer Capital may have significant influence over matters submitted to our stockholders for approval, including 
the election and removal of directors and the approval of any merger, consolidation, or sale of all or substantially all of our assets. 
Furthermore, as a thinly traded stock, if Baker Brothers, Boxer Capital or any other of our major stockholders determine to exit 
from the industry or from their holdings in us, for whatever reason, the impact on our share price could be detrimental over a 
prolonged period of time.

Future sales and issuances of our common stock or rights to purchase common stock, including pursuant to our equity 
incentive plans, could result in additional dilution of the percentage ownership of our stockholders and could cause our stock 
price to fall.

We expect that significant additional capital will be needed in the future to continue our planned operations. To the extent 
we raise additional capital by issuing equity securities, our stockholders may experience substantial dilution. We may sell common 
stock, convertible securities or other equity securities in one or more transactions at prices and in a manner we determine from 
time to time. If we sell common stock, convertible securities or other equity securities in more than one transaction, investors may 
be materially diluted by subsequent sales. These sales may also result in material dilution to our existing stockholders, and new 
investors could gain rights superior to our existing stockholders.

Pursuant to our 2013 Equity Incentive Plan ("the 2013 Plan"), and our 2013 Employee Stock Purchase Plan ("the ESPP"), 
our management is authorized to grant stock options and other equity-based awards to our employees, directors and consultants, 
and to sell our common stock to our employees, respectively. Any increase in the number of shares outstanding as a result of the 
exercise of outstanding options, the vesting or settlement of outstanding stock awards, or the purchase of shares pursuant to the 
ESPP will cause our stockholders to experience additional dilution, which could cause our stock price to fall.

Our ability to use our U.S. net operating loss carryforwards and certain other tax attributes may be limited.

Under  Section 382  of  the  Internal  Revenue  Code  of  1986,  as  amended  ("the  Code"),  if  a  corporation  undergoes  an 
"ownership change," 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 U.S. net operating loss carryforwards ("NOLs"), and other pre-change U.S. tax 
attributes (such as research tax credits) to offset its post-change income may be limited. We may experience ownership changes 
in the future as a result of subsequent shifts in our stock ownership. As a result, if we earn net taxable income, our ability to use 
our pre-change U.S. net operating loss 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.

Because  we  do  not  anticipate  paying  any  cash  dividends  on  our  common  stock  in  the  foreseeable  future,  capital 

appreciation, if any, would be our stockholders’ only source of gain.

We have never declared or paid any cash dividends on our common shares, and we currently expect that earnings, if any, 
and cash flow will primarily be retained and used in our operations, including servicing any debt obligations we may have now 
or in the future. Accordingly, although we do not anticipate paying any dividends in the foreseeable future, we may not be able to 
generate sufficient cash flow in order to allow us to pay future dividends on, or make any distributions with respect to our common 
stock. As a result, capital appreciation, if any, of our common stock would be our stockholders’ sole source of gain on their 
investment in our common stock for the foreseeable future.

41

 
 
 
Item 1B.     Unresolved Staff Comments

None.

Item 2.     Properties

Our  corporate  headquarters  is  located  at  9393 Towne  Centre  Drive,  San  Diego,  California  92121  where  we  occupy 
approximately 18,000 square feet of office and lab space. The lease will expire on January 31, 2018. We believe that our existing 
facilities are adequate to meet our current needs. 

Item 3.     Legal Proceedings

None.

Item 4.     Mine Safety Disclosures

Not applicable.

42

       
  
 
 
PART II

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

          Our common stock has been listed on The NASDAQ Capital Market since July 15, 2013 under the symbol "MRTX". 
Prior to that date, there was no public market for our common stock in the United States as our common stock was listed on the 
Toronto Stock Exchange.

On March 3, 2017, the last reported sale price for our common stock on The NASDAQ Capital Market was $5.60 per 
share. The following table sets forth the range of high and low sales prices per share of our common stock as reported on The 
NASDAQ Capital Market for the period indicated.

Year Ended December 31, 2016

Fourth Quarter

Third Quarter

Second Quarter

First Quarter

Year Ended December 31, 2015

Fourth Quarter

Third Quarter

Second Quarter

First Quarter

High

Low

$

$

6.70

7.22

$ 24.43

$

$

$

4.60

4.40

5.31

$ 30.85

$ 17.94

$ 43.20

$ 29.14

$ 52.00

$ 20.68

$ 37.43

$ 25.21

$ 30.76

$ 18.26

As of March 3, 2017, we had 16 stockholders of record, which excludes stockholders whose shares were held in nominee 
or street name by brokers. The actual number of common stockholders is greater than the number of record holders, and includes 
stockholders who are beneficial owners, but whose shares are held in street name by brokers and other nominees. This number of 
holders of record also does not include stockholders whose shares may be held in trust by other entities. We have never declared 
or paid any cash dividends on our capital stock. We currently intend to retain any future earnings for funding operations and, 
therefore, do not anticipate paying any cash dividends in the foreseeable future.

43

 
  
Stock Performance Graph and Cumulative Total Return

TT

The graph below shows the cumulative total stockholder return assuming the investment of $100 on July 15, 2013 (and the 
reinvestment of dividends thereafter) in each of (i) Mirati Therapeutic, Inc.’s common stock, (ii) the NASDAQ Composite Index
and (iii) the NASDAQ Biotechnology Index. The comparisons in the graph below are based upon historical data and are not 
indicative of, or intended to forecast, future performance of our common stock or Indexes.

COMPARISON OF 41 MONTH CUMULATIVE TOTAL RETURN*
Among Mirati Therapeutics, Inc., the NASDAQ Composite Index 
and the NASDAQ Biotechnology Index

$600

$500

$400

$300

$200

$100

$0
7/15/13

9/13

12/13

3/14

6/14

9/14

12/14

3/15

6/15

9/15

12/15

3/16

6/16

9/16

12/16

Mirati Therapeutics, Inc.

NASDAQ Composite

NASDAQ Biotechnology

*$100 invested on 7/15/13 in stock or 6/30/13 in index, including reinvestment of dividends.
Fiscal year ending December 31.

Recent Sales of Unregistered Securities

During the twelve months ended December 31, 2016, we issued and sold the following unregistered securities:

WW
Warrant exer

cise

In 2011 and 2012, we issued common stock warrants in connection with the issuance of common stock through private 
placements. The warrant certificates provide that the warrant holder may elect to exercise their warrant and, in lieu of making the 
cash payment upon such exercise, receive upon such exercise a net number of common shares determined according to a formula 
prescribed in the warrant certificate. For the twelve months ended December 31, 2016, four holders of warrants exercised 289,789
shares of the Company's common stock were exercised via cashless exercises and 313,756 shares were exercised for cash generating 
proceeds of $2.1 million, resulting in the issuance of an aggregate of 603,545 shares of our common stock.

The issuances of the securities described above were deemed to be exempt from registration under the Securities Act of 
1933, as amended, in reliance on Rule 506 of Regulation D in that each issuance of securities was to an accredited investor under 
Rule 501 of Regulation D and did not involve a public offering. 
The recipients of securities in each of these transactions acquired 
the securities for investment only and not with a view to or for sale in connection with any distribution thereof and appropriate 
to the securities issued in these transactions. There were no underwriters employed in connection with any
legends were affixed 
of the transactions set forth above.

ff

ff

Purchases of Equity Securities by the Issuer and 

r

Affiliated Purchasers

None.

44

Item 6.  Selected Consolidated Financial Data

The following table presents selected historical financial data for the years ended December 31, 2016, 2015, 2014, 2013 
and 2012. All the selected historical financial data has been derived from our Audited Consolidated Financial Statements and is 
stated in thousands except for per share information.

Please read the following selected financial data in conjunction with Item 7, "Management's Discussion and Analysis of 
Financial Condition and Results of Operations" and our Audited Consolidated Financial Statements and related Notes thereto 
included elsewhere in this Annual Report on Form 10-K.

Year Ended December 31,

2016

2015

2014

2013

2012

Statements of Operations Data:

Loss from operations

Net loss

Comprehensive loss

Basic and diluted net loss per share

Weighted average common shares outstanding, 

basic and diluted

$

$

(83,779) $
(83,118)
(83,143)

(64,714) $
(64,544)
(64,507)

(39,104) $
(43,698)
(43,684)

(31,999) $
(52,859)
(52,872)

(4.20) $

(3.82) $

(3.24) $

(4.78) $

(20,498)
(20,286)
(20,286)
(3.00)

19,787,349

16,901,826

13,483,467

11,057,040

6,762,985

2016

2015

2014

2013

2012

As of December 31,

Balance Sheet Data:

Cash, cash equivalents and short-term investments $

56,734

$

122,327

$

29,303

$

62,070

$

Working capital

Total assets

Accumulated deficit

Total stockholders' equity

44,553

63,444
(389,751)
48,309

115,604

128,017
(306,633)
118,176

27,261

33,479
(242,089)
28,062

25,563

64,537
(198,391)
25,885

36,983

33,989

39,801
(140,491)
34,416

45

 
 
 
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 thereto included elsewhere in this Annual Report on Form 10-K. Some of 
the information contained in this discussion and analysis or set forth elsewhere in this Annual Report on Form 10-K, including 
information with respect to our plans and strategy for our business and related financing, includes forward-looking statements 
that involve risks and uncertainties. As a result of many factors, including those factors set forth in the "Risk Factors" section of 
this Annual Report on Form 10-K, our actual results could differ materially from the results described in or implied by the forward-
looking statements contained in the following discussion and analysis.

References in the following discussion to "we", "our", "us", "Mirati" or "the Company" refer to Mirati Therapeutics, Inc. and its 
subsidiaries. 

Company Overview 

We are a clinical-stage biopharmaceutical company focused on developing a pipeline of oncology products including 
candidates intended to treat specific genetic and epigenetic drivers of cancer in selected subsets of cancer patients with unmet 
needs. Additionally, we are evaluating our product candidates in combination with checkpoint inhibitors (anti-PD-1 and PD-L1) 
to determine whether they will enhance the efficacy of those agents in patients with non-small cell lung cancer ("NSCLC") and 
other solid tumors. We believe that an increased understanding of the genomic factors that drive tumor cell growth can lead to the 
development of cancer drugs that target these genomic factors, resulting in increased efficacy while reducing side effects. 

Our clinical pipeline consists of three product candidates: glesatinib, sitravatinib and mocetinostat. Both glesatinib and 
sitravatinib are orally-bioavailable, spectrum-selective kinase inhibitors with distinct target profiles that are in development for 
the treatment of patients with NSCLC and other solid tumors. Glesatinib is in Phase 2 clinical development, and targets the MET 
and Axl receptor tyrosine kinase families ("RTKs"). Sitravatinib is in Phase 1b clinical development and targets genetic alterations 
in RET gene rearrangements, CHR4q12 amplifications, CBL mutations and AXL alterations. We are also evaluating sitravatinib 
in a multi-arm Phase 2 clinical trial to determine their ability to enhance the clinical efficacy of nivolumab, a checkpoint inhibitor 
approved for the treatment of patients with a variety of solid tumors including NSCLC and metastatic Renal Cell Carcinoma 
(“RCC”). Our third candidate is mocetinostat, an orally-bioavailable, Class 1 selective histone deacetylase ("HDAC") inhibitor. 
Mocetinostat is in Phase 1b/2 clinical development in combination with durvalumab, MedImmune Limited’s ("MedImmune") 
anti-PD-L1 immune checkpoint inhibitor, for the treatment of patients with NSCLC. 

Our novel kinase inhibitors, glesatinib and sitravatinib, are intended to treat specific mutations that drive the growth of 
cancer or are implicated in cancer drug resistance or pathogenic processes such as tumor angiogenesis. Sitravatinib is a potent 
inhibitor  of  the Tyro, Axl,  Mer  ("TAM")  family  of  kinases  which  we  believe  may  lead  to  enhanced  anti-tumor  immunity  in 
combination with immune checkpoint inhibitors by changing the tumor microenvironment from a tolerogenic to an immunogenic 
state and increasing anti-tumor immune response by reducing T-cell and macrophage suppressor effects. Our HDAC inhibitor, 
mocetinostat, acts through important epigenetic mechanisms, the effects of which could potentially enhance the efficacy of immune 
checkpoint inhibitors when used in combination.  

Two candidates are in pre-clinical development. The first is a highly-potent and potentially best-in-class LSD1 inhibitor 
with potential for rapid clinical proof-of-concept in small cell lung cancer ("SCLC") or acute myeloid leukemia ("AML"). An 
investigational new drug ("IND") submission is planned for this compound in late 2017. Additionally, a mutant-selective KRAS 
inhibitor program is advancing to candidate selection phase and prototype inhibitors have demonstrated marked tumor regression 
in KRAS mutant tumor models, with an IND candidate selection anticipated by the end of 2017. We plan to identify additional 
drug development opportunities by leveraging our deep scientific understanding of molecular drug targets and mechanisms of 
resistance and potentially in-licensing or internally discovering promising, early-stage novel drug candidates.

We were incorporated under the laws of the State of Delaware on April 29, 2013 as Mirati Therapeutics, Inc. and our 

corporate headquarters are located in San Diego, California.

Program Updates

Glesatinib

We presently have two ongoing clinical trials of glesatinib: a single-arm Phase 2 clinical trial for the treatment of NSCLC 
patients with genetic alterations of MET and a Phase 1b clinical trial in patients with genetic alterations of MET and Axl in NSCLC 
and other solid tumors.

46

 
 
 
 
 
 
On January 5, 2017, we provided a clinical update focused on our experience with a spray dried dispersion (“SDD”) 
formulation of glesatinib that was implemented in the ongoing Phase 1b and Phase 2 clinical trials in May 2016. As more fully 
described under "Item 1. Business" section, we reported the following (all data as of a cut-off date of December 2, 2016):

•  Adverse-event related (AE-related) dose reductions occurred in 17% of patients treated with the SDD formulation versus 

46% of patients treated with the prior soft gel formulation.

• 

• 

In 13 evaluable patients with Met Exon 14 deletion across both the Phase 1b and Phase 2 clinical trials, 4 patients achieved 
a confirmed response and two patients achieved an unconfirmed response (one of which remained on study) reflecting 
an objective response rate (“ORR”) of 46% including confirmed and unconfirmed responses. Tumor reductions were 
observed in 11 of 13 patients, the longest duration of a patient on study was more than 55 weeks and the patient remained 
on study.

In 8 evaluable patients with MET amplification, two patients achieved an unconfirmed response (neither remained on 
study).  Tumor reductions were observed in six of the eight evaluable patients, the longest duration of a patient on study 
was more than 24 weeks and the patient remained on study.

The Company expects to provide an additional update on the glesatinib program in the second half of 2017. 

Sitravatinib

Sitravatinib is being evaluated in a Phase 1b expansion clinical trial designed to evaluate its safety and efficacy in multiple 
pre-specified  cohorts  of  cancer  patients  with  RET  gene  rearrangements,  CHR4q12  amplifications,  CBL  mutations  and  AXL
alterations.

As more fully described under "Item 1. Business" section, on January 5, 2017 we provided a clinical update of the ongoing 

Phase 1b clinical trial as follows (all data as of a cut-off date of December 9, 2016): 

•  A total of six NSCLC patients with RET gene rearrangements had been enrolled, four of whom were evaluable. 

•  Of the four evaluable patients, one patient achieved a confirmed PR and one patient achieved an unconfirmed PR on 
initial scan, representing a 50% ORR, including confirmed and unconfirmed responses. Both patients remained on study. 
Tumor reductions were observed in all four evaluable patients and the longest duration of a patient on study was more 
than 46 weeks and the patient remained on study. 

•  The Phase 1b trial is also enrolling NSCLC patients with CBL mutations, CHR4q12 amplification and AXL alterations. 

As of the data cut-off date, no patients with these genetic mutations were evaluable.

Sitravatinib is also being evaluated in combination with nivolumab, a checkpoint inhibitor approved for the treatment of 
patients  with  a  variety  of  solid  tumors  including  NSCLC  and  metastatic  RCC.  Pre-clinical  data  indicate  sitravatinib  is  an 
exceptionally potent inhibitor of the TAM and split (KDR, KIT, PDGFRA) family tyrosine kinases which regulate multiple stages 
in the cancer immunity cycle and are thought to enhance anti-tumor immunity by improving the efficacy of checkpoint inhibitors 
(anti PD-1/PD-L1). Enrollment of this multicenter Phase 2 clinical trial in patients with NSCLC commenced in November 2016.

The Company expects to provide an additional update on the sitravatinib program in the third quarter of 2017.

Mocetinostat

A Phase 1b/2 clinical trial combining mocetinostat and durvalumab, MedImmune’s monoclonal antibody inhibiting PD-
L1, continues to enroll patients with advanced solid tumors and NSCLC. The Company expects to provide an additional update 
on the mocetinostat program mid-year 2017.

47

 
 
 
 
 
 
Liquidity Overview 

At December 31, 2016, we had $56.7 million of cash, cash equivalents and short-term investments compared to $122.3 
million at December 31, 2015. In January 2017, we completed a public offering of our common stock and pre-funded common 
stock warrants that generated net proceeds of $66.8 million. We have not generated any revenue from product sales. To date, we 
have funded our operations primarily through the sale of our common stock and through up-front payments, research funding and 
milestone payments under previous collaborative arrangements. To fund future operations, we will likely need to raise additional 
capital as discussed more fully below under the heading "Liquidity and Capital Resources." 

Critical Accounting Policies and Significant Judgments and Estimates

Our discussion and analysis of financial condition and results of operations are based upon our consolidated financial 
statements, which have been prepared in accordance with U.S. generally accepted accounting principles. The preparation of these 
financial statements requires us to make significant estimates and judgments that affect the reported amounts of assets, liabilities, 
revenue and expenses and related disclosures. On an ongoing basis, our actual results may differ significantly from our estimates.

While our significant accounting policies are more fully described in Note 2 to our consolidated financial statements 
appearing  elsewhere  in  this Annual  Report  on  Form  10-K,  we  believe  the  following  accounting  policies  to  be  critical  to  the 
judgments and estimates used in the preparation of our consolidated financial statements.

Accrued Research and Development Expenses 

We accrue and expense clinical trial activities performed by third parties based upon estimates of the proportion of work 
completed over the life of the individual clinical trial and patient enrollment rates in accordance with agreements established with 
Clinical Research Organizations ("CROs") and clinical trial sites. We determine the estimates by reviewing contracts, vendor 
agreements and purchase orders, and through discussions with internal clinical personnel and external service providers as to the 
progress or stage of completion of trials or services and the agreed-upon fee to be paid for such services. However, 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. 

We make estimates of our accrued expenses as of each balance sheet date in our financial statements based on facts and 
circumstances known to us at that time. If the actual timing of the performance of services or the level of effort varies from the 
estimate, we will adjust the accrual accordingly. Nonrefundable advance payments for goods and services, including fees for 
process development or manufacturing and distribution of clinical supplies that will be used in future research and development 
activities, are deferred and recognized as expense in the period that the related goods are consumed or services are performed. 

Share-Based Compensation

We measure and recognize compensation expense for share-based payments based on estimated fair value. We estimate 
the fair value of stock options granted using the Black-Scholes option-pricing model. The Black-Scholes option- pricing model 
requires  the  use  of  certain  estimates  and  highly  judgmental  assumptions  that  affect  the  amount  of  share-based  compensation 
expense recognized in our consolidated financial statements. These assumptions include the historical volatility of our stock price, 
expected term of the options, the risk-free interest rate and expected dividend yields. Share-based compensation is recognized 
using the graded accelerated vesting method. If any of the assumptions used in our calculation change significantly, share-based 
compensation expense may differ materially from what we have recorded in the current period.

Financial Operations Overview 

Research and Development Expenses

Research and development expenses consist primarily of: 

• 

• 

salaries and related expenses for personnel, including expenses related to stock options or other share-based 
compensation granted to personnel in development functions;

fees paid to external service providers such as CROs and contract manufacturing organizations related to clinical 
trials;

48

 
 
 
 
 
 
 
• 

contractual obligations for clinical development, clinical sites, manufacturing and scale-up, and formulation of 
clinical drug supplies; and 

• 

costs for allocated facilities and depreciation of equipment. 

We record research and development expenses as incurred. We account for nonrefundable advance payments for goods 
and services that will be used in future research and development activities as expense when the services have been performed or 
when the goods have been received. At this time, due to the risks inherent in the clinical development process and the early stage 
of  our  product  development  programs  we  are  unable  to  estimate  with  any  certainty  the  costs  we  will  incur  in  the  continued 
development of glesatinib, sitravatinib and mocetinostat. The process of conducting clinical trials necessary to obtain regulatory 
approval and manufacturing scale-up to support expanded development and potential future commercialization is costly and time 
consuming. Any failure by us or delay in completing clinical trials, manufacturing scale up or in obtaining regulatory approvals 
could lead to increased research and development expense and, in turn, have a material adverse effect on our results of operations. 
We expect that our research and development expenses may increase if we are successful in advancing glesatinib, sitravatinib, 
mocetinostat or any of our preclinical programs into more advanced stages of clinical development.

General and Administrative Expenses

General  and  administrative  expenses  consist  primarily  of  salaries  and  related  benefits,  including  share-based 
compensation,  related  to  our  executive,  finance,  business  development,  legal  and  support  functions.  Other  general  and 
administrative expenses include professional fees for auditing and tax services, rent and utilities and insurance. 

Results of Operations

Comparison of the Years Ended December 31, 2016 and 2015 

The following table summarizes our results of operations for the year ended December 31, 2016 and 2015 (in thousands):

Research and development expenses

General and administrative expenses

Other income, net

Research and Development Expenses

Year Ended December 31,

2016

2015

Increase

(Decrease)

$

68,487

$

48,959

$

15,292

661

15,755

170

19,528
(463)
491

Our research and development efforts during the years ended December 31, 2016 and 2015 were focused primarily on 
our oncology programs, including our two lead kinase programs, glesatinib and sitravatinib, and our HDAC inhibitor program, 
mocetinostat. The following table summarizes our research and development expenses, in thousands:

Third-party research and development expenses:

Glesatinib

Sitravatinib

Mocetinostat

Preclinical and early discovery

Total third-party research and development expenses

Salaries and other employee related expense

Share-based compensation expense

Other research & development costs

Research and development expense

Year Ended December 31,

2016

2015

Increase

(Decrease)

$

29,974

$

21,699

$

7,346

4,613

9,492

51,425

8,963

5,461

2,638

3,250

5,371

6,830

37,150

6,579

3,669

1,561

8,275

4,096
(758)
2,662

14,275

2,384

1,792

1,077

$

68,487

$

48,959

$

19,528

Research  and  development  expenses  for  the  year  ended  December 31,  2016  were  $68.5  million  compared  to  $49.0 
million during the year ended December 31, 2015. The increase of $19.5 million during the year ended December 31, 2016 primarily 
relates to an increase in third-party research and development expense of $14.3 million. The increase in third-party research and 

49

 
 
 
 
 
 
 
 
development expense relates to an increase in expenses associated with development expenses for glesatinib of $8.3 million and 
sitravatinib of $4.1 million and an increase in our ongoing expenses associated with our preclinical and early discovery expenses 
of $2.7 million. The increase in glesatinib expenses is due to our ongoing Phase 2 clinical trial, which began in late 2015, and 
include increased expenses associated with identifying eligible patients and investigator payments. Sitravatinib expenses increased 
in  connection  with  our  ongoing  Phase  1b  clinical  trial  and  include  increased  manufacturing  expenses,  CRO  service  fees  and 
expenses associated with identifying eligible patients. The increase in early discovery expenses is due to a one-time license fee 
of $2.5 million related to an early stage discovery project. 

The increase in salaries and related expense and share-based compensation resulted from an increase in the number of 
research and development employees during the twelve months ended December 31, 2016 compared to the same period of 2015. 
Based upon our current development plans we expect our research and development expenses to continue to increase as we advance 
the clinical development of our current and future drug candidates.

General and Administrative Expenses

General and administrative expenses for the year ended December 31, 2016 were $15.3 million compared to $15.8 million
for the same period in 2015. The comparable level of expenses for the years ended December 31, 2016 and 2015 reflect a consistent 
level of general and administrative activities in both years.

Other Income, Net

Other income, net consisted primarily of interest income of $0.7 million for the year ended December 31, 2016 and $0.2 

million for the year ended December 31, 2015. 

Comparison of the Years Ended December 31, 2015 and 2014 

The  following  table  summarizes  the  results  of  our  operations  for  the  years  ended  December 31,  2015  and  2014  (in 

thousands):

Research and development, net

General and administrative

Restructuring costs

Other income (expense), net

Change in fair value of warrant liability

Year Ended December 31,

2015

2014

Increase
(Decrease)

$

48,959

$

26,071

$

22,888

15,755

—

170

—

12,699

334
(77)
(4,517)

3,056
(334)
247

4,517

50

 
 
 
 
 
Research and Development Expenses

Our research and development efforts during the years ended December 31, 2015 and 2014 were focused primarily on 
our oncology programs, including our two lead kinase programs, glesatinib and sitravatinib, and our HDAC inhibitor program, 
mocetinostat. The following table summarizes our research and development expenses, in thousands:

Third-party research and development expenses:

Glesatinib

Sitravatinib

Mocetinostat

Preclinical and early discovery

Total third-party research and development expenses

Salaries and other employee related expense

Share-based compensation expense

Other research & development costs
Research and development expense

Year Ended December 31,

2015

2014

Increase

(Decrease)

$

21,699

$

7,273

$

14,426

3,250

5,371

6,830

37,150

6,579

3,669

1,561
48,959

$

2,932

4,507

2,946

17,658

4,459

2,565

1,389
26,071

$

318

864

3,884

19,492

2,120

1,104

172
22,888

$

Research  and  development  expenses  for  the  year  ended December 31,  2015 were $49.0  million compared  to $26.1 
million during the year ended December 31, 2014. The increase of $22.9 million for the year ended December 31, 2015 primarily 
relates to an increase in third-party expenses of $19.5 million and to a lesser extent an increase in salaries and other employee 
related expenses. The increase in third-party development expenses primarily relates to an increase in expenses associated with 
our ongoing clinical trials including an increase in related manufacturing expenses, primarily for glesatinib which is currently in 
Phase 2, and to a lesser extent mocetinostat. Additionally, our preclinical and early discovery costs increased for the year ended 
December 31, 2015 compared to the same period of 2014 due to increased chemistry synthesis costs associated with our early 
stage discovery projects, as well as increased data management costs. The increase in salaries and related expense and share-based 
compensation expense, is driven by an increase in the number of research and development employees during the year ended 
December 31, 2015 compared to the same period of 2014. 

General and Administrative Expenses

General and administrative expenses for the year ended December 31, 2015 were $15.8 million compared to $12.7 

million for the same period in 2014. The increase of $3.1 million for the year ended December 31, 2015 is primarily the result 
of increased share-based compensation expenses and increased salaries and related expenses due to an increase in the number 
of general and administrative employees during the twelve months ended December 31, 2015 compared to the same period of 

Other Income (Expense), Net

Other income (expense), net for the year ended December 31, 2015 consisted primarily of interest income of $0.2 million. 
Other income (expense), net for the year ended December 31, 2014 was expense of $0.1 million primarily due to the impact of 
foreign exchange losses partially offset by interest income.

Change in Fair Value of Warrant Liability

The change in fair value of warrant liability represents expense or income associated with fair value adjustments to the 
warrant  liability  recorded  during  the  period.  During  the  year  ended  December  31, 2014,  we  recorded  expense  of  $4.5 
million associated  with  the  change  in  fair  value  of  warrant  liability.  During  the  second  half  of  2014,  we  amended  all  of  the 
outstanding warrant agreements to allow for the warrants to be denominated in U.S. Dollars. As a result of this amendment, the 
warrants qualified for equity classification, were reclassified into stockholders' equity at their fair value as of the amendment dates 
and revaluations of fair value are no longer required. 

51

 
 
 
 
 
 
 
Liquidity and Capital Resources

To date, we have funded our operations primarily through the sale of our common stock and through up-front payments, 
research funding and milestone payments under previous collaborative arrangements. Since inception, we have primarily devoted 
our resources to funding research and development programs, including discovery research, preclinical and clinical development 
activities.

At December 31, 2016, we had $56.7 million of cash, cash equivalents and short-term investments compared to $122.3 
million at December 31, 2015. In January 2017 we completed a public offering of our common stock and pre-funded common 
stock warrants that generated net proceeds of $66.8 million and in 2015 we completed two public offerings of our common stock 
that generated net proceeds of $143.3 million.

We have incurred losses in each year since our inception. Our net losses were $83.1 million, $64.5 million and $43.7 
million for the years ended December 31, 2016, 2015 and 2014, respectively. As of December 31, 2016, we had an accumulated 
deficit of $389.8 million. Substantially all of our operating losses resulted from expenses incurred in connection with our product 
development programs, our research activities and general and administrative costs associated with our operations. 

Based  on  our  current  and  anticipated  level  of  operations,  we  believe  that  our  cash,  cash  equivalents  and  short-term 
investments, together with the $66.8 million of net proceeds from the public offering of our common stock and pre-funded common 
stock warrants in January 2017, will be sufficient to meet our anticipated obligations for at least one year from the date this annual 
report on Form 10-K is filed with the SEC. To fund future operations, we will likely need to raise additional capital. The amount 
and timing of future funding requirements will depend on many factors, including the timing and results of our ongoing development 
efforts, the potential expansion of our current development programs, potential new development programs and related general 
and administrative support. We anticipate that we will seek to fund our operations through public or private equity or debt financings 
or other sources, such as potential collaboration agreements. We cannot make assurances that anticipated additional financing will 
be available to us on favorable terms, or at all. Although we have previously been successful in obtaining financing through our 
equity securities offerings, there can be no assurance that we will be able to do so in the future. 

The following table provides a summary of the net cash flow activity for each of the periods set forth below (in thousands):

Net cash used in operating activities

Net cash provided by (used in) investing activities

Net cash provided by financing activities

Increase (decrease) in cash

Net cash used in operating activities

Year Ended December 31,

$

2016
(68,017) $
38,255

2,652
(27,110)

2015
(50,714) $
(50,753)
144,367

42,900

2014
(32,748)
24,219

887
(7,642)

Net cash used for operating activities was $68.0 million, $50.7 million and $32.7 million for the years ended December 31, 
2016, 2015 and 2014, respectively. Cash used in operating activities during 2016 primarily related to our net loss of $83.1 million, 
adjusted for non-cash items such as share-based compensation expense of $10.6 million and net cash inflows from a change in 
our operating assets and liabilities of $4.3 million. Cash used in operating activities during 2015 primarily related to our net loss 
of $64.5 million, adjusted for non-cash items such as share-based compensation expense of $10.3 million, amortization of premium 
on investments of $0.3 million, and net cash inflows from a change in our operating assets and liabilities of $3.0 million. Cash 
used in operating activities during 2014 primarily related to our net loss of $43.7 million, adjusted for non-cash items such as the 
share-based compensation expense of $7.1 million, change in fair value of warrant liability of $4.5 million, amortization of premium 
on investment of $0.5 million and net cash outflows from a change in our operating assets and liabilities of $1.4 million. 

Net cash provided by (used in) investing activities

Investing activities provided cash of $38.3 million and $24.2 million for the years ended December 31, 2016 and 2014, 
respectively and used cash of $50.8 million for the year ended December 31, 2015. The net cash provided by investing activities 
during 2016 is primarily a result of increased disposals and maturities of short-term investments partially offset by purchases of 
short-term investments. The net cash used by investing activities during 2015 is primarily a result of increased purchases of short-
term investments due to our February and September 2015 public offerings of common stock partially offset by disposals and 

52

 
 
 
 
 
 
 
 
maturities of short-term investments. The net cash provided by investing activities during 2014 was primarily due to disposal and 
maturities of short-term investments offset by purchases of short-term investments. 

Net cash provided by financing activities

Net  cash  provided  by  financing  activities  was  $2.7  million,  $144.4  million  and  $0.9  million  for  the  years  ended 
December 31, 2016, 2015 and 2014, respectively. Net cash provided by financing activities during 2016 consists of proceeds from 
the exercise of stock options and warrants of $2.4 million as well as proceeds from purchases pursuant to our employee stock 
purchase plan of $0.3 million. Net cash provided by financing activities during 2015 consists of net proceeds from the issuance 
of common stock from our 2015 public offerings of common stock totaling $143.3 million, proceeds from exercise of common 
stock options and warrants of $0.6 million and proceeds from stock issuances under the employee stock purchase plan of $0.5 
million. Net cash provided by financing activities during 2014 consisted of proceeds from exercise of common stock options and 
warrants of $0.9 million.

Contractual Obligations and Commitments

The following table summarizes our contractual obligations and commitments as of December 31, 2016 that will affect 

our future liquidity (in thousands):

Operating lease obligations(1)

Total Contractual Obligations

Total

Less Than
1 year

1 -3 
Years

3 -5
Years

More Than
5 Years

$

$

330

330

$

$

305

305

$

$

25

25

$

$

— $

— $

—

—

(1)  In June 2014 we entered into a multi-year non-cancelable building lease for office space in San Diego, California. The lease 
expires in January 2018.

We enter into contracts in the normal course of business with clinical sites for the conduct of clinical trials, CROs for 
clinical research studies, professional consultants for expert advice and other vendors for clinical supply manufacturing or other 
services. These contracts generally provide for termination on notice, and therefore are cancelable contracts and not included in 
the table of contractual obligations and commitments. 

Off-Balance Sheet Arrangements

During the years ended December 31, 2016 and 2015, we did not have any off-balance sheet arrangements (as defined 
by applicable SEC regulations) that are reasonably likely to have a current or future material effect on our financial condition, 
results of operations, liquidity, capital expenditures or capital resources.

JOBS Act

In April 2012, the JOBS Act was enacted. Section 107 of the JOBS Act provides that an emerging growth company can 
take advantage of the extended transition period provided in Section 7(a)(2)(B) of the Securities Act for complying with new or 
revised accounting standards. Thus, an emerging growth company can delay the adoption of certain accounting standards until 
those standards would otherwise apply to private companies. We have irrevocably elected not to avail ourselves of this extended 
transition period and, as a result, we will adopt new or revised accounting standards on the relevant dates on which adoption of 
such standards is required for other companies.

We are in the process of evaluating the benefits of relying on other exemptions and reduced reporting requirements 
provided by the JOBS Act. Subject to certain conditions set forth in the JOBS Act, as an “emerging growth company,” we intend 
to rely on certain of these exemptions, including without limitation with respect to, (1) providing an auditor’s attestation report 
on our system of internal controls over financial reporting pursuant to Section 404(b) of the Sarbanes-Oxley Act and (2) complying 
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, 
known as the auditor discussion and analysis. We will remain an emerging growth company until the earliest of (1) the end of the 
fiscal year in which the market value of our common stock that is held by non-affiliates exceeds $700 million as of the end of the 
second fiscal quarter, (2) the end of the fiscal year in which we have total annual gross revenue of $1 billion or more during such 
fiscal year, (3) the date on which we issue more than $1 billion in non-convertible debt in a three-year period, or (4) December 
31, 2018.

53

 
 
 
 
 
 
 
Item 7A.     Quantitative and Qualitative Disclosures about Market Risk

Some of our short-term investments have market risk in that a change in prevailing interest rates may cause the principal 
amount of the investment to fluctuate. Financial instruments that potentially subject us to significant concentrations of credit risk 
consist primarily of cash, cash equivalents and short-term investments. We invest our excess cash primarily in commercial paper 
and debt instruments of financial institutions, corporations, U.S. government-sponsored agencies and the U.S. Treasury. We mitigate 
credit risk by maintaining a well-diversified portfolio and limiting the amount of investment exposure as to institution, maturity 
and investment type. We invest our excess cash in accordance with our investment policy. 

Because of the short-term maturities of our cash equivalents and short-term investments, we do not believe that an increase 
in market rates would have any significant impact on the realized value of our investments. If a 1% change in interest rates were 
to have occurred on December 31, 2016, this change would not have had a material effect on the fair value of our investment 
portfolio as of that date.

54

 
 
Item 8.     Financial Statements and Supplementary Data

The financial statements and supplemental data required by this item are set forth at the pages indicated in Part IV, Item 15

(a)(1) of this annual report.

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 

As  required  by  Rule 13a-15(b) and  Rule  15d-15(b)  of  the  Exchange Act,  our  management,  including  our  principal 
executive officer and our principal financial officer, conducted an evaluation as of the end of the period covered by this Annual 
Report on Form 10-K of the effectiveness of the design and operation of our disclosure controls and procedures. Based on that 
evaluation, management has concluded that as of December 31, 2016, the Company’s disclosure controls and procedures were  
effective at the reasonable assurance level and we believe the consolidated financial statements included in this Form 10-K for 
the year ended December 31, 2016 present, in all material respects, our financial position, results of operations, comprehensive 
loss and cash flows for the periods presented in conformity with U.S. generally accepted accounting principles.  

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 Exchange Act Rule 13a-15(f). 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, 2016, our management assessed the effectiveness of our internal control over financial reporting 
using the criteria set  forth by the Committee  of  Sponsoring Organizations of the Treadway Commission  in Internal Control-
Integrated Framework (2013 Framework). Based on this assessment, our management concluded that, as of December 31, 2016, 
our internal control over financial reporting was effective based on those criteria.

This Annual Report on Form 10-K does not include an attestation report of our registered public accounting firm due to 

a transition period established by the JOBS Act for emerging growth companies.

Changes in Internal Control Over Financial Reporting

There were no changes in our internal control over financial reporting identified in management's evaluation pursuant to 
Rules 13a-15(d) or 15d-15(d) of the Exchange Act during the quarter ended December 31, 2016 that materially affected, or are 
reasonably likely to materially affect, our internal control over financial reporting.

Item 9B.     Other Information

Recently Adopted Accounting Pronouncements 

See “Notes to Financial Statements-Note 3-Recent Accounting Pronouncements” of our annual financial statements. 

55

 
 
 
 
 
 
 
  
 
 
Item 10.     Directors, Executive Officers and Corporate Governance

PART III

The information required by this item with respect to directors is incorporated by reference from the information under 
the captions "Election of Directors," "Section 16(a) Beneficial Ownership Reporting Compliance," and "Code of Ethics" contained 
in  the  proxy  statement  to  be  filed  with  the  SEC  pursuant  to  Regulation 14A  in  connection  with  our  2017  annual  meeting  of 
stockholders. The information required by this item with respect to executive officers appears under Part I of this annual report 
on Form 10-K under the caption "Business-Executive Officers and Directors."

Item 11.     Executive Compensation

 The information required by this item is incorporated by reference to the information under the captions "Non-Employee 
Director  Compensation,"  "Executive  Compensation"  and  "Compensation  Committee  Interlocks  and  Insider  Participation" 
contained in the proxy statement to be filed with the SEC pursuant to Regulation 14A in connection with our 2017 annual meeting 
of stockholders.

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

The  information  required  by  this  item  is  incorporated  by  reference  to  the  information  under  the  captions  "Security 
Ownership of Certain Beneficial Owners and Management" and "Equity Compensation Plan Information" contained in the proxy 
statement to be filed with the SEC pursuant to Regulation 14A in connection with our 2017 annual meeting of stockholders.

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

The information required by this item is incorporated by reference to the information under the captions "Election of 
Directors" and "Certain  Relationships and Related Transactions" contained in the proxy statement to be filed with the SEC pursuant 
to Regulation 14A in connection with our 2017 annual meeting of stockholders.

Item 14.     Principal Accountant Fees and Services

The information required by this item is incorporated by reference to the information under the caption contained in 
"Ratification of Selection of Independent Registered Public Accounting Firm" contained in the proxy statement to be filed with 
the SEC pursuant to Regulation 14A in connection with our 2017 annual meeting of stockholders.

56

         
        
         
         
         
Item 15.  Exhibits, Financial Statement Schedules

PART IV

1. Financial Statements. We have filed the following documents as part of this Annual Report:

Consolidated Financial Statements
Report of Independent Registered Public Accounting Firm

Financial Statements:

Consolidated Balance Sheets

Consolidated Statements of Operations and Comprehensive Loss

Consolidated Statements of Changes in Stockholders' Equity

Consolidated Statements of Cash Flows

Notes to Consolidated Financial Statements

Page

58

59

60

61

62

63

2. Financial Statement Schedules. All schedules are omitted because they are not applicable or the required information is shown 
in the Financial Statements or notes thereto.

57

 
 
 
Report of Independent Registered Public Accounting Firm

The Board of Directors and Stockholders
Mirati Therapeutics, Inc.

We have audited the accompanying consolidated balance sheets of Mirati Therapeutics, Inc. as of December 31, 2016 and 2015, 
and the related consolidated statements of operations and comprehensive loss, changes in stockholders’ equity, and cash flows for 
each of the three years in the period ended December 31, 2016.  These financial statements are the responsibility of the Company’s 
management. Our responsibility is to express an opinion on these financial statements based on our audits.

We conducted our audits in accordance with the standards of the Public Company Accounting Oversight Board (United States). 
Those standards require that we plan and perform the audit to obtain reasonable assurance about whether the financial statements 
are free of material misstatement. We were not engaged to perform an audit of the Company’s internal control over financial 
reporting. Our audits included consideration of internal control over financial reporting as a basis for designing audit procedures 
that are appropriate in the circumstances, 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. An audit also includes examining, on a test 
basis, evidence supporting the amounts and disclosures in the financial statements, assessing the accounting principles used and 
significant estimates made by management, and evaluating the overall financial statement presentation. We believe that our audits 
provide a reasonable basis for our opinion.

In our opinion, the financial statements referred to above present fairly, in all material respects, the consolidated financial position 
of Mirati Therapeutics, Inc. at December 31, 2016 and 2015, and the consolidated results of its operations and its cash flows for 
each of the three years in the period ended December 31, 2016, in conformity with U.S. generally accepted accounting principles.

San Diego, California 
March 9, 2017

     /s/ Ernst & Young LLP 

58

 
 
 
Mirati Therapeutics, Inc.
CONSOLIDATED BALANCE SHEETS
(in thousands, except share and per share data)

ASSETS

Current assets

Cash and cash equivalents

Short-term investments

Other current assets
Total current assets

Property and equipment, net

Other long-term assets

Total assets

LIABILITIES AND STOCKHOLDERS' EQUITY

Current liabilities

Accounts payable and accrued liabilities

Total current liabilities

Other liabilities

Total liabilities

Commitments and contingencies
Stockholders' equity

December 31,

2016

2015

$

22,383

$

34,351

2,821

59,555

629

3,260

49,493

72,834

3,075

125,402

614

2,001

$

$

63,444

$

128,017

15,002

$

15,002

133

15,135

9,798

9,798

43

9,841

Preferred stock, $0.001 par value, 10,000,000 shares authorized; none issued and
outstanding at both December 31, 2016 and December 31, 2015
Common stock, $0.001 par value; 100,000,000 authorized; 19,937,095 and 19,282,935
issued and outstanding at December 31, 2016 and December 31, 2015, respectively
Additional paid-in capital

Accumulated other comprehensive income

Accumulated deficit

Total stockholders' equity

—

20

428,507

9,533
(389,751)
48,309

—

19

415,232

9,558
(306,633)
118,176

Total liabilities and stockholders' equity

$

63,444

$

128,017

See accompanying notes

59

 
 
 
 
 
 
 
 
 
 
Mirati Therapeutics, Inc.
CONSOLIDATED STATEMENTS OF OPERATIONS AND COMPREHENSIVE LOSS
(in thousands, except share and per share data)

Year Ended December 31,

2016

2015

2014

Expenses

Research and development

General and administrative

Restructuring costs

Total operating expenses

Loss from operations

Other income (expense), net

Change in fair value of warrant liability
Net loss

Unrealized gain (loss) on available-for-sale investments
Comprehensive loss

Basic and diluted net loss per share

$

68,487

$

48,959

$

15,292

—

83,779
(83,779)
661

—
(83,118) $
(25) $
(83,143) $
(4.20) $

15,755

—

64,714
(64,714)
170

—
(64,544) $
37
$
(64,507) $
(3.82) $

$

$

$

$

Weighted average common shares outstanding, basic and diluted

19,787,349

16,901,826

26,071

12,699

334

39,104
(39,104)
(77)
(4,517)
(43,698)
14
(43,684)
(3.24)
13,483,467

See accompanying notes

60

 
 
 
 
Mirati Therapeutics, Inc.
CONSOLIDATED STATEMENTS OF CHANGES IN STOCKHOLDERS' EQUITY
(in thousands, except share data)

Balance at January 1, 2014

Net loss for the year

Share-based compensation expense

Reclassification of warrants from liability

Exercise of options for cash

Net exercise of warrants

Unrealized gain on investments

Balance at December 31, 2014

Net loss for the year

Share-based compensation expense

Issuance of common stock, net of costs
Issuance of common stock from Employee Stock

Purchase Plan ("ESPP")

Exercise of options for cash

Net exercise of warrants

Unrealized gain on investments

Balance at December 31, 2015

Net loss for the year

Share-based compensation expense

Issuance of common stock from ESPP

Exercise of options for cash

Exercise of warrants for cash

Net exercise of warrants

Unrealized loss on investments

Balance at December 31, 2016

Common Stock

Shares

Amount

13,446,976

—

—

—

76,224

43,526

—

13,566,726

$

—

—

4,837,500

32,645

36,566

809,498

—

19,282,935

$

—

—

28,483

22,132

313,756

289,789

—

19,937,095

$

13

—

—

—

1

—

—

14

—

—

4

—

—

1

—

19

—

—

—

—

1

—

—

20

Additional
paid-in
capital

214,756

Accumulated
other
comprehensive
income

Accumulated
deficit

Total
stockholders'
equity

9,507

(198,391)

25,885

—

7,050

36,931

886

993

—

—

—

—

—

—

14

(43,698)

(43,698)

—

—

—

—

—

7,050

36,931

887

993

14

$ 260,616

$

9,521

$

(242,089) $

28,062

—

10,254

143,289

522

552

(1)

—

—

—

—

—

—

—

37

(64,544)

(64,544)

—

—

—

—

—

—

10,254

143,293

522

552

—

37

$ 415,232

$

9,558

$

(306,633) $

118,176

—

10,624

297

240

2,114

—

—

—

—

—

—

—

—

(25)

(83,118)

(83,118)

—

—

—

—

—

—

10,624

297

240

2,115

—

(25)

$ 428,507

$

9,533

$

(389,751) $

48,309

See accompanying notes

61

 
 
Mirati Therapeutics, Inc.
CONSOLIDATED STATEMENTS OF CASH FLOWS
(in thousands)

Operating activities:

Net loss

Non-cash adjustments reconciling net loss to operating cash flows

Depreciation of property and equipment

Amortization of premium on investments

Share-based compensation expense

Change in fair value of warrant liability

Changes in operating assets and liabilities

Other current assets

Other long-term assets

Accounts payable and accrued liabilities

Other current and long term liabilities
Cash flows used in operating activities

Investing activities:

Purchases of short-term investments

Disposal and maturities of short-term investments

Purchases of property and equipment

Cash flows provided by (used in) investing activities

Financing activities:

Proceeds from issuance of common stock, net of issuance costs

Proceeds from issuance under employee stock purchase plan

Proceeds from exercise of common stock options and warrants

Cash flows provided by financing activities

Increase (decrease) in cash and cash equivalents

Cash and cash equivalents, beginning of year
Cash and cash equivalents, end of year

Supplemental disclosures of non-cash financing activities:

Years Ended December 31,

2016

2015

2014

$ (83,118) $ (64,544) $

(43,698)

180

7

212

337

10,624

10,254

—

—

254
(1,259)
5,196

99
(68,017)

(70,269)
108,720
(196)
38,255

—

297

2,355

2,652
(27,110)
49,493

279
(1,675)
4,370

53
(50,714)

(104,954)
54,530
(329)
(50,753)

143,293

522

552

144,367

42,900

6,593

199

534

7,050

4,517

(1,209)
(326)
151

21
(32,748)

(10,468)
35,073
(386)
24,219

—

—

887

887
(7,642)
14,235

$

22,383

$

49,493

$

6,593

Net exercise of warrants

$

— $

— $

993

See accompanying notes

62

 
 
 
 
 
 
 
 
 
 
 
 
Mirati Therapeutics, Inc.

Notes to Consolidated Financial Statements

1. Description of Business

Mirati  Therapeutics, Inc.  ("Mirati"  or  the  "Company")  is  a  clinical-stage  biopharmaceutical  company  focused  on 
developing a pipeline of targeted oncology products. The Company focuses its development programs on drugs intended to treat 
specific genetically defined and selected subsets of cancer patients with unmet needs.

The Company's common stock has been listed on the NASDAQ Capital Market since July 15, 2013 under the ticker 
symbol "MRTX."  The Company has a wholly owned subsidiary in Canada, MethylGene, Inc. ("MethylGene"). The Company 
also  has  an  indirect,  wholly-owned  subsidiary,  MethylGene  US  Inc.,  which  was  incorporated  in  Princeton,  New  Jersey  on 
December 20, 2011 and started business activity in 2012. MethylGene US Inc. ceased operations effective January 1, 2014. As a 
result of the arrangement agreement discussed in Note 2 under the heading "Basis of Presentation," Mirati became the parent 
company and the primary operating company during 2013. Refer to Note 2 for further discussion of the Company’s corporate 
structure. 

2. Summary of Significant Accounting Policies

Basis of Presentation

These consolidated financial statements are prepared in accordance with accounting principles generally accepted in the 
United States ("U.S. GAAP"). These consolidated financial statements include the accounts of the Company, MethylGene and 
MethylGene US Inc. All significant inter-company transactions, balances and expenses have been eliminated upon consolidation.

Mirati was incorporated under the laws of the State of Delaware on April 29, 2013. On May 8, 2013, the Company's 
Board of Directors approved and the Company entered into an arrangement agreement ("Arrangement") with MethylGene. Upon 
completion of the Arrangement, MethylGene became the Company's wholly-owned subsidiary. 

These consolidated financial statements are presented in United States ("U.S.") Dollars, which effective January 1, 2013, 

is also the functional currency of the Company.

Use of Estimates

The preparation of the Company's audited consolidated financial statements in conformity with U.S. GAAP requires 
management to make estimates and assumptions that affect the reported amounts of assets and liabilities and disclosure of contingent 
assets and liabilities at the date of the financial statements and the reported amounts of expenses during the reporting period.

Reported amounts and note disclosures reflect the overall economic conditions that are most likely to occur and anticipated 
measures management intends to take. Actual results could differ materially from those estimates. Estimates and assumptions are 
reviewed quarterly. Any revisions to accounting estimates are recognized in the period in which the estimates are revised and in 
any future periods affected.

Cash, Cash Equivalents and Short-term Investments

Cash and cash equivalents consist of cash and highly liquid securities with original maturities at the date of acquisition 
of ninety days or less. Investments with an original maturity of more than ninety days are considered short-term investments and 
have been classified by management as available-for-sale. These investments are classified as current assets, even though the 
stated maturity date may be one year or more beyond the current balance sheet date, which reflects management’s intention to use 
the proceeds from sales of these securities to fund its operations, as necessary. Such investments are carried at fair value, with 
unrealized gains and losses included as a separate component of stockholders’ equity. Realized gains and losses from the sale of 
available-for-sale securities or the amounts, net of tax, reclassified out of accumulated other comprehensive income, if any, are 
determined on a specific identification basis.

63

 
 
 
 
 
 
 
 
Concentration of Credit Risk

The Company invests its excess cash in accordance with its investment policy.  The Company's investments are comprised 
primarily of commercial paper and debt instruments of financial institutions, corporations, U.S. government-sponsored agencies 
and  the  U.S. Treasury. The  Company  mitigates  credit  risk  by  maintaining  a  diversified  portfolio  and  limiting  the  amount  of 
investment exposure as to institution, maturity and investment type. Financial instruments that potentially subject the Company 
to significant credit risk consist principally of cash equivalents and short-term investments.

Property and Equipment, Net 

Property and equipment is stated at historical cost less accumulated depreciation. Historical cost includes expenditures 
that are directly attributable to the acquisition of the items. All repairs and maintenance are charged to net loss during the financial 
period in which they are incurred.

Depreciation of property and equipment is calculated using the straight-line method over the estimated useful lives of  

the assets, as follows:

Computer equipment

Office and other equipment

Laboratory equipment

Leasehold improvements

3 years

6 years

6 years

The lesser of the lease term or the life of the asset

On disposal or impairment of property and equipment, the cost and related accumulated depreciation is removed from 

the consolidated financial statements and the net amount, less any proceeds, is included in net loss.

Impairment of Long-Lived Assets

The Company reviews its long-lived assets for impairment whenever events or changes in circumstances indicate that 
the carrying value of an asset may not be recoverable. If such circumstances are determined to exist, an estimate of undiscounted 
future cash flows produced by the long-lived asset, including its eventual residual value, is compared to the carrying value to 
determine whether impairment exists. In the event that such cash flows are not expected to be sufficient to recover the carrying 
amount of the assets, the assets are written-down to their estimated fair values. Fair value is estimated through discounted cash 
flow models to project cash flows from the asset. The Company recognized no impairment charges for the years ended December 31, 
2016 and 2015 and immaterial impairment charges related to property and equipment for the year ended December 31, 2014.

Reclassification of W

In 2011 and 2012, MethylGene issued common stock warrants in connection with the issuance of common stock through 
private placements (the "2011 Warrants" and the "2012 Warrants"). The exercise prices of the 2011 and 2012 Warrants were 
denominated in Canadian dollars. Upon the issuance of the 2011 and 2012 Warrants, the net proceeds were allocated to common 
stock and warrants based on their relative fair values, and the fair value of the issued common stock warrants was calculated 
utilizing the Black-Scholes option-pricing model. The allocated fair value was then recorded as warrants within stockholders’ 
equity on the consolidated balance sheet.

Effective January 1, 2013, the Company changed its functional currency which changed how the 2011 and 2012 warrants 
were accounted for as they continued to have exercise prices denominated in Canadian dollars. At each reporting period subsequent 
to January 1, 2013, the fair value of the warrant liability was recalculated and any corresponding increase or decrease to the warrant 
liability was recorded as change in fair value of warrant liability on the consolidated statement of operations and comprehensive 
loss. The estimated fair value was determined using the Black-Scholes option-pricing model based on the estimated value of the 
underlying common stock at the valuation measurement date, the remaining contractual term of the warrants, risk-free interest 
rates, expected dividends and expected volatility of the price of the underlying common stock. During the second half of 2014, 
the Company amended all of its outstanding warrant agreements to allow for the warrants to be denominated in U.S. Dollars. As 
a result of this amendment, the amended warrants qualified for equity classification and were reclassified into stockholders’ equity 
at their fair value as of the amendment date, and as of the amendment date, revaluations of fair value are no longer required. For 
the years ended December 31, 2016 and 2015, the company recorded no warrant valuation expense. For the year ended December 
31, 2014, the Company recorded warrant valuation expense of $4.5 million, which is reported as change in fair value of warrant 
liability in the condensed consolidated statement of operations and comprehensive loss.

64

 
 
 
 
 
 
Share-Based Compensation

We measure and recognize compensation expense for share-based payments based on estimated fair value. We estimate 
the fair value of stock options granted using the Black-Scholes option-pricing model. The Black-Scholes option-pricing model 
requires  the  use  of  certain  estimates  and  highly  judgmental  assumptions  that  affect  the  amount  of  share-based  compensation 
expense recognized in our consolidated financial statements. These assumptions include the historical volatility of our stock price, 
expected term of the options, the risk-free interest rate and expected dividend yields. Share-based compensation is recognized 
using the graded accelerated vesting method. If any of the assumptions used in our calculation change significantly, share-based 
compensation expense may differ materially from what we have recorded in the current period.

Investment Tax Credits

The Company's accounts include claims for investment tax credits ("ITCs") relating to scientific research and experimental 
development activities of the Company. The qualification and recording of these activities for investment tax credit purposes are 
established by the Canadian federal and Provincial Tax Acts and are subject to audit by the taxation authorities. Refundable ITCs 
are reflected as reductions of expenses or reductions of the cost of the assets to which they relate when there is reasonable assurance 
that the assistance will be received and all conditions have been complied with. The non-refundable ITCs are carried forward for 
a time and will be recognized when it is more likely than not that the Company will become subject to Canadian federal taxes, at 
which time, these ITCs will be applied as a reduction of tax expense. As operations in Canada ceased in early 2014, there were 
no new ITCs earned for the years ended December 31, 2016 or 2015.

Research and Development Expenses

Research and development expenditures are charged to net loss in the period in which they are incurred and are comprised 
of  the  following  types  of  costs  incurred  in  performing  research  and  development  activities:  clinical  trial  and  related  clinical 
manufacturing  costs,  salaries  and  benefits  including  share-based  compensation  expense,  costs  for  allocated  facilities  and 
depreciation of equipment, contract services, license fees paid in connection with our early discovery efforts and data management 
costs.

Income Taxes

Income taxes have been accounted for using the asset and liability method. Under the asset and liability method, deferred 
tax assets and liabilities are recognized for the future tax consequences attributable to differences between the financial carrying 
amounts of existing assets and liabilities and their respective tax bases and operating loss and tax credit carryforwards. Deferred 
tax assets and liabilities are measured using enacted tax rates applicable to taxable income in the years in which those temporary 
differences are expected to be recovered or settled. The effect on deferred tax assets and liabilities of a change in tax rates is 
recognized in net loss in the period that includes the enactment date. A valuation allowance against deferred tax assets is recorded 
if, based upon the weight of all available evidence, it is more likely than not that some or all of the deferred tax assets will not be 
realized. For uncertain tax positions that meet "a more likely than not" threshold, the Company recognizes the benefit of uncertain 
tax positions in the consolidated financial statements.

Segment Reporting

Operating segments are components of a business where separate discrete financial information is available for evaluation 
by the chief operating decision-maker for purposes of making decisions regarding resource allocation and assessing performance. 
To date, the Company has viewed its operations and managed its business as one segment operating primarily in the United States.

Net Loss Per Share

Basic net loss per common share is calculated by dividing the net loss attributable to common stockholders by the weighted-
average number of common shares outstanding during the period, without consideration for potentially dilutive securities. Diluted 
net loss per share is computed by dividing the net loss attributable to common stockholders by the weighted-average number of 
common shares and potentially dilutive securities outstanding for the period. Common share equivalents outstanding, determined 
using  the  treasury  stock  method,  are  comprised  of  shares  that  may  be  issued  under  the  Company’s  stock  option  and  warrant 
agreements.

65

 
 
 
 
 
 
The following table presents the weighted average number of potentially dilutive securities not included in the calculation 

of diluted net loss per share due to the anti-dilutive effect of the securities:

Common stock options
Common stock warrants
Total

3. Recently Issued and Recently Adopted Accounting Pronouncements 

Recently Issued Accounting Pronouncements

Year ended

December 31,

2015
582,662
1,546,201
2,128,863

2016
173,776
315,834
489,610

2014
253,595
1,515,445
1,769,040

From time to time, new accounting pronouncements are issued by the Financial Accounting Standards Board ("FASB") or 

other standard setting bodies that are adopted by the Company as of the specified effective date. 

In March 2016, the FASB issued Accounting Standard Update ("ASU") 2016-09, Compensation-Stock Compensation 
(Topic 718). The new guidance changes the accounting and simplifies various aspects of the accounting for share-based payments 
to employees. The guidance allows for a policy election to account for forfeitures as they occur or based on an estimated number 
of awards that are expected to vest. ASU 2016-09 is effective for annual periods beginning after December 15, 2016, with early 
adoption permitted. The Company will adopt this standard as of January 1, 2017 and will begin to account for forfeitures as they 
occur beginning on that date. We expect the adoption of this standard will result in an adjustment to beginning retained earnings 
of $0.4 million. 

In February 2016, the FASB issued ASU 2016-02, Leases (Topic 842). Under the new guidance, lessees are required to 
recognize most lease assets and lease liabilities on their balance sheets and record expenses on their income statements in a manner 
similar to current accounting. The new guidance is effective for fiscal years beginning after December 15, 2018, with early adoption 
permitted. The primary impact of this new accounting guidance will be related to our facilities lease and the Company is currently 
evaluating the impact that this guidance will have on its consolidated financial statements and related financial statement disclosures.

In January 2016, the FASB issued ASU No. 2016-01, Financial Instruments - Overall (Subtopic 825-10): Recognition 
and Measurement of Financial Assets and Financial Liabilities. The new guidance enhances the reporting model for financial 
instruments and includes amendments to address aspects of recognition, measurement, presentation and disclosure. The update 
to  the  standard  is  effective  for  public  companies  for  interim  and  annual  periods  beginning  after  December  15,  2017. 
The Company does  not  believe  the  adoption  of  this  standard  will  have  a  material  impact  on  its  financial  position,  results  of 
operations or related financial statement disclosures.

In May 2014, the FASB issued ASU 2014-09, Revenue from Contracts with Customers (Topic 606), which will replace 
numerous requirements in U.S. GAAP, including industry-specific requirements, and provide companies with a single revenue 
recognition model for recognizing revenue from contracts with customers. The core principle of the new standard is that a company 
should  recognize  revenue  to  depict  the  transfer  of  promised  goods  or  services  to  customers  in  an  amount  that  reflects  the 
consideration to which the company expects to be entitled in exchange for those goods or services. In August 2015, the FASB 
approved a proposal to defer the effective date of the guidance until annual and interim reporting periods beginning after December 
15, 2017. Although we currently do not have any revenue contracts, we anticipate early adopting this standard effective January 
1, 2017 using the full retrospective method of adoption so that, in the event we enter into any revenue contracts, the contracts will 
be accounted for under the new guidance from inception of the contract.

Recently Adopted Accounting Pronouncements

In August 2014, the FASB issued ASU 2014-15, Presentation of Financial Statements-Going Concern (Subtopic 205-40): 
Disclosure of Uncertainties about an Entity’s Ability to Continue as a Going Concern. Under the new guidance, management is 
required  to  assess  an  entity’s  ability  to  continue  as  a  going  concern,  and  to  provide  related  footnote  disclosures  in  certain 
circumstances. The provisions of this ASU are effective for annual periods ending after December 15, 2016, and for annual and 
interim periods thereafter; early adoption is permitted. We adopted this guidance as of December 31, 2016 and the adoption did 
not require any additional disclosures in our consolidated financial statements for the year ended December 31, 2016. 

66

 
 
 
 
 
 
In November 2015, the FASB issued ASU No. 2015-17, Balance Sheet Classification of Deferred Taxes, to simplify the 
presentation of deferred taxes. This amendment requires that all deferred tax assets and liabilities, along with any related valuation 
allowances, be classified as noncurrent on the balance sheet. ASU 2015-17 is effective for annual and interim reporting periods 
ending  after  December 15,  2016.  Early  adoption  is  permitted,  and  the  new  guidance  may  be  applied  either  prospectively  or 
retrospectively. We have adopted this guidance prospectively as of December 31, 2015 and the adoption has no impact on our 
consolidated balance sheet since we have a full valuation allowance.

4.  Investments

The following tables summarize our short-term investments (in thousands): 

As of December 31, 2016

Corporate debt securities

Commercial paper

Corporate debt securities

Commercial paper

Maturity
1 year or less

1 year or less

Maturity
1 year or less

1 year or less

Amortized
cost
$ 20,622

13,717

$ 34,339

Amortized
cost
$ 27,644

45,158

$ 72,802

Gross
unrealized
gains

Gross
unrealized
losses

$

$

— $

15

15

$

Estimated
fair value
(3) $ 20,619
—
13,732
(3) $ 34,351

As of December 31, 2015

Gross
unrealized
gains

Gross
unrealized
losses

$

$

— $

54

54

$

Estimated
fair value
(22) $ 27,622
—
45,212
(22) $ 72,834

Unrealized  gains  and  losses  on  available-for-sale  securities  are  included  as  a  component  of  comprehensive  loss. At 
December 31, 2016, the Company did not have any securities in material unrealized loss positions. The Company reviews its 
investments to identify and evaluate investments that have an indication of possible other-than-temporary impairment. Factors 
considered in determining whether a loss is other-than-temporary include the length of time and extent to which fair value has 
been less than the cost basis, the financial condition and near-term prospects of the investee, and the Company’s intent and ability 
to hold the investment for a period of time sufficient to allow for any anticipated recovery in market value. The Company does 
not intend to sell any investments prior to recovery of their amortized cost basis for any investments in an unrealized loss position. 

5. Fair Value Measurements

The Company has certain financial assets and liabilities recorded at fair value which have been classified as Level 1, 2 or 3 

within the fair value hierarchy as described in the accounting standards for fair value measurements.

The authoritative guidance for fair value measurements defines fair value as the exchange price that would be received for 
an asset or paid to transfer a liability (an exit price) in the principal or the most advantageous market for the asset or liability in 
an orderly transaction between market participants on the measurement date. Market participants are buyers and sellers in the 
principal  market  that  are  (i) independent,  (ii) knowledgeable,  (iii) able  to  transact,  and  (iv) willing  to  transact. The  guidance 
prioritizes the inputs used in measuring fair value into the following hierarchy:

•  Level 1-  Quoted prices (unadjusted) in active markets for identical assets or liabilities;

•  Level 2-  Inputs other than quoted prices included within Level 1 that are either directly or indirectly observable; and

•  Level 3-  Unobservable inputs in which little or no market activity exists, therefore requiring an entity to develop its 

own assumptions about the assumptions that market participants would use in pricing.

67

 
 
 
The following table summarizes the assets and liabilities measured at fair value on a recurring basis (in thousands):

Assets

Cash and cash equivalents:

Cash

Money market funds

Total cash and cash equivalents

Short-term investments:

Corporate debt securities

Commercial paper

Total short-term investments

Total

Assets

Cash and cash equivalents:

Cash

Money market funds

Corporate debt securities

Commercial paper

Total cash and cash equivalents

Short-term investments:

Corporate debt securities

Commercial paper

Total short-term investments

December 31, 2016

Total

Level 1

Level 2

Level 3

$

2,728

$

2,728

$

— $

19,655

22,383

19,655

22,383

—

—

20,619

13,732

34,351

—

—

—

20,619

13,732

34,351

$

56,734

$

22,383

$

34,351

$

December 31, 2015

Total

Level 1

Level 2

Level 3

$

875

$

875

$

18,875

6,749

22,994

49,493

27,622

45,212

72,834

18,875

—

—

19,750

—

—

—

— $

—

6,749

22,994

29,743

27,622

45,212

72,834

Total

$

122,327

$

19,750

$

102,577

$

—

—

—

—

—

—

—

—

—

—

—

—

—

—

—

The Company’s investments in Level 1 assets are valued based on publicly available quoted market prices for identical 
securities as of December 31, 2016 and 2015. The Company determines the fair value of Level 2 related securities with the aid of 
valuations provided by third parties using proprietary valuation models and analytical tools. These valuation models and analytical 
tools use market pricing or prices for similar instruments that are both objective and publicly available, including matrix pricing 
or reported trades, benchmark yields, broker/dealer quotes, issuer spreads, two-sided markets, benchmark securities, bids and/or 
offers. There were no transfers between fair value measurement levels for the years ended December 31, 2016 and 2015. 

68

 
6. Other Current Assets and Other Long-Term Assets

Other current assets consisted of the following (in thousands): 

Prepaid expenses
Deposits and other receivables
Interest receivables

December 31,

2016

2015

$

$

1,879
759
183
2,821

$

$

2,287
551
237
3,075

The other long-term assets balance as of December 31, 2016 consists of $3.3 million in deposits paid in conjunction with 

the Company's research and development activities compared to $2.0 million as of December 31, 2015.

7. Property and Equipment, Net

Property and equipment, net consisted of the following (in thousands):

Computer equipment

Office and other equipment

Laboratory equipment

Leasehold improvements

Gross property and equipment

Less: Accumulated depreciation

Property and equipment, net

December 31,

2016

2015

329

301

563

63

1,256
(627)
629

$

$

329

256

425

51

1,061
(447)
614

$

$

The Company incurred depreciation expense of $0.2 million during the years ended December 31, 2016, 2015 and 2014, 

respectively. 

8. Accounts Payable and Accrued Liabilities

Accounts payable and accrued liabilities consisted of the following (in thousands):

Accounts payable
Accrued clinical, development and other expenses

Accrued compensation and benefits

Other current liabilities

December 31,

2016

2015

$

$

$

6,296
5,743

2,923

40

15,002

$

2,104
5,311

2,352

31

9,798

69

 
 
 
 
 
 
 
 
 
9. Stockholders' Equity

Common Stock

The following shares were reserved for future issuance:

Common stock options outstanding and available for future grant

Warrants to purchase common stock

Employee Stock Purchase Plan

Warrants

December 31, 2016

3,452,409

695,383

238,872

4,386,664

The  Company  issued  warrants  in  connection  with  private  placements  of  common  stock  in  November  2012. As  of 

December 31, 2016 the following warrants for common stock were issued and outstanding:  

Issue date
November 21, 2012

Expiration date
November 21, 2017

Exercise price

$

7.86

Number of warrants
outstanding

695,383

During the year ended December 31, 2016, warrants for 289,789 shares of the Company's common stock were exercised 
via cashless exercises and 313,756 shares were exercised for cash generating proceeds of $2.1 million and the Company issued a 
total of 603,545 shares of common stock.

During  the  years  ended  December 31,  2015  and  2014,  warrants  for 1,037,330 and 73,964 shares  of  the  Company's 
common stock were exercised via cashless exercises and the Company issued a total of 809,498 and 43,526 shares of common 
stock, respectively.

10. Share-Based Compensation

Equity Incentive Plan 

The Company has in place a stock option plan (the "Stock Option Plan") for the benefit of employees, directors, officers 
and consultants of the Company. In May 2013 our Board of Directors adopted the 2013 Equity Incentive Plan (the "2013 Plan"). 
The 2013 Plan was approved by our stockholders in connection with the Arrangement. The 2013 Plan is a continuation of and 
successor to the Stock Option Plan and no further grants will be made under the Stock Option Plan. As of December 31, 2016, 
there were approximately 0.6 million stock options available to be issued.

To date, share-based compensation awards under either the Stock Option Plan or the 2013 Plan consist of incentive and 
non-qualified stock options. Stock options granted under each of the plans must have an exercise price equal to at least 100% of 
the fair market value of our common stock on the date of grant and generally vest over four years. The Stock Option Plan has 
contractual terms ranging from five to seven years and the 2013 Plan has contractual terms ranging from seven to ten years.  

70

 
 
 
 
 
 
 
The following table summarizes our stock option activity and related information for the year ended December 31, 2016:

Balance outstanding as of December 31, 2015

Granted

Exercised

Canceled/forfeited

Expired

Balance outstanding as of December 31, 2016

Options exercisable at December 31, 2016

Options vested and expected to vest at December 31, 2016

Weighted
average
exercise
price

Weighted-
Average
Remaining
Contractual
Term (years)

Aggregate
Intrinsic
Value
(millions)

16.71

16.90

10.85

20.61

23.28

16.57

15.42

16.57

7.0

5.3

7.0

$

$

$

21.95

—

21.95

Number of
options
1,932,880

$

1,082,724

$
(22,132) $
(172,642) $
(7,488) $
$

2,813,342

1,402,702

2,813,342

$

$

The total intrinsic value of stock options exercised was $0.3 million for the year ended December 31, 2016 and $0.6 
million for the years ended December 31, 2015 and 2014, respectively. The Company received total cash of $0.2 million, $0.6 
million and $0.9 million for the exercise of options for the years ended December 31, 2016, 2015 and 2014, respectively. The total 
fair value of options vested during the years ended December 31, 2016, 2015 and 2014 was $8.6 million, $6.5 million and $3.0 
million, respectively. Upon option exercise, the Company issues new shares of our common stock. 

Total share-based compensation expense by statement of operations classification is presented below (in thousands):

Research and development expense

General and administrative expense

Year ended December 31,

2016

2015

2014

$

$

5,461

5,163

10,624

$

$

3,669

6,585

10,254

$

$

2,565

4,485

7,050

For the years ended December 31, 2016, 2015 and 2014, no share-based compensation expense was capitalized and there 

were no recognized tax benefits associated with the share-based compensation charge.

The fair value of options granted is estimated at the date of grant using the Black-Scholes option pricing model. The 
assumptions used for the specified reporting periods and the resulting estimates of weighted-average estimated fair value per share 
of options granted during those periods are as follows:

Risk-free interest rate

Dividend yield

Volatility factor

Expected term (in years)

Weighted average estimated fair value per share

Year Ended December 31,

2016
1.5%

—%

101.7%

6.0

$13.32

2015
1.5%

—%

104.3%

6.0

$19.44

2014
2.1%

—%

113.0%

6.7

$16.09

Risk-Free Interest Rate - The risk-free interest rate is the rate for periods equal to the expected term of the stock option 

based on U.S. Treasury zero-coupon bonds.  

Dividend Yield - The dividend yield is based on the Company’s history and expectation of dividend payouts. The Company 

has not paid, and does not intend to pay dividends.

Volatility  Factor  -  The  expected  volatility  assumption  was  determined  by  examining  the  historical  volatility  of  the 

Company's stock. 

71

 
 
 
 
 
 
 
 
 
 
Expected Term - The expected term represents the weighted average period the stock options are expected to be outstanding. 
The Company uses the simplified method for estimating the expected term as provided by the Securities and Exchange Commission. 
The simplified method calculates the expected term as the average time-to-vesting and the contractual life of the options. The 
Company believes this methodology is appropriate given the Company's limited history as a U.S. public company.  

The total compensation cost not yet recognized as of December 31, 2016 related to non-vested option awards was $8.0 

million which will be recognized over a weighted-average period of 1.3 years.

2013 Employee Stock Purchase Plan

In May 2013, the Company's Board of Directors adopted the ESPP. The ESPP was approved by the Company's stockholders 
in connection with the Arrangement. In December 2014, the ESPP became effective and the first purchase period began. The ESPP 
permits eligible employees to make payroll deductions to purchase up to $25,000 of the Company’s common stock on regularly 
scheduled purchase dates at a discount. Offering periods under the ESPP are not more than six months in duration and shares are 
purchased at 85% of the lower of the closing price for the Company’s common stock on the first day of the offering period or the 
date of purchase. The ESPP initially authorized the issuance of 300,000 shares of the Company’s common stock pursuant to rights 
granted to employees for their payroll deductions. As of December 31, 2016, 61,128 shares have been issued out of the plan.

11.  Employee Benefit Plan 

The Company has a defined contribution 401(k) plan (the "Plan") for all employees. Employees are eligible to participate 
in the Plan if they are at least 21 years of age or older. Under the terms of the Plan, employees may make voluntary contributions 
as a percentage of compensation. The Company matches up to 4% of an employee's contributions, subject to a limit of $2,500 per 
year. Expense associated with the Company's matching contribution totaled $0.1 million for the years ended December 31, 2016, 
2015 and 2014, respectively. 

12. Income Taxes 

The Company had no federal income tax expense and immaterial state tax expense for the years ended December 31, 

2016, 2015 and 2014. 

The differences between the effective income tax rate and the statutory tax rates during the years ended 2016, 2015 and 

2014 are as follows (in thousands):

Net loss before tax

Statutory combined US federal and state tax rate

Statutory federal and state taxes

Increase (decrease) in taxes recoverable resulting from:

Effect of change in valuation allowance

Non-deductible share-based compensation

Non-deductible warrant expenses for tax purposes

Tax credits

Share issue costs - temporary difference

Differential in income tax rates of foreign subsidiary

Uncertain Tax Positions

Return to provision and other true-ups

Other differences

Income tax benefit

Year Ended December 31,

2016
(83,118)

$

2015
(64,544)

$

$

34.00%

(28,260)

34.00%

(21,945)

2014
(43,698)

39.83%

(17,405)

28,446

1,247

—
(2,906)
(78)
261

3,921
(2,619)
(12)
— $

$

22,350

923

—
(2,430)
(184)
31

1,961
(899)
193

— $

12,273

930

1,799
(227)
(184)
3,047

47

—
(280)
—

72

 
 
 
 
 
 
 
 
 
 
Deferred Tax

The following table summarizes the significant components of our deferred tax assets (in thousands):

December 31,

2016

2015

Deferred tax assets:

Tangible and intangible depreciable assets

$

990

$

Stock compensation

Provisions

Financing fees

Net operating loss carry forwards

Capital loss carryforward

Scientific research and experimental development expenditures

Research and development tax credits

Total gross deferred tax assets

Less valuation allowance

Net deferred tax assets

6,635

853

—

66,489

51

5,531

4,266

84,815
(84,815)

$

— $

199

4,429

725

78

42,864

102

5,552

2,411

56,360
(56,360)
—

Total valuation allowance increased by $28.5 million for the year ended December 31, 2016. The Company has established 
a full valuation allowance against its deferred tax assets as of December 31, 2016 due to the uncertainty surrounding the realization 
of such assets as evidenced by the cumulative losses from operations through December 31, 2016.

For  Canadian  federal  income  tax  purposes,  the  Company's  Canadian  federal  scientific  research  and  experimental 
development expenditures amounted to $19.9 million at December 31, 2016 and 2015 and $20.1 million at December 31, 2014
and  for  provincial  income  tax  purposes  amounted  to  $21.6  million  at  December 31,  2016  and  2015  and  $22.7  million  at 
December 31, 2014. As operations in Canada ceased during 2014, the expenditures incurred for the year ended December 31, 
2016 and 2015 were much lower than previous years. These expenditures are available to reduce future taxable income and have 
an unlimited carry forward period. Scientific research and development expenditures are subject to verification by the taxation 
authorities, and accordingly, these amounts may vary by a material amount. In addition, the Company has research and development 
tax credit carryforwards for U.S. federal and state income tax purposes as of December 31, 2016 of $4.4 million and $2.0 million, 
respectively. The federal credits will begin to expire in 2034 unless utilized and the state credits have an indefinite life.  

At December 31, 2016, the Company's net operating loss carry forwards ("NOLs") for U.S. federal and state income 
taxes were $133.4 million and $77.3 million, respectively and the Company's NOLs for Canadian federal and provincial income 
tax purposes were $79.2 million and $78.5 million, respectively. The NOLs are available to offset future taxable income from 
both U.S. federal and state tax sources, as well as Canadian federal and provincial tax sources and the tax benefits of which have 
not been recognized in the consolidated financial statements. The NOLs expire as follows (in thousands):

US

Canada

Federal

State

Federal

Provincial

Expires in:
2030
2031
2032
2033
2034
2035
2036

$

— $
—
—
3,261
7,260
53,345
69,508
$133,374

— $
—
—
2,286
22,162
52,878
—
$ 77,326

5,907
7,059
13,308
18,623
32,401
1,084
777
$ 79,159

$

5,985
7,066
12,433
19,385
31,809
1,084
777
$ 78,539

The future utilization of the US federal and state NOL carryforwards to offset future taxable income may be subject to 
an annual limitation as a result of ownership changes that may have occurred previously or may occur in the future. The Tax 
Reform Act  of  1986  (the  "Act")  limits  a  company's  ability  to  utilize  certain  tax  credit  carryforwards  and  net  operating  loss 

73

 
 
 
 
 
 
 
 
 
carryforwards in the event of a cumulative change in ownership in excess of 50% as defined in the Act. The Canadian Federal and 
Provincial Tax Acts maintain similar rules in the case of acquisition of control.

The Company files income tax returns in the U.S. (federal and state) and Canada (federal and provincial). The Company’s 
U.S. operations have not been audited for any open taxation years. The Company has experienced losses for U.S. tax purposes 
and therefore, the taxation authorities may review any loss year, if and when the losses are utilized.

For Canadian tax purposes, the Company remains subject to federal and provincial audit for the December 31, 2012 and 
subsequent taxable years. Where taxation years remain open, the Company considers it reasonably possible that issues may be 
raised or tax positions agreed to with the taxation authorities, which may result in increases or decreases of the balance of non-
refundable ITCs and NOLs. However, an estimate of such increases and decreases cannot be currently made.

A reconciliation of the beginning and ending amounts of unrecognized tax positions are as follows (in thousands): 

Federal

December 31,

2016

2015

2014

Unrecognized tax positions, beginning of year

$

509

$

42

$

35

$

Gross increase — current period tax positions
Gross decrease — prior period tax positions

Gross increase — prior period tax positions

Expiration of statute of limitations

Unrecognized tax positions, end of year

$

598
(9)
—
(3)
1,095

445
(4)
26

—

$

509

$

35
(28)
—

—

42

$

Provincial/State

December 31,

2016
2,274

195
—

4,866
(2)
7,333

2015

2014

$

18

$

259
(3)
2,000

—

$

2,274

$

6

12
—

—

—

18

If recognized, none of the unrecognized tax positions would impact the Company's income tax benefit or effective tax 
rate as long as the Company's deferred tax assets remain subject to a full valuation allowance. The Company does not expect any 
significant increases or decreases to the Company's unrecognized tax positions within the next 12 months. 

The Company recognizes interest and penalties related to unrecognized tax benefits in income tax expense. The Company 
had no accrual for interest or penalties on tax matters as of December 31, 2016 and 2015 and the Company had no ongoing tax 
audits as of December 31, 2016.

13. Investment Tax Credits

In prior years, the Company was entitled to claim Canadian federal and provincial ITCs for eligible scientific research 
and development expenditures. The Company recorded ITCs based on management's best estimates of the amount to be recovered 
and ITCs claimed are subject to audit by the taxation authorities and accordingly, may vary by a material amount. The Company 
has not recorded federal or provincial ITCs since the year ended December 31, 2013, as the primary operations of the Company 
were moved from Canada to San Diego, California in early 2014.  

The Company's non-refundable Canadian federal ITCs as of December 31, 2016 are $3.9 million and relate to scientific 
research and development expenditures, which may be utilized to reduce Canadian federal income taxes payable in future years. 
The benefits of the non-refundable Canadian federal ITCs have not been recognized in the financial statements and will be recorded 
as a reduction of tax expense when realized.

The non-refundable investment tax credits expire as follows (in thousands):

Expires in:
2030
2031
2032
2033

FEDERAL ITC

$

$

764
1,000
1,125
1,018
3,907

74

 
 
 
 
 
 
 
 
 
 
 
 
 
14. Commitments and Contingencies

On June 24, 2014, the Company entered into a lease agreement for approximately 18,000 square feet of completed office 
and laboratory space located in San Diego, California. The office space under the lease is the Company's corporate headquarters. 
The lease commenced in phases, 2,300 square feet of space which commenced on July 1, 2014 at an initial monthly rent of $5,900
per month and 15,600 square feet of space which commenced on March 27, 2015 at an initial monthly rent of $18,200 per month. 
The leased property is subject to a 3% annual rent increase following availability that result in the Company recording deferred 
rent over the term of the lease. In addition to such base monthly rent, the Company is obligated to pay certain customary amounts 
for its share of operating expenses and facility amenities. The lease will expire on January 31, 2018. 

Future minimum payments required under the lease are summarized as follows (in thousands):

 Year Ending December 31:

2017

2018

Thereafter

 Total minimum lease payments

$

$

305

25

—

330

Total lease expense for the years ended December 31, 2016, 2015 and 2014 was $0.8 million, $0.6 million and $0.4 

million, respectively.

15. Selected Quarterly Financial Data (Unaudited)

The  following  is  a  summary  of  the  quarterly  results  of  the  Company  for  the  years  ended  December 31,  2016  and 

2015 (unaudited, in thousands, except for per share data):

Three Months Ended

Year Ended

Operating Loss

Net loss

Per common share:
Loss per share, basic and diluted (1)

Operating Loss

Net loss

Per common share:
Loss per share, basic and diluted(1)

3/31/16

6/30/16

9/30/16

12/31/16

$ (22,118)   $ (22,227)   $ (19,581)   $ (19,853)   $

(21,914)  

(22,061)  

(19,421)  

(19,722)  

December 31, 2016
(83,779)
(83,118)

$

(1.13)   $

(1.11)   $

(0.97)   $

(0.99)   $

(4.20)

Three Months Ended

Year Ended

3/31/15

6/30/15

9/30/15

12/31/15

$ (11,986)   $ (15,516)   $ (18,724)   $ (18,488)   $

(11,940)  

(15,446)  

(18,741)  

(18,417)  

December 31, 2015
(64,714)
(64,544)

$

(0.77)   $

(0.95)   $

(1.11)   $

(0.96)   $

(3.82)

(1)    Net loss per share is computed independently for each of the quarters presented. Therefore, the sum of the quarterly per-share 
calculations will not necessarily equal the annual per share calculation. 

16. Subsequent Events

Sale of Common 

In January 2017, the Company sold 5,002,702 million shares of our common stock at a public offering price of $5.60 per 
share and sold warrants to purchase up to 7,258,263 shares of our common stock at a public offering price of $5.599 per warrant 
share. The public offering price for the warrants was equal to the public offering price of the common stock, less the $0.001 per 
share exercise price of each warrant. After deducting underwriter discounts and offering expenses, the Company received net 
proceeds from the transaction of $66.8 million.

75

 
 
 
 
 
 
Pursuant to the requirements of Section 13 or 15(d) of the Securities Exchange Act of 1934, as amended, the Registrant has 
duly caused this report to be signed on its behalf by the undersigned, thereunto duly authorized.

SIGNATURES

MIRATI THERAPEUTICS, INC.

Date: March 9, 2017

by:

/s/ Charles M. Baum

President and Chief Executive Officer

(Principal Executive Officer)

Date: March 9, 2017

by:

/s/ Jamie A. Donadio

Senior Vice President and Chief Financial Officer

(Principal Financial and Accounting Officer)

POWER OF ATTORNEY

KNOW ALL PERSONS BY THESE PRESENTS, that each person whose signature appears below constitutes and appoints Charles 
M. Baum, Ph.D. and Jamie A. Donadio as his or her true and lawful attorneys-in-fact, and each of them, with full power of 
substitution, for him or her in any and all capacities, to sign any amendments to this Annual Report on Form 10-K and to file the 
same, 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 either of them, or his or their substitute or substitutes 
may do or cause to be done by virtue hereof.

76

Pursuant to the requirements of the Securities Exchange Act of 1934, this Annual Report on Form 10-K has been 

signed below by the following persons on behalf of the registrant and in the capacities and on the dates indicated.

Signature

Title

Date

/S/ CHARLES M. BAUM
Charles M. Baum, M.D., Ph.D.

/S/ JAMIE A. DONADIO
Jamie A. Donadio

/S/ RODNEY LAPPE
Rodney Lappe, Ph.D.

/S/ MICHAEL GREY
Michael Grey

/S/ HENRY J. FUCHS
Henry J. Fuchs, M.D.

/S/ CRAIG JOHNSON
Craig Johnson

/S/ Bruce L.A. Carter
Bruce L.A. Carter, Ph.D.

President, Chief Executive Officer and Director
(Principal Executive Officer)

March 9, 2017

Senior Vice President and Chief Financial Officer
(Principal Financial and Accounting Officer)

March 9, 2017

Chairman of the Board

March 9, 2017

Director

Director

Director

Director

March 9, 2017

March 9, 2017

March 9, 2017

March 9, 2017

77

 
 
 
 
 
 
 
 
Exhibit
number

2.1

3.1

3.2

3.3

4.1

4.2

10.1

10.2

10.3

10.4

10.5+
10.6+

10.7+
10.8*

10.9*

10.10*

10.11+

10.12+

10.13

10.14

10.15+

10.16+

10.17+

10.18+
10.19+

10.20+
10.21+

10.22+

10.23+

10.24+
10.25+

21.1

23.1

23.2
31.1

31.2

INDEX TO EXHIBITS 

Description of document

Arrangement Agreement, dated May 8, 2013, by and between MethylGene Inc. and the Registrant.(2)
Amended and Restated Certificate of Incorporation.(1)
Bylaws.(1)
Amendment to Bylaws. (8)
Form of Common Stock Certificate.(2)
Form of Warrant to Purchase Common Stock.(12)
Form of Securities Purchase Agreement relating to the 2011 private placement.(1)
Form of Securities Purchase Agreement relating to the 2012 private placement.(1)
Form of Warrant Certificate issued in connection with the 2011 private placement.(1)
Form of Warrant Certificate issued in connection with the 2012 private placement.(1)
Amended and Restated Incentive Stock Option Plan.(1)
Amended and Restated 2013 Equity Incentive Plan and Form of 2013 Equity Incentive Plan and Form of Stock 
Option Grant Notice and Form of Stock Option Agreement thereunder.(9)
Form of 2013 Employee Stock Purchase Plan.(1)
Collaboration and License Agreement, dated October 16, 2003, by and between MethylGene Inc. and Taiho 
Pharmaceutical Co. Ltd.(1)
Amendment Number One to Collaboration and License Agreement, dated January 25, 2005, by and between 
MethylGene Inc. and Taiho Pharmaceutical Co., Ltd.(1)
Letter Agreement, dated January 25, 2005, by and between MethylGene Inc. and Taiho Pharmaceutical Co., Ltd., 
relating to Collaboration and License Agreement dated October 16, 2003.(1)
Senior Executive Employment Agreement, dated September 24, 2012, by and among MethylGene Inc. and 
Dr. Charles M. Baum.(1)
Amended and Restated Employment Agreement, dated July 2, 2013, by and between the Registrant and Dr. Charles 
M. Baum.(3)
Sublease Agreement, dated May 28, 2013, by and between Amylin Pharmaceuticals, LLC and MethylGene US, Inc.(4)
Lease Agreement, dated June 24, 2014, by and between the Company and ARE-SD Region No. 20, LLC. (6)
Letter Agreement, dated August 30, 2013, by and between the Registrant and Dr. Isan Chen.(5)
Letter Agreement, dated May 20, 2013, by and between Methylgene Inc. and James Christensen.(7)
Form of Indemnity Agreement.(5)
Amended and Restated Non-Employee Director Compensation Policy. (10)
Transition and Separation Letter Agreement, dated June 24, 2016, by and between Mirati Therapeutics, Inc. and Mark 
J. Gergen.(11)
Letter Agreement, dated September 13, 2016, by and between Mirati Therapeutics, Inc. and Christopher LeMasters.
Amendment to Amended and Restated Employment Agreement, dated December 19, 2016, by and between the
Registrant and Dr. Charles Baum.
Amendment to Letter Agreement, dated December 19, 2016, by and between the Registrant and Jamie Donadio.

Amendment to Letter Agreement, dated December 19, 2016, by and between the Registrant and Dr. Isan Chen.

Amendment to Letter Agreement, dated December 19, 2016, by and between the Registrant and James Christensen.

Amendment to Letter Agreement, dated December 19, 2016, by and between the Registrant and Christopher
LeMasters.
Subsidiaries of the Registrant.(1)
Consent of Independent Registered Public Accounting Firm- US.

Consent of Independent Registered Public Accounting Firm- Canada.

Certification of the Principal Executive Officer pursuant to Rule 13a-14(a) or 15d-14(a) of the Securities Exchange
Act of 1934.

Certification of the Principal Financial Officer pursuant to Rule 13a-14(a) or 15d-14(a) of the Securities Exchange Act
of 1934.

78

32.1

Certifications Pursuant to U.S.C. Section 1350, As Adopted Pursuant to Section 906 of the Public Company
Accounting Reform and Investor Protection Act of 2002.

101.INS XBRL Instance Document.

101.SCH XBRL Taxonomy Extension Schema Document.

101.CAL XBRL Taxonomy Extension Schema Document.

101.DEF XBRL Taxonomy Extension Definition Linkbase Document.

101.LAB XBRL Taxonomy Extension Label Linkbase Document.

101.PRE XBRL Taxonomy Extension Presentation Linkbase Document.

+ 

* 

(1) 

(2) 

(3) 

(4) 

(5) 

(6) 

(7) 

(8) 

(9) 

(10) 

(11) 

(12) 

Indicates management contract or compensatory plan.

We have received confidential treatment for certain portions of this agreement, which have been omitted and filed 
separately with the SEC pursuant to Rule 406 under the Securities Act.

Incorporated by reference to Mirati Therapeutics, Inc.’s Registration Statement on Form 10-12B (No. 001-35921), filed 
with the Securities and Exchange Commission on May 10, 2013.

Incorporated by reference to Mirati Therapeutics, Inc.’s Amended Registration Statement on Form 10-12B/A 
(No. 001-35921), filed with the Securities and Exchange Commission on June 14, 2013.

Incorporated by reference to Mirati Therapeutics, Inc.’s Amended Registration Statement on Form 10-12B/A 
(No. 001-35921), filed with the Securities and Exchange Commission on July 9, 2013.

Incorporated by reference to Mirati Therapeutics, Inc.’s Quarterly Report on Form 10-Q for the quarter ended June 30, 
2013, filed with the Securities and Exchange Commission on August 13, 2013.

Incorporated by reference to Mirati Therapeutics, Inc.’s Registration Statement on Form S-1 (No. 333-191544), filed with 
the Securities and Exchange Commission on October 3, 2013.

Incorporated by reference to Mirati Therapeutics, Inc.’s Current Report on Form 8-K, filed with the Securities and 
Exchange Commission on June 27, 2014.

Incorporated by reference to Mirati Therapeutics, Inc.’s Annual Report on Form 10-K for the year ended December 31, 
2014, filed with the Securities and Exchange Commission on March 9, 2015.

Incorporated by reference to Mirati Therapeutics, Inc.’s Current Report on Form 8-K, filed with the Securities and 
Exchange Commission on June 16, 2016.

Incorporated by reference to Mirati Therapeutics, Inc.’s Quarterly Report on Form 10-Q for the quarter ended September 
30, 2016, filed with the Securities and Exchange Commission on November 3, 2016 (for the Amended and Restated 2013 
Equity Incentive Plan) and Mirati Therapeutics, Inc.’s Registration Statement on Form 10-12B (No. 001-35921), filed 
with the Securities and Exchange Commission on May 10, 2013 (for the Form of Stock Option Grant Notice and Form of 
Stock Option Agreement thereunder).

Incorporated by reference to Mirati Therapeutics, Inc.’s Annual Report on Form 10-K for the year ended December 31, 
2015, filed with the Securities and Exchange Commission on March 9, 2016.

Incorporated by reference to Mirati Therapeutics, Inc.’s Quarterly Report on Form 10-Q for the quarter ended June 30, 
2016, filed with the Securities and Exchange Commission on August 4, 2016.

Incorporated by reference to Mirati Therapeutics, Inc.’s Current Report on Form 8-K, filed with the Securities and 
Exchange Commission on January 6, 2017.

79

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[THIS PAGE INTENTIONALLY LEFT BLANK]

[THIS PAGE INTENTIONALLY LEFT BLANK]

CORPORATE INFORMATION

EXECUTIVE MANAGEMENT
Charles M. Baum, MD, Ph.D.
(cid:22)(cid:56)(cid:39)(cid:57)(cid:45)(cid:38)(cid:39)(cid:50)(cid:59)(cid:2)(cid:33)(cid:50)(cid:38)(cid:2)(cid:6)(cid:44)(cid:45)(cid:39)(cid:40)(cid:2)(cid:9)(cid:63)(cid:39)(cid:36)(cid:60)(cid:2245)(cid:61)(cid:39)(cid:2)(cid:19)(cid:259)(cid:36)(cid:39)(cid:56)

Isan Chen
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(cid:33)(cid:50)(cid:38)(cid:2)(cid:6)(cid:44)(cid:45)(cid:39)(cid:40)(cid:2)(cid:17)(cid:39)(cid:38)(cid:45)(cid:36)(cid:33)(cid:161)(cid:2)(cid:33)(cid:50)(cid:38)(cid:2)(cid:8)(cid:39)(cid:61)(cid:39)(cid:161)(cid:51)(cid:54)(cid:49)(cid:39)(cid:50)(cid:59)(cid:2)(cid:19)(cid:259)(cid:36)(cid:39)(cid:56)

Christopher C. LeMasters
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(cid:6)(cid:44)(cid:45)(cid:39)(cid:40)(cid:2)(cid:5)(cid:60)(cid:57)(cid:45)(cid:50)(cid:39)(cid:57)(cid:57)(cid:2)(cid:19)(cid:259)(cid:36)(cid:39)(cid:56)

James G. Christensen
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(cid:33)(cid:50)(cid:38)(cid:2)(cid:6)(cid:44)(cid:45)(cid:39)(cid:40)(cid:2)(cid:25)(cid:36)(cid:45)(cid:39)(cid:50)(cid:2245)(cid:41)(cid:36)(cid:2)(cid:19)(cid:259)(cid:36)(cid:39)(cid:56)(cid:2)

Jamie A. Donadio
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(cid:6)(cid:163)(cid:33)(cid:45)(cid:56)(cid:39)(cid:2)(cid:25)(cid:87)(cid:2)(cid:22)(cid:33)(cid:38)(cid:43)(cid:39)(cid:295)
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Dennis M. Hester
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Perry C. Johnston
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Vickie Reed
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CORPORATE HEADQUARTERS 
9393 Towne Centre Drive, Suite 200 
San Diego, CA 92121

(cid:5)(cid:19)(cid:3)(cid:24)(cid:8)(cid:2)(cid:19)(cid:10)(cid:2)(cid:8)(cid:13)(cid:24)(cid:9)(cid:6)(cid:26)(cid:19)(cid:24)(cid:25)
Rodney Lappe
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Charles M. Baum, MD, Ph.D.
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Bruce L.A. Carter
(cid:8)(cid:45)(cid:56)(cid:39)(cid:36)(cid:59)(cid:51)(cid:56)

(cid:12)(cid:39)(cid:50)(cid:56)(cid:64)(cid:2)(cid:14)(cid:87)(cid:2)(cid:10)(cid:60)(cid:36)(cid:44)(cid:57)
(cid:8)(cid:45)(cid:56)(cid:39)(cid:36)(cid:59)(cid:51)(cid:56)

Michael Grey
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Craig Johnson
(cid:8)(cid:45)(cid:56)(cid:39)(cid:36)(cid:59)(cid:51)(cid:56)

(cid:26)(cid:24)(cid:3)(cid:18)(cid:25)(cid:10)(cid:9)(cid:24)(cid:2)(cid:3)(cid:11)(cid:9)(cid:18)(cid:26) 
Computershare

INDEPENDENT REGISTERED  
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Ernst & Young LLP

CORPORATE COUNSEL 
Cooley LLP

INVESTOR RELATIONS/ 
MEDIA CONTACT 
Christopher C. LeMasters
(cid:45)(cid:56)(cid:124)(cid:49)(cid:45)(cid:56)(cid:33)(cid:2471)(cid:87)(cid:36)(cid:51)(cid:49)

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MIRATI THERAPEUTICS, INC. 
9393 Towne Centre Drive, Suite 200 

San Diego, CA 92121 

858.332.3410