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Rexahn Pharmaceuticals, Inc.

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FY2016 Annual Report · Rexahn Pharmaceuticals, Inc.
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to Stockholders    
Letter    to Stockholders
CEOCEOCEOCEO    Letter
to Stockholders
to Stockholders
Letter
Letter

Dear Rexahn Stockholders,    

Rexahn is developing novel targeted cancer therapeutics, with recent data showing efficacy 
against  the  toughest to  treat  cancers  and  minimized  side  effects.   In 2016,  we advanced 
clinical  testing  of  our  three  proprietary  product  candidates  and  reported  positive  findings 
from  each  of  our  drug-development  programs.    The  data  we  are  generating  from  these 
programs suggest that RX-3117, Supinoxin™ and Archexin® are emerging as first-in-class or 
best-in-class therapeutics with promising clinical benefits in patients with cancers that are 
very difficult to treat.   In the year ahead, we look forward to reporting new findings from our 
studies that will be important valuation catalysts for our products and our company. 

RX-3117  is  currently  in  a  Phase  IIa  clinical  proof-of-concept  study  for  the  treatment  of 
metastatic  pancreatic  cancer  and  advanced  bladder  cancer.    It  is  a  novel,  oral  small 
molecule  nucleoside  analogue  which  has  demonstrated  activity  against  drug-resistant 
cancers  such  as  pancreatic,  bladder,  colon  and  other  cancers.    We  recently  initiated  the 
second  stage  of  a  Phase  IIa  clinical  trial  in  patients  with  metastatic  pancreatic  cancer, 
following  encouraging  findings  of  safety  and  preliminary  efficacy  in  the  first  stage  of  the 
trial  which  we  reported  in  November  2016  at  the  European  Society  for  Medical  Oncology 
(ESMO)  Congress.    More  recent  data  from  the  study  were  presented  in  January  at  the 
American  Society  for  Clinical  Oncology  (ASCO)  2017  Gastrointestinal  Cancer  Symposium, 
demonstrating the drug’s positive effects on progression-free survival among patients who 
have  failed  three  or  more  prior  cancer  therapies.  Current  options  for  these  patients  are 
usually  limited  to  palliative  or  best  supportive  care;  there  are  no  drugs  approved  for 
metastatic pancreatic cancer patients that have failed two or more prior therapies.  

We are greatly encouraged by these findings which support the development of RX-3117 as 
both  monotherapy  and,  in  a  study  to be  started  later this  year,  as a  combination  therapy 
with  Abraxane®  for  the  treatment  of  pancreatic  cancer.    We  expect  to  report  additional 
data  from  the  current  Phase  IIa  monotherapy  study  this  year.    RX-3117  has  been 
designated an orphan drug by the FDA for the treatment of pancreatic cancer. 

During the third quarter of 2016, we launched a Phase IIa study of RX-3117 in patients with 
advanced muscle invasive bladder cancer for which where there is a high unmet need for 
new treatments.  This multi-center, open-label study is measuring progression-free survival 
and  changes  in  tumor  size.    Initial  results are  expected  to be available  during  the  second 
half of 2017. 

Supinoxin is currently in development as a treatment for patients with triple-negative breast 
cancer  (TNBC).  It  is  an  orally  active  inhibitor  of  a  unique  cancer  protein  that  has  shown 
activity against more than 100 human cancer cell lines.  In October at ESMO, we presented 
Phase I  findings  showing  no dose-limiting  toxicities  from  the  drug at the doses  we  tested 
and  preliminary  evidence  of  efficacy  in  patients  with  a  range  of  different  cancer  tumors.  
We  recently  initiated  a  Phase  IIa  study  of  Supinoxin  in  patients  with  metastatic  triple 
negative breast cancer; we expect to report initial data from this trial during the second half 
of 2017.  Based on the outcome of this initial study, we may conduct additional studies of 
Supinoxin in combination with other anticancer agents in TNBC.   

    
    
 
 
 
 
 
 
Archexin, our  novel inhibitor  of  the  cancer cell-signaling  protein  AKT-1,  has  advanced  into 
the second stage of Phase IIa testing for the treatment of metastatic renal cell carcinoma.  
As we reported at ASCO in June, Archexin has been safe and well tolerated at the doses we 
have  tested  and  has  shown  preliminary  evidence  of  dose-dependent  reductions  in  tumor 
size for patients in stage one of the trial.  We look forward to completing enrollment and 
reporting results of the Phase IIa study later this year. 

Our  commitment  to  innovation  in  cancer  treatment  was  reflected  in  the  U.S.  patent  we 
received in October for our chemotherapeutic RX-21101 that combines Rexahn’s nano-drug 
delivery and targeting technology with docetaxel, a widely used cancer drug.  RX-21101 has 
been selected for preclinical development by the National Cancer Institute (NCI) because of 
its potential to treat a variety of cancers, while minimizing nerve damage, a frequent side 
effect of standard of care docetaxel. 

In 2017, we look forward to reporting data from all of our ongoing Phase IIa studies – RX-
3117  in  pancreatic  and  bladder  cancer,  Supinoxin  in  breast  cancer  and  Archexin  in 
metastatic renal cell  carcinoma.   Thanks  to  the  expansion  of  our  management team  and 
our  successful  stock  offerings  in  2016,  we  believe  we  have  the  human  and  financial 
resources to execute our clinical programs successfully this year as we work to create value 
for shareholders and create innovative new medicines for patients. 

We greatly appreciate your continued support of Rexahn and look forward to reporting on 
our progress in 2017.   

Sincerely, 

Peter D. Suzdak, Ph.D. 
Chief Executive Officer 

 
 
 
 
 
 
 
 
 
 
 
 
Pipeline Overview    
Oncology Pipeline Overview
Rexahn Oncology 
Rexahn 
Pipeline Overview
Pipeline Overview
Oncology 
Oncology 
Rexahn 
Rexahn 

Rexahn’s  mission  is  to  improve  the  lives  of  cancer  patients  by  developing  next  generation 
cancer  therapies  that  specifically  target  cancer  cells  leading  to  increased  efficacy  while 
minimizing  side  effects  traditionally  associated  with  cancer  treatment.    The  Company  has 
built  a  diverse  portfolio  of  novel  oncology  assets  that  includes  three  clinical-stage 
investigational  anti-cancer  compounds  currently  in  clinical  trials,  and  a  robust  oncology 
research platform.   

Stage Oncology Programs:    
Clinical----Stage Oncology Programs:
Clinical
Stage Oncology Programs:
Stage Oncology Programs:
Clinical
Clinical

3117  –  An  orally-administered  next  generation,  cancer  cell  specific  nucleoside 
RXRXRXRX----3117
31173117
agent  that  induces  apoptotic  cell  death  selectively  in  cancer  cells.    RX-3117  is 
currently in Phase IIa clinical trials in both metastatic pancreatic cancer and muscle 
invasive bladder cancer.  

Supinoxin™
Supinoxin™ - An orally administered potential first-in-class small molecule inhibitor of 
Supinoxin™
Supinoxin™
phosphorylated-p68, a protein that we believe plays a key role in cancer cell growth, 
progression  and  metastasis.    We  have  recently  initiated  a  Phase  IIa  clinical  trial  of 
Supinoxin in patients with triple negative breast cancer.  

Archexin®®®® - A unique anti-cancer drug candidate which inhibits the activated form of 
Archexin
Archexin
Archexin
the cancer cell signaling protein phosphorylated Akt-1 which is found only in cancer 
cells and is involved in cancer cell growth and drug resistance. Archexin is currently in 
Phase IIa clinical trial in metastatic renal cell carcinoma (RCC). 

A Novel Next Generation Nucleoside Compound    
3117 ––––    A Novel Next Generation Nucleoside Compound
RXRXRXRX----3117 
A Novel Next Generation Nucleoside Compound
A Novel Next Generation Nucleoside Compound
3117 
3117 

RX-3117  is  an  orally  bioavailable,  small  molecule,  investigational  anti-cancer  therapy  that 
works through a well-proven mechanism of action but is unique in that it is activated only in 
cancer cells, thus sparing healthy cells from destruction.   

A  novel,  cancer-cell  specific  nucleoside  analogue,  RX-3117  is  a  prodrug  activated  by  the 
enzyme  Uridine  Cytidine  Kinase,  or  ‘UCK2’,  which  is  present  predominantly  in  cancer  cells.  
Once  activated  by  UCK2,  RX-3117  inhibits  DNA  and  RNA  synthesis  leading  to  cancer  cell 
death.  Because UCK2 is overexpressed in multiple human tumors – but has a very limited 
presence in healthy tissues, RX-3117 offers the potential for a targeted anti-cancer therapy 
with an improved efficacy and safety profile. 

Preclinical  studies  of  RX-3117  in  patient-derived  and  cancer  cell  xenograft  models  have 
demonstrated  broad  anti-tumor  activity  and  –  most  importantly,  an  ability  to  treat  cancer 
cells that have become resistant to gemcitabine, an anticancer treatment that is widely used 
for  pancreatic  cancer,  bladder  cancer  and  other  indications.      Approximately,  25-40%  of 
tumors  eventually  become  resistant  to  gemcitabine,  leading  to  disease  progression  and 
limited options for further treatment.  RX-3117 may be effective in some of those patients.    

 
 
    
 
 
 
  
    
 
    
    
 
 
 
RX-3117  has  shown  broad  spectrum  anti-tumor  activity  against  over  100  different  human 
cancer cell lines and efficacy in 17 different mouse xenograft models.  In preclinical mouse 
xenograft studies, RX-3117 demonstrated superior efficacy to gemcitabine. In addition, RX-
3117  retained  its  full  anti-tumor  activity  in  human  cancer  cell  lines  made  resistant  to  the 
anti-tumor effects of gemcitabine, supporting a unique, highly-targeted mechanism of action.   

RX-3117  is  currently  being  investigated  in  a  Phase  IIa  multicenter,  open-label  single-agent 
study that is ongoing at 10 clinical centers in the United States. These patients have failed all 
conventional  therapies  with  a life  expectancy  measured in  weeks.  The  study  follows a  two-
stage design.  In stage 1 of the trial, up to 10 patients with relapsed or refractory metastatic 
pancreatic cancer were enrolled.  Based on predefined criteria, if 20% or more of the patients 
show  progression  free  survival  of > 4  months,  or  an  objective  clinical  response  rate  and 
reduction in tumor size, then an additional 40 pancreatic cancer patients can be enrolled into 
stage 2. 

An  update  from  this  study  was  presented  in  January  2017  at  the  American  Society  for 
Clinical  Oncology  (ASCO)  2017  Gastrointestinal  Cancer  Symposium.    In  the  current  study 
more  than  20%  of  patients  treated  with  RX-3117  exhibited  progression  free  survival  of 
greater than 5.6 months (with one patient having progression free survival of 7.2 months). An 
additional 20%, for a total of 40%, of the patients exhibited progression free survival of 2.5 
months. These patients had already failed 3 or more prior cancer therapies. Current options 
for these patients are usually limited to palliative or best supportive care and these patients 
normally  have  an  expected  survival  of  less  than  2  months. RX-3117  was  shown  to  be  safe 
and well tolerated in this patient group.  

Patients in Stage 1 of the clinical trial are still being monitored for survival.  However, since 
the predefined efficacy criteria have been achieved, stage 2 of the study has been initiated 
which entails enrolling an additional 40 metastatic pancreatic cancer patients. An initial data 
read out from stage 2 of the trial is expected in late 2Q or early 3Q 2017. 

Rexahn's development  strategy  for  RX-3117  in pancreatic  cancer is  to  continue  to develop 
the drug candidate as monotherapy for patients with metastatic disease who have failed on 
two  or  more  prior  therapies,  and  also,  in  parallel,  to  develop  RX-3117  in  combination  with 
Abraxane® (paclitaxel  protein  bound)  for  patients  with  metastatic  pancreatic  cancer  who 
have received no prior chemotherapy treatment.  Since there are currently no drugs approved 
for patients who have failed two or more therapies, there may be an accelerated regulatory 
pathway  for  approval  for  this  patient  population,  assuming  RX-3117  continues  to  generate 
efficacy data.  Rexahn plans to initiate a Phase IIa clinical trial of RX-3117 in combination 
with  Abraxane® in  newly  diagnosed  metastatic  pancreatic  cancer  patients  who  have 
received no prior chemotherapy.  RX-3117 has Orphan Designation in the US for pancreatic 
cancer. 

Rexahn  has  also  initiated  the  first  stage  of  a  Phase  IIa  study  of  RX-3117  in  patients  with 
muscle-invasive  bladder  cancer.   The  initial  readout  of  the  first  stage  is  expected  during 
2017.  

Class Inhibitor of a Unique Cancer Protein    
A Potential First----inininin----Class Inhibitor of a Unique Cancer Protein
Supinoxin ––––    A Potential First
Supinoxin 
Class Inhibitor of a Unique Cancer Protein
Class Inhibitor of a Unique Cancer Protein
A Potential First
A Potential First
Supinoxin 
Supinoxin 

Supinoxin™  (RX-5902)  is  an  orally  administered,  potential  first-in-class,  small  molecule 
inhibitor of a unique cancer protein – phosphorylated-p68 (P-p68) which is present mainly in 
cancer cells and absent in normal cells.  P-p68 is believed to interact with and increase the 

 
 
 
activity of multiple cancer-related genes, and play a prominent role in tumor progression and 
metastasis.  High  levels  of  P-p68  has  been  observed  in  many  solid  tumors,  including, 
melanoma, colon, ovarian, breast and lung tumors. 

In preclinical studies, Supinoxin has been shown to inhibit proliferation of cancer cells in over 
100  different  human  cancer  cell  lines,  including,  breast,  ovarian,  colon,  pancreas,  and 
stomach cancers, and has shown potent activity in drug-resistant cancer cells. In preclinical 
animal  models,  where  human  cancer  cells  from  triple  negative  breast  cancer,  ovarian, 
melanoma,  pancreas,  or renal  tumors  were  grafted  into animals,  treatment  with  Supinoxin 
resulted in a significant reduction in tumor growth.  

Supinoxin has been evaluated in a Phase I multi-center, dose-finding, open-label, single agent 
clinical  study  in  patients  with  advanced  or  metastatic  solid  tumors.      Updated  results  from 
this  trial  were  presented  in  October  2016  at  the  ESMO  conference,  showing  continued 
evidence of single-agent, clinical activity. Initial signs of clinical activity have been observed 
in  patients  with  breast,  neuroendocrine,  paraganglioma,  head  and  neck  and  colorectal 
cancers, with seven patients experiencing disease stabilization and three patients continuing 
treatment beyond one year.   

A Phase IIa clinical study in patients with triple negative breast cancer (TNBC) patients was 
initiated  in  February  2017.    The  Phase  IIa  clinical  proof-of-concept  study  is  an  open-label 
evaluation of the safety and efficacy of Supinoxin™ monotherapy in patients with metastatic 
triple negative breast cancer who have failed multiple prior chemotherapeutic regimens.  The 
study will recruit an initial 10 patients and can be extended up to 50 patients, if warranted, 
based  on  the  data  readout  from  the  initial  cohort  of  patients.  The  primary  endpoint  is 
progression free survival.  Patients will be enrolled at seven study sites in the United States. 
Based  on  the  initial clinical data,  we may  conduct  additional clinical studies  looking  at  the 
combination of Supinoxin together with other anti-cancer agents in TNBC. 

1 Inhibitor    
Class Akt----1 Inhibitor
A Potential Best----inininin----Class Akt
Archexin    ––––    A Potential Best
Archexin
1 Inhibitor
1 Inhibitor
Class Akt
Class Akt
A Potential Best
A Potential Best
Archexin
Archexin

Archexin is a unique antisense oncology drug candidate that specifically inhibits the cancer 
cell signaling protein Akt-1, which is highly overexpressed in cancer cells. Archexin is the only 
specific  inhibitor  of  Akt-1  in  clinical  development.  The  activated  form  of  Akt-1,  which  is 
involved in cancer cell growth, survival, angiogenesis, and drug resistance, has been shown to 
be  present  or  elevated  in  more  than  12  different  human  cancer  cell  lines,  including 
pancreatic and renal cell carcinoma.  

In two clinical trials, Archexin appeared to be safe and well tolerated at all dose levels tested 
with no dose-limiting toxicities.  The FDA has granted Orphan Drug Designation to Archexin in 
the treatment of five cancers: renal cell, pancreatic, ovarian, stomach, and glioblastoma.  

Rexahn  is  currently  conducting  a  Phase  IIa  clinical  trial  of  Archexin  in  patients  with 
metastatic renal cell carcinoma (RCC). This is a multi-center study designed to evaluate the 
efficacy of Archexin in combination with everolimus to treat metastatic renal cell carcinoma 
patients.    Everolimus  is  widely  used  in  the  treatment  of  RCC  but  resistance  develops  over 
time, partly due to raised Akt-1 levels.  Our expectation is that the combination with Archexin 
may improve overall efficacy and delay the onset on resistance.  This trial is being conducted 
in two stages. The first stage is a dose ranging study to determine the maximum tolerated 
dose of Archexin in combination with everolimus. Results from Stage 1, presented at ASCO 
2016,  showed  that  in  metastatic  RCC  patients  that  have  previously  received  multiple  anti-

 
 
 
    
 
 
cancer therapies, Archexin treatment produced both stable disease, which persisted for up to 
383 days or a median of 165.5 days, and a reduction in tumor burden. 

At the dose levels tested to date, Archexin appeared to be safe and well tolerated.  The most 
commonly  reported  adverse  event  in  patients  taking  both  Archexin  and  everolimus  was 
thrombocytopenia.  To date, no adverse events have been dose limiting.   

Stage  2  of  the  Phase  IIa  clinical  study,  which  commenced  enrolling  patients  in  2016,  is  a 
randomized,  open-label,  two-arm  study  of  Archexin  in  combination  with  everolimus,  versus 
everolimus  alone,  to  determine  safety  and  efficacy  of  the  combination.  The  trial  is 
anticipated  to  enroll  up  to  30  metastatic  RCC  patients  who  will  be  randomized  to  receive 
either  Archexin in  combination  with  everolimus, or  everolimus alone,  in a ratio  of  2:1.    The 
maximum  tolerated  dose  of  250  mg/m2/day  of  Archexin  –  identified  in  Stage  1,  will  be 
administered along with 10 mg of everolimus versus 10 mg everolimus alone. 

The  primary  endpoint  of  Stage  2  is  the  percentage  of  progression  free  patients  following 
eight  cycles  of  therapy.  Patients  are  scanned  (CT  or  MRI)  for  the  assessment  of  tumor 
progression  after  every  2  cycles  of  therapy.    Secondary  endpoints  include  pharmacokinetic 
profile, incidence of adverse events, changes in clinical laboratory tests and vital signs over 
time, tumor response, duration of response, time to response, and response rate. Exploratory 
endpoints  include  blood levels  of  Akt  pathway  biomarkers, tumor  apoptosis  biomarkers, or 
other relevant biomarkers. Data from Stage 2 of this ongoing clinical study are expected to 
be available mid-2017. 

Metastatic  RCC  represents  an  attractive  market  opportunity  with  an  estimated  annual 
incidence of 90,000 patients worldwide. Metastatic RCC patients receiving standard of care 
treatment have a poor prognosis with an overall survival of less than two years.  

Oncology Research Programs    
Oncology Research Programs
Oncology Research Programs
Oncology Research Programs

rugs::::        
Approved Chemotherapy Drugs
latform for FDA----Approved Chemotherapy D
Drug Delivery Platform for FDA
NanoNanoNanoNano----Drug Delivery P
rugs
rugs
Approved Chemotherapy D
Approved Chemotherapy D
latform for FDA
latform for FDA
Drug Delivery P
Drug Delivery P

Rexahn’s  Nano-Polymer-Drug  Conjugate  System 
(NPDCS)  combines  FDA-approved 
chemotherapies  with  a  proprietary  polymer  carrier  that  is  designed  to  target  the  delivery 
chemotherapy  drugs  directly  into  the  tumor  while  bypassing  healthy  cells.  This  approach 
minimizes the level of freely-circulating drug in the body while maximizing the drug exposure 
at the tumor site, potentially increasing efficacy and minimizing toxic side effects.  

ancer Therapeutic    
olymer Anti----CCCCancer Therapeutic
A Proprietary Nano----PPPPolymer Anti
21101 ––––    A Proprietary Nano
RXRXRXRX----21101 
ancer Therapeutic
ancer Therapeutic
olymer Anti
olymer Anti
A Proprietary Nano
A Proprietary Nano
21101 
21101 

RX-21101 combines Rexahn’s nano-drug delivery system with docetaxel, a widely-used, FDA-
approved chemotherapy drug. RX-21101 may enhance efficacy while reducing the systemic 
toxicity of traditional docetaxel delivery by specifically targeting the tumor site and reducing 
drug exposure elsewhere in the body.  The National Cancer Institute’s (NCI) Nanotechnology 
Characterization  Laboratory  has  selected  RX-21101  for  funding  of  the  further  preclinical 
development of this program, under NCI’s preclinical characterization program. 

 
 
 
 
 
 
 
    
    
 
 
 
    
 
    _________________________________________________________________________________________________  

UNITED STATES 

SECURITIES AND EXCHANGE COMMISSION 

Washington, D.C. 20549 

FORM 10-K 

(Mark One) 
(cid:1) ANNUAL REPORT PURSUANT TO SECTION 13 OR 15(d) OF 
THE 
SECURITIES EXCHANGE ACT OF 1934 
For the fiscal year ended December 31, 2016 

OR 

(cid:3) TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) 
OF 
THE SECURITIES EXCHANGE ACT OF 1934 

For the transition period from                to               

Commission File No.:001-34079 

Rexahn Pharmaceuticals, Inc. 

(Exact name of registrant as specified in its charter) 

Delaware 
(State or other jurisdiction of incorporation or organization)    

11-3516358 
(I.R.S. Employer Identification Number) 

15245 Shady Grove Road, Suite 455 
Rockville, MD 20850 
(Address of principal executive offices, including zip code) 

Telephone: (240) 268-5300 
(Registrant’s telephone number, including area code) 

Title of Each Class 
Common Stock, $0.0001 par value per share 

Name of Each Exchange On Which Registered 
NYSE MKT 

Indicate by check mark if the registrant is a well-known seasoned issuer, as defined by Rule-405 of the Securities 
Act. Yes (cid:3) No(cid:1) 

Indicate by check mark if the registrant is not required to file reports pursuant to Section 13 or Section 15(d) of the 
Exchange Act.   
Yes (cid:3)  No (cid:1) 

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:1)  No (cid:3) 

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 
(§232.405 of this chapter) during the preceding 12 months (or for such shorter period that the registrant was required 
to submit and post such files). Yes (cid:1) No (cid:3) 

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:1)   

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 definition of “accelerated filer,” “large accelerated filer” and “smaller reporting 
company” in Rule 12b-2 of the Exchange Act. (Check one): 
(cid:3) 
Large Accelerated Filer 
(cid:3) 
Non-Accelerated Filer 
(Do not check if a smaller reporting company) 

Accelerated Filer 
Smaller reporting company 

(cid:1) 
(cid:3) 

Indicate by check mark whether the registrant is a shell company (as defined in Rule 12b-2 of the Exchange Act) 
Yes (cid:3)  No (cid:1) 

State the aggregate market value of the voting and non-voting common equity held by non-affiliates computed by 
reference to the price at which the common equity was last sold, or the average bid and asked price of such common 
equity, as of the last business day of the registrant’s most recently completed second fiscal quarter: As of June 30, 
2016, the aggregate market value of the registrant’s common stock held by non-affiliates of the registrant was 
$51,498,946 based on the closing price reported on NYSE MKT.   

Indicate the number of shares outstanding of each of the issuer’s classes of common stock, as of the latest 
practicable date:   

Class 
Common Stock, $0.0001 par value per share 

Outstanding as of February 24, 2017 
237,443,785 shares 

DOCUMENTS INCORPORATED BY REFERENCE 

Certain portions of the registrant’s Definitive Proxy Statement for its 2017 Annual Meeting of 
Stockholders, which is expected to be filed with the U.S. Securities and Exchange Commission within 120 days 
after the end of the registrant’s fiscal year ended December 31, 2016, are incorporated by reference into Part III of 
this Annual Report on Form 10-K. 

    
 
 
 
 
 
 
 
 
 
 
 
 
 
  
  
 
 
 
 
 
 
 
Cautionary Statement Regarding Forward-Looking Statements. 

This Annual Report on Form 10-K contains statements (including certain projections and 

business trends) accompanied by such phrases as “believe,” “estimate,” “expect,” “anticipate,” “will,” 
“intend” and other similar expressions, that are “forward-looking statements” as defined in the Private 
Securities Litigation Reform Act of 1995.    We caution that forward-looking statements are based largely 
on our expectations and are subject to a number of known and unknown risks and uncertainties that are 
subject to change based on factors that are, in many instances, beyond our control.  Actual results, 
performance or achievements may differ materially from those contemplated, expressed or implied by the 
forward-looking statements.   

Although we believe that the expectations reflected in our forward-looking statements are 
reasonable as of the date we make them, actual results could differ materially from those currently 
anticipated due to a number of factors, including risks relating to: 

• 

• 

• 

• 

• 

• 

• 

• 

• 

• 

• 

• 

our understandings and beliefs regarding the role of certain biological mechanisms and processes 
in cancer; 

our drug candidates being in early stages of development, including in pre-clinical development; 

our ability to initially develop drug candidates for orphan indications to reduce the time-to-market 
and take advantage of certain incentives provided by the U.S. Food and Drug Administration; 

our  ability  to  transition  from  our  initial  focus  on  developing  drug  candidates  for  orphan 
indications to candidates for more highly prevalent indications; 

our ability to successfully and timely complete clinical trials for our drug candidates in clinical 
development; 

uncertainties  related  to  the  timing,  results  and  analyses  related  to  our  drug  candidates  in 
pre-clinical development; 

our  ability  to  obtain  the  necessary  U.S. and  international  regulatory  approvals  for  our  drug 
candidates; 

our  reliance  on  third-party  contract  research  organizations  and  other  investigators  and 
collaborators for certain research and development services; 

our  ability  to  maintain  or  engage  third-party  manufacturers  to  manufacture,  supply,  store  and 
distribute supplies of our drug candidates for our clinical trials; 

our ability to form strategic alliances and partnerships with pharmaceutical companies and other 
partners for sales and marketing of certain of our product candidates; 

demand for and market acceptance of our drug candidates; 

the  scope  and  validity  of  our  intellectual  property  protection  for  our  drug  candidates  and  our 
ability to develop our candidates without infringing the intellectual property rights of others; 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
• 

• 

our lack of profitability and the need for additional capital to operate our business; and 

other risks and uncertainties, including those set forth herein under the caption “Risk Factors” and 
those detailed from time to time in our filings with the Securities and Exchange Commission.   

These forward-looking statements are made only as of the date hereof, and we undertake no obligation to 
update or revise the forward-looking statements, whether as a result of new information, future events or 
otherwise. 

 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
TABLE OF CONTENTS 

PART I 
    Item 1  Description of Business 
    Item 1A  Risk Factors 
    Item 1B  Unresolved Staff Comments 
    Item 2  Description of Property 
    Item 3 
    Item 4  Mine Safety Disclosures 

Legal Proceedings 

Selected Financial Data 

PART II 
    Item 5  Market for Common Equity, Related Stockholder Matters, and Issuer Purchases of Equity Securities 
    Item 6 
    Item 7  Management’s Discussion and Analysis of Financial Condition and Results of Operations 
    Item 7A  Qualitative and Quantitative Disclosures About Market Risk 
Financial Statements and Supplementary Data 
    Item 8 
    Item 9 
Changes In and Disagreements with Accountants on Accounting and Financial Disclosure 
    Item 9A  Controls and Procedures 
    Item 9B  Other Information 

PART III 
    Item 10  Directors, Executive Officers, and Corporate Governance 
    Item 11  Executive Compensation 
    Item 12  Security Ownership of Certain Beneficial Owners and Management and Related Stockholder Matters     
    Item 13  Certain Relationships and Related Transactions; and Director Independence   
    Item 14  Principal Accounting Fees and Services 
    Item 15  Exhibits, Financial Statement Schedules 

SIGNATURES 

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Unless the context requires otherwise, any references in this Annual Report on Form 10-K to “we,” “us,” 
“our,” the “Company” or “Rexahn” refers to Rexahn Pharmaceuticals, Inc. 

PART I 

Item 1.    Description of Business 

Overview   

We are a clinical stage biopharmaceutical company dedicated to the discovery, development and 
commercialization  of  innovative  treatments  for  cancer.  Our  mission  is  to  improve  the  lives  of  cancer 
patients  by  developing  next-generation  cancer  therapies  that  are  designed  to  maximize  efficacy  while 
minimizing  the  toxicity  and  side  effects  traditionally  associated  with  cancer  treatment.  Our  clinical 
pipeline  features  three  oncology  product  candidates  in  Phase  II  clinical  development  and  additional 
compounds  in  pre-clinical  development.  Our  strategy  is  to  continue  building  a  significant  pipeline  of 
innovative oncology product candidates that we intend to commercialize with partners. Our three clinical 
stage drug candidates in active development are RX-3117, SupinoxinTM (RX-5902) and Archexin®.   

•  RX-3117 is a small molecule nucleoside compound with an anti-metabolite mechanism of action, 
and  we  believe  it  has  therapeutic  potential  in  a  broad  range  of  cancers,  including  pancreatic, 
bladder,  colon,  and  lung  cancer.    We  completed  an  exploratory  Phase  I  clinical  study  of 
RX-3117  that  showed  a  level  of  oral  bioavailability  of  RX-3117  in  humans.    In  this  trial, 
RX-3117 appeared to be safe and well tolerated with a predictable pharmacokinetic profile for an 
orally  administered  agent,  with  preliminary  evidence  of  single  agent  activity.  We  are  currently 
conducting a Phase IIa clinical trial of RX-3117 in patients with relapsed or refractory pancreatic 
cancer,  and  a  Phase  IIa  clinical  trial  in  patients  with advanced  muscle-invasive  bladder  cancer.   
RX-3117 has received “orphan drug designation” from the U.S. Food and Drug Administration 
(“FDA”)  for  pancreatic  cancer.    Orphan  drug  designation  provides  tax  incentives  for  clinical 
research  and  a  waiver  from  user  fees  under  certain  circumstances.  In  addition,  an  orphan  drug 
generally  receives  seven  years  of  exclusivity  after  approval  for  a  designated  use,  during  which 
time,  the  FDA  generally  cannot  approve  another  product  with  the  same  active  moiety  for  the 
same indication.     

•  Supinoxin,  or  RX-5902, 

first-in-class 

is  a  potential 

small  molecule 

inhibitor  of 
phosphorylated-p68, a protein that we believe plays a key role in cancer cell growth, progression 
and  metastasis  through  its  interaction  with  beta-catenin.    Phosphorylated  p68,  which  is  highly 
expressed in cancer cells, but not in normal cells, results in up-regulation of cancer-related genes 
and a subsequent proliferation of cancer cells and tumor growth.    Supinoxin selectively blocks 
phosphorylated p68, thereby decreasing the proliferation or growth of cancer cells in preclinical 
models.      We  have  evaluated  Supinoxin  in  a  Phase  I  dose  escalation  study  in  patients  with  a 
diverse range of metastatic, treatment-refractory tumors, including breast, ovarian, colorectal, and 
neuro-endocrine tumors.    In February, 2017, we initiated a Phase IIa clinical study of Supinoxin 
in patients with metastatic triple negative breast cancer (“TNBC”).   

•  Archexin  is  a  potential  best-in-class,  potent  inhibitor  of  the  protein  kinase  Akt-1,  which  we 
believe  plays  a  critical  role  in  cancer  cell  proliferation,  survival,  angiogenesis,  metastasis  and 
drug  resistance.    Archexin  has  received  orphan  drug  designation  from  the  FDA  for  renal  cell 
carcinoma  (“RCC”),  glioblastoma,  ovarian  cancer,  stomach  cancer  and  pancreatic  cancer.    We 
have completed a pilot Phase IIa clinical trial of Archexin for the treatment of pancreatic cancer.   
We  are  currently  conducting  a  Phase  IIa  proof-of-concept  clinical  trial  of  Archexin  in  patients 

1 

 
 
 
 
 
 
 
 
with metastatic renal cell carcinoma who have failed first line treatment to evaluate its safety and 
efficacy in combination with AFINITOR® (everolimus).   

We  also  have  one  drug  candidate 

in  pre-clinical  development:  RX-21101,  an   

N-(2-Hydroxypropyl) methacrylamide-docetaxel-folate, which we believe may provide increased efficacy 
against  tumors  with  potentially  fewer  side  effects  as  a  result  of  specific  tumor  targeting  and  increased 
stability in the body.     

In  addition  to  our  drug  development  efforts,  we  are  also  working  on  proprietary  research 
technologies,  including  our  multi-target  aimed  ligands  platform  and  nano-based  drug  delivery  systems. 
Our unique ligand discovery platform, The Inhibitors of Multi-Expression Signals (“TIMES”), permits us 
to identify potentially important targets that control multiple genes or signaling events in cancer cells. Our 
3-D Gateway of Ligand Discovery (“3-D GOLD”) integrates three-dimensional molecular modeling with 
databases  of  chemicals  and  proteins  and  ligand  filtering  and  generation,  which  helps  us  discover  novel 
lead compounds.    Leveraging this system, we believe that we are able to effectively develop predictive 
models,  formulate  and  test  hypotheses  for  optimizing  efficacy,  and  increase  drug  safety  and 
bioavailability early in the drug discovery process. Our nano-based drug delivery systems, such as those 
used  in  the  multiple  nanoliposomal-  and  nanopolymer-based  anti-cancer  drugs  that  we  are  currently 
testing, may increase the availability of a drug at the disease site, minimize adverse reactions, and provide 
longer duration of action. 

Company Background 

We trace our history to the March 2001 founding of Rexahn, Corp, which in 2005 merged with 
and  into  Rexahn  Pharmaceuticals,  Inc.  (formerly  Corporate  Road  Show.com  Inc.).    Dr.  Peter  Suzdak, 
our Chief Executive Officer since February 2013, has extensive experience in corporate management and 
drug  development,  particularly  in  the  field  of  oncology.    Dr.  Chang  Ahn,  our  founder,  Chief  Scientist 
and  Chairman  Emeritus  of  our  Board  of  Directors,  is  a  former  FDA  reviewer  and  National  Cancer 
Institute  (“NCI”)  research  scientist.    He  guided  our  initial  research  and  commercialization  efforts  in 
targeted oncology drugs.     

Our common stock is currently listed on the NYSE MKT under the trading symbol “RNN.” Our 
principal corporate office is located at 15245 Shady Grove Road, Suite 455, Rockville, Maryland 20850 
in Maryland’s I-270 technology corridor.    Our telephone number is (240) 268-5300.   

2 

 
 
 
 
 
 
 
Industry and Disease Markets   

Market Overview 

Our primary research and development focus is on oncology therapeutics.   A key component of 
our strategy is to develop innovative drugs that are potential first-in-class or market-leading compounds for 
the treatment of cancer. According to the Centers for Disease Control and Prevention, cancer claims the 
lives of more than half a million Americans each year and is the second leading cause of death among 
Americans.   In 2017, the World Health Organization estimated that 14 million new cases of cancer are 
diagnosed  annually  worldwide  and  that  the  incidence  will  to  increase  to  24  million  by  2022.   A   2017 
American Cancer Society report projected that an estimated 1.7 million new cancer cases will be diagnosed 
in the United States in 2017.    In 2015, Evaluate Pharma projected that global annual sales of cancer drugs 
would grow to $153 billion by 2020.   

Current Cancer Treatments 

Traditional cancer treatments involve surgery, radiation therapy and chemotherapy.    Surgery is 
widely used to treat cancer, but may result in related or significant complications and may be ineffective 
if metastasis has occurred.    Radiation therapy, or radiotherapy, can be highly effective in treating certain 
types of cancer.    In radiation therapy, ionizing radiation deposits energy that injures or destroys cells in 
the area being treated by damaging their genetic material, making it impossible for these cells to continue 
to grow.    Although radiation damages both cancer cells and normal cells, the normal cells are generally 
able  to  repair  themselves  and  function  properly.    Chemotherapy  involves  the  use  of  cytotoxic  cancer 
drugs to destroy cancer cells by interfering with various stages of the cell division process.    For certain 
cancers  and  in  certain  patients,  these  drugs  have  limited  efficacy  and  debilitating  adverse  side  effects. 
Administration  of  cytotoxic  cancer  drugs  may  also  result  in  the  development  of  multiple  drug,  or 
multi-drug,  resistance,  which  is  a  condition  that  results  when  certain  tumor  cells  that  have  survived 
treatment with cytotoxic drugs are no longer susceptible to treatment by those and other drugs.    Recent 
advances  in  cancer treatment  include  the  use  of  immunotherapies  to  stimulate  the  body’s  own  immune 
system  to  kill  cancer  cells.    Immunotherapy  can  significantly  improve  survival  in  certain  cancers, 
including  melanoma,  non-small  cell  lung  cancer,  head  and  neck  tumors,  lymphoma  and  renal  cell 
carcinoma.    However, immunotherapy approaches have not been effective in all tumor types and there is 
a  risk  of  over-stimulation  of  the  immune  system  that  can  lead  to  life-threatening  side-effects,  such  as 
colitis, pneumonia, and hepatitis. 

Unmet Needs in Cancer   

Despite  significant  advances  in  cancer  research  and  treatments,  many unmet needs still remain 

including:   

•  Long-term  management  of  cancers:    Surgery,  radiation  therapy  or  chemotherapy  may  not 
result  in  long-term  remission,  although  surgery  and  radiation  therapies  are  considered 
effective methods for some cancers.    There is a need for more effective drugs and adjuvant 
therapies to treat relapsed and refractory cancers. 

•  Multi-drug  resistance:    Multi-drug  resistance  is  a  major  obstacle  to  effectively  treating 

various cancers with chemotherapy. 

•  Debilitating toxicity by chemotherapy:    Chemotherapy as a mainstay of cancer treatment can 
induce severe adverse reactions and toxicities, adversely affecting quality of life or life itself. 

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Market Opportunity 

There are several factors that we believe are favorable for commercializing new cancer drugs that 

may have the potential to be first-in-class or market leaders, including: 

•  Expedited Regulatory or Commercialization Pathways.    Drugs for life-threatening diseases such 
as  cancer  are  often  candidates  for  fast  track  designation,  breakthrough  therapy  designation, 
priority review and accelerated approval, each of which may lead to approval sooner than would 
otherwise be the case. 

•  Favorable  Environment  for  Formulary  Access  and  Reimbursement.    We  believe  cancer  drugs 
with  proven  efficacy  would  gain  rapid  market  uptake,  formulary  listing  and  third-party  payor 
reimbursement.    Drugs with orphan designations are generally reimbursed by third-party payors 
because there are few, if any, alternatives.     

•  Low  Marketing  Costs.    We  believe  the  marketing  of  new  drugs  to  oncologists  can  be 
accomplished  with  a smaller  sales force and lower  related costs than  a sales  force  that  markets 
widely to primary care physicians and general practitioners. 

Our Strategy   

Our strategy is to continue building a significant product pipeline of innovative drug candidates 

that we intend to commercialize alone or with partners.    This strategy has several key components. 

Develop Innovative Therapeutics with the Potential to be First-in-Class or Market Leaders 

We  plan  to  focus  our  research  and  development  pipeline  on  potential  first-in-class  or 
market-leading  compounds  for  the  treatment  of  cancer.    By  expanding  the  breadth  and  depth  of  our 
oncology pipeline, we aim to develop an industry-leading oncology therapeutics franchise.    Our pipeline 
spans several major classes of cancer drugs, including molecular targeted therapies and nano-medicines 
for  targeted  delivery  of  compounds  and  small  molecule  cytotoxic  compounds.  Differentiated  target 
product  profiles  and  proprietary  discovery  and  research  technology  platforms  further  support  these 
strategic efforts.     

Clinically Develop Drug Candidates as Orphan Drugs 

We intend to initially develop drug candidates for cancers that are orphan indications. Under the 
Orphan Drug Act, the FDA may grant orphan drug designation to new drugs developed to treat diseases 
generally affecting less than 200,000 patients.    Benefits associated with orphan drug designation include 
tax  incentives  for  research  and  development  and  an  exemption  from  user  fees  under  certain 
circumstances.  Although  the  standards  for  orphan  drug  approval  are  not  different  than  for  non-orphan 
products,  the  path  to  approval  may  be  faster  because  clinical  trials  may  be  smaller  due  to  the  smaller 
patient population. Further, a drug that is approved for its orphan-designated indication generally receives 
seven  years  of  orphan  drug  exclusivity,  during  which  the  FDA  generally  may  not  approve  any  other 
application for a product containing the same active moiety and proposed for the same indication.    An 
approved orphan drug also may qualify for an exemption from the branded prescription drug fee.    We 
plan to develop drug candidates for cancers that are orphan indications in order to take advantage of the 
benefits of orphan drug designation during development and the exclusivity available under the Orphan 
Drug Act for approved products, as well as the potential for reduced time to market. Drugs intended to 
treat  rare  diseases  or  conditions  also  may  qualify  for  fast  track  designation,  breakthrough  therapy 

4 

 
 
 
 
 
 
 
 
 
 
designation, accelerated approval and/or priority review, any or all of which may speed the development 
and approval process. 

Establish Partnerships with Large Pharmaceutical Companies 

We  seek  to  establish  strategic  alliances  and  partnerships  with  larger  pharmaceutical  companies 

for the commercialization and co-development of our drug candidates. 

In-License Unique Technology 

We continually review opportunities to in-license and advance compounds in oncology that have 

value-creating potential and will strengthen our clinical development pipeline.     

Capitalize on Our Management Team’s Expertise for Drug Development 

Our management team possesses clinical development experience in oncology and several other 
therapeutic areas which facilitates strategic approaches to and competitive advantages in, the design, risk 
assessment  and  implementation  of  drug  development  programs.  Our  management  team  also  has  prior 
experience in pharmaceutical alliances, product launches and marketing. 

Our Pipeline Drug Candidates 

Clinical Stage Pipeline 

RX-3117: Oral Small Molecule Nucleoside 

RX-3117  is a  novel,  investigational  oral small  molecule nucleoside  compound.    In  pre-clinical 
models when activated (phosphorylated) by uridine-cytidine kinase 2, a protein that is overexpressed in 
various human cancer cells, RX-3117 is incorporated into DNA or RNA of cells and inhibits both DNA 
and  RNA  synthesis,  which  induces  apoptotic  cell  death  of  tumor  cells.  We  believe  RX-3117  has 
therapeutic potential in a broad range of cancers including pancreatic, bladder, lung, cervical, non-small 
cell lung cancer and colon cancer.    RX-3117 has received orphan drug designation from the FDA for the 
treatment of patients with pancreatic cancer.    RX-3117 has also been shown in animal models to inhibit 
the growth of gemcitabine-resistant human cancers and improve overall survival.     

RX-3117 has demonstrated broad spectrum anti-tumor activity against over 100 different human 
cancer cell lines and efficacy in 17 different mouse xenograft models. Notably, the efficacy of RX-3117 
in the mouse xenograft models was superior to that of gemcitabine.   Further, RX-3117 still retains its full 
anti-tumor activity in human cancer cell lines made resistant to the anti-tumor effects of gemcitabine.   In 
August 2012, we reported the completion of an exploratory Phase I clinical trial of RX-3117 in cancer 
patients  conducted  in  Europe,  to  investigate  the  oral  bioavailability,  safety  and  tolerability  of  the 
compound.  In  this  study,  oral  administration  of  a  50  mg  dose  of  RX-3117  demonstrated  an  oral 
bioavailability of 56% and a plasma half-life (T1/2) of 14 hours. In addition, RX-3117 appeared to be safe 
and well tolerated in all subjects throughout the dose range tested. 

Final  results  from  the  Phase  Ib  clinical  trial  of  RX-3117  presented  at  the  American  Society  of 
Clinical Oncology Annual Meeting in June 2016 showed evidence of single agent activity. Patients in the 
study had generally received four or more cancer therapies prior to enrollment. In this study, 12 patients 
experienced  stable  disease  persisting  for  up  to  276  days  and  three  patients  showed  evidence  of  tumor 
burden reduction. A maximum tolerated dose of 700 mg was identified in the study.    At the doses tested 

5 

 
 
 
 
 
 
 
 
 
 
 
 
 
to  date,  RX-3117,  administered  orally,  appeared  to  be  safe  and  well  tolerated  with  a  predictable 
pharmacokinetic profile following oral administration. 

In  March  2016,  we  initiated  a  multi-center  Phase  IIa  clinical  trial  of  RX-3117  in  patients  with 
relapsed  or  refractory  pancreatic  cancer  to  further  evaluate  the  safety  and  anti-cancer  properties  of  this 
compound. Patients in the trial will receive a 700 mg daily oral dose of RX-3117, for five consecutive 
days, followed by two days off, for three weeks, followed by a week of rest, in a 28 day cycle for up to 
eight treatment cycles, or until their disease progresses.    The study is designed as a two-stage study with 
10 patients in stage 1 and an additional 40 in stage 2.    According to pre-set criteria, if greater than 20% 
of  the  patients  have  an  increase  in  progression free  survival  of  more  than four  months,  or  an  objective 
clinical response rate and reduction in tumor size, then an additional 40 pancreatic cancer patients would 
be enrolled into stage 2. Secondary endpoints include time to disease progression, overall response rate 
and duration of response, as well as pharmacokinetic assessments and safety parameters.       

In September 2016, we initiated stage 2 of this Phase IIa clinical trial.    The decision to proceed 
was based on satisfying the predefined criteria for preliminary efficacy for stage 1 of the trial.    RX-3117 
was safe and well tolerated with preliminary efficacy seen in pancreatic cancer patients for whom three or 
more prior therapies had been ineffective. 

In September 2016, we commenced enrollment in a Phase IIa trial of RX-3117 in patients with 
advanced bladder cancer.    This Phase IIa clinical trial is a multicenter, open-label, single-agent study of 
RX-3117  being  conducted  at  10  clinical  centers  in  the  United  States.  RX-3117  is  being  administered 
orally five times weekly on a three weeks on, one week off dosing schedule.   The primary endpoint for 
the trial is an assessment of the progression free survival rate or an objective clinical response rate and 
reduction in tumor size.   Secondary endpoints include time to disease progression, overall response rate 
and duration of response, as well as pharmacokinetic assessments and safety. 

Based  on  the  progress  of  the  RX-3117  clinical  development  program  and  the  level  of  interest 
expressed from a number of oncology-focused pharmaceutical companies, we are continuing discussions 
with multiple companies to explore collaborative business structures in an effort to maximize the potential 
value of the program. 

Supinoxin: Potential First-in-Class p68 RNA Helicase Inhibitor 

Supinoxin is  a  potential  first-in-class  small  molecule inhibitor  of  phosphorylated-p68,  a  protein 
that we believe plays a key role in cancer growth, progression and metastasis. Phosphorylated p68, which 
is highly expressed in cancer cells, but not in normal cells, results in up-regulation of cancer-related genes 
and  a  subsequent  proliferation  of  cancer  cells  and  tumor  growth.    Supinoxin  selectively  blocks 
phosphorylated p68, thereby decreasing the proliferation or growth of cancer cells.    In pre-clinical tissue 
culture  models  and  in-vivo  xenograft  models,  Supinoxin  has  exhibited  single-agent  tumor  growth 
inhibition,  potential  synergy  with  cytotoxic  agents  and  activity  against  drug  resistant  cancer  cells.    In 
particular,  in  in-vivo  xenograft  models  of  human  triple  negative  breast  cancer  and  pancreatic  cancer, 
treatment with Supinoxin on days one through 20 in mouse models produced a dose-dependent inhibition 
of tumor growth and a survival benefit. 

Supinoxin was evaluated in a Phase I dose-escalation clinical trial in cancer patients with solid 
tumors designed to evaluate the safety, tolerability, dose-limiting toxicities and the recommended Phase II 
dose.  Secondary  endpoints  include  pharmacokinetic  analyses  and  an  evaluation  of  the  preliminary 
anti-tumor effects of Supinoxin.    We completed enrollment in this study in 2016. 

6 

 
 
 
 
 
 
 
 
 
Updated results from the Phase I clinical trial of Supinoxin were presented in October 2016 at the 

2016 European Society for Medical Oncology Congress.     

The  results  showed  evidence  of  single-agent,  clinical  activity  of  Supinoxin.    In  this  study, 
Supinoxin preliminarily appeared to be safe and well tolerated at the doses and dosing schedules tested with 
no dose limiting toxicities or treatment-related serious adverse events.    The most frequently reported drug 
related adverse events were mild nausea, vomiting and fatigue. Initial signs of clinical activity have been 
observed.    Twenty-four subjects were enrolled (11 female, 13 male), and seven subjects experienced stable 
disease in breast, neuroendocrine, paraganglioma, head/neck or colorectal cancer.    Three subjects received 
treatment for more than one year. Approximately 55% of the subjects had received four or more therapies 
prior to their enrollment in the Phase I clinical study.     

We  initiated  a  Phase  IIa  study  of  Supinoxin  in  patients  with  triple  negative  breast  cancer  in 
February 2017.    The study will evaluate the safety and preliminary efficacy of Supinoxin in patients with 
metastatic  triple  negative  breast  cancer  who  have  failed  prior  treatments.  We  also  plan  to  evaluate 
Supinoxin in combination with other anticancer agents in TNBC, assuming positive data from this initial 
study.     

Based  on  the  progress  of  the  Supinoxin  clinical  development  program  and  the  level  of  interest 
expressed  from  a  number  of  oncology-focused  pharmaceutical  companies,  we  are  continuing  our 
discussions with multiple companies to explore collaborative business structures in an effort to maximize 
the potential commercial value of the program. 

Archexin:    Potential Best-in-Class Anti-Cancer Akt-1 Inhibitor 

Archexin  is  a  potential  best-in-class,  potent  inhibitor  of  the  protein  kinase  Akt-1,  which  we 
believe  plays  a  critical  role  in  cancer  cell  proliferation,  survival,  angiogenesis,  metastasis  and  drug 
resistance. Archexin has received orphan drug designation from the FDA for RCC, glioblastoma, ovarian 
cancer,  stomach  cancer  and  pancreatic  cancer.  We  believe  Archexin  is  differentiated  from  other  Akt-1 
inhibitors by its ability to inhibit both activated and inactivated forms of Akt-1, and as a result it is not 
expected to lead to drug resistance, which has been observed with other protein kinase inhibitors.    Other 
targeted  drugs  may  only  inhibit  inactivated  Akt-1  and  may  also  cause  drug  resistance.    Akt-1  is 
over-activated in patients with many cancers, including breast, colorectal, gastric, pancreatic, prostate and 
melanoma cancers.    Akt-1 activity may be inhibited by signaling molecules upstream of Akt-1 in cancer 
cells through the use of vascular endothelial growth factor and epidermal growth factor receptor inhibitors, 
but  this  treatment  only  indirectly  affects  the  activity  of  native  Akt-1.    Because  signal  transmission  for 
cancer progression and resistance occurs when Akt-1 is activated, we believe it is also important to inhibit 
activated Akt-1.    We believe Archexin inhibits both activated and native Akt-1. 

Archexin is an antisense oligonucleotide compound that is complementary to Akt-1 mRNA and 
highly  selective  for  inhibiting  mRNA  expression,  which  leads  to  reduced  production  of  Akt-1  protein.   
Archexin preliminarily appeared to be safe and well tolerated with minimal side effects in a Phase I study 
in  patients  with  advanced  cancers,  where  Grade  3  fatigue  was  the  only  dose-limiting  toxicity  and  no 
significant hematological abnormalities were observed. The main objectives of the Phase I study were to 
determine  the  maximum  tolerated  dose,  dose  limiting  toxicity  and  pharmacokinetic  parameters  for 
Archexin  monotherapy.    The  Archexin  Phase  I  study  design  was  an  open  label,  single  arm  ascending 
dose, safety and tolerability study.     

We completed a Phase IIa clinical trial for Archexin that was designed to assess the safety and 
efficacy  of  Archexin  in  combination  with  gemcitabine.  Gemcitabine  is  used  to  treat  pancreatic,  breast, 
ovarian, and lung cancers, and may be used for other cancers as well. The study enrolled 31 patients with 

7 

 
 
 
 
 
 
 
 
metastatic pancreatic cancer in the United States and India and showed that treatment with Archexin in 
combination with gemcitabine provided a median survival rate of 9.1 months compared to the historical 
survival rate of 5.7 months for single-agent gemcitabine therapy. We are not currently seeking to further 
develop Archexin in combination with gemcitabine.   

We are conducting an ongoing Phase IIa proof-of-concept clinical trial of Archexin to study its 
safety  and  efficacy  in  patients  with  metastatic  RCC.  In  this  trial,  Archexin  is  being  administered  in 
combination with Afinitor® (everolimus).    The trial is being conducted in two stages.    Stage 1 was a dose 
ranging  study,  with  up  to  three  dose  groups  with  three  RCC  patients  each,  to  determine  its  maximum 
tolerated dose (“MTD”) in combination with everolimus.    In January 2016, we completed Stage 1 of the 
study and commenced enrollment in Stage 2, which is a randomized, open-label, two-arm dose expansion 
study of everolimus versus Archexin in combination with everolimus to determine safety and efficacy of 
the combination.    This phase of the trial (Stage 2) is anticipated to enroll up to 30 RCC patients who will be 
randomized to receive either Archexin in combination with everolimus, or everolimus alone, in a ratio of 
2:1 The MTD was determined to be 250 mg/m2/day of Archexin, which was identified in Stage 1 and will 
be administered in Stage 2 along with 10 mg of everolimus compared to 10 mg everolimus alone. 

Pre-Clinical Pipeline 

RX-21101:    Nano-polymer Anti-cancer Drug 

RX-21101 is an investigational anti-cancer nano-polymer drug that we believe can mitigate some 
of  the  limitations  of  cytotoxic  compounds,  such  as  poor  solubility  and  severe  adverse  reactions. 
Conjugating  water-soluble  and  non-toxic  N-(2-Hydroxypropyl)methacrylamide 
to  conventional 
anti-cancer  compounds  may  bolster  efficacy  while  lowering  toxicity  by  specific  tumor  targeting  and 
increased  stability  in  the  body.  In  June  2015,  RX-21101  was  selected  by  NCI’s  Nanotechnology 
Characterization Laboratory for its pre-clinical characterization program to facilitate the advancement of 
RX-21101 towards human clinical trials.     

Research and Development Process 

We  have  engaged  third-party  contract  research  organizations  and  other  investigators  and 
collaborators, such as universities and medical institutions, to conduct our pre-clinical studies, toxicology 
studies and clinical trials. Engaging third-party contract research organizations is typical practice in our 
industry. However, relying on such organizations means that the clinical trials and other studies described 
above are being conducted at external locations and that the completion of these trials and studies is not 
within our direct control. Trials and studies may be delayed due to circumstances outside our control, and 
such delays may result in additional expenses for us. 

Competition 

We  compete  against  fully  integrated  pharmaceutical  companies  and  smaller  companies  that  are 
collaborating  with  larger  pharmaceutical  companies,  as  well  as  academic  institutions,  government 
agencies and other public and private research organizations. Many of these competitors, either alone or 
together  with  their  collaborative  partners,  operate  larger  research  and  development  programs  or  have 
substantially greater financial resources than we do, as well as more experience in: 

•  developing drugs; 

•  undertaking pre-clinical testing and human clinical trials; 

8 

 
 
 
 
 
 
 
 
•  obtaining FDA and other regulatory approvals of drugs; 

• 

• 

formulating and manufacturing drugs; and 

launching, marketing and selling drugs. 

Large  pharmaceutical companies  currently  sell  both generic and  proprietary  compounds  for the 
treatment  of  cancer.  In  addition,  companies  developing  oncology  therapies  represent  substantial 
competition. Many of these organizations have substantially greater capital resources, larger research and 
development staff and facilities, longer drug development history in obtaining regulatory approvals and 
greater manufacturing and marketing capabilities than we do. These organizations also compete with us to 
attract qualified personnel, parties for acquisitions, joint ventures or other collaborations. 

We are aware of products under development by our competitors that target the same indications 
as  our  clinical  stage  drug  candidates.  If  approved,  Archexin  could  compete  with  other  Akt-1  inhibitors 
under  development  by  other  companies  including  Merck  &  Company,  Inc.,  GlaxoSmithKline, 
AstraZeneca,  Gilead  Sciences,  MEI  Pharma,  PIQUR  Therapeutics  and  others.    Archexin  will  also 
compete with carbozantinib (Exelexis) and lenvatinib (Eisai), multi-kinase inhibitors that were approved 
for RCC in 2016, and also with FDA-approved immunotherapy nivolumab (BMS). If approved, RX-3117 
could  compete  with  other  compounds  with  an  anti-metabolite  mechanism  of  action  in  cancers,  such  as 
sapacitabine, which is under development by Cyclacel.    We are not currently aware of known inhibitors 
of phosphorylated p68 that would compete with Supinoxin if Supinoxin were approved, but other drugs 
with  a  different  mechanism  of  action  are  in  development  for  the  same  indications,  such  as 
Immunomedics’ sacitazumab govitecan and Celldex’s Glenbatumumab vedotin, both in development for 
triple  negative  breast  cancer.  Our  competitors  may  succeed  in  developing  products  that  are  more  safe 
and/or effective than ours, which could render our product candidates less competitive prior to recovery 
by us of expenses incurred with respect to their development.   

Government Regulation   

Regulation by governmental authorities in the United States and in other countries is a significant 
consideration in our product development, manufacturing and marketing strategies.    We expect that all 
of our drug candidates will require regulatory approval by the FDA and by similar regulatory authorities 
in foreign countries prior to commercialization and will be subjected to rigorous pre-clinical, clinical, and 
post-approval  testing  to  demonstrate  safety  and  effectiveness,  as  well  as  other  significant  regulatory 
requirements  and  restrictions  in  each  jurisdiction  in  which  we  would  seek  to  market  our  products.   
U.S. federal  laws  and  regulations  govern  the testing,  development,  manufacture,  quality  control,  safety, 
effectiveness,  approval,  storage,  labeling,  record  keeping,  reporting,  distribution,  import,  export  and 
marketing of all biopharmaceutical products intended for therapeutic purposes.    We believe that we and 
the  third  parties  that  work  with  us  are  in  compliance  in  all  material  respects  with  currently  applicable 
rules and regulations, however, any failure to comply could have a material negative impact on our ability 
to successfully develop and commercialize our products, and therefore on our financial performance.    In 
addition,  these  rules  and  regulations  are  subject  to  change.    For  example,  in  December  2016,  the  21st 
Century Cures Act (“Cures Act”) was signed into law. The Cures Act included numerous provisions that 
may  be  relevant  to  our  product  candidates,  including  provisions  designed  to  speed  development  of 
innovative therapies and provide funding for certain cancer-related research and technology development.   
Because the Cures Act has only recently been enacted, it is difficult to know whether, how, or when it 
may  affect  our  business.    Similarly,  further  legislative  and  regulatory  changes  appear  possible  in  the 
115th United States Congress and under the Trump Administration, and it is difficult to foresee whether, 
how, or when such changes may affect our business. 

9 

 
 
 
 
 
 
 
 
Obtaining  governmental  approvals  and  maintaining  ongoing  compliance  with  applicable 
regulations  are  expected  to  require  the  expenditure  of  significant  financial  and  human  resources  not 
currently  at  our  disposal.    We  plan  to  fulfill  our  short-term  needs  through  consulting  agreements  and 
joint  ventures  with  academic  or corporate  partners  while  developing  our own  internal  infrastructure  for 
long-term corporate growth. 

Development and Approval 

The  process  to  obtain  approval  for  biopharmaceutical  compounds  for  commercialization  in  the 
United States and many other countries is lengthy, complex and expensive, and the outcome is far from 
certain.    Although  foreign  requirements  for  conducting  clinical  trials  and  obtaining  approval  may  be 
different than in the United States, they often are equally rigorous and the outcome cannot be predicted 
with confidence. A key component of any submission for approval in any jurisdiction is pre-clinical and 
clinical data demonstrating the product’s safety and effectiveness.     

Pre-clinical Testing.    Before testing any compound in humans in the United States, a company 
must  develop  pre-clinical  data,  generally  including  laboratory  evaluation  of  product  chemistry  and 
formulation, as well as toxicological and pharmacological studies in animal species to assess safety and 
quality.    Certain  types  of  animal  studies  must  be  conducted  in  compliance  with  the  FDA’s  Good 
Laboratory  Practice  regulations  and  the  Animal  Welfare  Act,  which  is  enforced  by  the  Department  of 
Agriculture. 

IND  Application.    In  the  United  States,  FDA  regulations  require  that  the  person  or  entity 
sponsoring  or  conducting  a  clinical  study  for  the  purpose  of  investigating  a  candidate’s  safety  and 
effectiveness  submit  to  the  FDA  an  investigational  new  drug  (“IND”)  application,  which  contains 
pre-clinical testing results and provides a basis for the FDA to conclude that there is an adequate basis for 
testing  the  drug  in  humans.    If  the  FDA  does  not  object  to  the  IND  application  within  30  days  of 
submission, the clinical testing proposed in the IND may begin.    Even after the IND has gone into effect 
and clinical testing has begun, the FDA may put the clinical trials on “clinical hold,” suspending (or in 
some cases, ending) them because of safety concerns or for other reasons.     

Clinical  Trials.    Clinical  trials  involve  administering  a  drug  to  human  volunteers  or  patients, 
under  the  supervision  of  a  qualified  clinical  investigator.    Clinical  trials  are  subject  to  extensive 
regulation.    In  the  United  States,  this  includes  compliance  with  the  FDA’s  bioresearch  monitoring 
regulations and Good Clinical Practice (“GCP”) requirements, which establish standards for conducting, 
recording data from, and reporting the results of, clinical trials, with the goal of assuring that the data and 
results are credible and accurate and that study participants’ rights, safety and well-being are protected.   
Each  clinical  trial  must  be  conducted  under  a  protocol  that  details  the  study  objectives,  parameters  for 
monitoring safety and the efficacy criteria, if any, to be evaluated.    The protocol is submitted to the FDA 
as part of the IND and reviewed by the agency before the study begins.    Additionally, each clinical trial 
must be reviewed, approved and conducted under the auspices of an Institutional Review Board (“IRB”).   
The  sponsor  of  a  clinical  trial,  the  investigators  and  IRBs  each  must  comply  with  requirements  and 
restrictions  that  govern,  among  other  things,  obtaining  informed  consent  from  each  study  subject, 
complying with the protocol and investigational plan, adequately monitoring the clinical trial, and timely 
reporting  adverse  events.    Foreign  studies  conducted  under  an  IND  must  meet  the  same  requirements 
applicable to studies conducted in the United States.    However, if a foreign study is not conducted under 
an IND, the data may still be submitted to the FDA in support of a product application, if the study was 
conducted in accordance with GCP and the FDA is able to validate the data. 

10 

 
 
 
 
 
 
 
 
Sponsors  of  clinical  trials  are  required  to  make  public  certain  information  about  active  clinical 
trials  and  trial  results  by  posting  the  information  on  government  or  independent  websites,  such  as 
http://clinicaltrials.gov.    Clinical testing is typically performed in three phases. 

In Phase I, the drug is administered to a small number of human subjects to confirm its safety and 
to  develop  detailed  profiles  of  its  pharmacological  and  pharmacokinetic  actions  (i.e.,  absorption, 
distribution,  metabolism,  and  excretion).    Although  Phase  I  trials  typically  are  conducted  in  healthy 
human subjects, in some instances (including, for example, with some cancer therapies) the study subjects 
are patients with the targeted disease or condition. 

In Phase II, the drug is administered to groups of patients (usually no more than several hundred) 
to develop initial data regarding efficacy against the targeted disease and determine the requisite dose and 
dose intervals, and generate additional information regarding the drug’s safety.    In a typical development 
program, additional animal toxicology studies precede this phase.    In some cases, the trial can be split 
into Phase IIa and IIb studies in order to test smaller subject pools.    Some Phase I clinical studies may 
proceed in parallel with some Phase II studies.     

In Phase III, the drug is administered to a larger group of patients (usually from several hundred 
to several thousand or more).    Phase III studies also can include patients with concomitant diseases and 
medications.    Larger patient populations are evaluated in Phase III at multiple study sites and registration 
studies may be conducted concurrently for the sake of time and efficiency.    The extensive clinical testing 
is intended to obtain additional information about product safety and effectiveness necessary to evaluate 
the drug’s overall risk-benefit profile and to provide a basis for physician labeling.    Phase III data often 
form the core basis on which the FDA evaluates the product’s safety and effectiveness when considering 
an application to market the drug. 

The study sponsor, the FDA or an IRB may suspend or terminate a clinical trial at any time on 
various  grounds,  including  a  determination  that  study  subjects  are  being  exposed  to  an  unacceptable 
health  risk.    Additionally,  success  in  early-stage  clinical  trials  does  not  assure  success  in  later-stage 
clinical  trials,  and  data  from  clinical  trials  are  not  always  conclusive  and  may  be  subject  to  alternative 
interpretations that could delay, limit or prevent approval. 

NDA Submission and Review.    After completing the clinical studies, a sponsor seeking approval 
to market a drug in the United States submits to the FDA a New Drug Application (“NDA”).    The NDA 
is  a  comprehensive,  multi-volume  application  intended  to  demonstrate  the  product’s  safety  and 
effectiveness and includes, among other things, pre-clinical and clinical data, information about the drug’s 
composition,  the  sponsor’s  plans  for  manufacturing  and  packaging  and  proposed  labeling.    When  an 
NDA is submitted, the FDA makes an initial determination as to whether the application is sufficiently 
complete to be accepted for review.    If the application is not, the FDA may refuse to accept the NDA for 
filing  and  request  additional  information.    A  refusal  to  file,  which  requires  resubmission  of  the  NDA 
with the requested additional information, delays review of the application.   

FDA performance goals regarding the timeliness of NDA review generally provide for action on 
an  NDA  within  12  months  of  its  submission.    That  deadline  can  be  extended  under  certain 
circumstances, including by the FDA requests for additional information.    The targeted action date can 
also  be  shortened  to  eight  months  after  submission,  for  products  that  are  intended  to  treat  serious  or 
life-threatening conditions and demonstrate the potential to address unmet medical needs.    Additionally, 
the  FDA  has  programs  for  enhanced  communication  and  consultation  and  other  steps  to  expedite 
submission  and  consideration  of  such  products.    For  example,  the  Fast  Track  program  is  intended  to 
expedite or facilitate the process for reviewing new drugs that demonstrate the potential to address unmet 
medical needs involving serious or life-threatening diseases or conditions. If a drug receives Fast Track 

11 

 
 
 
 
 
 
 
 
designation,  the  FDA  may  consider  reviewing  sections  of  the  NDA  on  a  rolling  basis,  rather  than 
requiring the entire application to be submitted to begin the review. Products with Fast Track designation 
also may be eligible for more frequent meetings and correspondence with the FDA about the product’s 
development.    Other FDA programs intended to expedite development and review include Accelerated 
Approval, which allows approval on the basis of a surrogate endpoint that is reasonably likely to predict 
clinical benefit and Breakthrough Therapy designation, which is available for drugs under development 
for serious or life-threatening conditions and where preliminary clinical evidence shows that the drug may 
have substantial improvement on at least one clinically significant endpoint over available therapy.    If a 
drug receives Breakthrough Therapy designation, it will be eligible for all of the benefits of Fast Track 
designation,  as  well  as  for  more  intensive  guidance  from  the  FDA  on  an  efficient  drug  development 
program and a commitment from the agency to involve senior FDA managers in such guidance.    Even if 
a product qualifies for Fast Track designation or Breakthrough Therapy designation, the FDA may later 
decide  that the  product  no  longer  meets  the  conditions  for qualification,  and/or  may  determine  that  the 
product  does  not  meet  the  standards  for  approval.    We  anticipate,  but  cannot  ensure,  that  our  product 
candidates will qualify for such programs. 

If  it  concludes  that  an  NDA  does  not  meet  the  regulatory  standards  for  approval,  the  FDA 
typically issues a Complete Response letter, which communicates the reasons for the agency’s decision 
not to approve the application and may request additional information, including additional clinical data.   
An  NDA  may  be  resubmitted  with  the  deficiencies  addressed,  but  that  does  not  guarantee  approval.   
Data from clinical trials are not always conclusive, and the FDA’s interpretation of data may differ from 
the  sponsor’s.    Obtaining  approval  can  take  years,  requires  substantial  resources  and  depends  on  a 
number  of  factors,  including  the  severity  of  the  targeted  disease  or  condition,  the  availability  of 
alternative  treatments,  and  the  risks  and  benefits  demonstrated  in  clinical  trials.    Additionally,  as  a 
condition of approval, the FDA may impose restrictions that could affect the commercial prospects of a 
product, such as a Risk Evaluation and Mitigation Strategy, and could require post-approval commitments 
to conduct additional studies or conduct surveillance programs to monitor the drug’s effects.     

Moreover, once a product is approved, information about its safety or effectiveness from actual 
use  can  limit  or  prevent  successful  commercialization,  either  because  of  regulatory  action  or  market 
forces.    Post-approval  modifications  to  a  drug  product,  such  as  changes  in  indications,  labeling  or 
manufacturing processes or facilities, may require development and submission of additional information 
or data in a new or supplemental NDA, which would also require FDA approval. 

One  of  our  drug  candidates,  Archexin  is  an  antisense  oligonucleotide  (“ASO”)  compound.  To 
date, the FDA has not approved any NDAs for any ASO compounds for cancer treatment; however, the 
FDA  has  approved  the  ASO  compounds  fomivirsen  (marketed  as  Vitravene®)  as  a  treatment  for 
cytomegalovirus  retinitis,  and  mipomersen  sodium  (marketed  as  Kynamro®),  as  a  treatment  for 
homozygous  familial  hypercholesterolemia.  In  addition,  Archexin  is  in  a  drug  class  known  as  Akt-1 
inhibitors, and drugs from this class have not been approved by the FDA to date.   

We have not submitted an NDA for any of our drug candidates. 

Exclusivity  and  Patent  Protection.    In  the  United  States  and  elsewhere,  certain  regulatory 
exclusivities  and  patent  rights  can  provide  an  approved  drug  product  with  protection  from  certain 
competitors’  products  for  a  period  of  time  and  within  a  certain  scope.    In  the  United  States,  those 
protections include exclusivity under the Orphan Drug Act, which is available for drugs intended to treat 
rare  diseases  or  conditions,  which  generally  are  diseases  or  conditions  that  affect  fewer  than 
200,000 persons in  the  United  States.    If  a  sponsor  demonstrates  that a  drug  is intended  to  treat a  rare 
disease or condition and meets other qualifying criteria, the FDA grants orphan drug designation to the 
product  for  that  use.    A  product  that  has  received  orphan  drug  designation  is  eligible  for  research  and 

12 

 
 
 
 
 
 
development tax credits and is exempt from user fees under certain circumstances.    Additionally, a drug 
that  is  approved  for  its  orphan-designated  indication  generally  receives  seven  years  of  orphan  drug 
exclusivity.    During that period, the FDA generally may not approve any other application for a product 
containing the same active moiety and proposed for the same indication.    There are exceptions, however, 
most  notably  when  the  later  product  is  shown  to  be  clinically  superior  to  the  product  with  exclusivity.   
An  approved  orphan  drug  also  may  qualify  for  an  exemption  from  the  branded  prescription  drug  fee.   
Products that qualify for orphan designation may also qualify for other FDA programs that are intended to 
expedite  the  development  and  approval  process  and,  as  a  practical  matter,  clinical  trials  for  orphan 
products  may  be  smaller,  simply  because  of  the  smaller  patient  population.    Nonetheless,  the  same 
approval standards apply to orphan-designated products as for other drugs.     

Archexin  has  received  orphan  drug  designation  from  the  FDA  for  RCC,  glioblastoma,  ovarian 
cancer,  stomach  cancer  and  pancreatic  cancer.    RX-3117  received  orphan  drug  designation  for 
pancreatic cancer in September 2014. 

Generic Competition.    Any drug candidates approved for commercial marketing under an NDA 
would  be  subject  to  the  provisions  of  the  Drug  Price  Competition  and  Patent  Term  Restoration  Act  of 
1984, known as the Hatch-Waxman Act.    Among other things, the Hatch-Waxman Act establishes two 
abbreviated  approval  pathways  for  drug  products  that  are  in  some  way  follow-on  versions  of  already 
approved  NDA  products,  including  generic  versions  of  the  approved  product,  which  may  be  approved 
under an Abbreviated New Drug Application by a showing that the generic product is the “same as” the 
approved  product  in  key  respects.    Those  abbreviated  approval  pathways  generally  are  available, 
however, after expiration of certain periods of regulatory exclusivity and/or extended patent protection, 
which  the  Hatch-Waxman  Act  also  provides.    These  protections  include:  (1)  five  years  of  regulatory 
exclusivity  for  a  new  chemical  entity  (generally,  the  first  approval  of  a  product  containing  a  particular 
active  moiety),  during  which  an  application for  a  follow-on  product  cannot  be  accepted  for review;  (2) 
three years of exclusivity for the approval of an NDA or supplemental NDA that contains data from new 
clinical  investigations  that  were  necessary  for  approval,  during  which  the  follow-on  product  may  not 
receive  final  approval;  and  (3)  up  to  five  years’  extension  of  the  term  of  a  patent  covering  a  drug  that 
contains an active ingredient not previously approved.    The Hatch-Waxman Act also provides a means 
for the sponsor of an approved NDA to act before approval of a proposed ANDA to sue to protect patents 
claiming the drug substance, drug product, or an approved method of using the drug.    The laws of other 
key  markets  likewise  create  both  opportunities  for  exclusivity  periods  and  patent  protections  and  the 
possibility  of  generic  competition  once  such  periods  or  protections  have  either  expired  or  have  been 
successfully challenged by generic entrants. 

Post-Approval Regulation 

Once approved, products are subject to continuing extensive regulation by the FDA.    If ongoing 
regulatory requirements are not met, or if safety problems occur after a product reaches market, the FDA 
may take actions to change the conditions under which the product is marketed, including suspending or 
even  withdrawing  approval.    In  addition  to  FDA  regulation,  the  healthcare  industry,  and  therefore  our 
business, is also subject to extensive federal, state, local and foreign regulation.     

Good  Manufacturing  Practices.    Companies  engaged  in  manufacturing  drug  products  or  their 
components must comply with applicable current Good Manufacturing Practice (“cGMP”) requirements, 
which  include  requirements  regarding  organization  and  training  of  personnel,  building  and  facilities, 
equipment, control of components and drug product containers, closures, production and process controls, 
packaging  and  labeling  controls,  holding  and  distribution,  laboratory  controls  and  records  and  reports.   
The  FDA  inspects  equipment,  facilities  and  manufacturing  processes  before  approval  and  conducts 
periodic  re-inspections  after  approval.    Failure  to  comply  with  applicable  cGMP  requirements  or  the 

13 

 
 
 
 
 
 
     
conditions  of  the  product’s  approval  may  lead  the  FDA  to  take  administrative  enforcement  action.   
Although  we  periodically  monitor  FDA  compliance  of  the  third  parties  on  which  we  rely  for 
manufacturing  our  drug  products,  we  cannot  be  certain  that  our  present  or  future  third-party 
manufacturers will consistently comply with cGMP or other applicable FDA regulatory requirements. 

Sales and Marketing.    Once a product is approved, its advertising, promotion and marketing will 
be  subject  to  close  regulation,  including  with  regard  to  promotion  to  healthcare  practitioners, 
direct-to-consumer advertising, communications regarding unapproved uses, industry-sponsored scientific 
and  educational  activities  and  promotional  activities  involving  the  internet.  In  addition  to  FDA 
restrictions on marketing of pharmaceutical products, state and federal fraud and abuse laws have been 
applied to restrict certain marketing practices in the pharmaceutical industry for many years.    Some of 
the pertinent laws are open to a variety of interpretations. In addition, these laws and their interpretations 
are subject to change.   

Other  Requirements.    Companies  that  manufacture  or  distribute  drug  products  pursuant  to 
approved  NDAs  must  meet  numerous  other regulatory  requirements,  including adverse  event  reporting, 
submission of periodic reports, and record-keeping obligations. 

Fraud and Abuse Laws.    At such time as we market, sell and distribute any products for which 
we obtain marketing approval, it is possible that our business activities could be subject to scrutiny and 
enforcement under one or more federal or state health care fraud and abuse laws and regulations, which 
could  affect  our  ability  to  operate  our  business.    These  restrictions  under  applicable  federal  and  state 
health care fraud and abuse laws and regulations that may affect our ability to operate include: 

•  The federal Anti-Kickback Law, which prohibits, among other things, knowingly or willingly 
offering, paying, soliciting or receiving remuneration, directly or indirectly, in cash or in kind, 
to induce or reward the purchasing, leasing, ordering or arranging for or recommending the 
purchase, lease or order of any health care items or service for which payment may be made, 
in  whole  or  in  part,  by  federal  healthcare  programs  such  as  Medicare  and  Medicaid.  This 
statute has been interpreted to apply to arrangements between pharmaceutical companies on 
one  hand  and  prescribers,  purchasers  and  formulary  managers  on  the  other.  Further,  the 
Affordable Care Act clarified among other things that liability may be established under the 
federal Anti-Kickback Law without proving actual knowledge of the statute or specific intent 
to violate it. In addition, the Affordable Care Act amended the Social Security Act to provide 
that  the  government  may  assert  that  a  claim  including  items  or  services  resulting  from  a 
violation  of  the  federal  Anti-Kickback  Law  constitutes  a  false  or  fraudulent  claim  for 
purposes  of  the  federal  civil  False  Claims  Act.  Although  there  are  a  number  of  statutory 
exemptions and regulatory safe harbors to the federal Anti-Kickback Law protecting certain 
common  business  arrangements  and activities  from  prosecution  or  regulatory  sanctions,  the 
exemptions and safe harbors are drawn narrowly, and practices that do not fit squarely within 
an exemption or safe harbor, or for which no exception or safe harbor is available, may be 
subject to scrutiny; 

•  The  federal  civil  False  Claims  Act,  which  prohibits,  among  other  things,  individuals  or 
entities from knowingly presenting, or causing to be presented, a false or fraudulent claim for 
payment of government funds or knowingly making, using or causing to be made or used, a 
false  record  or  statement  material  to  an  obligation  to  pay  money  to  the  government  or 
knowingly  concealing  or  knowingly  and  improperly  avoiding,  decreasing  or  concealing  an 
obligation  to  pay  money  to  the  federal  government.  Many  pharmaceutical  and  other 
healthcare  companies  have  been  investigated  and  have  reached  substantial  financial 
settlements  with  the  federal  government  under  the  civil  False  Claims  Act  for  a  variety  of 

14 

 
 
 
 
 
alleged improper marketing activities, including: providing free product to customers with the 
expectation that the customers would bill federal programs for the product; providing sham 
consulting fees, grants, free travel and other benefits to physicians to induce them to prescribe 
the  company’s  products;  and  inflating  prices  reported  to  private  price  publication  services, 
which are used to set drug payment rates under government healthcare programs. In addition, 
in recent years the government has pursued civil False Claims Act cases against a number of 
pharmaceutical  companies  for  causing  false  claims  to  be  submitted  as  a  result  of  the 
marketing of their products for unapproved, and thus non-reimbursable, uses. Pharmaceutical 
and other healthcare companies also are subject to other federal false claim laws, including, 
among  others,  federal  criminal  healthcare  fraud  and  false  statement  statutes  that  extend  to 
non-government health benefit programs; 

•  Analogous state laws and regulations, such as state anti-kickback and false claims laws, may 
apply to items or services reimbursed under Medicaid and other state programs or, in several 
states, apply regardless of the payor. Some state laws also require pharmaceutical companies 
to report expenses relating to the marketing and promotion of pharmaceutical products and to 
report  gifts and  payments  to  certain  healthcare  providers in  the  states.  Other  states  prohibit 
providing  meals  to  prescribers  or  other  marketing  related  activities.  In  addition,  California, 
Connecticut,  Nevada  and  Massachusetts  require  pharmaceutical  companies  to  implement 
compliance programs or marketing codes of conduct.   

•  The  federal  Physician  Payment  Sunshine  Act,  being  implemented  as  the  Open  Payments 
Program,  requires  certain  pharmaceutical  manufacturers  to  engage  in  extensive  tracking  of 
payments  and  other  transfers  of  value  to  physicians  and  teaching  hospitals,  and  to  submit 
such data to the Centers for Medicare and Medicaid Services (“CMS”), which will then make 
all  of  this  data  publicly  available  on  the  CMS  website.  Pharmaceutical  manufacturers  with 
products  for  which  payment  is  available  under  Medicare,  Medicaid  or  the  State  Children’s 
Health Insurance Program are required to track reportable payments and must submit a report 
to CMS on or before the 90th day of each calendar year disclosing reportable payments made 
in the previous calendar year.    Failure to comply with the reporting obligations may result in 
civil monetary penalties; 

•  The federal Foreign Corrupt Practices Act of 1997 and other similar anti-bribery laws in other 
jurisdictions 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.    Recently, there has been a substantial increase in anti-bribery law enforcement 
activity by U.S. regulators, with more frequent and aggressive investigations and enforcement 
proceedings  by  both  the  Department  of  Justice  and  the  U.S.  Securities  and  Exchange 
Commission (the “SEC”).    Violations of 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 internal or government investigations or legal or regulatory 
proceedings,  including  lawsuits  brought  by  private  litigants,  may  also  follow  as  a 
consequence. 

Violations of any of the laws described above or any other governmental regulations are punishable by 
significant  civil,  criminal  and  administrative  penalties,  damages,  fines  and  exclusion  from 
government-funded  healthcare  programs,  such  as  Medicare  and  Medicaid.    Although  compliance 
programs  can  mitigate  the  risk  of  investigation  and  prosecution  for  violations  of  these  laws,  the  risks 
cannot  be  entirely  eliminated.    Moreover,  achieving and  sustaining  compliance  with  applicable federal 
and state privacy, security and fraud laws may prove costly. 

15 

 
Privacy  Laws.    We  are  also  subject  to  laws  and  regulations  covering  data  privacy  and  the 
protection of health-related and other personal information. The legislative and regulatory landscape for 
privacy and data protection continues to evolve, and there has been an increasing focus on privacy and 
data protection issues which may affect our business, including recently enacted laws in all jurisdictions 
where  we  operate.   Numerous  federal  and  state  laws,  including  state  security  breach  notification  laws, 
state  health  information  privacy  laws  and  federal  and  state  consumer  protection  laws,  govern  the 
collection, use and disclosure of personal information. Failure to comply with such laws and regulations 
could  result  in  government  enforcement  actions  and  create  liability  for  us  (including  the  imposition  of 
significant penalties), private litigation and/or adverse publicity that could negatively affect our business.   
In  addition,  if  we  successfully  commercialize  our  drug  candidates,  we  may  obtain  patient  health 
information from healthcare providers who prescribe our products and research institutions we collaborate 
with, and they are subject to privacy and security requirements under the Health Insurance Portability and 
Accountability  Act  of  1996,  as  amended  by  the  Health  Information  Technology  for  Economic  and 
Clinical Health Act (“HIPAA”).   Although we are not directly subject to HIPAA other than with respect 
to  providing  certain  employee  benefits,  we  could  potentially  be  subject  to  criminal  penalties  if  we 
information  maintained  by  a 
knowingly  obtain  or  disclose 
HIPAA-covered entity in a manner that is not authorized or permitted by HIPAA. 

identifiable  health 

individually 

Coverage and Reimbursement 

Significant uncertainty exists as to the coverage and reimbursement status of any drug candidates 
for which we may obtain regulatory approval.    The regulations that govern marketing approvals, pricing 
and  reimbursement  for  new  drug  products  vary  widely  from  country  to  country.  Current  and  future 
legislation may significantly change the approval requirements in ways that could involve additional costs 
and cause delays in obtaining approvals. Some countries require approval of the sale price of a drug before 
it can be marketed. In many countries, the pricing review period begins after marketing or product licensing 
approval  is  granted.  In  some  foreign  markets,  prescription  pharmaceutical  pricing  remains  subject  to 
continuing  governmental  control  even  after  initial  approval  is  granted.  As  a  result,  we  might  obtain 
marketing approval for a product in a particular country, but then be subject to price regulations that delay 
our commercial launch of the product, possibly for lengthy time periods, which could negatively impact the 
revenues we are able to generate from the sale of the product in that particular country. Adverse pricing 
limitations may hinder our ability to recoup our investment in one or more product candidates even if our 
product candidates obtain marketing approval. 

Our ability to commercialize any products successfully also will depend in part on the extent to 
which coverage and adequate reimbursement for these products and related treatments will be available in a 
timely manner from government third-party  payors,  including  government  healthcare  programs  such  as 
Medicare  and  Medicaid,  commercial  health  insurers  and  managed  care  organizations.    Government 
authorities  and  other  third-party  payors,  such  as  private  health  insurers  and  health  maintenance 
organizations,  determine  which  medications  they  will  cover  and  establish  reimbursement  levels.   
Third-party  payors  may  limit  coverage  to  specific  products  on  an  approved  list,  or  formulary,  which 
might not include all of FDA approved products for a particular indication.    The process for determining 
whether a payor will provide coverage for a product may be separate from the process for setting the price 
or reimbursement rate that the payor will pay for the product once coverage is approved.     

A primary trend in the U.S. healthcare industry and elsewhere is cost containment.    Government 
healthcare  programs  and  other  third-party  payors  are  increasingly  challenging  the  prices  charged  for 
medical  products  and  services  and  examining  the  medical  necessity  and  cost-effectiveness  of  medical 
products  and  services,  in  addition  to  their  safety  and  efficacy,  and  have attempted to control costs by 
limiting coverage and the amount of reimbursement for particular medications. Increasingly, third-party 

16 

 
 
 
 
 
 
payors are requiring that drug companies provide them with predetermined discounts from list prices and 
are  challenging  the  prices  charged  for  medical  products.  We  cannot  be  sure  that  coverage  and 
reimbursement  will  be  available  promptly  or  at  all  for  any  product  that  we  commercialize  and,  if 
reimbursement is available, what the level of reimbursement will be. Moreover, eligibility for coverage and 
reimbursement does not imply that any drug will be paid for in all cases. Limited coverage may impact the 
demand for, or the price of, any product candidate for which we obtain marketing approval. If coverage and 
reimbursement  are  not  available  or  reimbursement  is  available  only  to  limited  levels,  we  may  not 
successfully commercialize any product candidate for which we obtain marketing approval.   

Payors also are increasingly considering new metrics as the basis for reimbursement rates, such as 
average sales price (“ASP”), average manufacturer price (“AMP”) and actual acquisition cost. The existing 
data for reimbursement based on these metrics is relatively limited, although certain states have begun to 
survey acquisition cost data for the purpose of setting Medicaid reimbursement rates.    CMS surveys and 
publishes retail community pharmacy acquisition cost information in the form of National Average Drug 
Acquisition Cost (“NADAC”) files to provide state Medicaid agencies with a basis of comparison for their 
own reimbursement and pricing methodologies and rates.    It may be difficult to project the impact of these 
evolving reimbursement mechanics on the willingness of payors to cover our products for which we receive 
regulatory approval. 

If we successfully commercialize any of our products, we may participate in the Medicaid Drug 
Rebate  Program.    Participation  is  required  for  federal  funds  to  be  available  for  our  products  under 
Medicaid and Medicare Part B.    Under the Medicaid Drug Rebate Program, we would be required to pay a 
rebate to  each  state Medicaid  program  for  our covered  outpatient  drugs  that  are  dispensed  to  Medicaid 
beneficiaries and paid for by a state Medicaid program as a condition of having federal funds being made 
available to the states for our drugs under Medicaid and Part B of the Medicare program.     

Federal law requires that any company that participates in the Medicaid Drug Rebate Program also 
participate  in  the  Public  Health  Service’s  340B  drug  pricing  program  in  order  for  federal  funds  to  be 
available  for  the  manufacturer’s  drugs  under  Medicaid  and  Medicare  Part  B.    The  340B  drug  pricing 
program  requires  participating  manufacturers  to  agree  to  charge  statutorily-defined  covered  entities  no 
more than the 340B “ceiling price” for the manufacturer’s covered outpatient drugs.    These 340B covered 
entities include a variety of community health clinics and other entities that receive health services grants 
from  the  Public  Health  Service,  as  well  as  hospitals  that  serve  a  disproportionate  share  of  low-income 
patients.     

In  addition,  in  order  to  be  eligible  to  have  its  products  paid  for  with  federal  funds  under  the 
Medicaid  and  Medicare  Part  B  programs  and  purchased  by  certain  federal  agencies  and  grantees,  a 
manufacturer  also  must  participate  in  the  Department  of  Veterans  Affairs  Federal  Supply  Schedule 
(“FSS”),  pricing  program,  established  by  Section  603  of  the  Veterans  Health  Care  Act  of  1992  (the 
“VHCA”).    Under  this  program,  the  manufacturer  is  obligated  to  make  its  innovator  and  single  source 
products  available  for  procurement  on  an  FSS  contract  and  charge  a  price  to  four  federal  agencies, 
Department of Veterans Affairs, Department of Defense (“DoD”), Public Health Service, and Coast Guard, 
that is no higher than the statutory Federal Ceiling Price.    Moreover, pursuant to regulations issued by the 
DoD TRICARE Management Activity (“TMA”), now the Defense Health Agency (“DHA”), to implement 
Section 703 of the National Defense Authorization Act for Fiscal Year 2008, manufacturers are required to 
provide rebates on utilization of their innovator and single source products that are dispensed to TRICARE 
beneficiaries  by  TRICARE  network  retail  pharmacies.    The  formula  for  determining  the  rebate  is 
established  in  the  regulations  and  is  based  on  the  difference  between  the  annual  non-federal  average 
manufacturer price and the Federal Ceiling Price (these price points are required to be calculated by us 
under  the  VHCA).  The  requirements  under  the  340B,  FSS,  and  TRICARE  programs  could  reduce  the 

17 

 
 
 
 
 
revenue we may  generate from any products that are commercialized in the future and could adversely 
affect our business and operating results. 

There  may  be  significant  delays  in  obtaining  coverage  and  reimbursement  for  newly  approved 
drugs, and coverage may be more limited than the purposes for which the drug is approved by the FDA or 
comparable foreign regulatory authorities. Moreover, eligibility for coverage and reimbursement does not 
imply  that  a  drug  will  be  paid  for  in  all  cases  or  at  a  rate  that  covers  our  costs,  including  research, 
development, manufacture, sale and distribution. Interim reimbursement levels for new drugs, if applicable, 
may also not be sufficient to cover our costs and may only be temporary. Reimbursement rates may vary 
according to the use of the drug and the clinical setting in which it is used, may be based on reimbursement 
levels already set for lower cost drugs and may be incorporated into existing payments for other services.   
Net prices for drugs may be reduced by mandatory discounts or rebates required by government healthcare 
programs or private payors and by any future relaxation of laws that presently restrict imports of drugs from 
countries where they may be sold at lower prices than in the United States. Limited  coverage  may  impact 
the  demand  for,  or  the  price  of,  any  product  candidate  for  which  we  obtain  marketing  approval.   
Third-party  payors  also  may  seek  additional  clinical  evidence,  including  expensive  pharmacoeconomic 
studies, beyond the data required to obtain marketing approval, demonstrating clinical benefits and value 
in  specific  patient  populations,  before  covering  our  products  for  those  patients.    If  reimbursement  is 
available  only  for  limited  indications,  we  may  not  be  able  to  successfully  commercialize  any  product 
candidate  for  which  we  obtain  marketing  approval.    Our  inability  to  promptly  obtain  coverage  and 
profitable reimbursement rates from both government-funded and private payors for any approved products 
that we develop could have a material adverse effect on our operating results, our ability to raise capital 
needed to commercialize products and our overall financial condition. 

United States Healthcare Reform 

The  United  States  and  many  foreign  jurisdictions  have  enacted  or  proposed  legislative  and 
regulatory changes affecting the healthcare system that could prevent or delay marketing approval of our 
product candidates, restrict or regulate post-approval activities and affect our ability to profitably sell any 
product  candidate  for  which  we  obtain  marketing  approval.  The  United  States  government,  state 
legislatures  and  foreign  governments  also  have  shown  significant 
implementing 
cost-containment  programs  to  limit  the  growth  of  government-paid  healthcare  costs,  including  price 
controls, restrictions on reimbursement and requirements for substitution of generic products for branded 
prescription drugs. 

interest 

in 

In recent years, Congress has considered reductions in Medicare reimbursement levels for drugs 
administered by physicians. CMS, the agency that administers the Medicare and Medicaid programs, also 
has authority to revise reimbursement rates and to implement coverage restrictions for some drugs. Cost 
reduction initiatives and changes in coverage implemented through legislation or regulation could decrease 
utilization of and reimbursement for any approved products, which in turn would affect the price we can 
receive  for  those  products.  While  Medicare  regulations  apply  only  to  drug  benefits  for  Medicare 
beneficiaries, private payors often follow Medicare coverage policy and payment limitations in setting their 
own reimbursement rates. Therefore, any reduction in reimbursement that results from federal legislation or 
regulation may result in a similar reduction in payments from private payors. 

In March 2010, President Obama signed into law the Affordable Care Act.    This law substantially 
changes  the  way  healthcare  is  financed  by  both  governmental  and  private  insurers,  and  significantly 
impacts the  pharmaceutical  industry.    The  Affordable  Care  Act  is intended  to  broaden  access to health 
insurance,  reduce  or  constrain  the  growth  of  healthcare  spending,  enhance  remedies  against  healthcare 
fraud and abuse, add new transparency requirements for healthcare and health insurance industries, impose 
new  taxes  and fees  on  pharmaceutical and  medical  device  manufacturers,  and  impose  additional  health 

18 

 
 
 
 
 
 
policy  reforms.  Among  other  things,  the  Affordable  Care  Act  expanded  manufacturers’  rebate  liability 
under the Medicaid Drug Rebate Program by increasing the minimum Medicaid rebate for both branded 
and generic drugs, expanded the 340B program, and revised the definition of AMP, which could increase 
the  amount  of  Medicaid  drug  rebates  manufacturers  are  required  to  pay  to  states.  The  legislation  also 
extended Medicaid drug rebates, previously due only on fee-for-service Medicaid utilization, to include the 
utilization of Medicaid managed care organizations as well and created an alternative rebate formula for 
certain new formulations of certain existing products that is intended to increase the amount of rebates due 
on  those  drugs.    On  February  1,  2016,  CMS  issued  final  regulations  to  implement  the  changes  to  the 
Medicaid Drug Rebate program under the Affordable Care Act.    These regulations became effective on 
April 1, 2016.    Moreover, legislative changes to the Affordable Care Act remain possible and appear likely 
in the 115th United States Congress and under the Trump Administration, which could include changes 
that,  among  other  things,  decrease  the  number  of  individuals  with  health  coverage.  We  expect  that  the 
Affordable Care Act, as currently enacted or as it may be amended in the future, and other healthcare reform 
measures that may be adopted in the future could have a material adverse effect on our industry generally 
and on our ability to successfully commercialize our product candidates, if approved. 

The Affordable Care Act requires pharmaceutical manufacturers of branded prescription drugs to 
pay  a  branded  prescription  drug  fee  to  the  federal  government.    Each  individual  pharmaceutical 
manufacturer pays a prorated share of the branded prescription drug fee of $3.0 billion in 2016, based on the 
dollar  value  of  its  branded  prescription  drug  sales  to  certain  federal  programs  identified  in  the  law.   
Furthermore, the new law requires manufacturers to provide a 50% discount off the negotiated price of 
prescriptions filled by beneficiaries in the Medicare Part D coverage gap, referred to as the “donut hole.”   

The Affordable Care Act also expanded the Public Health Service’s 340B drug pricing discount 
program.    As noted above, the 340B drug pricing program requires participating manufacturers to agree to 
charge statutorily-defined covered entities no more than the 340B “ceiling price” for the manufacturer’s 
covered  outpatient  drugs.    The  Affordable  Care  Act  expanded  the  340B  program  to  include  additional 
types  of  covered  entities:  certain  free-standing  cancer  hospitals,  critical  access  hospitals,  rural  referral 
centers and sole community hospitals, each as defined by the Affordable Care Act. The Affordable Care 
Act  exempts  “orphan  drugs”—those  designated  under  section  526  of  the  Food,  Drug,  and  Cosmetic 
Act—from the ceiling price requirements for these newly-eligible entities.    Because the 340B ceiling price 
is determined based on AMP and Medicaid drug rebate data, the revisions to the Medicaid rebate formula 
and AMP definition could cause the required 340B discounts to increase. 

In addition, other legislative changes have been proposed and adopted since the Affordable Care 
Act was enacted.    For example, recent legislative enactments have resulted in Medicare payments being 
subject to a two percent reduction, referred to as sequestration, until 2025.    Continuation of sequestration 
or enactment of other reductions in Medicare reimbursement for drugs could affect our ability to achieve 
a profit on any candidate products that are approved for marketing.   

We expect that the Affordable Care Act, as well as other healthcare reform measures that have been 
adopted and may be adopted in the future, may result in more rigorous coverage criteria and in additional 
downward pressure on the price that we receive for any approved product and could seriously harm our 
future revenues. Any reduction in reimbursement from Medicare, Medicaid, or 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. 

19 

 
 
 
 
 
Foreign Regulation 

In  addition  to  regulations  in  the  United  States,  we  will  be  subject  to  a  number  of  significant 
regulations  in  other  jurisdictions  regarding  clinical  trials,  approval,  manufacturing,  marketing  and 
promotion and safety reporting.    These requirements and restrictions vary from country to country, but 
in many instances are similar to the United States requirements, and failure to comply with them could 
have the same negative effects as noncompliance in the United States. 

Sales and Marketing 

We do not currently have the sales and marketing infrastructure in place that would be necessary 
to  sell  and  market  products.  As  our  drug  candidates  progress  in  clinical  trials,  we  may  build  the 
commercial  infrastructure  that  would  be  needed  to  successfully  market  and  sell  any  successful  drug 
candidate. For drug candidates that may require larger clinical trials or sales efforts, we intend to establish 
strategic alliances and partnerships with large pharmaceutical companies during the development process. 

Research Technologies 

Our research technologies are focused on our proprietary multi-target aimed ligands platform and 
nano-based  drug  delivery,  which  are  described  further  below.  For  a  discussion  of  collaboration 
arrangements pursuant to which we obtain research and development services from universities, research 
institutions and other organizations, see “Collaboration and License Agreements” in this Item 1. 

The Inhibitors of Multi-Expression Signals (TIMES) 

TIMES  is  our  platform  for  discovering  ligands,  which  are  molecules  coordinated  to  a  central 
atom or molecule in a larger chemical complex, that target multi-expression signals. Because cancer is a 
complex disease caused by multiple factors as well as genetic modifications, cancer treatment involves a 
combination of drugs with different mechanisms of action, which may result in compounding the degree 
and  extent  of  toxicities  to  which  a  patient  is  exposed.    TIMES  permits  us  to  control  multiple  targets 
important  for  cancer  proliferation  with  a  single  agent.    In  doing  so,  we  utilize  a  proprietary, 
genomics-based integrated, gene expression system to identify potentially important targets that control 
multiple genes or signaling events in cancer cells. 

3-D Gateway of Ligand Discovery (3-D GOLD) 

3-D  GOLD  is  a  drug  discovery  platform  that  integrates  three-dimensional  (“3D”)  molecular 
modeling, databases of chemicals and proteins and ligand filtering and generation. The chemical database 
contains  3D  structures  of  approximately  seven  million  compounds.  Our  proprietary  docking  tools 
quantitative structure-activity relationship tool for innovative discovery are parts of the platform. Ligand 
filtering  highlights  similarities  in  pharmacophore  and  3D  fingerprinting,  while  ligand  generation  helps 
optimize the identification of such similarities.   

Nano-medicine Drug Delivery   

We have developed unique proprietary drug delivery nano-systems that we believe may increase 
the availability of a drug at the disease site, minimize adverse reactions, and provide longer duration of 
action.  We  are  currently  testing  multiple  nanoliposomal-  and  nanopolymer-based  anti-cancer  drugs.   
RX-21101 is an investigational nanoliposomal-based drug. 

20 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
Manufacturing and Distribution 

We  have  no  experience  in  drug  formulation  or  manufacturing,  and  we  lack  the  resources  and 
expertise  to  formulate  or  manufacture  our  own  drug  candidates  internally.  Therefore,  we  rely  on 
third-party  expertise  to  support  us  in  this  area.  We  have  entered  into  contracts  with  third-party 
manufacturers to manufacture, supply, store and distribute supplies of our drug candidates for our clinical 
trials. If any of our drug candidates receive FDA approval, we expect to rely on third-party contractors to 
manufacture  our  drugs.  We  have  no  current  plans  to  build  internal  manufacturing  capacity  for  any 
product, and we have no long-term supply arrangements. 

Intellectual Property   

We  generally  seek  proprietary  patent  and  intellectual  property  (“IP”)  protection  for  our  drug 
candidates, processes, and other know-how. In addition to patent protection, we rely upon trade secrets, 
know-how, continuing technological innovation and licensing opportunities to develop and safeguard and 
maintain our IP. 

We hold U.S. and foreign patents for our drug candidates that expire from 2023 to 2036. We hold 
U.S.,  European  and  Japanese  patents  for  RX-3117,  Supinoxin  and  Archexin.    In  addition  to  these 
patents, we have issued or pending patents in other jurisdictions.   

The patent portfolios for our most advanced programs are summarized below: 

RX-3117: 

The RX-3117 patent portfolio consists of three patent families.    The first family consists of 
patents  that  have  been  issued  in  the  United  States,  Europe,  Japan  and  other  jurisdictions.  The 
patents in this  family  include  composition  of  matter, use,  and  process  claims  of  varying  scope, 
including picture claims to RX-3117 or a pharmaceutically acceptable salt thereof. The patents in 
this  first  family  expire  in 2025,  but  may  be  extended  by  patent  term  extension  and  orphan  and 
market  exclusivity.  The  second  family  consists  of  patents  that  have  been  issued  in  the  United 
States, and are pending in Europe, Japan and other jurisdictions. The patents in the second family 
include process claims that cover RX-3117.    The patents in this second family expire in 2034.   
The  third  family  consists  of  a  patent  that  is  pending  in  the  United  States.  This  patent  would 
include  use  and  process  claims  that  generically  cover  RX-3117.    This  patent  would  expire  in 
2036. 

Supinoxin: 

The Supinoxin patent portfolio consists of three patent families. The first family consists of 
patents that have been issued in the United States and Europe, and are pending in Japan and other 
jurisdictions.  The  patents  in  the  first  family  include  composition  of  matter,  use,  and  process 
claims of varying scope, including picture claims to Supinoxin or a pharmaceutically acceptable 
salt thereof. The patents in this first family expire in 2025 and may be extended up to five years in 
the  United  States.    We  also  expect  Supinoxin  will  be  protected  with  market  exclusivity  in 
Europe for  a  minimum  of  ten  years  post-approval.    The second  family  consists  of  patents  that 
are pending in the United States, Europe, Japan and other jurisdictions. The patents in the second 
family include composition of matter, process and use claims that cover Supinoxin.    The patents 
in this second family would expire in 2034. The third family consists of a patent that is pending in 
the United States. The patent in the third family would include use and process claims that cover 
Supinoxin.    This patent would expire in 2036.     

21 

 
 
 
 
 
 
 
 
Archexin: 

The Archexin patent portfolio consists of a patent family that includes patents that have been 
issued  in  the  United  States,  Europe,  Japan  and  other  jurisdictions.    The  patents  in  this  family 
include  composition  of  matter  and  use  claims  of  varying  scope,  including  picture  claims  to 
Archexin  or  a  pharmaceutically  acceptable  salt  thereof.  The  expiration  date  of  these  patents 
ranges from 2023 to 2025, and may be extended by up to five years in certain countries including 
the  United  States.    In  addition,  it  is  expected  that  Archexin  will  be  protected  from  generic 
launches by market and orphan designations for up to seven years in the United States, and ten 
years in Europe and Japan. 

Collaboration and License Arrangements 

We  have  numerous  collaborative  research  and  development  relationships  with  universities, 

research institutions pharmaceutical companies and other organizations. 

Rexgene Biotech Co., Ltd. (“Rexgene”) 

In  February  2003,  we  entered  into  a  research  collaboration  agreement  with  Rexgene,  which  is 
engaged in the development of pharmaceutical products in Asia. Rexgene has agreed to assist us with the 
research,  development  and  clinical  trials  necessary  for  registration  of  Archexin  in  Asia.    Under  the 
agreement, we have granted Rexgene an exclusive license, with right to sublicense, to make, have made, 
use, sell and import Archexin in Asia. In accordance with the agreement, Rexgene paid us a one-time fee 
of $1,500,000 in 2003. Rexgene also agreed to pay us a royalty fee of 3% of net sales of licensed products 
related to Archexin on a country-by-country basis in all countries in Asia by Rexgene or any sublicensee 
of Rexgene. 

The agreement expires upon the last to expire of all U.S. and foreign patents presently or in the 
future  issued  that  cover  Archexin,  which  we  currently  expect  to  occur  in  2025.  The  agreement  is 
terminable by either party for the other party’s material breach, subject to a 90 day cure period. To date, 
the only amounts we have received under the agreement are from the initial one-time fee of $1,500,000 
paid in 2003. 

Korea Research Institute of Chemical Technology (“KRICT”) 

In  June  2009,  we  entered  into  a  license  agreement  with  KRICT  to  acquire  rights  to  all  of 
KRICT’s  intellectual  property  related  to  quinoxaline-piperazine  derivatives,  which  includes  Supinoxin.   
We paid an initial license fee of $100,000 in July 2009, and will pay a one-time milestone payment of 
$1,000,000  to  KRICT  upon  marketing  approval  from  FDA  for  the  first  commercial  product  stemming 
from intellectual property (the “Milestone Payment”).    Upon payment of the Milestone Payment all of 
the  rights  previously  licensed  to  us  will  be  transferred  to  us  and  the  agreement  will  terminate.    The 
agreement  is  terminable  by  either  party  for  the  other  party’s  material  breach,  subject  to  a  60  day  cure 
period. To date, we have paid only the $100,000 initial license fee pursuant to this agreement. 

The University of Maryland Baltimore (“UMB”)  

In July 2013, we entered into an exclusive license agreement with UMB for a novel drug delivery 
platform,  Nano-Polymer-Drug  Conjugate  Systems.    This  platform  combines  existing  chemotherapeutic 
agents  with  a  proprietary  polymer  carrier  that  contains  a  signaling  moiety  to  direct  the  agents  into  a 
tumor.    RX-21101  is  our  first  drug  candidate  utilizing  this  platform  and  is  a  conjugated  form  of 
docetaxel,  a  common  chemotherapy  agent.    This  agreement  requires  us  to  make  payments  to  UMB  if 

22 

 
 
 
 
 
 
 
 
RX-21101  or  any  other  products  developed  from  the  licensed  delivery  platform  achieve  development 
milestones.     

The Ohio State University 

In October 2013, we entered into an exclusive license agreement with the Ohio State Innovation 
Foundation, an affiliate of The Ohio State University, for a novel oligonucleotide drug delivery platform, 
Lipid-Coated  Albumin  Nanoparticle  (“LCAN”).    The  LCAN  platform  incorporates  both  cationic  lipid 
and  cationized  albumin  that  can  form  an  electrostatic  complex  with  oligonucleotides  and  be 
co-encapsulated  by  lipids.    The  agreement  requires  us  to  make  payments  to  the  Ohio  State  Innovation 
Foundation if any products from the licensed delivery platform achieve development milestones.     

Total Research and Development Costs 

We have incurred research and development costs of $10,089,149, $12,148,226 and $7,015,901 
for the years ended December 31, 2016, 2015 and 2014 respectively.    Research and development costs 
primarily consist of clinical trials and pre-clinical development costs, as well as payroll costs for research 
and development personnel.   

Employees 

We  currently  have  20  full-time  employees,  all  of  whom  are  based  either  at  our  Rockville, 
Maryland  office  or  our  Gaithersburg,  Maryland  lab  facility.    Our  employees  are  not  covered  by  any 
collective  bargaining  agreement  and  we  have  never  experienced  a  work  stoppage.    We  believe  our 
relationships with our employees are satisfactory. 

Available Information   

Under the Securities Exchange Act of 1934, as amended (the “Exchange Act”), we are required to 
file  annual,  quarterly  and  current  reports,  proxy  statements  and  other  information  with  the  SEC.    Any 
document we file with the SEC may be read and copied at the SEC’s Public Reference Room at 100 F 
Street, N.E., Washington, D.C. 20549. Please call the SEC at (800) SEC-0330 for further information about 
the public reference room. The SEC maintains a website at www.sec.gov that contains reports, proxy and 
information statements and other information regarding issuers that file electronically with the SEC.   

We make available, free of charge, on our website at www.rexahn.com our Annual Report on Form 
10-K, Quarterly Reports on Form 10-Q and Current Reports on Form 8-K and all amendments thereto, as 
soon as reasonably practicable after they are filed with or furnished to the SEC. Investors are encouraged to 
access these reports and the other information about our business on our website. Information found on our 
website is not part of this Annual Report on Form 10-K (this “Annual Report”). We will also provide copies 
of this Annual Report, free of charge, upon written request to the Investor Relations Department at our main 
address, 15245 Shady Grove Road, Suite 455, Rockville MD, 20850. 

Also posted on our website, and available in print upon written request of any shareholder to our 

Investor Relations Department, are the charters of the standing committees of our Board

23 

 
 
 
 
  
 
 
 
 
Item 1A.    Risk Factors. 

You should carefully consider the risks described below together with the other information included in 
this Form 10-K. Our business, financial condition or results of operations could be adversely affected by 
any of these risks. If any of these risks occur, the value of our common stock could decline. 

Risks Related to Our Financial Position and Capital Needs 

We  currently  have  no  product  revenues,  have  incurred  negative  cash  flows  from  operations  since 
inception and will need to raise additional capital to operate our business. 

To  date,  we  have  generated  no  product  revenues  and  have  incurred  negative  cash  flow  from 
operations.  Until  we  receive  approval  from  the  FDA  or  other  regulatory  authorities  for  our  drug 
candidates, we cannot sell our drugs and will not have product revenues. We expect to continue to incur 
significant  development  and  other  expenses  related  to  our  ongoing  operations.    Therefore,  for  the 
foreseeable  future,  we  will  have  to  fund  all  of  our  operations  and  capital  expenditures  from  the  net 
proceeds of equity or debt offerings, cash on hand, licensing fees and grants, if any.    If we are not able to 
raise sufficient funds, we will have to reduce our research and development activities. We will first reduce 
research and development activities associated with our pre-clinical compounds. To the extent necessary, 
we will then reduce our research and development activities related to some or all of our clinical stage 
product candidates.   

Unforeseen events, difficulties, complications and delays may occur that could cause us to utilize 
our existing capital at a faster rate than projected, including the progress of our research and development 
efforts, the cost and timing of regulatory approvals and the costs of protecting our intellectual property 
rights.  We  may  seek  additional  financing  to  implement  and  fund  other  drug  candidate  development, 
clinical trial and research and development efforts, including clinical trials for other new drug candidates, 
as well as other research and development projects. 

We will need additional financing to continue to develop our drug candidates, which may not be 
available  on  favorable  terms,  if  at  all.  If  we  are  unable  to  secure  additional  financing  in  the  future  on 
acceptable terms, or at all, we may be unable to complete our planned pre-clinical and clinical trials or 
obtain  approval  of  our  drug  candidates  from  the  FDA  and  other  regulatory  authorities.  In  addition,  we 
may be forced to reduce or discontinue product development or product licensing, reduce or forego sales 
and  marketing  efforts  and  forego  attractive  business  opportunities  in  order  to  improve  our  liquidity  to 
enable us to continue operations. Any additional sources of financing will likely involve the sale of our 
equity securities or securities convertible into our equity securities, which may have a dilutive effect on 
our stockholders. 

We are not currently profitable and may never become profitable. 

To  date,  we  have  generated  no  product  revenues  and  have  incurred  negative  cash  flow  from 
operations.  Our  accumulated  deficit  as  of  December  31,  2016  and  2015  was  $115,024,209  and 
$105,716,864, respectively. For the years ended December 31, 2016, 2015 and 2014, we had net losses of 
$9,307,345,  $14,384,556,  and  $18,521,601,  respectively.  Even  if  we  succeed  in  developing  and 
commercializing  one  or  more  of  our  drug  candidates,  we  expect  to  incur  substantial  losses  for  the 
foreseeable  future  and  may  never  become  profitable.  We  also  expect  to  continue  to  incur  significant 
operating  and  capital  expenditures  and  anticipate  that  our  expenses  will  increase  substantially  in  the 
foreseeable future, based on the following considerations: 

24 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
• 

• 

• 

• 

• 

continued pre-clinical development and clinical trials for our current and new drug candidates; 

finding suitable partners to help us research, develop and commercialize new drug candidates; 

efforts to seek regulatory approvals for our drug candidates; 

implementing additional internal systems and infrastructure; 

in-licensing additional technologies to develop; and 

•  hiring additional personnel or entering into relationships with third parties to perform functions 

that we are unable to perform on our own. 

We also expect to continue to experience negative cash flow for the foreseeable future as we fund 
our operations and capital expenditures. Until we have the capacity to generate revenues, we are relying 
upon  outside  funding  resources  to  fund  our  cash  flow  requirements.  If  these  resources  are  depleted  or 
unavailable,  we  may  be  unable  to  continue  to  expand  our  operations  or  otherwise  capitalize  on  our 
business opportunities, and our business, financial condition and results of operations would be materially 
adversely affected. 

We have a limited operating history, and we have not demonstrated an ability to commercialize drug 
candidates. 

We are a clinical-stage company with a limited number of drug candidates. We currently do not 
have  any  products  that  have  gained  regulatory  approval,  and  we  have  not  demonstrated  an  ability  to 
perform the functions necessary for the successful commercialization of any of our drug candidates. The 
successful commercialization of our drug candidates will require us to first perform a variety of functions, 
including: 

• 

conducting pre-clinical and clinical trials; 

•  participating in regulatory approval processes; 

• 

• 

formulating and manufacturing products; and 

conducting sales and marketing activities. 

To  date,  our  operations  have  been  limited  to  organizing  and  staffing  the  Company,  acquiring, 
developing  and  securing  our  proprietary  technology,  and  undertaking  drug  candidate  research  and 
development,  including  pre-clinical  trials  and  clinical  trials  of  our  principal  drug  candidates.  These 
operations provide a limited basis for assessing our ability to commercialize drug candidates. 

Our common stock could be at risk for delisting from the NYSE MKT if the NYSE MKT notifies us 
that the stock has sold for a substantial period of time at a low price per share and thereafter, our stock 
price does not increase. If it is delisted, our common stock and the liquidity of our common stock would 
be impacted. 

Our  common  stock  is  listed  on  the  NYSE  MKT.    Section  1003(f)(v)  of  the  NYSE  Company 
Guide provides that a  company’s  common  stock  may  be delisted  from  the  NYSE  MKT if  it sells  for a 
substantial period of time at a low price per share and the Company fails to effect a reverse stock split or 

25 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
otherwise demonstrate sustained price improvement within a reasonable time after being notified that the 
NYSE MKT deems such action to be appropriate under all the circumstances.    While the NYSE MKT 
has not provided notice that the NYSE MKT deems it appropriate for us to effect a reverse stock split, 
given the Company’s recent trading prices, the NYSE MKT may deliver such a letter if the price of our 
common stock does not increase. 

Delisting  from  the  NYSE  MKT  may  adversely  affect  our  ability  to  raise  additional  financing 
through the public or private sale of equity securities, may significantly affect the ability of investors to 
trade our securities and may negatively affect the value and liquidity of our common stock.    Delisting also 
could  have  other  negative  results,  including  the  potential  loss  of  employee  confidence,  the  loss  of 
institutional  investors  or  interest  in  business  development  opportunities.    Moreover,  we  committed  in 
connection with the sale of securities to use commercially reasonably efforts to maintain the listing of our 
common stock during such time that certain warrants are outstanding. 

If our common stock was to be delisted from the NYSE MKT and we were not able to list our 
common stock on another exchange, our common stock could be quoted on the OTC Bulletin Board or in 
the “pink sheets.” As a result, we could face significant adverse consequences including, among others: 

• 

• 

• 

• 

• 

a limited availability of market quotations for our securities; 

a determination that the Common Stock is a “penny stock,” which will require brokers trading in 
the  Common  Stock  to  adhere  to  more  stringent  rules  and  possibly  result  in  a  reduced  level  of 
trading activity in the secondary trading market for our securities; 

a limited amount of news and little or no analyst coverage for the Company; 

the  Company  would  no  longer  qualify  for  exemptions  from  state  securities  registration 
requirements, which may require us to comply with applicable state securities laws; and 

a  decreased  ability  to  issue  additional  securities  (including  pursuant  to  short-form  registration 
statements on Form S-3) or obtain additional financing in the future. 

Risks Related to Our Business 

Several  of  our  drug  candidates  are  in  clinical  trials,  which  are  very  expensive,  time-consuming  and 
difficult to design and implement. 

Our drug candidates are in various stages of development and require extensive clinical testing. 
Such  testing  is  expensive  and  time-consuming  and  requires  specialized  knowledge  and  expertise.   
Archexin entered a Phase IIa clinical trial in January 2014, RX-3117 entered a Phase IIa clinical trial in 
March  2016  and another  Phase  IIa  trial  in  September  2016,  and  Supinoxin  entered  a  Phase  IIa  clinical 
trial in February 2017. 

Human clinical trials are very expensive and difficult to design and implement, in part because 
they are subject to rigorous regulatory requirements. The clinical trial process is also time-consuming, and 
the outcome is not certain; the results of pre-clinical studies and early clinical trials may not be predictive 
of the results of later-stage clinical trials. We estimate that clinical trials of our current drug candidates 
will take multiple years to complete. Furthermore, failure can occur at any stage of a clinical trial, and we 
could  encounter  problems  that  cause  us  to  abandon  or  repeat  clinical  trials.  The  commencement  and 
completion of clinical trials may be delayed or precluded by a number of factors, including: 

26 

 
 
 
 
 
 
•  delay  or  failure  in  reaching  agreement  with  the  FDA  or  a  foreign  regulatory  authority  on  the 

design of a given trial, or in obtaining authorization to commence a trial; 

•  delay  or  failure  in  reaching  agreement  on  acceptable  terms  with  prospective  contract  research 

organizations and clinical trial sites; 

•  delay or failure in obtaining approval of an IRB to conduct a clinical trial at a given site; 

•  withdrawal of clinical trial sites from our clinical trials as a result of changing standards of care of 

the ineligibility of a site to participate; 

•  delay or failure in recruiting and enrolling study subjects; 

•  delay or failure in having subjects complete a clinical trial or return for post-treatment follow up; 

• 

• 

• 

• 

clinical  sites  or  investigators  deviating  from  trial  protocol,  failing  to  conduct  the  trial  in 
accordance with applicable regulatory requirements, or dropping out of a trial; 

inability to identify and maintain a sufficient number of trial sites; 

failure of third-party clinical trial managers to meet their contractual obligations or deadlines; 

the need to modify a study protocol; 

•  unforeseen safety issues; 

• 

• 

• 

• 

• 

• 

• 

emergence of dosing issues; 

lack of effectiveness during clinical trials; 

change in the standard of care of the indication being studied; 

reliance on third-party suppliers for the clinical trial supply of drug candidates; 

inability to monitor patients adequately during or after treatment; 

lack of sufficient funding to finance the clinical trials; and 

changes in governmental regulations or administrative action. 

We, the FDA or an IRB may suspend a clinical trial at any time if it appears that we are exposing 
participants to unacceptable health risks or if the FDA finds deficiencies in our IND applications or the 
conduct of these trials. Additionally, we may have difficulty enrolling patients in our clinical trials.    If 
we  experience  such  difficulties,  we  may  not  be  able  to  complete  a  clinical  trial  or  we  may  experience 
significant delays in completing a clinical trial.  

27 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
If  the  results  of  our  clinical  trials  fail  to  support  the  approval  of  any  of  our  drug  candidates,  the 
completion  of  development  of  that  candidate  may  be  significantly  delayed,  or  we  may  be  forced  to 
abandon  development  altogether,  which  will  significantly  impair  our  ability  to  generate  product 
revenues. 

Even if our clinical trials are completed as planned, we cannot be certain that clinical results will 
support approval of our drug candidates. Success in pre-clinical testing and early clinical trials does not 
ensure that later clinical trials will be successful, and we cannot be sure that the results of later clinical 
trials will replicate the results of prior clinical trials and pre-clinical testing. The clinical trial process may 
fail to demonstrate that one or more of our drug candidates is safe and effective for indicated uses. As a 
result, we may have to conduct additional clinical trials or may decide to abandon a drug candidate, in 
which case we may never recognize any revenue related to such candidate. Standard of care treatments 
may change, which may require additional clinical trials. Repeating clinical trials or conducting additional 
clinical trials will increase our development costs and delay the filing of an NDA and, ultimately, delay 
our ability to commercialize our drug candidates and generate product revenues.   

We may  not  obtain  the  necessary  U.S.  or  worldwide  regulatory approvals to  commercialize  our  drug 
candidates,  and  we cannot  guarantee  how  long it  will  take  the  FDA  or  other comparable  regulatory 
agencies to review applications for our drug candidates. 

We will need the FDA approval to commercialize our drug candidates in the United States and 
approvals  from  the  comparable  regulatory  authorities  to  commercialize  our  drug  candidates  in  foreign 
jurisdictions. 

The  time  it  takes  to  obtain  approval,  either  in  the  United  States  or  foreign  jurisdictions,  is 
unpredictable,  but  typically  takes  many  years,  depending  upon  a  variety  of  factors,  including  the  type, 
complexity  and  novelty  of  the  drug  candidate.  Obtaining  approval  requires  substantial  resources  and  is 
subject to regulatory authorities’ substantial discretion.    In addition, approval policies, regulations or the 
type and amount of clinical data necessary to gain approval may change during the course of a product 
candidate’s  development  and  may  vary  among  jurisdictions.  We  cannot  guarantee  that  any  of  our  drug 
candidates will ultimately be approved by the FDA or any other regulatory authority, or the length of time 
obtaining approval will take.   One of our drug candidates, Archexin, is an ASO compound. To date, the 
FDA  has  approved  very  few  ASO  compounds.    In  addition,  Archexin  is  in  the  drug  class  known  as 
Akt-1 inhibitors that to date have not been approved by the FDA, nor have we submitted an NDA for an 
Akt-1 inhibitor. 

Our product candidates could fail to receive regulatory approval from the FDA or a comparable 

foreign authority for a variety of reasons, including: 

•  disagreement with the design or implementation of our clinical trials; 

• 

• 

• 

failure  to  demonstrate  to  the  authority’s  satisfaction  that  the  product  candidate  is  safe  and 
effective for the proposed indication; 

failure of clinical trials to meet the level of statistical significance required for approval; 

failure to demonstrate that the product’s benefits outweigh its risks; 

•  disagreement with our interpretation of pre-clinical or clinical data; and 

• 

inadequacies in the manufacturing facilities or processes of third-party manufacturers. 

28 

 
 
 
 
 
 
 
 
 
 
 
 
 
The FDA or a comparable foreign authority may require us to conduct additional pre-clinical and 
clinical  testing,  which  may  delay  or  prevent  approval  and  our  commercialization  plans  or  cause  us  to 
abandon the development program.    Further, any approval we receive may be for fewer or more limited 
indications than we request, may not include labeling claims necessary for successful commercialization 
of the product candidate, or may be contingent upon our conducting costly post-marketing clinical trials.   
Any of these scenarios could materially harm the commercial prospects of a product candidate. 

Even  if  our  product  candidates  obtain  approval,  they  may  face  future  development  and  regulatory 
difficulties that can negatively affect commercial prospects. 

Even  if  we  obtain  approval  for  a  product  candidate,  it  would  be  subject  to  ongoing  regulatory 
requirements and restrictions of the FDA and comparable regulatory authorities regarding manufacturing, 
quality  control,  further  development,  labeling,  packaging,  storage,  distribution,  safety  surveillance, 
import,  export, advertising,  promotion,  recordkeeping  and  reporting.    Failure  by  us  or  any  of  the  third 
parties  on  which  we  rely  to  meet  those  requirements  can  lead  to  enforcement  action,  among  other 
consequences, that could significantly impair our ability to successfully commercialize a given product.   
If the FDA or a comparable regulatory authority becomes aware of new safety information, it can impose 
additional  restrictions  on  how  the  product  is  marketed  or  may  seek  to  withdraw  marketing  approval 
altogether. 

There  is  no  assurance  that  any  of  our  products  that  has  received  or  will  receive  orphan  drug 
designation will subsequently obtain orphan drug exclusivity, or that any such exclusivity will provide 
the desired benefit.     

Although we have obtained orphan drug designation for several uses of Archexin and one use of 
RX-3117 and may obtain additional orphan drug designation for these or other product candidates, we are 
not assured of being awarded orphan drug exclusivity or realizing the benefits of such exclusivity, even if 
any of these products is approved for its orphan-designated use.    If another company also holding orphan 
drug designation for a product containing the same active moiety intended for the same rare disease or 
condition  receives  approval  before  our  orphan-designated  product,  approval  of  our  product  could  be 
precluded for seven years because of that product’s orphan drug exclusivity, unless we could demonstrate 
our  product  to  be  clinically  superior  to  the  earlier-approved  product.    Similarly,  even  if  our  orphan 
designated drug were approved first and awarded seven-year orphan drug exclusivity, it would not block 
approval of the other product if that product were shown to be clinically superior, or if we fail to assure a 
sufficient  quantity  of  our  orphan  drug.    Additionally,  because  orphan  drug  exclusivity  is  product-  and 
indication-specific,  it  does  not  prevent  approval  of  another  drug  for  the  same  orphan  indication  or  the 
same drug for a different use.     

If physicians and patients do not accept and use our drugs, our ability to generate revenue from sales 
of our products will be materially impaired. 

Even if the FDA approves our drug candidates, physicians and patients may not accept and use 
them. Future acceptance and use of our products will depend upon a number of factors including, but not 
limited to: 

• 

awareness of a drug’s availability and benefits; 

•  perceptions by members of the health care community, including physicians, about the safety and 

effectiveness of our drugs; 

29 

 
 
 
 
 
 
 
 
 
 
 
 
 
•  pharmacological benefit and cost-effectiveness of our products relative to competing products; 

• 

• 

• 

availability of reimbursement for our products from government or other third-party payors; 

effectiveness of marketing and distribution efforts by us and our licensees and distributors, if any; 
and 

the price at which we sell our products. 

Because we expect sales of our current drug candidates, if approved, to generate substantially all 
of  our  product  revenues  for  the  foreseeable  future,  the  failure  of  any  of  these  drugs  to  find  market 
acceptance would harm our business and could require us to seek additional financing. 

Even if we are able to commercialize any of our product candidates, these products may become subject 
to unfavorable pricing regulations, third-party reimbursement practices or healthcare reform initiatives, 
which could harm our business. 

The regulations that govern marketing approvals, pricing and reimbursement for new drug products 
vary widely from country to country. Current and future legislation may significantly change the approval 
requirements in ways that could involve additional costs and cause delays in obtaining approvals. Some 
countries require approval of the sale price of a drug before it can be marketed. In  many countries, the 
pricing  review  period  begins  after  marketing  or  product  licensing  approval  is  granted.  In  some  foreign 
markets, prescription pharmaceutical pricing remains subject to continuing governmental control even after 
initial approval is granted. As a result, we might obtain marketing approval for a product in a particular 
country, but then be subject to price regulations that delay our commercial launch of the product, possibly 
for lengthy time periods, which could negatively impact the revenues we are able to generate from the sale 
of the product in that particular country. Adverse pricing limitations may hinder our ability to recoup our 
investment in one or more product candidates even if our product candidates obtain marketing approval. 

Our ability to commercialize any products successfully also will depend in part on the extent to 
which coverage and adequate reimbursement for these products and related treatments will be available in a 
timely manner from government third-party payors, including governmental healthcare programs such as 
Medicare  and  Medicaid,  commercial  health  insurers  and  managed  care  organizations.  Government 
authorities  and  other  third-party  payors,  such  as  private  health  insurers  and  health  maintenance 
organizations,  determine  which  medications  they  will  cover  and  establish  reimbursement  levels. 
Third-party  payors  may  limit  coverage  to  specific  products  on  an  approved  list,  or  formulary,  which 
might  not  include  all  of  the  FDA  approved  products  for  a  particular  indication.    The  process  for 
determining whether a payor will provide coverage for a product may be separate from the process for 
setting the price or reimbursement rate that the payor will pay for the product once coverage is approved. 

A primary trend in the U.S. healthcare industry and elsewhere is cost containment.    Government 
healthcare  programs  and  other  third-party  payors  are  increasingly  challenging  the  prices  charged  for 
medical  products  and  services  and  examining  the  medical  necessity  and  cost-effectiveness  of  medical 
products  and  services,  in  addition  to  their  safety  and  efficacy,  and  have attempted to control costs by 
limiting coverage and the amount of reimbursement for particular medications. Increasingly, third-party 
payors are requiring that drug companies provide them with predetermined discounts from list prices and 
are  challenging  the  prices  charged  for  medical  products.  We  cannot  be  sure  that  coverage  and 
reimbursement  will  be  available  promptly  or  at  all  for  any  product  that  we  commercialize  and,  if 
reimbursement is available, what the level of reimbursement will be. Moreover, eligibility for coverage and 
reimbursement does not imply that any drug will be paid for in all cases. Limited coverage may impact the 
demand for, or the price of, any product candidate for which we obtain marketing approval. If coverage and 

30 

 
 
 
 
 
 
 
 
reimbursement  are  not  available  or  reimbursement  is  available  only  to  limited  levels,  we  may  not 
successfully commercialize any product candidate for which we obtain marketing approval.   

Payors also are increasingly considering new metrics as the basis for reimbursement rates, such as 
ASP, AMP and actual acquisition cost.    The existing data for reimbursement based on these metrics is 
relatively  limited,  although  certain  states  have  begun  to  survey  acquisition  cost data for the  purpose  of 
setting  Medicaid  reimbursement  rates.    CMS,  surveys  and  publishes  retail  community  pharmacy 
acquisition cost information in the form of NADAC files to provide state Medicaid agencies with a basis of 
comparison  for  their  own  reimbursement  and  pricing  methodologies  and  rates.    It  may  be  difficult  to 
project the impact of these evolving reimbursement mechanics on the willingness of payors to cover our 
products for which we receive regulatory approval. 

If we successfully commercialize any of our products, we may participate in the Medicaid Drug 
Rebate  program.    Participation  is  required  for  federal  funds  to  be  available  for  our  products  under 
Medicaid and Medicare Part B.    Under the Medicaid Drug Rebate Program, we would be required to pay a 
rebate to  each  state Medicaid  program  for  our covered  outpatient  drugs  that  are  dispensed  to  Medicaid 
beneficiaries and paid for by a state Medicaid program as a condition of having federal funds being made 
available to the states for our drugs under Medicaid and Part B of the Medicare program.     

Federal law requires that any company that participates in the Medicaid Drug Rebate Program also 
participate  in  the  Public  Health  Service’s  340B  drug  pricing  program  in  order  for  federal  funds  to  be 
available  for  the  manufacturer’s  drugs  under  Medicaid  and  Medicare  Part  B.    The  340B  drug  pricing 
program  requires  participating  manufacturers  to  agree  to  charge  statutorily-defined  covered  entities  no 
more than the 340B “ceiling price” for the manufacturer’s covered outpatient drugs.    These 340B covered 
entities include a variety of community health clinics and other entities that receive health services grants 
from  the  Public  Health  Service,  as  well  as  hospitals  that  serve  a  disproportionate  share  of  low-income 
patients.     

In  addition,  in  order  to  be  eligible  to  have  its  products  paid  for  with  federal  funds  under  the 
Medicaid  and  Medicare  Part  B  programs  and  purchased  by  certain  federal  agencies  and  grantees,  a 
manufacturer also must participate in the FSS, pricing program, established by Section 603 of the VHCA.   
Under  this  program,  the  manufacturer  is  obligated  to  make  its  innovator  and  single  source  products 
available for procurement on an FSS contract and charge a price to four federal agencies, Department of 
Veterans Affairs, DoD, Public Health Service, and Coast Guard, that is no higher than the statutory Federal 
Ceiling Price.    Moreover, pursuant to regulations issued by the DoD TMA, now the DHA, to implement 
Section 703 of the National Defense Authorization Act for Fiscal Year 2008, manufacturers are required to 
provide rebates on utilization of their innovator and single source products that are dispensed to TRICARE 
beneficiaries  by  TRICARE  network  retail  pharmacies.    The  formula  for  determining  the  rebate  is 
established  in  the  regulations  and  is  based  on  the  difference  between  the  annual  non-federal  average 
manufacturer price and the Federal Ceiling Price (these price points are required to be calculated by us 
under  the  VHCA).  The  requirements  under  the  340B,  FSS,  and  TRICARE  programs  could  reduce  the 
revenue we may  generate from any products that are commercialized in the future and could adversely 
affect our business and operating results. 

There  may  be  significant  delays  in  obtaining  coverage  and  reimbursement  for  newly  approved 
drugs, and coverage may be more limited than the purposes for which the drug is approved by the FDA or 
comparable foreign regulatory authorities. Moreover, eligibility for coverage and reimbursement does not 
imply  that  a  drug  will  be  paid  for  in  all  cases  or  at  a  rate  that  covers  our  costs,  including  research, 
development, manufacture, sale and distribution. Interim reimbursement levels for new drugs, if applicable, 
may also not be sufficient to cover our costs and may only be temporary. Reimbursement rates may vary 
according to the use of the drug and the clinical setting in which it is used, may be based on reimbursement 
levels already set for lower cost drugs and may be incorporated into existing payments for other services. 
Net prices for drugs may be reduced by mandatory discounts or rebates required by government healthcare 

31 

 
 
programs or private payors and by any future relaxation of laws that presently restrict imports of drugs from 
countries where they may be sold at lower prices than in the United States.    Limited coverage may impact 
the  demand  for,  or  the  price  of,  any  product  candidate  for  which  we  obtain  marketing  approval.   
Third-party  payors  also  may  seek  additional  clinical  evidence,  including  expensive  pharmacoeconomic 
studies beyond the data required to obtain marketing approval, demonstrating clinical benefits and value 
in  specific  patient  populations,  before  covering  our  products  for  those  patients.    If  reimbursement  is 
available  only  for  limited  indications,  we  may  not  be  able  to  successfully  commercialize  any  product 
candidate  for  which  we  obtain  marketing  approval.    Our  inability  to  promptly  obtain  coverage  and 
profitable reimbursement rates from both government-funded and private payors for any approved products 
that we develop could have a material adverse effect on our operating results, our ability to raise capital 
needed to commercialize products and our overall financial condition. 

Changes in healthcare law and implementing regulations, including those based on recently enacted 
and future legislation, as well as changes in healthcare policy, may increase the difficulty and cost for us 
to commercialize our product candidates and affect the prices we may obtain. 

The  United  States  and  many  foreign  jurisdictions  have  enacted  or  proposed  legislative  and 
regulatory changes affecting the healthcare system that could prevent or delay marketing approval of our 
product candidates, restrict or regulate post-approval activities and affect our ability to profitably sell any 
product  candidate  for  which  we  obtain  marketing  approval.  The  United  States  government,  state 
implementing 
legislatures  and  foreign  governments  also  have  shown  significant 
cost-containment  programs  to  limit  the  growth  of  government-paid  healthcare  costs,  including  price 
controls, restrictions on reimbursement and requirements for substitution of generic products for branded 
prescription drugs. 

interest 

in 

In recent years, Congress has considered reductions in Medicare reimbursement levels for drugs 
administered  by  physicians.  CMS  also  has  authority  to  revise  reimbursement  rates  and  to  implement 
coverage  restrictions  for  some  drugs.  Cost  reduction  initiatives  and  changes  in  coverage  implemented 
through  legislation  or  regulation  could  decrease  utilization  of  and  reimbursement  for  any  approved 
products,  which  in  turn  would  affect  the  price  we  can  receive  for  those  products.  While  Medicare 
regulations apply only to drug benefits for Medicare beneficiaries, private payors often follow Medicare 
coverage policy and payment limitations in setting their own reimbursement rates. Therefore, any reduction 
in  reimbursement  that  results from  federal  legislation  or  regulation  may  result  in  a  similar reduction  in 
payments from private payors. 

In March 2010, President Obama signed into law the Patient Protection and Affordable Care Act, 
as amended by the Health Care and Education Reconciliation Act of 2010 (collectively, the “Affordable 
Care  Act”).    This  law  substantially  changes  the  way  healthcare  is  financed  by  both  governmental  and 
private  insurers,  and  significantly  impacts  the  pharmaceutical  industry.    The  Affordable  Care  Act  is 
intended  to  broaden  access  to  health  insurance,  reduce  or  constrain  the  growth  of  healthcare  spending, 
enhance remedies against healthcare fraud and abuse, add new transparency requirements for healthcare 
and  health  insurance  industries,  impose  new  taxes  and  fees  on  pharmaceutical  and  medical  device 
manufacturers, and impose additional health policy reforms. Among other things, the Affordable Care Act 
expanded  manufacturers’  rebate  liability  under  the  Medicaid  Drug  Rebate  Program  by  increasing  the 
minimum Medicaid rebate for both branded and generic drugs, expanded the 340B program, and revised 
the  definition  of  AMP.  The  legislation  also  extended  Medicaid  drug  rebates,  previously  due  only  on 
fee-for-service Medicaid utilization, to include the utilization of Medicaid managed care organizations as 
well and created an alternative rebate formula for certain new formulations of certain existing products that 
is intended to increase the amount of rebates due on those drugs.    On February 1, 2016, CMS issued final 
regulations to implement the changes to the Medicaid Drug Rebate program under the Affordable Care Act.   
These  regulations  became  effective  on  April  1,  2016.    Moreover,  legislative  changes  to  the  Affordable 
Care  Act  remain  possible  and  appear  likely  in  the  115th  United  States  Congress  and  under  the  Trump 

32 

 
 
 
 
Administration, which could include changes that, among other things, decrease the number of individuals 
with health coverage. We expect that the Affordable Care Act, as currently enacted or as it may be amended 
in the future, and other healthcare reform measures that may be adopted in the future could have a material 
adverse  effect  on  our  industry  generally  and  on  our  ability  to  successfully  commercialize  our  product 
candidates, if approved. 

The Affordable Care Act requires pharmaceutical manufacturers of branded prescription drugs to 
pay  a  branded  prescription  drug  fee  to  the  federal  government.    Each  individual  pharmaceutical 
manufacturer pays a prorated share of the branded prescription drug fee of $3.0 billion in 2016, based on the 
dollar  value  of  its  branded  prescription  drug  sales  to  certain  federal  programs  identified  in  the  law.   
Furthermore, the new law requires manufacturers to provide a 50% discount off the negotiated price of 
prescriptions filled by beneficiaries in the Medicare Part D coverage gap, referred to as the “donut hole.”   

The Affordable Care Act also expanded the Public Health Service’s 340B drug pricing discount 
program.    The  340B  drug  pricing  program  requires  participating  manufacturers  to  agree  to  charge 
statutorily-defined covered entities no more than the 340B “ceiling price” for the manufacturer’s covered 
outpatient  drugs.    The  Affordable  Care  Act  expanded  the  340B  program  to  include  additional  types  of 
covered entities: certain free-standing cancer hospitals, critical access hospitals, rural referral centers and 
sole community hospitals, each as defined by the Affordable Care Act. The Affordable Care Act exempts 
“orphan  drugs”—those  designated  under  section  526  of  the  Food,  Drug,  and  Cosmetic  Act—from  the 
ceiling price requirements for these newly-eligible entities.    Because the 340B ceiling price is determined 
based  on  AMP  and  Medicaid  drug  rebate  data,  the  revisions  to  the  Medicaid  rebate  formula  and  AMP 
definition described above could cause the required 340B discounts to increase. 

In addition, other legislative changes have been proposed and adopted since the Affordable Care 
Act was enacted.    For example, recent legislative enactments have resulted in Medicare payments being 
subject to a two percent reduction, referred to as sequestration, until 2025. Continuation of sequestration or 
enactment of other reductions in Medicare reimbursement for drugs could affect our ability to achieve a 
profit on any candidate products that are approved for marketing.   

We expect that the Affordable Care Act, as well as other healthcare reform measures that have 
and  may  be  adopted  in  the  future,  may  result  in  more  rigorous  coverage  criteria  and  in  additional 
downward pressure on the price that we receive for any approved product and could seriously harm our 
future  revenues.  Any  reduction  in  reimbursement  from  Medicare,  Medicaid,  or  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.   

If we are able to successfully commercialize any of our products and if we participate in the Medicaid 
drug  rebate  program  or  other  governmental  pricing  programs,  failure  to  comply  with  reporting  and 
payment  obligations  under  these  programs  could  result  in  additional  reimbursement  requirements, 
penalties,  sanctions  and  fines  which  could  have  a  material  adverse  effect  on  our  business,  financial 
condition, results of operations and growth prospects. 

The  Medicaid  Drug  Rebate  Program  and  other  governmental  pricing  programs  require 
participating  manufacturers  to report  pricing  data to the  government.    Pricing  calculations  vary  among 
products  and  programs  and  include  average  manufacturer  price  and  best  price  for  the  Medicaid  Drug 
Rebate  Program,  average  sales  price  for  certain  categories  of  drugs  that  are  paid  under  Part  B  of  the 
Medicare  program,  and  non-federal  average  manufacturer  price  for  the  FSS  pricing  program.    If  we 
successfully commercialize any of our products and participate in such governmental pricing programs, 
we  will  be  liable  for  errors  associated  with  our  submission  of  pricing  data.    That  liability  could  be 
significant.    For example, if we are found to have knowingly submitted false average manufacturer price, 

33 

 
 
 
 
 
 
average sales price, best price, or non-federal average manufacturer price information to the government, 
we may be liable for civil monetary penalties in the amount of $178,156 per item of false information.   
If  we  are  found  to  have  made  a  misrepresentation  in  the  reporting  of  average  sales  price,  the  statute 
provides for civil monetary penalties of up to $12,856 for each misrepresentation for each day in which 
the misrepresentation was applied.    Our failure to submit monthly/quarterly average manufacturer price, 
average sales price, and best price, and quarterly/annual non-federal average manufacturer price data on a 
timely basis could result in a civil monetary penalty of $17,816 per day for each day the information is 
late  beyond  the  due  date.    Such  failure  also  could  be  grounds  for  other  sanctions,  such  as  termination 
from the Medicaid Drug Rebate Program. 

If we fail to comply with data protection laws and regulations, we could be subject to government 
enforcement actions (which could include civil or criminal penalties), private litigation and/or adverse 
publicity, which could negatively affect our operating results and business. 

We  are  subject  to  data  protection  laws  and  regulations  (i.e.,  laws  and  regulations  that  address 
privacy and data security). In the U.S., numerous federal and state laws and regulations, including state 
data  breach  notification  laws,  state  health  information  privacy  laws,  and  federal  and  state  consumer 
protection  laws  (e.g.,  Section 5  of  the  Federal  Trade  Commission  Act),  govern  the  collection,  use, 
disclosure, and protection of health-related and other personal information. Failure to comply with data 
protection laws and regulations could result in government enforcement actions and create liability for us 
(which could include civil and/or criminal penalties), private litigation and/or adverse publicity that could 
negatively affect our operating results and business. In addition, we may obtain health information from 
third  parties  (e.g.,  healthcare  providers  who  prescribe  our  products)  that  are  subject  to  privacy  and 
security  requirements  under  HIPAA.  Although  we  are  not  directly  subject  to  HIPAA—other  than 
potentially with respect to providing certain employee benefits—we could be subject to criminal penalties 
if  we  knowingly  obtain  or  disclose  individually  identifiable  health  information  maintained  by  a 
HIPAA-covered  entity  in  a  manner  that  is  not  authorized  or  permitted  by  HIPAA.  HIPAA  generally 
requires  that  healthcare  providers  and  other  covered entities  obtain  written  authorizations from  patients 
prior  to  disclosing  protected  health  information  of  the  patient  (unless  an  exception  to  the  authorization 
requirement applies). If authorization is required and the patient fails to execute an authorization or the 
authorization fails to contain all required provisions, then we may not be allowed access to and use of the 
patient’s information and our research efforts could be impaired or delayed. Furthermore, use of protected 
health information that is provided to us pursuant to a valid patient authorization is subject to the limits 
set  forth  in  the  authorization  (e.g.,  for  use  in  research  and  in  submissions  to  regulatory  authorities  for 
product  approvals).  In  addition,  HIPAA  does  not  replace  federal,  state,  international  or  other  laws  that 
may grant individuals even greater privacy protections. 

Our  relationships  with  customers  and  third-party  payors  will  be  subject  to  applicable  anti-kickback, 
fraud  and  abuse,  transparency  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. 

Healthcare providers, physicians and third-party payors play a primary role in the recommendation 
and  prescription  of  any  product  candidates  for  which  we  obtain  marketing  approval.  Our  future 
arrangements with third-party payors and customers may expose us to broadly applicable fraud and abuse 
and other healthcare laws and regulations that may constrain the business or financial arrangements and 
relationships  through  which  we  market,  sell and distribute  our products for  which  we obtain  marketing 
approval.  Restrictions  under  applicable  federal  and  state  healthcare  laws  and  regulations,  include  the 
following:   

34 

 
 
 
 
 
 
 
• 

• 

• 

the federal Anti-Kickback Law prohibits persons from, among other things, 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, the referral of an individual for the 
furnishing or arranging for the furnishing, or the purchase, lease or order, or arranging for 
or recommending purchase, lease or order, any good or service for which payment may be 
made under a federal healthcare program such as Medicare and Medicaid; 

the federal civil False Claims Act imposes penalties, including through civil whistleblower 
or  qui  tam  actions,  against  individuals  or  entities  for,  among  other  things,  knowingly 
presenting, or causing to be presented, to the federal government, claims for payment that 
are false or fraudulent or making a false statement material to an obligation to pay money 
to  the  government  or  knowingly  concealing  or  knowingly  and  improperly  avoiding, 
decreasing, or concealing an obligation to pay money to the federal government; 

the  federal  Health  Insurance  Portability  and  Accountability  Act  of  1996,  or  HIPAA, 
imposes criminal liability for knowingly and willfully executing a scheme to defraud any 
healthcare benefit program, knowingly and willfully embezzling or stealing from a health 
care benefit program, willfully obstructing a criminal investigation of a health care offense, 
or knowingly and willfully making false statements relating to healthcare matters; 

•  HIPAA,  as  amended  by  the  Health  Information Technology  for  Economic  and Clinical 
Health Act of 2009 and its implementing regulations, also imposes obligations on certain 
covered entity health care providers, health plans and health care clearinghouses as well as 
their business associates that perform certain services involving the use or disclosure of 
individually identifiable health information, including mandatory contractual terms, with 
respect to safeguarding the privacy, security and transmission of individually identifiable 
health information; 

• 

• 

the federal Open Payments program, created under Section 6002 of the Affordable Care 
Act and its implementing regulations, 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 certain exceptions) to report annually to the 
CMS  information  related  to  “payments  or  other  transfers  of  value”  made  to  physicians 
(defined  to  include  doctors,  dentists,  optometrists,  podiatrists  and  chiropractors)  and 
teaching  hospitals,  and  applicable  manufacturers  and  applicable  group  purchasing 
organizations  to  report  annually  CMS  ownership  and  investment  interests  held  by 
physicians (as defined above) and their immediate family members; 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  certain  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  that  govern  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. 

35 

 
 
 
 
 
 
 
Efforts to  ensure  that  our business  arrangements  with  third  parties  will  comply  with  applicable 
healthcare laws and regulations will involve substantial costs. It is possible that governmental authorities 
will conclude that our business practices may not comply with current or future statutes, regulations or case 
law interpreting applicable fraud and abuse or other healthcare laws and regulations. If our operations are 
found to be in violation of any of these laws or any other governmental regulations that may apply to us, we 
may be subject to significant civil, criminal and administrative penalties, damages, fines, imprisonment, 
exclusion  from  government  funded  healthcare  programs,  such  as  Medicare  and  Medicaid,  and  the 
curtailment  or  restructuring  of  our  operations.  If  any  of  the  physicians  or  other  healthcare  providers  or 
entities with whom we expect to do business is found not to be in compliance with applicable laws, that 
person or entity may be subject to criminal, civil or administrative sanctions, including exclusions from 
government funded healthcare programs.    For a fuller discussion of the applicable anti-kickback fraud and 
abuse,  transparency  and  other  healthcare  laws  and  regulations  applicable  to  our  business,  see  Item  1, 
‘Description of Business – Government Regulation” 

Developments by competitors may render our products or technologies obsolete or non-competitive. 

We  compete  against  fully  integrated  pharmaceutical  companies  and  smaller  companies  that  are 
collaborating  with  larger  pharmaceutical  companies  as  well  as  academic  institutions,  government 
agencies and other public and private research organizations. Many of these competitors, either alone or 
together  with  their  collaborative  partners,  operate  larger  research  and  development  programs  or  have 
substantially greater financial resources than we do, as well as more experience in: 

•  developing drugs; 

•  undertaking pre-clinical testing and human clinical trials; 

•  obtaining FDA and other regulatory approvals of drugs; 

• 

• 

formulating and manufacturing drugs; and 

launching, marketing and selling drugs. 

Large  pharmaceutical companies  currently  sell  both generic and  proprietary  compounds  for the 
treatment  of  cancer.  In  addition,  companies  developing  oncology  therapies  represent  substantial 
competition. Many of these organizations have substantially greater capital resources, larger research and 
development staff and facilities, longer drug development history in obtaining regulatory approvals and 
greater manufacturing and marketing capabilities than we do. These organizations also compete with us to 
attract qualified personnel, parties for acquisitions, joint ventures or other collaborations. Our competitors 
may succeed in developing products that are more effective and/or safe than ours, which could render our 
product  candidates  less  competitive  prior  to  recovery  by  us  of  expenses  incurred  with  respect  to  their 
development. 

If we are unable to successfully manage our growth, our business may be harmed. 

In  addition  to  our  own  internally  developed  drug  candidates,  we  are  actively  seeking 
opportunities to in-license compounds in oncology and other therapeutic areas that are strategic additions 
to  our  product  pipeline.  Such  additional  drug  candidates  could  significantly  increase  our  capital 
requirements and place further strain on our resources, including on the time of our existing personnel, 
which  may  delay  or  otherwise  adversely  affect  the  development  of  our  existing  drug  candidates.  As  of 
December 31, 2016, we had 20 full-time employees. We may need to hire more employees as our product 

36 

 
 
 
 
 
 
 
 
 
 
 
 
pipeline and operations expand, further increasing the size of our organization and related expenses. If we 
are unable to manage our growth effectively, we may not efficiently use our resources, which may delay 
the  development  of  our  drug  candidates  and  negatively  impact  our  business,  results  of  operations  and 
financial condition. 

We  may  not  be  able  to  attract  and  retain  qualified  personnel  necessary  for  the  development  and 
commercialization  of  our  drug  candidates.  Our  success  may  be  negatively  impacted  if  key  personnel 
leave. 

Attracting  and  retaining  qualified  personnel  is  critical  to  our  future  success.  We  compete  for 
qualified  individuals  with  numerous  biopharmaceutical  companies,  universities  and  other  research 
institutions.  Competition  for  such  individuals  is  intense,  and  we  cannot  assure  you  that  we  will  be 
successful in engaging personnel with the skills and experience to support our business and research and 
development activities. 

Our key personnel, especially Dr. Chang H. Ahn, our Chairman Emeritus and Chief Scientist, Dr. 
Peter Suzdak, our Chief Executive Officer, Dr. Ely Benaim, our Chief Medical Officer, Dr. Lisa Nolan, 
our  Chief  Business  Officer,  and  Dr.  Tae  Heum  Jeong,  our  Chief  Financial  Officer,  provide  critical 
technical knowledge and expertise.    The loss of Dr. Ahn, Dr. Suzdak, Dr. Benaim, Dr. Nolan, Dr. Jeong, 
or any of the other members of our management team, could result in delays in product development and 
diversion of management resources, which could adversely affect our operating results. We do not have 
“key person” life insurance policies for any of our executive officers. 

We may incur substantial liabilities and may be required to limit commercialization of our products in 
response to product liability lawsuits.     

The testing and marketing of medical products entail an inherent risk of product liability. Product 
liability claims may be brought against us by subjects enrolled in our clinical trials, patients, healthcare 
providers or others using, administering or selling our products. Large judgments have been awarded in 
class action lawsuits based on drugs that had unanticipated side effects. If we cannot successfully defend 
ourselves  against  product  liability  claims,  we  may  incur  substantial  liabilities  or  be  required  to  limit 
commercialization  of  our  products.  Our  inability  to  obtain  sufficient  product  liability  insurance  at  an 
acceptable  cost  to  protect  against  potential  product  liability  claims  could  prevent  or  inhibit  the 
commercialization  of  pharmaceutical  products  we  develop,  alone  or  with  collaborators.  Although  we 
currently carry clinical trial insurance and product liability insurance we, or any collaborators, may not be 
able to maintain such insurance at a reasonable cost. Even if our agreements with any future collaborators 
entitle us to indemnification against losses, such indemnification may not be available or adequate should 
any claims arise. 

Risks Related to Reliance on Third Parties 

Much of our drug development program depends upon third-party researchers, and thus the conduct 
and completion of our clinical trials are, to some extent, beyond our control. 

We  have  engaged  third-party  contract  research  organizations  and  other  investigators  and 
collaborators, such as universities and medical institutions, to conduct our pre-clinical studies, toxicology 
studies and clinical trials. Engaging third-party contract research organizations is typical practice in our 
industry. However, relying on such organizations means that the clinical trials and other studies described 
above are being conducted at external locations and that the completion of these trials and studies is not 
within our direct control. Trials and studies may be delayed due to circumstances outside our control, and 
such delays may result in additional expenses for us. 

37 

 
 
 
 
 
 
 
 
 
 
While  we  make  every  effort  internally  to  oversee  the  work  of  third-party  contractors,  these 
collaborators are not our employees, and we cannot control the effort, time or other resources that they 
devote to our programs. Third parties may not assign priority to our programs or pursue them as diligently 
as we would if we were undertaking them ourselves. If outside collaborators fail to devote sufficient time 
and resources to our drug-development programs, or if their performance is substandard, the approval of 
our FDA applications and introduction of new drugs to the market may be delayed. These collaborators 
may also have relationships with other commercial entities, some of which may compete with us. If our 
collaborators assist our competitors at our expense, our competitive position would be harmed. 

We rely exclusively on third parties to formulate and manufacture our drug candidates, which exposes 
us to a number of risks that may delay development, regulatory approval and commercialization of our 
products or result in higher product costs. 

We  have  no  experience  in  drug  formulation  or  manufacturing  and  we  lack  the  resources  and 
expertise  to  formulate  or  manufacture  our  own  drug  candidates  internally.  Therefore,  we  rely  on 
third-party  expertise  to  support  us  in  this  area.  We  have  entered  into  contracts  with  third-party 
manufacturers to manufacture, supply, store and distribute supplies of our drug candidates for our clinical 
trials. If any of our drug candidates receives FDA approval, we expect to rely on third-party contractors to 
manufacture  our  drugs.  We  have  no  current  plans  to  build  internal  manufacturing  capacity  for  any 
product, and we have no long-term supply arrangements. 

Our reliance on third-party manufacturers exposes us to the following potential risks: 

•  We  may  be  unable  to  contract  with  third-party  manufacturers  on  acceptable  terms,  or  at  all, 
because the number of potential manufacturers is limited and potential manufacturers are subject 
to  FDA  approval.  FDA  approval  requires  testing  and  compliance  inspections.  In  addition,  any 
new manufacturer would have to be qualified and approved to produce our products after receipt 
of FDA approval, if any; 

•  Our  third-party  manufacturers  might  be  unable  to  formulate  and  manufacture  our  drugs  in  the 

volume and of the quality required to meet our clinical and commercial needs, if any; 

•  Our  third-party  manufacturers  may  not  perform  as  agreed  or  may  not  remain  in  the  contract 
manufacturing business for the time required to supply our clinical trials through completion or to 
successfully produce, store and distribute our commercial products, if approved; 

•  Drug  manufacturers  are  subject  to  ongoing  periodic  unannounced  inspection  by  the  FDA  and 
other  government  agencies  to  ensure  compliance  with  cGMP  and  other  government  regulations 
and  corresponding  foreign  standards.  We  do  not  have  control  over  third-party  manufacturers’ 
compliance with these regulations and standards, but we may ultimately be responsible for any of 
their failures; 

• 

If  any  third-party  manufacturer  makes  improvements  in  the  manufacturing  process  for  our 
products,  we  may  not  own,  or  may  have  to  share,  the  intellectual  property  rights  to  such 
improvements; and 

•  A  third-party  manufacturer  may  gain  knowledge  from  working  with  us  that  could  be  used  to 

supply one of our competitors with a product that competes with ours. 

38 

 
 
 
 
 
 
 
 
 
 
 
 
 
Each  of  these  risks  could  delay  or  have  other  adverse  impacts  on  our  clinical  trials  and  the 
approval  and  commercialization  of  our  drug  candidates,  potentially  resulting  in  higher  costs,  reduced 
revenues or both. 

We have no experience selling, marketing or distributing products and currently no internal capability 
to do so. 

We currently have no sales, marketing or distribution capabilities. While we intend to have a role 
in  the  commercialization  of  our  products,  we  do  not  anticipate  having  the  resources  in  the  foreseeable 
future  to  develop  global  sales  and  marketing  capabilities  for  all  of  our  proposed  products.  Our  future 
success depends, in part, on our ability to enter into and maintain collaborative relationships with other 
companies  that  have  sales,  marketing  and  distribution  capabilities,  a  strategic  interest  in  the  products 
under  development,  and  the  ability  to  successfully  market  and  sell  our  products.  To  the  extent  that  we 
decide  not  to,  or  are  unable  to,  enter  into  collaborative  arrangements  with  respect  to  the  sales  and 
marketing of our proposed products, significant capital expenditures, management resources and time will 
be required to establish and develop an in-house marketing and sales force with the necessary expertise. 
We  cannot  assure  you  that  we  will  be  able  to  establish  or  maintain  relationships  with  third-party 
collaborators or develop in-house sales and distribution capabilities. To the extent that we depend on third 
parties for marketing and distribution, any revenues we receive will depend upon the efforts of such third 
parties, as well as the terms of our agreements with such third parties, which cannot be predicted at this 
early stage of our development. We cannot assure you that such efforts will be successful. In addition, we 
cannot assure you that we will be able to market and sell our products in the United States or overseas. 

Risks Related to Our Intellectual Property 

If we fail to adequately protect or enforce our intellectual property rights or secure rights to patents of 
others, the value of our intellectual property rights would diminish, and our business and competitive 
position would suffer.     

Our success, competitive position and future revenues will depend in part on our ability and the 
abilities of our licensors and licensees to obtain and maintain patent protection for our products, methods, 
processes and other technologies, to preserve our trade secrets, to prevent third parties from infringing on 
our proprietary rights and to operate without infringing the proprietary rights of third parties. We have an 
active patent protection program that includes filing patent applications on new compounds, formulations, 
delivery systems and methods of making and using products and prosecuting these patent applications in 
the  United  States  and  abroad.  As  patents  issue,  we  also  file  continuation  applications  as  appropriate. 
Although we have taken steps to build a strong patent portfolio, we cannot predict: 

• 

• 

the  degree  and  range  of  protection  any  patents  will  afford  us  against  competitors,  including 
whether third parties find ways to invalidate or otherwise circumvent our licensed patents; 

if and when patents will issue in the United States or any other country; 

•  whether or not others will obtain patents claiming aspects similar to those covered by our licensed 

patents and patent applications; 

•  whether we will need to initiate litigation or administrative proceedings to protect our intellectual 

property rights, which may be costly whether we win or lose; 

•  whether  any  of  our  patents  will  be  challenged  by  our  competitors  alleging  invalidity  or 

39 

 
 
 
 
 
 
 
 
 
 
 
 
unenforceability and, if opposed or litigated, the outcome of any administrative or court action as 
to patent validity, enforceability or scope; 

•  whether  a  competitor  will  develop  a  similar  compound  that  is  outside  the  scope  of  protection 
afforded  by  a  patent  or  whether  the  patent  scope  is  inherent  in  the  claims  modified  due  to 
interpretation of claim scope by a court; 

•  whether  there  were  activities  previously  undertaken  by  a  licensor  that  could  limit  the  scope, 

validity or enforceability of licensed patents and intellectual property; or 

•  whether  a  competitor  will assert infringement  of  its patents  or  intellectual  property,  whether  or 

not meritorious, and what the outcome of any related litigation or challenge may be. 

Our  success  also  depends  upon  the  skills,  knowledge  and  experience  of  our  scientific  and 
technical personnel, our consultants and advisors as well as our licensors, sublicensees and contractors. 
To help protect our proprietary know-how and our inventions for which patents may be unobtainable or 
difficult  to  obtain,  we  rely  on  trade  secret  protection  and  confidentiality  agreements.  To  this  end,  we 
require all employees to enter into agreements that prohibit the disclosure of confidential information and, 
where  applicable,  require  disclosure  and  assignment  to  us  of  the  ideas,  developments,  discoveries  and 
inventions important to our business. These agreements may not provide adequate protection for our trade 
secrets, know-how or other proprietary information in the event of any unauthorized use or disclosure or 
the  lawful  development  by  others  of  such  information.  If  any  of  our  trade  secrets,  know-how  or  other 
proprietary information is disclosed, the value of our trade secrets, know-how and other proprietary rights 
would be significantly impaired, and our business and competitive position would suffer. 

Due to legal and factual uncertainties regarding the scope and protection afforded by patents and other 
proprietary rights, we may not have meaningful protection from competition. 

 Our  long-term  success  will  substantially  depend  upon  our  ability  to  protect  our  proprietary 
technologies  from  infringement,  misappropriation,  discovery  and  duplication  and  avoid  infringing  the 
proprietary  rights  of  others.  Our  patent  rights,  and  the  patent  rights  of  biopharmaceutical  companies  in 
general, are highly uncertain and include complex legal and factual issues. These uncertainties also mean 
that any patents that we own or may obtain in the future could be subject to challenge, and even if not 
challenged, may not provide us with meaningful protection from competition. Patents already issued to us 
or our pending applications may become subject to dispute, and any dispute could be resolved against us. 

In  connection  with  the  process  of  seeking  patent  protection  for  Supinoxin  in  Japan,  we  filed  a 
patent  application  including  claims  covering  Supinoxin  with  the  Japanese  Patent  Office  (“JPO”)  for 
examination.  The  JPO  initially  agreed  that  the  claims  covering  the  compound  for  Supinoxin  were 
allowable, but as a result of a mistake in the patent application filing as prepared and submitted by our 
Japanese patent attorney and incomplete review by the JPO’s patent examiner, the JPO issued a decision 
to  grant  a  patent  with  claims  that  did  not  include  Supinoxin’s  chemical  structure.   We  appealed  this 
decision with the JPO and requested withdrawal of the ‘decision to grant’ so that the correct claims would 
be  allowed, but  the JPO  refused  to  withdraw its decision. As  a result, and  in  accordance  with Japanese 
law and procedure for appealing patent application decisions, we have filed a lawsuit against the JPO in 
Tokyo  District  Court  to  cause  the  JPO  to  reverse  its  decision  to  grant  the  errant  patent  and  to  allow  a 
patent that includes claims covering Supinoxin.   The patent application at issue remains pending subject 
to the outcome of this action.    However, there can be no guarantee that we will be successful in winning 
the appeal to correct the error in the patent registration that would exclude the compound for Supinoxin.   
While the composition of matter patent on Supinoxin’s structure remains pending in Japan, we have also 
filed, or intend to file, additional patents covering method of use and manufacturing process that would 

40 

 
 
 
 
 
 
 
 
 
extend  to  2035/2036  if  approved.    We  also  expect  that  Supinoxin  will  be  covered  by  regulatory 
exclusivity up to ten years post approval.     

If we infringe the rights of third parties, we could be prevented from selling products and be forced to 
defend against litigation and pay damages. 

If our products, methods, processes and other technologies infringe the proprietary rights of other 

parties, we could incur substantial costs and may have to:     

•  obtain licenses, which may not be available on commercially reasonable terms, if at all; 

• 

• 

redesign our products or processes to avoid infringement; 

stop using the subject matter claimed in patents held by others, which could cause us to lose the 
use of one or more of our drug candidates; 

•  pay damages; or 

•  defend  litigation  or  administrative  proceedings  that  may  be  costly  whether  we  win  or  lose  and 

that could result in a substantial diversion of our management resources. 

Although we have not received any claims of infringement by any third parties to date, we expect 
that as our drug candidates move further into clinical trials and commercialization and our public profile 
is raised, we may be subject to such claims. 

Risks Related to Ownership of Our Common Stock 

An investment in shares of our common stock is very speculative and involves a very high degree of 
risk. 

To  date,  we  have  generated  no  revenues from  product sales  and  only  minimal  revenues  from  a 
research  agreement  with  a  minority  shareholder  and  interest  on  bank  account  balances  and  short-term 
investments.  Our  accumulated  deficit  as  of  December  31,  2016  and  2015  was  $115,024,209  and 
$105,716,864 respectively. For the years ended December 31, 2016, 2015 and 2014, we had net losses of 
$9,307,345, $14,384,556 and $18,521,601, respectively, partially as a result of expenses incurred through 
a combination of research and development activities related to the various technologies under our control 
and expenses supporting those activities. Until we receive approval from the FDA and other regulatory 
authorities for our drug candidates, we cannot sell our drugs and will not have product revenues. 

The market price of our common stock may fluctuate significantly. 

The market price of our common stock may fluctuate significantly in response to factors, some of 

which are beyond our control, such as: 

• 

• 

the announcement of new products or product enhancements by us or our competitors; 

changes in our relationships with our licensors or other strategic partners; 

•  developments concerning intellectual property rights and regulatory approvals; 

41 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
•  variations in our and our competitors’ results of operations; 

• 

• 

changes in earnings estimates or recommendations by securities analysts;   

changes in the structure of healthcare payment systems; and 

•  developments and market conditions in the pharmaceutical and biotechnology industries. 

Further, the stock market, in general, and the market for biotechnology companies, in particular, 
have  experienced extreme  price  and  volume  fluctuations.  Continued  market  fluctuations  could  result  in 
extreme volatility in the price of our common stock, which may be unrelated or disproportionate to our 
operating performance and which could cause a decline in the value of our common stock. You should 
also be aware that price volatility might be worse if the trading volume of our common stock is low.   

We will require additional capital funding the receipt of which may impair the value of our common 
stock. 

Our  future  capital  requirements  depend  on  many  factors,  including  our  research,  development, 
sales and marketing activities. We will need to raise additional capital through public or private equity or 
debt  offerings  or  through  arrangements  with  strategic  partners  or  other  sources  in  order  to  continue  to 
develop our drug candidates.    There can be no assurance that additional capital will be available when 
needed or on terms satisfactory to us, if at all.  To the extent we raise additional capital by issuing equity 
securities, our stockholders may experience substantial dilution and the new equity securities may have 
greater rights, preferences or privileges than our existing common stock. 

We have not paid dividends to our stockholders in the past, and we do not anticipate paying dividends 
to our stockholders in the foreseeable future. 

We have not declared or paid cash dividends on our common stock. We currently intend to retain 
all  future  earnings,  if  any,  to  fund  the  continuing  operation  of  our  business,  and  therefore  we  do  not 
anticipate  paying  dividends  on  our  common  stock  in  the  foreseeable  future.  As  a  result,  you  will  not 
realize any income from an investment in our common stock until and unless you sell your shares at a 
profit. 

We may be subject to securities litigation, which is expensive and could divert management attention. 

The  market  price  of  our  common  stock  may  be  volatile,  and  in  the  past  companies  that  have 
experienced  volatility  in  the  market  price  of  their  stock  have  been  subject  to  securities  class  action 
litigation.    We may be the target of this type of litigation in the future.    Securities litigation against us 
could  result  in  substantial  costs  and  direct  our  management’s  attention  from  other  business  concerns, 
which could seriously harm our business. 

42 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Item 1B.    Unresolved Staff Comments. 

None 

Item 2.      Description of Property. 

We lease approximately 7,103 square feet of office space in Rockville, Maryland.    We also lease 
approximately 1,100 square feet of laboratory space in Gaithersburg, Maryland.   The laboratory space is 
equipped with the requisite laboratory services required to conduct our business and we believe our existing 
facilities are adequate to meet our needs for the foreseeable future.   The office lease, which commenced on 
June 29, 2009, expires in June 2019.   The laboratory lease, which commenced on July  1, 2015 expires in 
June 2020.   We do not own any real property.   

Item 3.      Legal Proceedings. 

None   

Item 4.      Mine Safety Disclosures. 

Not Applicable 

43 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
  
 
 
 
 
 
PART II 

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

Our  common  stock  is  traded  on  the  NYSE  MKT,  under  the  ticker  symbol  “RNN”.    As  of 
February  24,  2017,  there  were  approximately  65  stockholders  of  record  of  our  common  stock.    The 
following table sets forth the high and low sales prices of our common shares as reported on the NYSE 
MKT during the periods indicated.     

Period 

2015 

First Quarter 
Second Quarter 
Third Quarter 
Fourth Quarter 

2016 

First Quarter 
Second Quarter 
Third Quarter 
Fourth Quarter 

Dividends 

High ($) 

Low ($) 

0.96 
0.81 
0.66 
0.53 

0.42 
0.34 
0.28 
0.23 

0.69 
0.60 
0.48 
0.35 

0.26 
0.24 
0.20 
0.13 

We  have  not  paid  any  cash  dividends  on  common  stock  and  do  not  expect  to  do  so  in  the 
foreseeable  future.    We  anticipate  that  any  earnings  generated  from  future  operations  will  be  used  to 
finance our operations.    No restrictions exist upon our ability to pay dividends. 

Purchase of Equity Securities by the Issuer and Affiliated Purchasers 

There were no repurchases of equity securities in 2016. 

Recent Sales of Unregistered Equity Securities 

None 

44 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Performance Graph 

The following graph compares the cumulative total stockholder return on $100 of our common 
stock for the period beginning December 31, 2011 through December 31, 2016, with the cumulative total 
return over such period for an identical investment in i) the NYSE Arca Biotechnology Index or ii) the 
NYSE MKT Composite Index.    This graph is not deemed to be “filed” with the SEC or subject to the 
liabilities of Section 18 of the Exchange Act, and the graph shall not be deemed to be incorporated by 
reference into any prior or subsequent filing by us under the Securities Act or the Exchange Act. 

45 

 
 
 
 
 
 
 
 
 
 
 
 
Item 6.    Selected Financial Data. 

The following selected data should be read in conjunction with “Item 7. Management’s 
Discussion and Analysis of Financial Condition and Results of Operations” and our financial statements 
included elsewhere in this Annual Report. 

Statement of Operations Data: 
Revenues 
Expenses: 
        General and administrative 
        Research and development 
Total expenses 
Loss from operations 
Other Income (Expense), net 
Net Loss 
Net Loss per share, basic and 
diluted 
Weighted average shares 
outstanding, basic and diluted 

$

$
$

2016 

For the Year Ended December 31, 
2014 

2013 

2015 

2012 

-  $

-  $

-  $

-  $

- 

6,324,236 
6,115,210 
12,148,226 
10,089,149 
18,263,436 
16,413,385 
(18,263,436) 
(16,413,385) 
7,106,040 
3,878,880 
(9,307,345) $ (14,384,556) $ (18,521,601) $
(0.11) $

6,253,328 
7,015,901 
13,269,229 
(13,269,229) 
(5,252,372) 

(0.08) $

(0.04) $

4,725,699 
3,253,139 
7,978,838 
(7,978,838) 
(1,520,586) 
(9,499,424) $
(0.07) $

3,186,634 
3,392,896 
6,579,530 
(6,579,530) 
352,860 
(6,226,670) 
(0.06) 

217,447,405 

182,388,226 

176,106,981 

128,649,303 

97,138,233 

Balance Sheet Data: 

Cash, Cash Equivalents, and 
Marketable Securities 

Working Capital 

Total Assets 

Warrant Liabilities 

Accumulated Deficit 

2016 

2015 

As of December 31, 
2014 

2013 

2012 

$ 20,315,580  $ 23,439,526  $ 32,698,296  $ 18,788,031  $ 13,586,543 

$ 19,041,597  $ 22,000,046  $ 30,970,020  $ 18,361,438  $ 12,923,514 

$ 21,043,532  $ 24,805,029  $ 33,533,060  $ 19,556,498  $ 14,919,308 

$

1,573,366  $

2,739,163  $

3,768,351  $

5,034,058  $

2,842,065 

$(115,024,209) $(105,716,864) $ (91,332,308) $ (72,810,707) $ (63,311,283) 

Total Stockholders' Equity 

$ 17,058,462  $ 18,775,548  $ 26,580,491  $ 12,625,488  $

9,533,989 

Common shares outstanding 

237,368,785 

197,413,785 

178,253,318 

146,717,795 

119,428,989 

46 

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

You  should  read the  following  discussion  and  analysis  of  our  results  of  operations, financial  condition 
and liquidity in conjunction with our financial statements and the related notes, which are included in this 
Annual Report.    Some of the information contained in this discussion and analysis or set forth elsewhere 
in  this  Annual  Report, including information  with  respect to  our  plans  and  strategies  for  our  business, 
statements  regarding  the  industry  outlook,  our  expectations  regarding  the  future  performance  of  our 
business, and the other non-historical statements contained herein are forward-looking statements.    See 
“Cautionary  Statement Regarding  Forward-Looking  Statements.”    You  should  also  review  the  “Risk 
Factors” section under this Item 1A of this Annual Report for a discussion of important factors that could 
cause  actual  results  to  differ  materially  from  the  results  described  herein  or  implied  by  such 
forward-looking statements. 

OVERVIEW 

We are a clinical stage biopharmaceutical company dedicated to the discovery, development and 
commercialization  of  innovative  treatments  for  cancer.  Our  mission  is  to  improve  the  lives  of  cancer 
patients  by  developing  next-generation  cancer  therapies  that  are  designed  to  maximize  efficacy  while 
minimizing  the  toxicity  and  side  effects  traditionally  associated  with  cancer  treatment.  Our  clinical 
pipeline features three product candidates in Phase II clinical development and additional compounds in 
pre-clinical  development.  Our  strategy  is  to  continue  building  a  significant  pipeline  of  innovative 
oncology product candidates that we will commercialize alone or with partners. 

Since  our  inception,  our  efforts  and  resources  have  been  focused  primarily  on  developing  our 
pharmaceutical technologies, raising capital and recruiting personnel.  We have no product sales to date, 
and we will not generate any product sales until we receive approval from the FDA or equivalent foreign 
regulatory bodies to begin selling our pharmaceutical candidates.  Our major sources of working capital 
have  been  proceeds  from  various  private  and  public  financings,  and  licensing  and  collaboration 
agreements with our strategic investors and partners.   

Critical Accounting Policies 

A  “critical  accounting  policy”  is  one  which  is  both  important  to  the  portrayal  of  our  financial 
condition  and  results  and  requires  our  management’s  most  difficult,  subjective  or  complex  judgments, 
often as a result of the need to make estimates about the effect of matters that are inherently uncertain.   
Our  accounting  policies are  in  accordance  with  U.S. generally  accepted accounting  principles and their 
basis  of  application  is  consistent  with  that  of  the  previous  year.    Our  significant  estimates  include 
assumptions  made  in  estimating  the  fair  values  of  stock-based  compensation,  warrant  liabilities, 
marketable  securities,  and  our  assessment  relating  to  costs  incurred  on  research  and  development 
contracts.   

Research and Development 

Research and development costs are expensed as incurred.    Research and development expenses 
consist  primarily  of  third  party  service  costs  under  research  and  development  agreements,  salaries  and 
related  personnel  costs,  as  well  as  stock-based  compensation  related  to  these  costs,  costs  to  acquire 
pharmaceutical  products  and  product  rights  for  development  and  amounts  paid  to  contract  research 
organizations, hospitals and laboratories for the provision of services and materials for drug development 
and clinical trials. 

47 

 
 
 
 
 
 
 
 
Costs incurred in obtaining the license rights to technology in the research and development stage 

that have no alternative future uses and are for unapproved product compounds are expensed as incurred 

As part of the process of preparing our financial statements, we are required to estimate our accrued 
expenses. This process involves reviewing open contracts and purchase orders, communicating with our 
personnel to identify services that have been performed on our behalf and estimating the level of service 
performed and the associated cost incurred for the service when we have not yet been invoiced or otherwise 
notified of the actual cost. The majority of our service providers invoice us monthly in arrears for services 
performed or when contractual milestones are met. 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. 
Examples of estimated accrued research and development expenses include fees paid to: 

•  Contract  Research  Organizations  (“CROs”)  and  investigative  sites  in  connection  with  clinical 

studies; 

•  Vendors related to product manufacturing, development, and distribution of clinical supplies; and 

•  Vendors in connection with preclinical development activities.   

We record expenses related to clinical studies and manufacturing development activities based on 
our estimates of the services received and efforts expended pursuant to contracts with multiple CROs and 
manufacturing vendors that conduct and manage these activities on our behalf. The financial terms of these 
agreements are subject to negotiation, vary from contract to contract, and may result in uneven payment 
flows. There may be instances in which payments made to our vendors will exceed the level of services 
provided and result in a prepayment of the expense. Payments under some of these contracts depend on 
factors  such  as  the  successful  enrollment  of  subjects  and  the  completion  of  clinical  trial  milestones.  In 
accruing service fees, we estimate the time period over which services will be performed, enrollment of 
subjects, number of sites activated and the level of effort to be expended in each period. If the actual timing 
of the  performance  of services  or the  level  of effort varies  from  our estimate, we  adjust the  accrued or 
prepaid expense balance accordingly. Although we do not expect our estimates to be materially different 
from amounts actually incurred, if our estimates of the status and timing of services performed differ from 
the actual status and timing of services performed, we may report amounts that are too high or too low in 
any particular period. To date, there have been no material differences from our estimates to the amounts 
actually incurred. 

Fair Value of Financial Instruments 

The  carrying  amounts  reported  in  the  accompanying  financial  statements  for  cash  and  cash 
equivalents,  prepaid  expenses  and  other  current  assets  and  accounts  payable  and  accrued  expenses 
approximate fair value because of the short-term maturity of these financial instruments.    The fair value 
methodology for our warrant liabilities and marketable securities is described in detail in Item 8 of this 
Annual Report on Form 10-K. 

Income Taxes 

We  account  for  income  taxes  in  accordance  with  Accounting  Standards  Codification  (“ASC”) 
740,  “Income  Taxes.”    Deferred  tax  assets  and  liabilities  are  recorded  for  differences  between  the 
financial  statement  and  tax  basis  of  the  assets  and  liabilities  that  will  result  in  taxable  or  deductible 
amounts in the future based on enacted tax laws and rates.    ASC 740 requires that a valuation allowance 
be established when it is more likely than not that all portions of a deferred tax asset will not be realized.   
A review of all positive and negative evidence needs to be considered, including a company’s current and 
past  performance,  the  market  environment  in  which  the  company  operates,  length  of  carryback  and 

48 

 
 
 
   
 
 
carryforward  periods  and  existing  contracts  that  will  result  in  future  profits.    Income  tax  expense  is 
recorded for the amount of income tax payable or refundable for the period, increased or decreased by the 
change in deferred tax assets and liabilities during the period. 

As a result of our significant cumulative losses, we determined that it was appropriate to establish 

a valuation allowance for the full amount of our deferred tax assets. 

The  calculation  of  our  tax  liabilities  involves  the  inherent  uncertainty  associated  with  the 
application  of  complex  tax  laws.    We  are  subject  to  examination  by  various  taxing  authorities.    We 
believe that as a result of our losses sustained to date, any examination would result in a reduction of our 
net operating loss carryforward rather than a tax liability.    As such, we have not provided for additional 
taxes estimated under ASC 740.   

Warrant Liabilities 

In  accordance  with  ASC  480,  “Distinguishing  Liabilities  from  Equity,”  we  record  warrant 
liabilities  at  fair  value  due  to  provisions  in  our  warrant  agreements,  as  discussed  further  in  Note  12, 
Warrants, in the Notes to the Financial Statements of Item 8 of this Annual Report.    We reevaluate the 
fair  value  of  our  warrants  at  each  reporting  period,  and  changes  in  the  fair  value  between  reporting 
periods is recorded as “unrealized gain (loss) on fair value of warrants” in the statement of operations.     

Stock-Based Compensation 

In accordance with ASC 718, “Stock Compensation” compensation costs related to share-based 
payment transactions, including employee stock options, are to be recognized in the financial statements. 
In  addition,  we  adhere  to the  guidance set  forth  within  SEC  Staff  Accounting  Bulletin  No.  107  (“SAB 
107”), which provides the Staff’s views regarding the interaction between ASC 718 and certain SEC rules 
and  regulations,  and  provides  interpretations  with  respect  to  the  valuation  of  share-based  payments  for 
public companies.       

We  estimate  the  fair  value  of  stock  options  using  the  Black-Scholes  valuation  model.  The 

Black-Scholes model requires the input of highly subjective assumptions. These assumptions include: 

Expected  Term-the  expected  term  was  estimated  using  the  simplified  method  whereby  the 
expected term equals the arithmetic average of the vesting term and the original contractual term 
of the option. 

Volatility-historical trading volatility of our stock on the date of grant for a period consistent with 
the expected term 

Risk-Free  Interest  Rate-the  risk-free  interest  rate  is  based  on  the zero-coupon U.S.  Treasury 
instruments  on  the  date  of  grant  with  a  maturity  date  consistent  with  the  expected  term  of  our 
stock option grants. 

Expected Dividend -to date, we have not declared or paid any cash dividends and do not have any 
plans to do so in the future. Therefore, we used an expected dividend yield of zero. 

As  required,  we  review  our  valuation  assumptions  at  each  grant  date  and,  as  a  result,  we  may 
change our valuation assumptions used to value employee stock-based awards granted in future periods. 
Employee and director stock-based compensation costs are to be recognized over the vesting period of the 
award. 

49 

 
 
 
 
 
Concentration of Credit Risk 

ASC 825, “Financial Instruments,” requires disclosure of any significant off-balance sheet risk and 
credit risk concentration.    We do not have significant off-balance sheet risk or credit concentration.    We 
maintain cash and short-term investments with major financial institutions.    From time to time we have 
funds on deposit with commercial banks that exceed federally insured limits.    The balances are insured by 
the  Federal  Deposit  Insurance  Corporation  up  to $250,000.  At  December  31,  2016,  our  uninsured  cash 
balance was $11,078,473. Management does not consider this to be a significant credit risk as the banks are 
large, established financial institutions. 

Recently Issued Accounting Standards 

See  Note  2,  “Summary  of  Significant  Accounting  Policies  in  the  Notes  to  the  Financial 
Statements”,  in  the  Notes  to  Financial  Statements  of  this  Annual  Report  for  a  discussion  of  recent 
accounting pronouncements.   

Results of Operations 

Comparison of the Years Ended December 31, 2016 and December 31, 2015 

Total Revenues 

We had no revenues for the years ended December 31, 2016 or 2015. 

General and Administrative Expenses 

General  and  administrative  expenses  consist  primarily  of  salaries  and  related  expenses  for 
executive, finance and other administrative personnel, recruitment expenses, professional fees and other 
corporate expenses, including business development, investor relations, and general legal activities. 

General and administrative expenses increased approximately $209,000, or 3.4%, to $6,324,000 
for  the  year  ended  December  31,  2016  from  $6,115,000  for  the  year  ended  December  31,  2015.    The 
year over year increase is primarily attributable to an increase in personnel expenses. 

Research and Development Expenses 

Research  and  development  expenses  decreased  approximately  $2,059,000,  or  16.9%,  to 
$10,089,000 for the year ended December 31, 2016, from $12,148,000 for the year ended December 31, 
2015.    Decreased research and development costs for the year ended December 31, 2016 were primarily 
attributable to lower manufacturing costs for our drug candidates due to a significant supply of our drug 
candidates already being available to us from earlier manufacturing campaigns.    During the year ended 
December  31,  2016,  we  incurred  approximately  $2,564,000  of  drug  manufacturing  costs,  compared  to 
approximately $5,614,000 during the year ended December 31, 2015.    Because the volume and timing of 
drug  manufacturing  does  not  correlate  directly  with  the  level  and  timing  of  clinical  trial  activity,  we 
expect expenses related to drug manufacturing costs to vary from period to period based not only on the 
progress of clinical trials, but also when we engage in manufacturing activities.    The decreases to drug 
manufacturing  costs  were  partially  offset  by  increases  in  clinical  costs  related  to  patient  and  site 
enrollment and personnel costs.    We expect expenses to increase in the year ending December 31, 2017 
compared  to  the  year  ended  December  31,  2016  due  to  increased  patient  enrollments  in,  and  further 
progress of, our clinical trials. 

50 

 
 
 
 
 
 
 
 
 
 
 
 
 
The  table  below  summarizes  the  approximate  amounts  incurred  on  each  of  our  research  and 

development projects for the years ended December 31, 2016 and 2015: 

Clinical Candidates: 

RX-3117 
Supinoxin 
Archexin 

For the Year Ended December 31,   

2016 

2015 

$ 

  2,290,000 $ 
  2,230,800  
  1,573,800   

  4,062,000 
  2,839,000 
  1,547,000 

Preclinical, Personnel and Overhead 

  3,994,549   

  3,700,226 

Total Research and Development Expenses 

$ 

  10,089,149 $ 

  12,148,226 

Interest Income 

Interest  income  increased  approximately  $15,000  or  14.8%  to  $118,000  for  the  year  ended 
December  31,  2016  from  $103,000  for  the  year  ended  December  31,  2015.    The  increase  is  primarily 
attributable to higher interest rates on cash and cash equivalents, and marketable securities for the year 
ended December 31, 2016 compared to the year ended December 31, 2015. 

Mediation Settlement 

During  the  year  ended  December  31,  2016,  we  received  approximately  $1,771,000  from  a 
binding,  one-time  settlement  agreement  with  one  of  our  Japanese  patent  attorneys  in  exchange  for  our 
agreement not to bring any future claims related to a patent filing in Japan. 

Unrealized Gain on Fair Value of Warrants 

Our warrants are recorded as liabilities at fair value, and the warrants are valued using a lattice 
model.    Changes in the fair value of warrants are recorded as an unrealized gain or loss in our statement 
of operations.    During the years ended December 31, 2016 and 2015, we recorded unrealized gains on 
the fair value of our warrants of approximately $5,530,000 and $3,987,000 respectively.    Estimating fair 
values  of  warrants  requires  the  development  of  significant  and  subjective  estimates  that  may,  and  are 
likely  to,  change  over  the  duration  of  the  warrant  with  related  changes  to  external  market  factors.  The 
unrealized  gains for the  years ended  December  31,  2016  and  2015 primarily  resulted from  a  decreased 
stock price underlying the common stock at December 31, 2016 and 2015, and from the greater number 
of warrants outstanding in 2016 compared to 2015. 

Financing Expense 

We incurred approximately $313,000 and $211,000 of financing expenses during the years ended 
December 31, 2016 and 2015, respectively, related to our registered direct offerings in September 2016, 
March 2016, and November 2015.     

Net Loss 

As  a  result  of  the  above,  net  loss  for  the  years  ended  December  31,  2016  and  2015  was 

approximately $9,307,000 and $14,385,000 or $0.04 and $0.08 per share, respectively. 

51 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Comparison of the Years Ended December 31, 2015 and December 31, 2014 

Total Revenues 

We had no revenues for the years ended December 31, 2015 or 2014. 

General and Administrative Expenses 

General  and  administrative  expenses  consist  primarily  of  salaries  and  related  expenses  for 
executive, finance and other administrative personnel, recruitment expenses, professional fees and other 
corporate expenses, including business development, investor relations, and general legal activities. 

General and administrative expenses decreased approximately $138,000, or 2.2%, to $6,115,000 
for  the  year  ended  December  31,  2015  from  $6,253,000  for  the  year  ended  December  31,  2014.    The 
year over year decrease is primarily attributable to a decrease in professional fees.   

Research and Development Expenses 

Research  and  development  expenses  increased  approximately  $5,132,000,  or  73.2%,  to 
$12,148,000 for the year ended December 31, 2015, from $7,016,000 for the year ended December 31, 
2014.    The  increase  is  primarily  attributable  to  the  advancement  of  our  drug  candidates.    During  the 
year ended December 31, 2015, we incurred additional clinical trial and drug manufacturing costs as we 
have advanced our clinical trials for RX-3117, Supinoxin and Archexin.    The increase is also partially 
attributable to an increase in personnel expenses.   

The  table  below  summarizes  the  approximate  amounts  incurred  on  each  of  our  research  and 

development projects for the years ended December 31, 2015 and 2014: 

Clinical Candidates: 

RX-3117 
Supinoxin 
Archexin 

For the Year Ended December 31,   

2015 

2014 

$ 

  4,062,000 $ 
  2,839,000  
  1,547,000   

  1,897,000 
  1,351,000 
  1,215,000 

Preclinical, Personnel and Overhead 

  3,700,226   

  2,552,901 

Total Research and Development Expenses 

$ 

  12,148,226 $ 

  7,015,901 

Interest Income 

Interest  income  decreased  approximately  $31,000  or  22.9%  to  $103,000  for  the  year  ended 
December  31,  2015 from  $134,000 for  the  year  ended  December  31,  2014.    The  decrease is  primarily 
attributable to lower aggregate balances of cash, cash equivalents, and marketable securities for the year 
ended December 31, 2015 compared to the year ended December 31, 2014. 

52 

 
 
 
 
 
 
 
     
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
   
 
 
 
 
Unrealized Gain (Loss) on Fair Value of Warrants 

Our warrants are recorded as liabilities at fair value, and the warrants are valued using a lattice 
model.    Changes in the fair value of warrants are recorded as an unrealized gain or loss in our statement 
of  operations.    During  the  years  ended  December  31,  2015  and  2014,  we  recorded  unrealized  gains 
(losses)  on  the  fair  value  of  our  warrants  of  approximately  $3,987,000  and  $(5,180,000)  respectively.   
Estimating  fair  values  of warrants  requires the  development  of  significant  and subjective  estimates that 
may, and are likely to, change over the duration of the warrant with related changes to external market 
factors. The unrealized gain for the year ended December 31, 2015 primarily resulted from a decreased 
stock  price  underlying  the common  stock  at  December  31,  2015,  while the  unrealized loss  for the  year 
ended December 31, 2014 primarily resulted from an increased price of the underlying common stock at 
December 31, 2014 and on the dates during the year when warrant holders exercised their warrants.   

Financing Expense 

We incurred approximately $211,000 and $206,000 of financing expenses during the years ended 
December 31, 2015 and 2014, respectively, related to our registered direct offerings in November 2015 
and January 2014, respectively.     

Net Loss 

As  a  result  of  the  above,  net  loss  for  the  years  ended  December  31,  2015  and  2014  was 

approximately $14,385,000 and $18,522,000 or $0.08 and $0.11 per share, respectively. 

Research and Development Projects 

Research  and  development  costs  are  expensed  as  incurred.  These  costs  consist  primarily  of 
salaries  and  related  personnel  costs,  costs  to  acquire  pharmaceutical  products  and  product  rights  for 
development  and  amounts  paid  to  contract  research  organizations,  hospitals  and  laboratories  for  the 
provision of services and materials for drug development and clinical trials.  Costs incurred in obtaining 
the license rights to technology in the research and development stage that have no alternative future uses 
are  expensed  as incurred.  Our  research  and  development  programs  are  related to  our  oncology  clinical 
stage  drug  candidates,  RX-3117,  Supinoxin  and  Archexin,  and  our  pre-clinical  stage  drug  candidate, 
RX-21101.  As  we  expand  our  clinical  studies,  we  expect  to  enter  into  additional  development 
agreements.  Significant additional expenditures will be required if we complete our clinical trials, start 
new  trials,  apply  for  regulatory  approvals,  continue  development  of  our  technologies,  expand  our 
operations and bring our products to market.  The eventual total cost of each clinical trial is dependent on 
a number of uncertainties such as trial design, the length of the trial, the number of clinical sites and the 
number of patients.  The process of obtaining and maintaining regulatory approvals for new therapeutic 
products is lengthy, expensive and uncertain.  Because the successful development of our most advanced 
drug candidates, RX-3117, Supinoxin, and Archexin is uncertain, and because RX-21101 is in early-stage 
development, we are unable to estimate the costs of completing our research and development programs, 
the  timing  of  bringing  such  programs  to  market  and,  therefore,  when  material  cash  inflows  could 
commence from the sale of these drug candidates, if any.  If these projects are not completed as planned, 
our results of operations and financial condition would be negatively affected.   

53 

 
 
 
 
 
 
 
 
 
 
 
 
RX-3117   

  RX-3117  is  a  novel,  investigational  oral  small  molecule  nucleoside  compound.    We  believe 
RX-3117  has  therapeutic  potential  in  a  broad  range  of  cancers  including  pancreatic,  bladder,  lung, 
cervical, non-small cell lung cancer and colon cancer.    Additional information about RX-3117, including 
about  the  current  Phase IIa clinical, can  be  found  in  Item  1  of  this  Annual  Report.    We  expect  that 
expenses related to RX-3117 will increase in 2017 compared to 2016 as we continue patient enrollment 
for our pancreatic and advanced bladder cancer clinical trials. 

Supinoxin (RX-5902) 

Supinoxin is  a  potential  first-in-class  small  molecule inhibitor  of  phosphorylated-p68,  a  protein 
that we believe plays a key role in cancer growth, progression and metastasis. Phosphorylated p68 results 
in up-regulation of cancer-related genes and a subsequent proliferation of cancer cells and tumor growth.   
Additional information about Supinoxin, including about the Phase I dose-escalation clinical trial in cancer 
patients  with  solid  tumors  designed  to  evaluate  the  safety,  tolerability,  dose-limiting  toxicities  and 
recommended Phase II dose, can be found in Item 1  of this Annual Report.    We  expect  that  expenses 
related  to  Supinoxin  will  remain  flat  in  2017  compared  to  2016  as  we  initiated  a  Phase  IIa  study  in 
patients with triple negative breast cancer. 

Archexin   

Archexin  is  a  potential  best-in-class,  potent  inhibitor  of  the  protein  kinase  Akt-1,  which  we 
believe  plays  a  critical  role  in  cancer  cell  proliferation,  survival,  angiogenesis,  metastasis  and  drug 
resistance.    Additional  information  about  Archexin,  including  about  the  ongoing  two-stage  Phase  IIa 
proof-of-concept clinical trial of Archexin in patients with metastatic renal cell carcinoma to evaluate its 
safety  and  efficacy, can be found in Item 1 to this Annual Report.    We expect that expenses related to 
Archexin will remain flat in 2017 compared to 2016 as we continue in Stage 2 of the trial. 

Pre-clinical Pipeline 

We expect that expenses related to our pre-clinical pipeline, including RX-21101, will remain flat 

in 2017 compared to 2016 as we continue testing and development.   

Research and Development Process 

We  have  engaged  third-party  contract  research  organizations  and  other  investigators  and 
collaborators, such as universities and medical institutions, to conduct our pre-clinical studies, toxicology 
studies and clinical trials.    Engaging third-party contract research organizations is typical practice in our 
industry. However, relying on such organizations means that the clinical trials and other studies described 
above are being conducted at external locations and that the completion of these trials and studies is not 
within our direct control. Trials and studies may be delayed due to circumstances outside our control, and 
such delays may result in additional expenses for us. 

54 

 
 
 
 
 
 
 
 
 
 
 
Liquidity and Capital Resources   

Cash Flows 

The table below summarizes our net cash flow activity: 

Net Cash Used in Operating Activities 
Net Cash Provided by (Used In) Investing Activities 
Net Cash Provided by Financing Activities 
Net Increase (Decrease) in Cash and Cash Equivalents   

2016 

For the Year Ended December 31, 
2015 
$    (13,227,101) $    (17,351,950) $   (11,041,211) 
  (22,661,045) 
  24,840,470 
  (8,861,786) 

  4,483,911  
  10,122,223  
  1,379,033 $ 

  9,554,394  
  8,170,751  

  373,195 $ 

2014 

$ 

Cash  used in  operating  activities  was  approximately  $13,227,000  for  the  year  ended  December 
31,  2016.    The  operating  cash  flows  during  the  year  ended  December  31,  2016  reflect  our  net  loss  of 
$9,307,000,  an  unrealized  gain  on  the  fair  value  of  warrants  of  $5,530,000  and  a  net  increase  of  cash 
components  of  working  capital  and  non-cash  charges  totaling  $1,610,000.    Cash  used  in  operating 
activities  was  approximately  $17,352,000  for  the  year  ended  December  31,  2015.    The  operating  cash 
flows during the year ended December 31, 2015 reflect our net loss of $14,385,000, an unrealized gain on 
the fair  value  of  warrants of  $3,987,000  and  a net  increase of cash  components  of  working  capital  and 
non-cash charges totaling $1,020,000.    Cash used in operating activities was approximately $11,041,000 
for the year ended December 31, 2014.    The operating cash flows during the year ended December 31, 
2014 reflect our net loss of $18,522,000, which includes an unrealized loss on fair value of warrants of 
$5,180,000 and a net increase of cash components of working capital and other non-cash charges totaling 
$2,301,000.     

Cash provided by investing activities was approximately $4,484,000 for the year ended December 
31,  2016,  which  consisted  of  $13,240,000  from  the  redemption  of  marketable  securities,  offset  by 
$8,747,000  and  $9,000  for  the  purchases  of  marketable  securities  and  equipment,  respectively.  Cash 
provided  by  investing  activities  was  approximately  $9,554,000  for  the  year  ended  December  31,  2015, 
which consisted of $17,525,000 from the redemption of marketable securities, offset by $7,909,000 and 
$62,000 for  the  purchases of  marketable  securities  and  equipment,  respectively.  Cash  used in investing 
activities  was  approximately  $22,661,000  for  the  year  ended  December  31,  2014,  which  consisted  of 
$26,076,000 and $41,000 for the purchases of marketable securities and equipment, respectively, offset 
by  a  decrease  in  restricted  cash  equivalents  of  $196,000  and  $3,260,000  from  the  redemption  of 
marketable securities.     

Cash  provided  by  financing  activities  was  approximately  $10,122,000  for  the  year  ended 
December 31, 2016 which consisted of net proceeds from our registered direct public offerings in March 
2016 and September 2016.    Cash provided by financing activities was approximately $8,171,000 for the 
year ended December 31, 2015, which consisted of net proceeds of $7,440,000 from our registered direct 
public  offering  in  November  2015  and  sales  from  our  at  market  issuance  agreement,  and  proceeds  of 
$709,000  and  $22,000  received  from  the  exercise  of  stock  options  and  stock  warrants,  respectively.   
Cash provided by financing activities was approximately $24,840,000 for the year ended December 31, 
2014,  which  consisted  of  net  proceeds  of  $18,634,000  from  our  registered  direct  public  offering  in 
January 2014, $259,000 from the exercise of stock options and $5,947,000 from the exercise of warrants.   

55 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Financings 

On  January  21,  2014  we  closed  a  registered  direct  public  offering  of  19,047,620  shares  of 
common stock and warrants to purchase up to 4,761,905 shares of common stock.    The common stock 
and warrants were sold in units consisting of one share of common stock and a warrant to purchase 0.25 
shares of common stock, at a price of $1.05 per unit, and the warrants have an exercise price of $1.28 per 
share.    The total gross proceeds of the offering were $20,000,001.    The warrants issued are exercisable 
beginning six months and one day after the closing date until the five-year anniversary of the closing date. 

On  November  12,  2015  we  closed  a  registered  direct  public  offering  of  16,666,667  shares  of 
common stock and warrants to purchase up to 12,500,000 shares of common stock.    The common stock 
and warrants were sold in units consisting of one share of common stock and a warrant to purchase 0.75 
shares of common stock at a price of $0.42 per unit, and the warrants have an exercise price of $0.53 per 
share.    The total gross proceeds of the offering were $7,000,000.    The warrants issued are exercisable 
beginning six months after the closing date until the five-year anniversary of the initial exercise date. 

On March 2, 2016 we closed a registered direct public offering of 15,625,000 shares of common 
stock  and  warrants  to  purchase  up  to  11,718,750  shares  of  common  stock.    The  common  stock  and 
warrants  were  sold  in  units  consisting  of  one  share  of  common  stock  and  a  warrant  to  purchase  0.75 
shares of common stock at a price of $0.32 per unit, and the warrants have an exercise price of $0.42 per 
share.    The  total  gross  proceeds  of  the  offering  were  $5,000,000.    The  warrants  are  exercisable 
beginning six months after the closing date until the five-year anniversary of the initial exercise date. 

On  September  19,  2016  we  closed  a  registered  direct  public  offering  of  24,000,000  shares  of 
common stock and warrants to purchase up to 18,000,000 shares of common stock.    The common stock 
and warrants were sold in units consisting of one share of common stock and a warrant to purchase 0.75 
shares of common stock at a price of $0.25 per unit, and the warrants have an exercise price of $0.30 per 
share.    The  total  gross  proceeds  of  the  offering  were  $6,000,000.    The  warrants  are  exercisable 
beginning six months after the closing date until the five-year anniversary of the initial exercise date. 

We  will  need  to  raise  additional  capital  through  public  or  private  equity  or  debt  offerings  or 
through  arrangements  with  strategic  partners  or  other  sources  in  order  to  continue  to  develop  our  drug 
candidates.    There can be no assurance that additional capital will be available when needed or on terms 
satisfactory to us, if at all.  If we are not able to raise sufficient additional capital, we will have to reduce 
our  research  and  development  activities.   We  will  first  reduce  research  and  development  activities 
associated  with  our  pre-clinical  compounds.  To  the extent  necessary,  we  will  then  reduce  our research 
and development activities related to some or all of our clinical drugs. 

At Market Issuance Sales Agreement 

On  March  16,  2015,  we  entered  into  an  at  market  issuance  sales  agreement  (the  “Sales 
Agreement”)  with MLV  &  Co.  LLC  (“MLV”),  pursuant  to  which  we  may  issue  and  sell  shares  of  our 
common stock having an aggregate offering price of up to $40 million from time to time, at our option, 
through MLV as our sales agent, subject to certain terms and conditions.    Any shares sold will be sold 
pursuant  to  our  effective  shelf  registration  statement  on  Form  S-3  (File  No.  333-196255),  as 
supplemented by a prospectus supplement dated March 16, 2015.    We will pay MLV a commission of 
3.0% of the gross proceeds of the sale of any shares sold through MLV.    There were no sales under the 
Sales Agreement in 2016.    As of December 31, 2016, we have sold 1,407,072 shares of common stock 
pursuant to the Sales Agreement for $1,042,573 in gross proceeds at a weighted average price of $0.7410 
per share.    Net proceeds to us were $1,005,715 after deducting commissions and other transaction costs.   
We are not obligated to make any further sales under the Sales Agreement and no assurance can be given 

56 

 
 
 
 
 
 
 
 
 
that we will sell any further shares under the Sales Agreement, or, if we do, as to the price or amount of 
shares that we will sell, or the dates on which any such sales will take place.    Pursuant to the securities 
purchase  agreement  entered  into  in  connection  with  our  registered  direct  offering,  which  closed  on 
September 19, 2016, we are prohibited from selling any additional shares under the Sales Agreement. 

Contractual Obligations     

The following table summarizes our contractual obligations as of December 31, 2016: 

Operating Leases 

Total 
  677,077 $ 

$ 

Less than 1 
year 
  255,731 $ 

  1 -3 Years 

3-5 Years 

More than 5 
years 

  386,878 $ 

  34,468 $ 

  - 

We also have obligations under various license agreements that become due and payable on the 
achievement of certain development, regulatory, or commercial milestones.    We have not included these 
commitments  on  our  balance  sheet  or  in  the  above  table  of  contractual  obligations  because  the 
achievement and timing of these events is neither fixed nor determinable. 

We  have  contracted  with  various  vendors  for  research  and  development  services,  the  terms  of 
which  require  payments  over  the  term  of  the  agreements,  usually  ranging  from  two  to  36  months.  The 
costs  to  be  incurred  are  estimated  and  are  subject  to  revision.  As  of  December  31,  2016,  the  total 
estimated  cost  to  complete  these  agreements  was  approximately  $4,960,000.    All  of  these  agreements 
may be terminated by either party upon appropriate notice as stipulated in the respective agreements, and 
therefore, are not included in the above table of contractual obligations. 

Current and Future Financing Needs 

We  have  incurred  negative  cash  flow  from  operations  since  we  started  our  business.  We  have 
spent, and expect to continue to spend, substantial amounts in connection with implementing our business 
strategy,  including  our  planned  product  development  efforts,  our  clinical  trials  and  our  research  and 
development  efforts.  We  will  need  to  raise  additional  capital  through  public  or  private  equity  or  debt 
offerings or through arrangements with strategic partners or other sources in order to continue to develop 
our drug candidates.    There can be no assurance that additional capital will be available when needed or 
on terms satisfactory to us, if at all.    If we are not able to raise sufficient additional capital, we will have 
to reduce our research and development activities. We believe our cash, cash equivalents, and marketable 
securities will be sufficient to cover our cash flow requirements for our current activities for at least the 
next 12 months from the date our financial statements are issued. 

The actual amount of funds we will need to operate is subject to many factors, some of which are 

beyond our control.    These factors include the following: 

• 

• 

• 

the progress of our product development activities; 

the number and scope of our product development programs; 

the progress of our pre-clinical and clinical trial activities; 

57 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
• 

the  progress  of  the  development  efforts  of  parties  with  whom  we  have  entered  into 
collaboration agreements; 

•  our ability to maintain current collaboration programs and to establish new collaboration 

arrangements; 

• 

• 

the  costs  involved  in  prosecuting  and  enforcing  patent  claims  and  other  intellectual 
property rights; and 

the costs and timing of regulatory approvals. 

Off-Balance Sheet Arrangements 

We do not have any off-balance sheet arrangements or holdings in variable interest entities.  

58 

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

For the year ended December 31, 2016, we are exposed to the following market risks: 

Interest Rate Risk 

We invest our cash in a variety of financial instruments.    At December 31, 2016, our cash and 
cash  equivalents  was  invested  primarily  in  short  term  bank  deposits  and  municipal  obligations,  all  of 
which  were  denominated  in  U.S.  dollars.    Due  to  the  conservative  nature  of  these  investments,  which 
primarily bear interest at fixed rates, we do not believe we have material exposure to interest rate risk.     

Foreign Currency Risk 

We are exposed to risks associated with foreign currency transactions on contracts with vendors 
associated outside of the United States.    Accordingly changes in the value of the U.S. dollar, relative to 
other currencies, may have an impact on our financial statements and earnings.    The number and dollar 
amount of contracts denominated in foreign currency is immaterial; therefore, we believe we do not have 
material exposure to foreign currency risk.           

Item 8.    Financial Statements and Supplementary Data. 

Our financial statements and the Report of the Independent Registered Public Accounting Firm 
thereon filed pursuant to this Item 8 and are included in this Annual Report on Form 10-K beginning on 
page F-1. 

59 

 
 
 
 
 
 
 
 
 
 
 
 
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.  Under  the  supervision  and  with  the 
participation of our management, including our Chief Executive Officer and Chief Financial Officer, we 
evaluated  the  effectiveness  of  the  design  and  operation  of  our  disclosure  controls  and  procedures  (as 
defined in Rule 13a-15(e) and 15d-15(e) under the Exchange Act) as of the end of the period covered by this 
report. Based upon that evaluation, our Chief Executive Officer and Chief Financial Officer concluded that 
our disclosure controls and procedures as of the end of the period covered by this report were effective such 
that the information required to be disclosed by us in reports filed under the Exchange Act is (i) recorded, 
processed, summarized and reported within the time periods specified in the SEC’s rules and forms and 
(ii) accumulated and communicated to our management, including our Chief Executive Officer and Chief 
Financial Officer, as appropriate to allow timely decisions regarding disclosure. A controls system cannot 
provide absolute assurance, however, that the objectives of the controls system are met, and no evaluation 
of controls can provide absolute assurance that all control issues and instances of fraud, if any, within a 
company have been detected. 

Changes  in  Internal  Control  Over  Financial  Reporting.    During  the  most  recent  quarter  ended 
December 31, 2016, there has been no change in our internal control over financial reporting (as defined in 
Rule 13a-15(f) and 15d-15(f) under the Exchange Act)    that has materially affected, or is reasonably likely 
to materially affect, our internal control over financial reporting. 

60 

 
 
 
 
 
 
 
 
 
 
MANAGEMENT’S REPORT ON INTERNAL CONTROL OVER FINANCIAL REPORTING 

Our  management  is  responsible  for  establishing  and  maintaining  adequate  internal  control  over 
financial  reporting  (as  defined  in  Rule 13a-15(f)  under  the  Exchange  Act).    Our  internal  control  over 
financial  reporting  is  a  process  designed  to  provide  reasonable  assurance  regarding  the  reliability  of 
financial  reporting  and the  preparation of  financial statements  for  external purposes  in  accordance  with 
generally accepted accounting principles and includes those policies and procedures that:     

• 

• 

• 

Pertain to the maintenance of records that, in reasonable detail, accurately and fairly 
reflect the transactions and the dispositions of our assets; 

Provide reasonable assurance that transactions are recorded as necessary to permit 
preparation  of  financial  statements  in  accordance  with  generally  accepted 
accounting principles, and that our receipts and expenditures are being made only in 
accordance with authorization of our management and the board of directors; and 

Provide  reasonable  assurance  regarding  prevention  or  timely  detection  of 
unauthorized acquisition, use, or disposition of our assets that could have a material 
effect on the financial statements.     

Because of its inherent limitations, internal control over financial reporting may not prevent or detect 
misstatements.    Also, projections of any evaluations of effectiveness to future periods are subject to risk 
that controls may become inadequate because of changes in conditions or because of declines in the degree 
of compliance with the policies or procedures.     

Our management, with the participation of the Chief Executive Officer and Chief Financial Officer, 
assessed the effectiveness of our internal control over financial reporting as of December 31, 2016.    In 
making  this  assessment,  our  management  used  the  criteria  set  forth  by  the  Committee  of  Sponsoring 
Organizations of the Treadway Commission in the Internal Control-Integrated Framework (2013). 

Based on this evaluation, our management, with the participation of the Chief Executive Officer and 
Chief  Financial  Officer,  concluded  that,  as  of  December  31,  2016,  our  internal  control  over  financial 
reporting was effective.     

Management’s  assessment  of  the  effectiveness  of  the  Company’s  internal  control  over  financial 
reporting  has  been  audited  by  Baker  Tilly  Virchow  Krause,  LLP,  an  independent  registered  public 
accounting firm.    Baker Tilly Virchow Krause, LLP has issued an attestation report on the effectiveness of 
the Company’s internal control over financial reporting, which appears herein.

61 

 
 
 
 
 
 
 
 
 
 
 
Report of Independent Registered Public Accounting Firm 

Board of Directors and Stockholders 
Rexahn Pharmaceuticals, Inc.   

We have audited Rexahn Pharmaceuticals, Inc.’s internal control over financial reporting as of December 
31,  2016,  based  on  criteria  established  in  Internal  Control—Integrated  Framework  (2013  framework) 
issued  by  the  Committee  of  Sponsoring  Organizations  of  the  Treadway  Commission  (COSO).  Rexahn 
Pharmaceuticals, Inc.’s management is responsible for maintaining effective internal control over financial 
reporting, and for its assessment of the effectiveness of internal control over financial reporting, included in 
the accompanying Management’s Report on Internal Control over Financial Reporting. Our responsibility 
is to express an opinion on the entity’s internal control over financial reporting based on our audit. 

We conducted our audit 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 effective internal control over financial reporting was maintained in all material 
respects. Our audit of internal control over financial reporting included obtaining an understanding of 
internal control over financial reporting, assessing the risk that a material weakness exists, and testing and 
evaluating the design and operating effectiveness of internal control based on the assessed risk. Our audit 
also included performing such other procedures as we considered necessary in the circumstances. We 
believe that our audit provides a reasonable basis for our opinion. 

An entity’s internal control over financial reporting is a process designed 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. An 
entity’s internal control over financial reporting includes those policies and procedures that (1) pertain to 
the maintenance of records that, in reasonable detail, accurately and fairly reflect the transactions and 
dispositions of the assets of the entity; (2) provide reasonable assurance that transactions are recorded as 
necessary to permit preparation of financial statements in accordance with generally accepted accounting 
principles, and that receipts and expenditures of the entity are being made only in accordance with 
authorizations of management and directors of the entity; and (3) provide reasonable assurance regarding 
prevention or timely detection of unauthorized acquisition, use, or disposition of the entity’s assets that 
could have a material effect on the financial statements. 

Because of its inherent limitations, internal control over financial reporting may not prevent or detect 
misstatements. Also, projections of any evaluation of effectiveness to future periods are subject to the risk 
that controls may become inadequate because of changes in conditions, or that the degree of compliance 
with the policies or procedures may deteriorate. 

In our opinion, Rexahn Pharmaceuticals, Inc. maintained, in all material respects, effective internal control 
over  financial  reporting  as  of  December 31,  2016,  based  on  criteria  established  in  Internal 
Control—Integrated Framework (2013 framework) issued by the Committee of Sponsoring Organizations 
of the Treadway Commission (COSO). 

62 

 
 
 
 
 
 
 
 
 
 
 
 
   
We  have  also  audited,  in  accordance  with  the  standards  of  the  Public  Company  Accounting  Oversight 
Board  (United  States),  the  balance  sheet  and  the  related  statements  of  operations,  comprehensive  loss, 
stockholders’ equity, and cash flows of Rexahn Pharmaceuticals, Inc., and our report dated February 24, 
2017 expressed an unqualified opinion. 

/s/ Baker Tilly Virchow Krause, LLP 

Wyomissing, Pennsylvania 
February 24, 2017

63 

 
 
 
Item 9B.    Other Information. 

None. 

64 

 
 
 
 
 
 
 
 
Item 10.    Directors, Executive Officers and Corporate Governance. 

PART III 

The information required by this Item is set forth in our 2017 Proxy Statement to be filed with the 

SEC within 120 days of December 31, 2016 and is incorporated into this Annual Report by reference. 

Item 11.    Executive Compensation. 

The information required by this Item is set forth in our 2017 Proxy Statement to be filed with the 

SEC within 120 days of December 31, 2016 and is incorporated into this Annual Report by reference. 

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

The information required by this Item is set forth in our 2017 Proxy Statement to be filed with the 

SEC within 120 days of December 31, 2016 and is incorporated into this Annual Report by reference. 

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

The information required by this Item is set forth in our 2017 Proxy Statement to be filed with the 

SEC within 120 days of December 31, 2016 and is incorporated into this Annual Report by reference. 

Item 14.    Principal Accounting Fees and Services. 

The information required by this Item is set forth in our 2017 Proxy Statement to be filed with the 

SEC within 120 days of December 31, 2016 and is incorporated into this Annual Report by reference. 

65 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Item 15.    Exhibits, Financial Statement Schedules. 

(a)  The following documents are filed as a part of this Annual Report: 

(1)  The following documents are filed as a part of this Annual Report: 

 Report of Baker Tilly Virchow Krause, LLP 

 Balance Sheet as of December 31, 2016 and December 31, 2015 

 Statement of Operations for the year ended December 31, 2016, 2015 and 2014 

Statement of Comprehensive Loss for the year ended December 31, 2016, 2015 and                 
2014 

F-1 

F-2 

F-3 

F-4 

 Statement of Stockholders’ Equity for the year ended December 31, 2016, 2015 and 2014 

F-5 

 Statement of Cash Flows for the year ended December 31, 2016, 2015 and 2014 

 Notes to the Financial Statements 

F-6 

F-7 

(2) All financial statement schedules have been omitted because they are not applicable or not 
required or because the information is included elsewhere in the financial statements or the 
Notes thereto. 

(3) See the accompanying Index to Exhibits filed as a part of this Annual Report, which list is 

incorporated by reference in this Item. 

(b) See the accompanying Index to Exhibits filed as a part of this Annual Report. 

(c)  Other schedules are not applicable. 

66 

 
 
 
 
  
 
 
 
 
  
 
  
 
 
 
  
 
 
 
 
 
  
 
 
 
 
 
 
 
 
 
 
 
 
  
 
 
 
 
 
  
 
 
 
 
 
  
 
 
 
  
  
   
 
  
 
 
 
  
 
  
 
 
 
 
 
 
 
SIGNATURES 

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

REXAHN PHARMACEUTICALS, INC. 

By:    /s/ Peter D. Suzdak 
Peter D. Suzdak 
Chief Executive Officer 

Pursuant to the requirements of the Securities Exchange Act of 1934, this report has been signed below by 
the following persons on behalf of the registrant and in the capacities and on the dates indicated: 

Name 

Title 

Date 

/s/ Peter D. Suzdak* 
Peter Suzdak 

/s/ Tae Heum Jeong* 
Tae Heum Jeong 

/s/ Peter Brandt* 
Peter Brandt 

/s/ Chang H. Ahn* 
Chang H. Ahn 

/s/ Charles Beever* 
Charles Beever 

/s/ Kwang Soo Cheong*  
Kwang Soo Cheong 

/s/ Mark Carthy* 
Mark Carthy 

/s/ Richard J. Rodgers*   
Richard J. Rodgers 

Chief Executive Officer and 
Director (Principal Executive 
Officer) 

Chief Financial Officer, and 
Secretary (Principal Financial and 
Accounting Officer) 

February 24, 2017 

February 24, 2017 

Chairman 

February 24, 2017 

Director 

Director 

Director 

Director 

Director 

February 24, 2017 

February 24, 2017 

February 24, 2017 

February 24, 2017 

February 24, 2017 

* By: /s/ Tae Heum Jeong, Attorney-in Fact 

Tae Heum Jeong, Attorney-in-Fact** 

** By authority of the power of attorney filed as Exhibit 24 hereto

67 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Report of Independent Registered Public Accounting Firm 

Board of Directors and Stockholders 
Rexahn Pharmaceuticals, Inc. 

We have audited the accompanying balance sheet of Rexahn Pharmaceuticals, Inc. as of December 31, 2016 
and 2015, and the related statements of operations, comprehensive loss, stockholders’ equity, and cash flows 
for each of the years in the three-year period ended December 31, 2016. These financial statements are the 
responsibility of the entity’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. An audit includes 
examining, on a test basis, evidence supporting the amounts and disclosures in the financial statements. An 
audit also includes assessing the accounting principles used and significant estimates made by management, 
as well as 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 financial 
position of Rexahn Pharmaceuticals, Inc. as of December 31, 2016 and 2015, and the results of its operations 
and its cash flows for each of the years in the three-year period ended December 31, 2016, in conformity with 
accounting principles generally accepted in the United States of America.   

We also have audited, in accordance with the standards of the Public Company Accounting Oversight Board 
(United States), Rexahn Pharmaceuticals, Inc.’s internal control over financial reporting as of December 31, 
2016, based on criteria established in Internal Control—Integrated Framework (2013 framework) issued by 
the Committee of Sponsoring Organizations of the Treadway Commission (COSO), and our report dated 
February 24, 2017 expressed an unqualified opinion. 

/s/ Baker Tilly Virchow Krause, LLP 

Wyomissing, Pennsylvania 
February 24, 2017 

F-1 

 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Balance Sheet 

Current Assets: 

Cash and cash equivalents 
Marketable securities 
Prepaid expenses and other current assets 

Total Current Assets 
Security Deposits 
Equipment, Net 
Total Assets 

Current Liabilities: 

December 31, 2016 

December 31, 2015 

ASSETS 

$ 

$ 

  11,578,473   $ 
  8,737,107  
  608,517 
  20,924,097 
  30,785  
  88,650  
  21,043,532  $ 

  10,199,440 
  13,240,086 
  1,221,818 
  24,661,344 
  30,785 
  112,900 
  24,805,029 

LIABILITIES AND STOCKHOLDERS’ EQUITY 

Accounts payable and accrued expenses 

$ 

  1,882,500  $ 

  2,661,298 

Deferred Research and Development Arrangement 

  450,000  

  525,000 

Other Liabilities 

Warrant Liabilities 

Total Liabilities   
Commitments and Contingencies (note 15) 
Stockholders’ Equity: 

  79,204  

  104,020 

  1,573,366  

  2,739,163 

  3,985,070 

  6,029,481 

Preferred stock, par value $0.0001, 100,000,000 authorized         
      shares, none issued and outstanding 
Common stock, par value $0.0001, 500,000,000 authorized 
shares, 237,368,785 and 197,413,785 issued and 
outstanding 
Additional paid-in capital 
Accumulated other comprehensive loss 
Accumulated deficit 

- 

-

  23,737 
  132,065,056  
  (6,122) 
  (115,024,209) 

  19,741 
  124,490,712 
  (18,041)
  (105,716,864)

Total Stockholders’ Equity 

  17,058,462 

  18,775,548 

Total Liabilities and Stockholders’ Equity   

$ 

  21,043,532  $ 

  24,805,029 

(See accompanying notes to the financial statements) 
F-2 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
   
 
   
 
 
 
 
 
 
   
   
 
 
  
 
 
 
   
 
   
 
 
 
   
 
   
 
 
 
   
 
   
 
 
   
 
   
   
 
   
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Statement of Operations 

For the Year Ended December 31,   
2015 

2014 

2016 

Revenues: 

Expenses: 

$ 

  -  $ 

  -  $ 

  - 

General and administrative 

Research and development 

  6,324,236 

  6,115,210   

  10,089,149 

  12,148,226   

  6,253,328 

  7,015,901 

Total Expenses 

  16,413,385 

  18,263,436   

  13,269,229 

Loss from Operations 

  (16,413,385) 

  (18,263,436)   

  (13,269,229) 

Other Income (Expense) 
Interest income 

Mediation settlement 

Unrealized gain (loss) on fair value of warrants 

Financing expense 

Total Other Income (Expense) 

  118,565 

  1,770,658 

  5,529,907 

  (313,090) 

  7,106,040 

  103,269   

  133,907 

  -   

  - 

  3,986,727   

  (5,180,107) 

  (211,116)   
  3,878,880   

  (206,172) 

  (5,252,372) 

Net Loss Before Provision for Income Taxes 

  (9,307,345) 

Provision for income taxes 

Net Loss 

Net loss per share, basic and diluted 

$ 

$ 

  - 

  (9,307,345)  $ 

  (14,384,556)   
  -   
  (14,384,556) $ 

  (18,521,601) 

  - 

  (18,521,601) 

  (0.04)  $ 

  (0.08) $ 

  (0.11) 

Weighted average number of shares outstanding, basic 
and diluted 

  217,447,405 

  182,388,226   

  176,106,981 

(See accompanying notes to the financial statements) 
F-3 

 
 
 
 
 
 
 
 
 
 
 
 
  
   
  
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
   
 
   
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Statement of Comprehensive Loss 

For the Year Ended December 31,   

2016 

2015 

2014 

Net Loss 

$ 

  (9,307,345)$ 

  (14,384,556) $ 

  (18,521,601) 

Unrealized gain (loss) on available-for-sale securities   

  11,919  

  15,606  

  (33,647) 

Comprehensive Loss 

$ 

  (9,295,426)$ 

  (14,368,950) $ 

  (18,555,248) 

(See accompanying notes to the financial statements) 
F-4 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Statement of Stockholders’ Equity 
For the Year Ended December 31, 2016, 2015 and 2014 

Common Stock 

Treasury Stock 

Number of 
Shares 

  Amount 

Additional 
Paid-in 
Capital 

Accumulated 
Deficit 

Number 
of Shares    Amount   

Accumulated 
Other 
Comprehensive 
Loss 

Total 
Stockholders' 
Equity 

146,732,000  $ 

  14,673 $    85,449,932 $    (72,810,707) 

  14,205 $    (28,410)$ 

  -$ 

  12,625,488 

  19,047,620   
  -  

  1,905  
  - 

  16,306,667  
  (1,159,582) 

  400,000   
  448,693   

  40  
  45  

  408,960  
  358,910  

  -  

  - 

  - 

  11,738,220   

  1,174  

  16,083,337  

  - 
  - 

  - 
  - 

  - 

  - 

  -  
  -  

  -  

  - 
  - 

  - 

  608,795  
  - 

  - 
  (18,521,601) 

  - 

  - 

  - 
  - 

  - 
  - 

  -  - 
  - 

  - 
  - 

  99,010  

(100,000) 

  - 

  - 
  - 

  - 

  - 

  - 
  - 

  - 

  - 
  - 

  - 
  - 

  - 

  - 

  - 
  - 

  16,308,572 
  (1,159,582)

  409,000 
  358,955 

  (100,000)

  16,084,511 

  608,795 
  (18,521,601)

  (33,647) 

  (33,647)

178,366,533  $ 

  17,837 $  118,057,019 $    (91,332,308) 

  113,215 $  (128,410)$ 

  (33,647)$ 

  26,580,491 

  18,073,739   
  -  

  1,807  
  - 

  5,248,266  
  (566,065) 

  150,000   
  889,428   

  47,300   

  15  
  89  

  4  

  101,985  
  708,528  

  31,699  

  -  

  - 

  1,037,679  

  - 
  - 

  - 
  - 

  - 

  - 

  - 
  - 

  - 
  - 

  - 

  - 

  - 
  - 

  - 
  - 

  - 

  - 

  (113,215)  
  -  

  (11) 
  - 

  (128,399) 
  - 

  (14,384,556) 

  (113,215) 
  - 

  128,410  
  - 

  - 
  - 

  - 
  - 

  - 

  - 

  - 
  - 

  5,250,073 
  (566,065)

  102,000 
  708,617 

  31,703 

  1,037,679 

  -
  (14,384,556)

  -  

  - 

  - 

  - 

197,413,785  $ 

  19,741 $  124,490,712 $  (105,716,864) 

  39,625,000   
  -  

  3,963  
  - 

  6,904,995  
  (837,755) 

  330,000   

  33  

  97,616  

  - 
  - 

  - 

  -  
  -  

  -  

  - 
  - 

  - 

  1,409,488  
  - 

  - 
  (9,307,345) 

  - 

  - 

  - 

  -$ 

  - 
  - 

  - 

  - 
  - 

  - 

  - 

  15,606  

  15,606 

  -$ 

  (18,041)$ 

  18,775,548 

  - 
  - 

  - 

  - 
  - 

  - 

  - 
  - 

  - 

  - 
  - 

  6,908,958 
  (837,755)

  97,649 

  1,409,488 
  (9,307,345)

  11,919  

  11,919 

237,368,785  $ 

  23,737 $  132,065,056 $  (115,024,209) 

  -$ 

  -$ 

  (6,122)$ 

  17,058,462 

Balances at   
January 1, 2014 

Issuance of common 
stock and units 

Stock issuance costs 

Common stock issued 
in exchange for services 
Stock options exercised  
Shares surrendered for 
net stock option 
exercise 
Stock warrants 
exercised 
Stock-based 
compensation 
Net loss 
Other comprehensive 
loss 
Balances at   
December 31, 2014 

Issuance of common 
stock and units 
Stock issuance costs 

Common stock issued 
in exchange for services 
Stock options exercised  
Stock warrants 
exercised 
Stock-based 
compensation 
Retirement of treasury 
stock 

Net loss 
Other comprehensive 
income 

Balances at   
December 31, 2015 

Issuance of common 
stock and units 
Stock issuance costs 

Common stock issued 
in exchange for services 

Stock-based 
compensation 

Net loss 

Other comprehensive 
income 

Balances at   
December 31, 2016 

(See accompanying notes to the financial statements) 
F-5 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Statement of Cash Flows 

Cash Flows from Operating Activities: 
Net loss 

Adjustments to reconcile net loss to net cash used in operating 
activities: 
Compensatory stock 

Depreciation and amortization 
Amortization of premiums and discounts on marketable 
securities, net 
Stock-based compensation 
Amortization of deferred research and development arrangements

Unrealized (gain) loss on fair value of warrants 
Financing expense 

Amortization of deferred lease incentive 
Deferred lease expenses 

Changes in assets and liabilities: 

Prepaid expenses and other assets 

Accounts payable and accrued expenses 

Net Cash Used in Operating Activities 

Cash Flows from Investing Activities: 

Restricted cash equivalents 

Purchase of equipment 
Purchase of marketable securities 

Redemption of marketable securities 

Net Cash Provided by (Used in) Investing Activities 

Cash Flows from Financing Activities: 

Issuance of common stock and units, net of issuance costs 

  10,122,223  

Proceeds from exercise of stock options 
Proceeds from exercise of stock warrants 

Net Cash Provided by Financing Activities 
Net Increase (Decrease) in Cash and Cash Equivalents 

Cash and Cash Equivalents – beginning of period 
Cash and Cash Equivalents - end of period 

Supplemental Cash Flow Information 

Non-cash financing and investing activities: 

Warrants issued 

Warrant liability extinguishment from exercise of warrants 

Shares withheld for net stock option exercise 

Retirement of treasury stock 

$ 

$ 

$ 

$ 

$ 

(See accompanying notes to the financial statements) 
F-6 

For the Year Ended December 31, 

2016 

2015 

2014 

$ 

  (9,307,345)$ 

  (14,384,556) 

  (18,521,601)

  97,649  

  32,916  

  22,321  

  1,409,488  
  (75,000) 

  (5,529,907) 
  313,090  

  (12,443) 
  (12,373) 

  102,000  
  27,498  

  409,000 

  28,325 

  30,875  

  10,228 

  1,037,679  
  (75,000) 
  (3,986,727) 
  211,116  
  (12,443) 
  (8,492) 

  608,795 
  (233,630)

  5,180,107 
  206,172 

  (12,443)
  7,834 

  613,301 

  (778,798) 
  (13,227,101) 

  (495,935) 
  202,035  
  (17,351,950) 

  (249,503)

  1,525,505 
  (11,041,211)

  - 

  (8,666) 
  (8,747,423) 

  13,240,000  
  4,483,911  

  - 
  - 

  10,122,223  
  1,379,033  

  10,199,440  
  11,578,473 $ 

  - 
  (62,302) 
  (7,908,304) 
  17,525,000  
  9,554,394  

  7,439,809  
  708,617  
  22,325  
  8,170,751  
  373,195  
  9,826,245  
  10,199,440  

  196,130 

  (41,249)
  (26,075,926)

  3,260,000 
  (22,661,045)

  18,634,247 

  258,955 
  5,947,268 

  24,840,470 
  (8,861,786)

  18,688,031 
  9,826,245 

  4,364,110 $ 

  2,966,917  

  3,691,429 

  -$ 

  -$ 

  -$ 

  9,378  

  10,137,243 

  - 

  100,000 

  128,410  

  -

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

1.  Operations and Organization 

Operations 

Rexahn  Pharmaceuticals,  Inc.  (the  “Company,”),  a  Delaware  corporation,  is  a  biopharmaceutical 
company  whose  principal  operations  are  the  discovery,  development  and  commercialization  of 
innovative  treatments  for  cancer.    The  Company  had  an  accumulated  deficit  of  $115,024,209  at 
December  31,  2016  and  anticipates  incurring  losses  through  fiscal  year  2017  and  beyond.    The 
Company  has  not  yet  generated  commercial  revenues  and  has  funded  its  operating  losses  to  date 
through the sale of shares of its common stock and warrants to purchase shares of its common stock, 
convertible debt, financings, interest income from cash, cash equivalents and marketable securities, 
and  proceeds  from  reimbursed  research  and  development  costs.    The  Company  believes  that  its 
cash,  cash  equivalents,  and  marketable  securities,  will  be  sufficient  to  cover  its  cash  flow 
requirements for its current activities at least for the next 12 months from the date these financial 
statements  were  issued.    Management  believes  it  has  the  capability  of  managing  the  Company’s 
operations within existing cash available by focusing on select research and development activities, 
selecting projects in conjunction with potential financings and milestones, and efficiently managing 
its general and administrative affairs. 

2. Summary of Significant Accounting Policies 

a) Cash and Cash Equivalents 

Cash  and  cash  equivalents  include  cash  on  hand  and  short-term  investments  purchased  with 
remaining maturities of three months or less at acquisition. 

b) Marketable Securities 

Marketable securities are considered “available-for-sale” in accordance with Financial Statement 
Accounting Board (“FASB”) Accounting Standards Codification (“ASC”) 320, “Debt and Equity 
Securities”, and thus are reported at fair value in the Company’s accompanying balance sheet, with 
unrealized  gains  and  losses  excluded  from  earnings  and  reported  as  a  separate  component  of 
stockholders’  equity.    Amounts  reclassified  out  of  accumulated  other  comprehensive  loss  into 
realized gains and losses are accounted for on the basis of specific identification and are included in 
other income or expense in the statement of operations.    The Company classifies such investments 
as current on the balance sheet as the investments are readily marketable and available for use in the 
Company’s current operations.     

c) Equipment 

Equipment is stated at cost less accumulated depreciation. Depreciation, based on the lesser of the 
term of the lease or the estimated useful life of the assets, is provided as follows: 

Life  Depreciation Method 

Furniture and fixtures 
Office equipment 
Lab equipment 
Computer equipment 
Leasehold improvements 

7 years  straight line 
5 years  straight line 
5-7 years  straight line 
3-5 years  straight line 
3-5 years  straight line 

F-7 

 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

d) Research and Development   

Research and development costs are expensed as incurred.    Research and development expenses 
consist primarily of third party service costs under research and development agreements, salaries 
and related personnel costs, including stock-based compensation, costs to acquire pharmaceutical 
products and product rights for development and amounts paid to contract research organizations, 
hospitals and  laboratories for the  provision  of  services  and  materials for  drug  development  and 
clinical trials. 

Costs incurred in obtaining the licensing rights to technology in the research and development stage 
that have no alternative future uses and are for unapproved product compounds are expensed as 
incurred. 

e) Use of Estimates 

The  preparation  of  financial  statements  in  conformity  with  accounting  principles  generally 
accepted in the United States requires management to make estimates and assumptions that affect 
the reported amounts of assets and liabilities and the disclosure of contingent assets and liabilities 
at the date of the financial statements and the reported amounts of revenues and expenses during the 
reporting period.    These estimates are based on management’s best knowledge of current events 
and actions the Company may undertake in the future.    Actual results may ultimately differ from 
these estimates.    These estimates are reviewed periodically and as adjustments become necessary, 
they are reported in earnings in the period in which they become available. 

f) Fair Value of Financial Instruments 

The  carrying  amounts  reported  in  the  accompanying  financial  statements  for  cash  and  cash 
equivalents,  prepaid  expenses  and  other  assets,  and  accounts  payable  and  accrued  expenses 
approximate fair value because of the short-term maturity of these financial instruments.    The fair 
value  of  warrant  liabilities  is  discussed  in  Note  12,  the  fair  value  of  marketable  securities  and 
certain other assets and liabilities is discussed in Note 16.   

F-8 

 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

g) Income Taxes 

The Company accounts for income taxes in accordance with ASC 740, “Income Taxes”.    Deferred 
tax assets and liabilities are recorded for differences between the financial statement and tax basis 
of the assets and liabilities that will result in taxable or deductible amounts in the future based on 
enacted tax laws and rates.    ASC 740 requires that a valuation allowance be established when it is 
more likely than not that all portions of a deferred tax asset will not be realized.    A review of all 
positive  and  negative  evidence  needs  to  be considered,  including  a  company’s current  and  past 
performance,  the  market  environment  in  which  the  company  operates,  length  of  carryback  and 
carryforward periods and existing contracts that will result in future profits.    Income tax expense is 
recorded for the amount of income tax payable or refundable for the period, increased or decreased 
by the change in deferred tax assets and liabilities during the period. 

As a result of the Company’s significant cumulative losses, the Company determined that it was 
appropriate to establish a valuation allowance for the full amount of deferred tax assets. 

The calculation of the Company’s tax liabilities involves the inherent uncertainty associated with 
the application of complex tax laws.    The Company is subject to examination by various taxing 
authorities.    The Company believes that, as a result of its loss carryforward sustained to date, any 
examination would result in a reduction of its net operating losses rather than a tax liability.    As 
such, the Company has not provided for any additional taxes that would be estimated under ASC 
740. 

h) Stock-Based Compensation 

In accordance with ASC 718, “Stock Compensation,” compensation costs related to share-based 
payment  transactions,  including  employee  stock  options,  are  to  be  recognized  in  the  financial 
statements.  In  addition,  the  Company  adheres  to  the  guidance  set  forth  within  Securities  and 
Exchange Commission (“SEC”) Staff Accounting Bulletin (“SAB”) No. 107, which provides the 
Staff’s views regarding the interaction between ASC 718 and certain SEC rules and regulations, 
and  provides  interpretations  with  respect  to  the  valuation  of  share-based  payments  for  public 
companies.   

i) Concentration of Credit Risk 

ASC 825, “Financial Instruments,” requires disclosure of any significant off balance sheet risk and 
credit risk concentration.    The Company does not have significant off-balance sheet risk or credit 
concentration.    The  Company  maintains  cash  and  cash  equivalents  with  major  financial 
institutions.    From time to time the Company has funds on deposit with commercial banks that 
exceed  federally  insured  limits.    The  balances  are  insured  by  the  Federal  Deposit  Insurance 
Corporation up to $250,000. At December 31, 2016, the Company’s uninsured cash balance was 
$11,078,473. Management does not consider this to be a significant credit risk as the banks are 
large, established financial institutions. 

j) Reclassification 

Certain amounts in the prior year’s financial statements have been reclassified to conform to the 
current year presentation with no material effect on the financial statements.   

F-9 

 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

k) Recent Accounting Pronouncements Affecting the Company 

Revenue from Contracts with Customers 

In May 2014, the FASB issued Accounting Standards Update (“ASU”) 2014-09, “Revenue from 
Contracts  with  Customers,”  a  comprehensive  new  revenue  recognition  standard  that  will 
supersede  nearly  all  existing  revenue  recognition  guidance  under  U.S.  GAAP.  The  standard’s 
core principle is that a company should recognize revenue when it transfers 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 and services, and provides a revenue recognition framework 
in accordance with this principle.    On August 12, 2015, the FASB issued ASU 2015-14, which 
defers the effective date of ASU 2014-09 by one year to December 15, 2017 for annual reporting 
periods beginning after that date and interim periods therein.    Early adoption of the standard is 
permitted,  but  not  before  the  original  effective  date  of  December  15,  2016.    The  Company  is 
currently  evaluating  the  impact  that  the  adoption  of  this  guidance  will  have  on  its  financial 
statements and future operating results. 

Disclosure of Uncertainties about an Entity’s Ability to Continue as a Going Concern 

In August 2014, the FASB issued ASU 2014-15, “Disclosure of Uncertainties about an Entity’s 
Ability  to  Continue  as  a  Going  Concern,”  which  requires  management  to  perform  interim  and 
annual assessments as to the entity’s ability to continue as a going concern and provides related 
disclosure guidance.    ASU 2014-15 is effective for reporting periods ending after December 15, 
2016,  with  early  adoption  permitted.  The  Company  adopted  this  pronouncement  for  the  year 
ended December 31, 2016.    This pronouncement did not have a material impact on its financial 
statements. 

Leases 

In  February  2016,  the  FASB  issued  ASU  2016-02,  “Leases,”  which  requires  an  entity  to 
recognize assets and liabilities arising from leases on the balance sheet and to provide additional 
disclosures  about  leasing  arrangements.    ASU  2016-02  will  be  effective  for  reporting  periods 
beginning  after  December  15,  2018,  with  early  adoption  permitted.  The  Company  is  currently 
evaluating the impact the adoption of this guidance will have on its financial statements. 

Compensation-Stock Compensation 

In  March  2016,  the  FASB  issued  ASU  2016-09,  “Compensation-Stock  Compensation: 
Improvements  to  Employee  Share  Based  Payment  Accounting,”  which  includes  multiple 
provisions  intended  to  simplify  various  aspects  of  accounting  for  share-based  payments.    The 
guidance  is  effective  for  reporting  periods  beginning  after  December  15,  2016,  with  early 
adoption  permitted.    The  Company  is  currently  evaluating  the  impact  the  adoption  of  this 
guidance will have on its financial statements. 

F-10 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

3.    Marketable Securities 

The following table shows the Company’s marketable securities’ adjusted cost, gross unrealized gains 
and losses, and fair value by significant investment category as of December 31, 2016 and 2015:   

Certificates of Deposit 
Commercial Paper 
Corporate Bonds 
Total Marketable Securities 

December 31, 2016 

Gross   
Unrealized
Gains 

Gross   
Unrealized 
Losses 

  197 $
  - 
  - 
  197 $

  -$ 

  (1,684) 
  (4,635) 
  (6,319)$ 

Fair 
Value 
  720,197 
  3,985,740 
  4,031,170 
  8,737,107 

$

Cost   
Basis 
  720,000 $
  3,987,424  
  4,035,805  
$   8,743,229 $

December 31, 2015 

Certificates of Deposit 
Commercial Paper 
Corporate Bonds 
Total Marketable Securities 

Cost   
Basis 
$   6,240,000 $
  2,981,307  
  4,036,820  
$   13,258,127 $

Gross   
Unrealized
Gains 

  571 $
  - 
  - 
  571 $

Gross   
Unrealized 
Losses 

Fair 
Value 
  6,234,996 
  2,977,570 
  4,027,520 
  (18,612)$    13,240,086 

  (5,575)$ 
  (3,737) 
  (9,300) 

The  Company  typically  invests  in  highly-rated  securities,  with  the  primary  objective  of  minimizing 
the potential risk of principal loss.    As of December 31, 2016, the Company had four investments of 
commercial paper with a fair value of $3,985,740 and unrealized losses of $1,684, and four corporate 
bonds  with  a  fair  value  of  $4,031,170  and  unrealized  losses  of  $4,635,  all  of  which  have  been 
unrealized  losses  for  less  than  12  months.    The  Company  does  not  intend  to  sell  its  marketable 
securities in an unrealized loss position.    Based upon the Company’s securities’ fair value relative to 
the cost, high ratings, and volatility of fair value, the Company considers the declines in market value 
of  its  marketable  securities  to  be  temporary  in  nature  and  does  not  consider  any  of  its  investments 
other-than-temporarily impaired, and anticipates that it will recover the entire amortized cost basis. 

As of December 31, 2016, all of the Company’s marketable securities are expected to mature in less 
than one year. 

F-11 

 
 
  
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

4.    Prepaid Expenses and Other Current Assets 

Deposits on contracts 
Prepaid expenses and other current assets 

December 31,    December 31,   

2016 

2015 

$

$

  179,476 $
  429,041

  501,170
  720,648

  608,517 $

  1,221,818

Deposits on contracts consist of deposits on research and development contracts for services that had 
not  been  incurred  as  of  the  balance  sheet  date.    Prepaid  expenses  and  other  assets include  prepaid 
general and administrative expenses, such as insurance, rent, investor relations fees and compensatory 
stock issued for services not yet incurred as of the balance sheet date.   

5.    Equipment, Net 

Furniture and fixtures 
Office and computer equipment 
Lab equipment 
Leasehold improvements 

December 31,    December 31,   

2016 

2015 

$

  78,794 $
  113,932
  431,650
  133,762

  78,794
  105,266
  431,650
  133,762

Total equipment 
Less: Accumulated depreciation and amortization 

  758,138
  (669,488)

  749,472
  (636,572)

Net carrying amount 

$

  88,650 $

  112,900

6.  Accounts Payable and Accrued Expenses 

Trade payables 
Accrued expenses 
Accrued research and development contract costs 
Payroll liabilities 

F-12 

December 31,    December 31,   

2016 

2015 

$

  430,013$ 
  141,190 
  499,889 
  811,408 

  774,543
  92,752
  1,515,151
  278,852

$

  1,882,500$ 

  2,661,298

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
   
 
 
 
 
 
  
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
   
  
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

7.    Deferred Research and Development Arrangements 

Rexgene Biotech Co., Ltd. 

In 2003, the Company entered into a collaborative research agreement with Rexgene Biotech Co., 
Ltd.  (“Rexgene”),  a  shareholder.    Rexgene  is  engaged  in  the  development  of  pharmaceutical 
products in Asia and has agreed to assist the Company with the research, development and clinical 
trials  necessary  for  registration  of  the  Company’s  drug  candidate  Archexin  in  Asia.    This 
agreement provides Rexgene with exclusive rights to license, sublicense, make, have made, use, sell 
and  import  Archexin  in  Asia.    In  accordance  with  the  agreement,  Rexgene  paid  the  Company  a 
one-time fee of $1,500,000 in 2003.    The agreement terminates at the later of 20 years or the term 
of  the  patent.    The  amortization  reduces  research  and  development  expenses  for  the  periods 
presented.     

The  Company  is  using  20  years  as  its  basis  for  recognition  and  accordingly  research  and 
development  expenses  were  reduced  by  $75,000  for each  of  the  years  ended  December  31,  2016, 
2015 and 2014.    The remaining $450,000 and $525,000 to be amortized at December 31, 2016 and 
2015, respectively, are reflected as a deferred research and development arrangement on the balance 
sheet.    The  payment  from  Rexgene  is  being  used  in  the  cooperative  funding  of  the  costs  of 
development of Archexin. Royalties of 3% of net sales of licensed products will become payable by 
Rexgene  to  the  Company  on  a  quarterly  basis  once  commercial  sales  of  Archexin  begin  in  Asia.   
The product is still under development and commercial sales in Asia are not expected to begin until 
at least 2018.    Under the terms of the agreement, Rexgene does not pay royalties on the Company’s 
net sales outside of Asia.   

Teva Pharmaceutical Industries, Ltd. 

The  Company  previously  had  an  arrangement  with  Teva  Pharmaceutical  Industries  Limited 
(“Teva”) where Teva provided funds for the pre-clinical development of RX-3117.    The proceeds 
received  from  Teva  were  recorded  as  restricted  cash  and  as  a  deferred  research  and  development 
arrangement  on  the  balance  sheet.    Costs  paid  for  the  development  of  RX-3117  reduced  the 
deferred  research  and  development  arrangement  and  therefore  were  not  an  expense  in  the 
Company’s  statement  of  operations.    During  the  year  ended  December  31,  2014,  $158,630  was 
reduced from deferred research and development arrangements.    As of December 31, 2014, there 
were no proceeds remaining, and therefore, no deferred research and development liability relating 
to Teva. 

F-13 

 
 
  
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

8. Other Liabilities 

Deferred Lease Incentive 

In accordance with the Company’s office lease agreement, as amended and further discussed in Note 
15, the Company has been granted leasehold improvement allowances from the lessor to be used for 
the  construction  cost  of  improvements  to  the  leased  property,  which  included  architectural  and 
engineering fees, government agency plan check, permit and other fees, sales and use taxes, testing 
and  inspection  costs  and  telephone  and  data  cabling  and  wiring  in  the  premises.    The  Company 
accounted for the benefit of the leasehold improvement allowance as a reduction of rental expense 
over the term of the office lease. 

The following table sets forth the cumulative deferred lease incentive: 

Deferred lease incentive 
Less accumulated amortization 

Balance 

Deferred Office Lease Expense 

December 31,   
2016 

December 31,   
2015 

$

$

  154,660  $ 

  (123,551) 

  154,660
  (111,108)

  31,109  $ 

  43,552

The lease agreement, as amended, provided for an initial annual base rent with annual increases over 
the following six years.    The Company recognizes rental expense on a straight-line basis over the 
term of the lease, which resulted in a deferred rent liability of $48,095 and $60,468 as of December 
31, 2016 and 2015, respectively. 

9.  Net Loss per Common Share 

Basic loss per common share is computed by dividing net loss by the weighted average number of 
shares of common stock outstanding for the period.    Diluted loss per common share is computed by 
dividing net loss by the weighted average number of shares of common stock outstanding, plus the 
number of common share equivalents that would be dilutive.    As of December 31, 2016, 2015 and 
2014, there  were  stock  options  and  warrants  to  acquire, in the  aggregate,  71,427,262,  39,082,886, 
and 24,606,677 shares of the Company’s common stock, respectively, that are potentially dilutive. 
However, diluted loss per share for all periods presented is the same as basic loss per share because 
the inclusion of common share equivalents would be anti-dilutive.   

F-14 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
  
  
  
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

10.  Common Stock   

The following transactions occurred during the years ended December 31, 2016, 2015 and 2014: 

Public Offerings 

January 2014 

On January 21, 2014, the Company closed on a registered direct public offering of 19,047,620 shares 
of common stock and warrants to purchase up to 4,761,905 shares of common stock.    The common 
stock  and  warrants  were  sold  in  units,  consisting  of  a  share  of  common  stock  and  a  warrant  to 
purchase 0.25 shares of common stock, at a price of $1.05 per unit, and the warrants have an exercise 
price of $1.28 per share.    The total gross proceeds of the offering were $20,000,001.    The warrants 
issued  became  exercisable  beginning  six  months  and  one  day  after  the  closing  date,  will  remain 
exercisable until the five-year anniversary of the closing date, and were recorded as liabilities at fair 
value.     

A summary of the allocation of the proceeds of the offering is shown below: 
Gross Proceeds: 

$

  20,000,001 

Allocated to warrant liabilities: 
Allocated to common stock and additional paid-in capital 

  3,691,429 
  16,308,572 

Total allocated gross proceeds: 

  $

  20,000,001 

The  closing  costs  of  $1,365,754  consisted  of  placement agent  and  other  professional fees.    Based 
upon the estimated fair value of the stock and warrants in the units, the Company allocated $206,172 
to financing expense and $1,159,582 as stock issuance costs.   

November 2015   

On  November  12,  2015,  the  Company  closed  on  a  registered  direct  public  offering  of  16,666,667 
shares of common stock and warrants to purchase up to 12,500,000 shares of common stock.    The 
common stock and warrants were sold in units, consisting of a share of common stock and a warrant 
to  purchase  0.75  shares  of  common  stock,  at  a  price  of  $0.42  per  unit,  and  the  warrants  have  an 
exercise price of $0.53 per share.    The total gross proceeds of the offering were $7,000,000.    The 
warrants  issued  became  exercisable  beginning  six  months  after  the  closing  date,  will  remain 
exercisable until the five-year anniversary of the initial exercise date, and were recorded as liabilities 
at fair value.     

A summary of the allocation of the proceeds of the offering is shown below: 
Gross Proceeds: 

$ 

  7,000,000 

Allocated to warrant liabilities: 
Allocated to common stock and additional paid-in capital 

Total allocated gross proceeds: 

  2,792,500 
  4,207,500 

$ 

  7,000,000 

The  closing  costs  of  $740,323  included  833,333  warrants  valued  at  $174,417  and  $565,906  for 
placement agent and other fees.    Based upon the estimated fair value of the stock and warrants in 
the  units,  the  Company  allocated  $211,116  to  financing  expense  and  $529,207  as  stock  issuance 
costs. 

F-15 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

March 2016 

On March 2, 2016, the Company closed on a registered direct public offering of 15,625,000 shares of 
common stock and warrants to purchase up to 11,718,750 shares of common stock.    The common 
stock  and  warrants  were  sold  in  units,  consisting  of  a  share  of  common  stock  and  a  warrant  to 
purchase  0.75  shares  of common  stock,  at  a  price  of $0.32  per  unit,  with an exercise  price for  the 
warrants of $0.42 per share.    The total gross proceeds of the offering were $5,000,000.    The issued 
warrants  issued  became  exercisable  beginning  six  months  after  the  closing  date,  will  remain 
exercisable until the five-year anniversary of the initial exercise date, and were recorded as liabilities 
at fair value.     

A summary of the allocation of the proceeds of the offering is shown below: 

Gross Proceeds: 

Allocated to warrant liabilities: 
Allocated to common stock and additional paid-in capital 

Total allocated gross proceeds: 

$

$

  5,000,000  

  2,419,922  
  2,580,078  

  5,000,000  

The  closing  costs  of  $575,751  included  781,250  warrants  valued  at  $155,938  and  $419,813  for 
placement agent and other fees.    Based upon the estimated fair value of the stock and warrants in 
the  units,  the  Company  allocated  $169,887  to  financing  expense  and  $405,864  as  stock  issuance 
costs. 

September 2016 

On  September  19,  2016,  the  Company  closed  on  a  registered  direct  public  offering  of  24,000,000 
shares of common stock and warrants to purchase up to 18,000,000 shares of common stock.    The 
common stock and warrants were sold in units, consisting of a share of common stock and a warrant 
to purchase 0.75 shares of common stock, at a price of $0.25 per unit, with an exercise price for the 
warrants  of  $0.30  per  share.    The  total  gross  proceeds  of  the  offering  were  $6,000,000.    The 
warrants issued will become exercisable beginning six months after the closing date, and will remain 
exercisable until the five-year anniversary of the initial exercise date, and were recorded as liabilities 
at fair value.     

A summary of the allocation of the proceeds of the offering is shown below: 

Gross Proceeds: 

Allocated to warrant liabilities: 
Allocated to common stock and additional paid-in capital 

$ 

  6,000,000 

  1,671,120 
  4,328,880 

Total allocated gross proceeds: 

$ 

  6,000,000 

The  closing  costs  of  $575,094  included  1,440,000  warrants  valued  at  $117,130  and  $457,964  for 
placement agent and other fees.    Based upon the estimated fair value of the stock and warrants in 
the  units,  the  Company  allocated  $143,203  to  financing  expense  and  $431,891  as  stock  issuance 
costs. 

F-16 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

At Market Offering 

On  March  16,  2015,  the  Company  entered  into  an  at  market  issuance  sales  agreement  (the  “Sales 
Agreement”) with MLV & Co. LLC (“MLV”) pursuant to which the Company may issue and sell 
shares  of  its  common  stock  having  an  aggregate  offering  price  of  up  to  $40  million  from  time  to 
time,  at  its  option,  through  MLV  as  its  sales  agent,  subject  to  certain  terms  and  conditions.  Any 
shares sold will be sold pursuant to the Company’s effective shelf registration statement on Form S-3 
(File  No. 333-196255),  as  supplemented  by  a  prospectus  supplement  dated  March  16,  2015.    The 
Company will pay MLV a commission of 3.0% of the gross proceeds of the sale of any shares sold 
through  MLV.  For  the  year  ended  December  31,  2015,  the  Company  sold  1,407,072  shares  of 
common  stock  pursuant  to  the  Sales  Agreement  for  $1,042,573  in  gross  proceeds  at  a  weighted 
average price of $0.7410 per share.    Net proceeds to the Company were $1,005,715 after deducting 
commissions  and  other  transaction  costs.    Pursuant  to  the  securities  purchase  agreement  entered 
into in connection with the Company’s registered direct offering that closed on September 19, 2016, 
the Company is prohibited from selling any additional shares under the Sales Agreement.   

Compensatory Shares 

The  Company  has  issued  restricted  shares  to  vendors  in  exchange  for  services.    The  table  below 
summarizes the shares issued and the related market value:   

Compensatory shares issued 
Aggregate market value 

$ 

  330,000 
  97,649  $ 

  150,000 
  102,000  $ 

For the Year Ended December 31,   

2016 

2015 

2014 
  400,000 
  409,000 

Stock Option and Stock Warrant Exercises 

The table below summarizes stock options and stock warrants exercised: 

Stock Option Exercises 
Number of shares issued 
Total cash received   

Stock Warrant Exercises 
Number of shares issued 
Total cash received   

Treasury Stock Transactions 

$ 

$ 

For the Year Ended December 31,   

2016 

2015 

2014 

  -
  - $ 

  -
  - $ 

  889,428 
  708,617  $ 

  448,693 
  258,955 

  47,300 
  22,325  $ 

  11,738,220 
  5,947,268 

On  April  14,  2014,  an  option  holder  exercised  stock  options  by  a  net  exercise.    The  Company 
withheld 99,010 shares in treasury as payment for the $100,000 aggregate exercise price. 

On  December  3,  2015,  the  Company  retired  113,215  shares  of  treasury  stock  with  an  aggregate 
purchase price of $128,410.   

F-17 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

11. Stock-Based Compensation 

As of December 31, 2016, the Company had 16,900,415 options outstanding. 

At  the  Company’s  Annual  Meeting  of  the  Stockholders  held  on  June  10,  2013,  the  Company’s 
stockholders voted to approve the Rexahn Pharmaceuticals, Inc. 2013 Stock Option Plan (the “2013 
Plan”).    Under  the  2013 Plan,  the  Company  grants  stock  options  to  key  employees,  directors  and 
consultants of the Company.    A total of 17,000,000 shares of common stock have been reserved for 
issuance  pursuant  to  the  2013  Plan.    As  of  December  31,  2016,  there  were  12,461,915  options 
outstanding under the 2013 Plan, and 4,530,585 shares were available for issuance. 

On  August  5,  2003,  the  Company  established  a  stock  option  plan  (the  “2003  Plan”).    Under  the 
2003  Plan,  the  Company  granted  stock  options  to  key  employees,  directors  and  consultants  of  the 
Company.    With the adoption of the 2013 Plan, no new stock options may be issued under the 2003 
Plan,  but  previously  issued  options  under  the  2003  Plan  remain  outstanding  until  their  expiration.   
As of December 31, 2016, there were 4,318,500 outstanding options under the 2003 Plan. 

In March 2016, the Company granted to a third party an option to purchase up to 120,000 shares of 
the Company’s common stock.    Of the Company’s outstanding options as of December 31, 2016, 
these were the only options that were not issued pursuant to the 2013 Plan or the 2003 Plan.   

At  the  Company’s  Annual  Meeting  of  the  Stockholders  held  on  June  9,  2016,  the  Company’s 
stockholders voted to approve an amendment to the 2013 Plan, including to provide for awards of 
restricted stock and restricted stock units.    As of December 31, 2016, no awards of restricted stock 
or restricted stock units had been granted 

For the majority of the grants to employees, the vesting period is either i) 30%, 30% and 40% on the 
first, second and third anniversaries, of the grant date, respectively, or ii) 25% each on the first four 
anniversaries.    Options  expire  between  five  and  ten  years  from  the  date  of  grant.  For  grants  to 
non-employee  consultants  of  the  Company,  the  vesting  period  is  between  one  and  three  years, 
subject to the fulfillment of certain conditions in the individual stock agreements, or 100% upon the 
occurrence of certain events specified in the individual stock agreements. 

Accounting for Awards 

Stock  option  compensation  expense  is  the  estimated  fair  value  of  options  granted  amortized  on  a 
straight-line basis over the requisite vesting service period for the entire portion of the award.    Total 
stock-based compensation recognized by the Company for the years ended December 31, 2016, 2015 
and 2014 is as follows: 

Statement of operations line item: 
General and administrative 
Research and development 

For the Year Ended December 31, 
2014 
2015 
2016 

$ 

  905,911  $
  503,577 

  665,063 $ 
  372,616  

  457,128 
  151,667 

Total 

$ 

  1,409,488  $

  1,037,679 $ 

  608,795 

F-18 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

Summary of Stock Option Transactions 

There were 5,926,391 stock options granted at exercise prices ranging from $0.18 to $0.37 with an 
aggregate  fair  value  of  $1,156,273  during  the  year  ended  December  31,  2016.    There  were 
4,201,316 stock options granted at exercise prices ranging from $0.54 to $0.89 with an aggregate fair 
value  of  $1,994,893  during  the  year  ended  December  31,  2015.    There  were  2,528,499  stock 
options  granted  at  exercise  prices  ranging  from  $0.68  to  $1.35  with  an  aggregate  fair  value  of 
$1,737,087 during the year ended December 31, 2014.     

The fair value of options at the date of grant was estimated using the Black-Scholes option pricing 
model.    The  Company  took  into  consideration  guidance  under  ASC  718,  “Compensation-Stock 
Compensation” and Staff Accounting Bulletin No. 107 (“SAB 107”) when reviewing and updating 
assumptions.     

Significant assumptions are determined as follows: 

Expected  Term-the  expected  term  was  estimated  using  the  simplified  method  whereby  the 
expected  term  equals  the  arithmetic  average  of  the  vesting  term  and  the  original  contractual 
term of the option. 

Volatility-historical trading volatility of the Company’s stock on the date of grant for a period 
consistent with the expected term. 

Risk-Free  Interest  Rate-the  risk-free  interest  rate  is  based  on  the zero-coupon U.S.  Treasury 
instruments on the date of grant with a maturity date consistent with the expected term of the 
Company’s stock option grants. 

Expected Dividend -to date, the Company has not declared or paid any cash dividends and do 
not have any plans to do so in the future. Therefore, the Company used an expected dividend 
yield of zero. 

The assumptions made in calculating the fair values of options are as follows:   

Black-Scholes assumptions 
Expected dividend yield 
Expected volatility 
Risk free interest rate 
Expected term (in years) 

Year Ended December 31,   

2016 

2015 

2014 

0% 
31-75% 
0.8-1.4% 

0% 
72-80% 
1.2-1.7% 

2-6 years 

5-6 years 

0% 
92-96% 
1.5-1.8% 
5 years 

F-19 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

The following table summarizes share-based transactions: 

Outstanding, January 1, 2016 
Granted 
Exercised 
Expired 
Cancelled 

Number of 
Options 
  12,590,982  $ 
  5,926,391  
  - 
  (730,000) 
  (886,958) 

Outstanding, December 31, 2016 
Exercisable, December 31, 2016 

  16,900,415  $ 
  7,929,179  $ 

Weighted 
Average 
Exercise 
Price 

  0.83 
  0.31 
  -
  1.37 
  0.89 

  0.62 
  0.78 

Weighted Average 
Remaining 
Contractual Term   

6.8 years $ 

Aggregate 
Intrinsic 
Value 
  26,500 

7.3 years $ 
5.8 years $ 

  -
  -

There  were  no  stock  options  exercised  during  the  year  ended  December  31,  2016.    The  total 
intrinsic value of the options exercised was $99,895 and $115,528 for the years ended December 31, 
2015  and  2014,  respectively.    The  weighted  average  fair  value  of  the  options  granted  was  $0.20, 
$0.47, and $0.69 for the years ended December 31, 2016, 2015 and 2014, respectively.   

A  summary  of  the  Company’s  unvested  options  as  of  December  31,  2016  and changes  during  the 
year ended December 31, 2016 is presented below: 

Unvested at January 1, 2016 
Granted 
Vested 
Cancelled 

Unvested at December 31, 2016 

2016 

Number of    Options 

Weighted Average Fair 
Value at Grant Date 

  5,888,432  $
  5,926,391  $
  (2,625,254)  $
  (218,333)  $

  8,971,236  $

  0.51 
  0.20 
  0.46 
  0.41 

  0.32 

As of December 31, 2016 there was $1,882,605 of total unrecognized compensation cost related to 
unvested stock options, which is expected to be recognized over a weighted average vesting period 
of 2.0 years.     

F-20 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
   
   
   
   
 
 
 
   
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

12. Warrants   

As of December 31, 2016, warrants to purchase 54,526,847 shares were outstanding, having exercise 
prices ranging from $0.30 to $1.28 and expiration dates ranging from December 4, 2017 to March 
19, 2022.       

2016 

2015 

  1.07 
  0.53 
  0.47 
  -

  0.80 

Number of 
warrants 

Weighted 
average exercise 
price 

Balance, January 1 
Issued during the period 
Exercised during the period 
Expired during the period 

  26,491,904  $ 
  31,940,000  $ 
  - $ 
  (3,905,057) $ 

  0.80 
  0.35 
  -
  1.37 

Number of 
warrants 
  13,205,871  $ 
  13,333,333  $ 
  (47,300) $ 
  - $ 

Weighted average 
exercise price 

Balance, December 31 

  54,526,847  $ 

  0.49 

  26,491,904  $ 

At December 31, 2016 the weighted average remaining contractual life of the outstanding warrants 
was 4.3 years.   

The  warrants issued  to  investors  in the  December  2012,  November  2015,  March  2016,  September 
2016, and previous offerings contain a provision for net cash settlement in the event that there is a 
fundamental  transaction  (contractually  defined  as  a  merger,  sale  of  substantially  all  assets,  tender 
offer  or  share  exchange).    If  a  fundamental  transaction  occurs  in  which  the  consideration  issued 
consists principally of cash or stock in a non-public company, then the warrant holder has the option 
to receive cash, equal to the fair value of the remaining unexercised portion of the warrant.    Due to 
this contingent redemption provision, the warrants require liability classification in accordance with 
ASC 480 and are recorded at fair value.    The warrants issued to investors in the July 2013, October 
2013  and  January  2014  offerings  contain  a  fundamental  transaction  provision,  but  the  warrant 
holders only have an option as to the type of consideration received if the holders of common stock 
receive an option as to their consideration.    In addition, the warrants issued in the December 2012, 
July 2013, October 2013, January 2014, November 2015, March 2016, September 2016 and previous 
offerings contain a cashless exercise provision that is exercisable only in the event that a registration 
statement is not effective. That provision may not be operative if an effective registration statement 
is not available because an exemption under the U.S. securities laws may not be available to issue 
unregistered  shares.    As  a  result,  net  cash  settlement  may  be  required,  and  the  warrants  require 
liability classification. 

ASC  820  provides  requirements  for  disclosure  of  liabilities  that  are  measured  at  fair  value  on  a 
recurring  basis  in  periods  subsequent  to  the  initial  recognition.    Fair  values  for  warrants  were 
determined using the Binomial Lattice (“Lattice”) valuation technique. The Lattice model provides 
for  dynamic  assumptions  regarding  volatility  and  risk-free  interest  rates  within  the  total  period  to 
maturity.  Accordingly,  within  the  contractual  term,  the  Company  provided  multiple  date  intervals 
over  which  multiple  volatilities  and  risk  free  interest  rates  were  used.  These  intervals  allow  the 
Lattice  model to  project  outcomes  along  specific  paths  that  consider  volatilities  and risk  free rates 
that would be more likely in an early exercise scenario. 

F-21 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

Significant assumptions are determined as follows:   
Trading market values—Published trading market values;   
Exercise price—Stated exercise price;   
Term—Remaining contractual term of the warrant;   
Volatility—Historical trading volatility for periods consistent with the remaining terms; and 
Risk-free rate—Yields on zero coupon government securities with remaining terms consistent with 
the remaining terms of the warrants.   

Due  to  the  fundamental  transaction  provision,  which  could  provide  for  early  redemption  of  the 
warrants,  the  model  also  considered  the  probability  the  Company  would  enter  into  a  fundamental 
transaction  during  the  remaining  term  of  the  warrant.  Because  the  Company  is  not  yet  achieving 
positive cash flow, management believes the probability of a fundamental transaction occurring over 
the  term  of  the  warrant  is  unlikely  and  therefore  estimates  the  probability  of  entering  into  a 
fundamental transaction to be 5%.    For valuation purposes, the Company also assumed that if such 
a transaction did occur, it was more likely to occur towards the end of the term of the warrants. 

The  significant  unobservable  inputs  used  in  the  fair  value  measurement  of  the  warrants  include 
management’s  estimate  of  the  probability  that  a  fundamental  transaction  may  occur  in  the  future.   
Significant  increases  (decreases)  in  the  probability  of  occurrence  would  result  in  a  significantly 
higher (lower) fair value measurement. 

The  following  table  summarizes  the  fair  value  of  the  warrants  as  of  the  respective  balance  sheet 
dates: 

Fair Value as of:   

December 31, 2016  December 31, 2015 
  2,590 
  - $ 
$ 
  9,818 
  121,420 
  169,349 
  131,476 
  2,169,375 
  135,135 
  -
  -
  -
  -
  2,739,163 

  49  
  2,060  
  3,708  
  714  
  260,500  
  13,542  
  358,945  
  21,320  
  854,640  
  57,888  
  1,573,366  $ 

$

Warrant Issuance: 
Expired Warrants 
December 2012 Investor Warrants   
July 2013 Investor Warrants   
October 2013 Investor Warrants 
January 2014 Investor Warrants 
November 2015 Investor Warrants 
November 2015 Placement Agent Warrants     
March 2016 Investor Warrants 
March 2016 Placement Agent Warrants 
September 2016 Investor Warrants 
September 2016 Placement Agent Warrants 
Total: 

F-22 

 
 
   
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

The following table summarizes the number of shares indexed to the warrants as of the respective 
balance sheet dates: 

Warrant Issuance 
Expired Warrants 
December 2012 Investor Warrants   
July 2013 Investor Warrants   
October 2013 Investor Warrants 
January 2014 Investor Warrants 
November 2015 Investor Warrants 
November 2015 Placement Agent Warrants     
March 2016 Investor Warrants 
March 2016 Placement Agent Warrants 
September 2016 Investor Warrants 
September 2016 Placement Agent Warrants 
Total: 

Number of Shares indexed as of: 

December 31, 2016 

  -
  174,300 
  2,000,000 
  2,317,309 
  4,761,905 
  12,500,000 
  833,333 
  11,718,750 
  781,250 
  18,000,000 
  1,440,000 
  54,526,847 

December 31, 2015 
  3,905,057 
  174,300 
  2,000,000 
  2,317,309 
  4,761,905 
  12,500,000 
  833,333 
  -
  -
  -
  -
26,491,904

The assumptions used in calculating the fair values of the warrants are as follows:   

Trading market prices 
Estimated future volatility 
Dividend 
Estimated future risk-free rate 
Equivalent volatility 
Equivalent risk-free rate 

December 31, 2016  December 31, 2015 

$ 

$ 

  0.14  
  104 % 
- 

1.06-2.44% 
51-60% 
0.59-1.25% 

  0.36  
  105 % 
- 

0.82-2.38% 
44-65% 
0.22-1.11% 

F-23 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

Changes in the fair value of the warrant liabilities, carried at fair value, as reported as “unrealized 
gain (loss) on fair value of warrants” in the statement of operations: 

Expired Warrants 
December 2012 Investor Warrants   
July 2013 Investor Warrants   
October 2013 Investor Warrants 
January 2014 Investor Warrants 
November 2015 Investor Warrants 
November 2015 Placement Agent 
Warrants     
March 2016 Investor Warrants 
March 2016 Placement Agent 
Warrants 
September 2016 Investor Warrants 
September 2016 Placement Agent 
Warrants 
Total: 

$ 

$ 

For the Year Ended December 31, 

2016 

  2,590 $ 
  9,769  
  119,360  
  165,641  
  130,762  
  1,908,875  
  121,593  
  2,060,977 
  134,617 
  816,480 
  59,243 
  5,529,907 $ 

2015 

  458,439 $ 
  70,856  
  666,894  
  780,407  
  1,347,724  
  623,125  
  39,282  
  -
  -
  -
  -

  3,986,727 $ 

2014 
  (1,059,400)
  (4,120,103)
  (1,272,731)
  (940,100)
  2,212,227 
  -
  -
  -
  -
  -
  -
  (5,180,107)

13. Mediation Settlement 

In connection with the process of seeking patent protection for Supinoxin in Japan, the Company had 
filed  a  patent  application  including  claims  covering  Supinoxin  with  the  Japanese  Patent  Office 
(“JPO”)  for  examination.  The  JPO  initially  agreed  that  the  claims  covering  the  compound  for 
Supinoxin were allowable, but as a result of a mistake in the patent application filing as prepared and 
submitted  by  the  Company’s  Japanese  patent  attorney  and  incomplete  review  by  the  JPO’s  patent 
examiner, the JPO issued a decision to grant a patent with claims that did not include Supinoxin’s 
chemical structure. The Company appealed this decision with the JPO to request withdrawal of the 
decision to grant so that the correct claims would be allowed, but the JPO refused to withdraw its 
decision.  As  a  result,  and  in  accordance  with  Japanese  law  and  procedure  for  appealing  patent 
application  decisions,  the Company  has  filed a  lawsuit against  the JPO  in Tokyo  District  Court  to 
cause the JPO  to  reverse its  decision to  grant  the  errant  patent  and  to  allow  a  patent  that  includes 
claims covering Supinoxin.   The patent application at issue remains pending subject to the outcome 
of  this  action.  While  the  composition  of  matter  patent  on  Supinoxin  structure  remains  pending  in 
Japan, the Company either has already or will have protection in Japan from its issued and pending 
patents  on  formulation,  method  of  use,  and  method  of  manufacturing  as  well  as  from  market 
exclusivity period. 

On  December  19,  2016,  the  Company  entered  into  a  binding  settlement  arrangement  with  the 
Company’s Japanese patent attorney in which the Japanese patent attorney agreed to pay a one-time 
settlement JPY 210,000,000, or $1,770,658, in exchange for the Company agreeing not to bring any 
future  claims  on  account  of  this  patent  filing.   The  settlement  payment  was  received  by  the 
Company by December 31, 2016. 

F-24 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

14. Income Taxes 

No  provision  for  federal  and  state  income  taxes  was  required  for  the  years  ended  December  31, 
2016,  2015  and  2014  due  to  the  Company’s  operating  losses  and  increased  deferred  tax  asset 
valuation allowance.    At December 31, 2016 and 2015, the Company had unused net operating loss 
carry-forwards  of  approximately  $111,605,000  and  $98,954,000,  respectively,  which  expire  at 
various  dates  through  2036.    Some  of  this  amount  may  be  subject  to  annual  limitations  under 
certain provisions of the Internal Revenue Code related to “changes in ownership.”     

As  of  December  31,  2016  and  2015,  the  deferred  tax  assets  related  to  the  aforementioned 
carry-forwards have been fully offset by valuation allowances, because significant utilization of such 
amounts is not presently expected in the foreseeable future.     

Deferred tax assets and valuation allowances consist of: 

Net Operating Loss Carryforwards 
Stock Compensation Expense 
Book tax differences on assets and liabilities 
Valuation Allowance 

Net Deferred Tax Assets 

December 31,   
2016 

December 31,   
2015 

$ 

$ 

  43,526,000 $ 
  1,968,000  
  547,000  
  (46,041,000) 

  38,592,000 
  1,891,000 
  380,000 
  (40,863,000)

  -$ 

  -

The Company files income tax returns in the U.S. federal and Maryland state jurisdictions.   Tax 
years for fiscal 2013 through 2016 are open and potentially subject to examination by the federal and 
Maryland state taxing authorities. 

F-25 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
  
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

15.  Commitments and Contingencies 

a)  The Company has contracted with various vendors for research and development services, the 
terms which require payments over the term of the agreements, usually ranging from two to 36 
months. The costs to be incurred are estimated and are subject to revision. As of December 31, 
2016,  the  total  estimated  cost  to  complete  these  agreements  was  approximately  $4,960,000.       
All of these agreements may be terminated by either party upon appropriate notice as stipulated 
in the respective agreements. 

b)  On  June  22,  2009,  the  Company  entered  into  a  License  Agreement  with  Korea  Research 
Institute of Chemical Technology (“KRICT”) to acquire the rights to all intellectual property 
related  to  quinoxaline-piperazine  derivatives  that  were  synthesized  under  a  Joint  Research 
Agreement.    The initial license fee was $100,000, all of which was paid as of December 31, 
2009.    The  agreement  with  KRICT  calls  for  a  one-time  milestone  payment  of  $1,000,000 
within  30  days  after  the  first  achievement  of  marketing  approval  of  the  first  commercial 
product arising out of or in connection with the use of KRICT’s intellectual properties.    As of 
December 31, 2016, the milestone has not occurred. 

c)  Office Space Lease 

On June 7, 2013, the Company signed the first amendment to its commercial lease agreement 
for 5,466 square feet of office space in Rockville, Maryland.    Under the lease agreement, the 
Company pays its allocable portion of real estate taxes and common area operating charges.   

On  July  26,  2014  the  Company  entered  into  the  second  amendment  to  the  lease  agreement.   
According to the terms of this amendment, the Company leased an additional 1,637 square feet 
of  office  space,  beginning  on  September  1,  2014  and  ending  on  August  31,  2015.    The 
Company  subsequently  renewed  the  lease  for  this  space  for  additional  one-year  terms, 
beginning on September 1, 2015 and 2016.   

Rent  paid  under  the  Company’s  lease  during  the  years  ended  December  31,  2016,  2015,  and 
2014 was $205,324, $202,529 and $155,057, respectively. 

Prior Laboratory Lease 

On  August  26,  2014  and  June  24,  2013,  the  Company  signed  one-year  renewals  to  use 
laboratory  space  commencing  on  July  1,  2014  and  2013,  respectively.    The  lease  required 
monthly  rental  payments  of  $4,554.    Rent  paid  under  the  Company’s  lease  during  the  years 
ended December 31, 2015, and 2014 was $27,324 and $54,648, respectively.     

Current Laboratory Lease 

On April 20, 2015, the Company signed a five-year lease agreement for 2,552 square feet of 
laboratory space commencing on July 1, 2015 and ending on June 30, 2020.    Under the lease 
agreement,  the  Company  pays  its  allocable  portion  of  real  estate  taxes  and  common  area 
operating charges. Rent paid under this lease during the years ended December 31, 2016 and 
2015 was $62,167 and $30,624, respectively. 

F-26 

 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

  Future rental payments over the next five years for all leases are as follows: 

For the year ending December 31: 

2017 
2018 
2019 
2020 

Total 

255,731 
233,923 
152,955 
34,468 

$ 

677,077 

d)  The Company has established a 401(k) plan for its employees.    The Company has elected to 
match 100% of the first 3% of an employee’s compensation plus 50% of an additional 2% of 
the employee’s deferral. Expense related to this matching contribution aggregated to $113,204, 
$121,519 and $91,241 for the years ended December 31, 2016, 2015 and 2014 respectively.   

e) 

In July 2013, the Company entered into an exclusive license agreement with the University of 
Maryland,  Baltimore  for  a  novel  drug  delivery  platform,  Nano-Polymer  Drug  Conjugate 
Systems.    RX-21101  is  the  Company’s  first  drug  candidate  utilizing  this  platform.    The 
agreement  requires  the  Company  to  make  payments  to  the  University  of  Maryland  if 
RX-21101  or  any  products  from  the  licensed  delivery  platform  achieve  development 
milestones.    As of December 31, 2016, no development milestones have occurred. 

f)    In  October  2013,  the  Company  signed  an  exclusive  license  agreement  with  the  Ohio  State 
Innovation  Foundation,  for  a  novel  oligonucleotide  drug  delivery  platform,  Lipid-Coated 
Albumin Nanoparticle.    The agreement requires the Company to make payments to the Ohio 
State  Innovation  Foundation  or  any  products  from  the  licensed  delivery  platform  achieve 
development  milestones.    As  of  December  31,  2016,  no  development  milestones  have 
occurred. 

F-27 

 
 
  
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

16.    Fair Value Measurements 

ASC 820 defines fair value as the price that would be received to sell an asset or paid to transfer a 
liability in an orderly transaction between market participants at the measurement date, not adjusted 
for transaction costs.    ASC 820 also establishes a fair value hierarchy that prioritizes the inputs to 
valuation techniques used to measure fair value into three broad levels giving the highest priority to 
quoted prices in active markets for identical assets or liabilities (Level 1) and the lowest priority to 
unobservable inputs (Level 3).     

The three levels are described below:   

Level 1 Inputs 

—

Unadjusted quoted prices in active markets for identical assets or 
liabilities that are accessible by the Company; 

Level 2 Inputs 

—

Quoted prices in markets that are not active or financial instruments for 
which all significant inputs are observable, either directly or indirectly; 

Level 3 Inputs 

—

Unobservable inputs for the asset or liability including significant 
assumptions of the Company and other market participants. 

The following tables present assets and liabilities that are measured at fair value on a recurring 
basis  and  are  categorized  using  the  fair  value  hierarchy.    There  have  been  no  changes  in  the 
methodologies used at December 31, 2016 and 2015.   

      Total     

Fair Value Measurements at December 31, 2016
Level 3

Level 1

Level 2

Assets: 
          Certificates of Deposit 
          Commercial Paper 
          Corporate Bonds 
Total Assets: 

$

$ 

  720,197  $

  3,985,740 
  4,031,170 
  8,737,107  $

Liabilities:   
          Warrant Liabilities 

$ 

  1,573,366 

  - $
  -
  -
  - $

-

  720,197  $

  3,985,740 
  4,031,170 
  8,737,107  $

  -
  -
  -
  -

- $

  1,573,366 

Assets: 
          Certificates of Deposit 
          Commercial Paper 
          Corporate Bonds 
Total Assets: 

Liabilities:   
          Warrant Liabilities 

      Total     

$ 

$ 

  6,234,996  $
  2,977,570 
  4,027,520 
  13,240,086  $

Fair Value Measurements at December 31, 2015
Level 3

Level 1

Level 2

  - $
  -
  -
  - $

  6,234,996  $
  2,977,570 
  4,027,520 
  13,240,086  $

  -
  -
  -
  -

$ 

  2,739,163 

-

- $

  2,739,163 

F-28 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

The fair value of the Company’s Level 2 marketable securities is determined by using quoted prices 
from independent pricing services that use market data for comparable securities in active or inactive 
markets.    A  variety  of  data  inputs,  including  benchmark  yields,  interest  rates,  known  historical 
trades and broker dealer quotes are using with pricing models to determine the quoted prices. 

The fair value methodology for the warrant liabilities is disclosed in Note 12. 

The carrying amounts reported in the financial statements for cash and cash equivalents (Level 1), 
prepaid  expenses  and  other  assets,  and  accounts  payable  and  accrued  expenses  approximate  fair 
value because of the short term maturity of these financial instruments. 

The following table sets forth a reconciliation of changes in the years ended December 31, 2016 and 
2015 in the fair value of the liabilities classified as Level 3 in the fair value hierarchy: 

Balance at January 1, 2016 
Additions 
Unrealized gains, net   
Transfers out of level 3 
Balance at December 31, 2016 

Balance at January 1, 2015 
Additions 
Unrealized gains, net   
Transfers out of level 3 
Balance at December 31, 2015 

Warrant Liabilities 

  2,739,163
  4,364,110
  (5,529,907)
  -
  1,573,366

Warrant Liabilities 

  3,768,351
  2,966,917
  (3,986,727)
  (9,378)
  2,739,163

$ 

$ 

$ 

$ 

Additions consist of the fair value of warrant liabilities upon issuance.    Transfers out of Level 3 for 
warrant liabilities consist of warrant exercises, where the liability is converted to additional paid-in 
capital upon exercise.    The Company’s policy is to recognize transfers in and transfers out as of the 
actual date of the event or change in circumstance that caused the transfer.       

F-29 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
  
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
  
 
REXAHN PHARMACEUTICALS, INC. 
Notes to Financial Statements 

17.    Select Quarterly Data (Unaudited) 

Revenues 
Expenses 
Loss from Operations 
Other Income, net 
Net Loss 
Net Loss per share, basic and diluted 

  March 31 
$ 

  - $ 

  4,863,981  
  (4,863,981)  
  714,939  
  (4,149,042) $ 
  (0.02) $ 

$ 
$ 

2016 
For the Quarter Ended 
June 30 

  - $ 

  3,912,782  
  (3,912,782)  
  2,146,958  
  (1,765,824) $ 
  (0.01) $ 

  September 30    December 31 
  - 
  - $ 
  3,919,047 
  (3,919,047) 
  3,393,564 
  (525,483) 
  (0.00)

  3,717,575  
  (3,717,575)  
  850,579  
  (2,866,996) $ 
  (0.01) $ 

2015 
For the Quarter Ended 

  March 31 
$ 

  - $ 

June 30 

  September 30    December 31 
  - 
  - $ 

  - $ 

  4,417,708  

  4,819,940  

  4,658,555  

  4,367,233 

  (4,417,708)  

  (4,819,940)  

  (4,658,555)  

  (4,367,233) 

  145,997  

  1,585,780  

  632,025  

  1,515,078 

  (4,271,711) $ 

  (3,234,160) $ 

  (4,026,530) $ 

  (2,852,155) 

  (0.02) $ 

  (0.02) $ 

  (0.02) $ 

  (0.02) 

$ 

$ 

Revenues 

Expenses 

Loss from Operations 

Other Income, net 

Net Loss per share 

Net Loss per share, basic and diluted 

18.    Subsequent Events 

Since  December  31,  2016,  the  Company  granted  3,905,600  stock  options  and  restricted  stock  units  to 
officers, employees and consultants. 

F-30 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
3.1 

3.2 

4.1 

4.2 

4.3 

4.4 

4.5 

4.6 

4.7 

4.8 

*10.1 

*10.2 

*10.3 

*10.4 

*10.5 

EXHIBIT INDEX 

Amended and Restated Certificate of Incorporation, filed as Appendix G to the Company’s 
Definitive Proxy Statement on Schedule 14A (File No. 000-50590) dated April 29, 2005, is 
incorporated herein by reference. 

Amended and Restated Bylaws, as amended, through March 21, 2014, filed as exhibit 3.2 to 
the Company’s Annual Report on Form 10-K on March 21, 2014, is incorporated herein by 
reference. 

Specimen Certificate for the Company’s Common Stock, par value $.0001 per share, filed as 
Exhibit 4.3 to the Company’s Registration Statement on Form S-8 (File No. 333-129294) 
dated October 28, 2005, is incorporated herein by reference. 

Form of Warrant for the Company’s Common Stock Purchase Warrants, filed as Exhibit 4.1 
to the Company’s Current Report on Form 8-K filed on November 30, 2012, is incorporated 
herein by reference. 

Form of Warrant for the Company’s Common Stock Purchase Warrants, filed as Exhibit 4.1 
to the Company’s Current Report on Form 8-K filed on July 24, 2013, is incorporated herein 
by reference. 

Form of Warrant for the Company’s Common Stock Purchase Warrants, filed as Exhibit 4.1 
to the Company’s Current Report on Form 8-K filed on October 16, 2013, is incorporated 
herein by reference. 

Form of Warrant for the Company’s Common Stock Purchase Warrants, filed as Exhibit 4.1 
to the Company’s Current Report on Form 8-K filed on January 15, 2014, is incorporated 
herein by reference.   

Form of Warrant for the Company’s Common Stock Purchase Warrants, filed as Exhibit 4.1 
to the Company’s Current Report on Form 8-K filed on November 6, 2015, is incorporated 
herein by reference. 

Form of Warrant for the Company’s Common Stock Purchase Warrants, filed as Exhibit 4.1 
to the Company’s Current Report on Form 8-K filed on February 26, 2016, is incorporated 
herein by reference. 

Form of Warrant for the Company’s Common Stock Purchase Warrants, filed as Exhibit 4.1 
to the Company’s Current Report on Form 8-K filed on September 14, 2016, is incorporated 
herein by reference. 

Rexahn Pharmaceuticals, Inc. Stock Option Plan, as amended, filed as Exhibit 4.4 to the 
Company’s Registration Statement on Form S-8 (File No. 333-129294) dated October 28, 
2005, is incorporated herein by reference. 

Form of Stock Option Grant Agreement for Employees, filed as Exhibit 4.5.1 to the 
Company’s Registration Statement on Form S-8 (File No. 333-129294) dated October 28, 
2005, is incorporated herein by reference. 

Form of Stock Option Grant Agreement for Non-Employee Directors and Consultants, filed 
as Exhibit 4.5.2 to the Company’s Registration Statement on Form S-8 (File No. 
333-129294) dated October 28, 2005, is incorporated herein by reference. 

Rexahn Pharmaceuticals, Inc. 2013 Stock Option Plan, filed as Exhibit 10.1 to the 
Company’s Registration Statement on Form S-8 (File No. 333-189240) dated June 11, 2013, 
is incorporated herein by reference. 

Form of Stock Option Grant Agreement under Rexahn Pharmaceuticals, Inc. 2013 Stock 
Option Plan filed as Exhibit 10.5 to the Company’s Annual Report on Form 10-K for the year 
ended December 31, 2015, filed on March 14, 2016, is incorporated herein by reference.   

 
 
 
 
 
*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 

Employment Agreement, dated as of September 9, 2010, by and between Rexahn 
Pharmaceuticals, Inc. and T. H. Jeong, filed as Exhibit 10.3 to the Company’s Current Report 
on Form 8-K filed on September 10, 2010, is incorporated herein by reference. 

Employment Agreement, dated as of February 4, 2013, by and between Rexahn 
Pharmaceuticals, Inc. and Peter Suzdak, filed as Exhibit 10.1 to the Company’s Current 
Report on Form 8-K filed on January 22, 2013, is incorporated herein by reference. 

Employment Agreement, dated as of March 25, 2013, by and between Rexahn 
Pharmaceuticals, Inc. and Chang H. Ahn, filed as Exhibit 10.1 to the Company’s Current 
Report on Form 8-K filed on March 29, 2013, is incorporated herein by reference. 

Employment Agreement, dated as of February 2, 2015, by and between Rexahn 
Pharmaceuticals, Inc. and Ely Benaim, M.D., filed as Exhibit 10.1 to the Company’s Current 
Report on Form 8-K filed on May 8, 2015, is incorporated herein by reference. 

Bonus Letter Agreement, dated as of August 2, 2016, by and between Rexahn 
Pharmaceuticals, Inc. and Ely Benaim, M.D., filed as Exhibit 10.2 to the Company’s 
Quarterly Report on Form 10-Q for the quarterly period ended June 30, 2016, is incorporated 
herein by reference. 

Employment Agreement, dated as of July 6, 2016, by and between Rexahn Pharmaceuticals, 
Inc. and Lisa Nolan, Ph.D., filed as Exhibit 10.2 to the Company’s Quarterly Report on Form 
10-Q for the quarterly period ended September 30, 2016, is incorporated herein by reference. 

Lease Agreement, dated June 5, 2009, by and between Rexahn Pharmaceuticals, Inc. and The 
Realty Associates Fund V, L.P., filed as Exhibit 10.4 to the Company’s Quarterly Report on 
Form 10-Q for the quarterly period ended June 30, 2009, is incorporated herein by reference. 

First Amendment to Lease Agreement, dated as of June 7, 2013, by and between Rexahn 
Pharmaceuticals, Inc. and SG Plaza Holdings, LLC, filed as Exhibit 10.1 to the Company’s 
Quarterly Report on Form 10-Q for the quarterly period ended June 30, 2013, is incorporated 
herein by reference. 

Second Amendment to Lease Agreement, dated as of July 26, 2014, by and between Rexahn 
Pharmaceuticals, Inc. and SG Plaza Holdings, LLC, filed as Exhibit 10.1 to the Company’s 
Quarterly Report on Form 10-Q for the quarterly period ended September 30, 2014, is 
incorporated herein by reference. 

Third Amendment to Lease Agreement, dated as of May 6, 2015, by and between Rexahn 
Pharmaceuticals, Inc. and SG Plaza Holdings, LLC, filed as Exhibit 10.1 to the Company’s 
Quarterly Report on Form 10-Q for the quarterly period ended June 30, 2015, is incorporated 
herein by reference. 

Fourth Amendment to Lease Agreement, dated as of April 4, 2016, by and between Rexahn 
Pharmaceuticals, Inc. and SG Plaza Holdings, LLC, filed as Exhibit 10.1 to the Company’s 
Quarterly Report on Form 10-Q for the quarterly period ended June 30, 2016, is incorporated 
herein by reference. 

Research Collaboration Agreement on RX-0201 Clinical Development, dated as of February 
6, 2003, filed as Exhibit 10.5 to the Company’s Annual Report on Form 10-K for the year 
ended December 31, 2005, is incorporated herein by reference. 

Form of Securities Purchase Agreement, dated as of July 23, 2013, by and between Rexahn 
Pharmaceuticals, Inc. and the purchasers identified on the signature pages thereto, filed as 
Exhibit 10.1 to the Company’s Current Report on Form 8-K filed on July 24, 2013, is 
incorporated herein by reference. 

 
 
 
 
10.19 

10.20 

10.21 

10.22 

10.23 

10.24 

12.1 

23.1 

24.1 

31.1 

31.2 

32.1 

32.2 

Form of Securities Purchase Agreement, dated as of October 10, 2013, by and between 
Rexahn Pharmaceuticals, Inc. and the purchasers identified on the signature pages thereto, 
filed as Exhibit 10.1 to the Company’s Current Report on Form 8-K filed on October 16, 
2014, is incorporated herein by reference. 

Form of Securities Purchase Agreement, dated as of January 15, 2014, by and between 
Rexahn Pharmaceuticals, Inc. and the purchasers identified on the signature pages thereto, 
filed as Exhibit 10.1 to the Company’s Current Report on Form 8-K filed on January 21, 
2014, is incorporated herein by reference. 

Form of Securities Purchase Agreement, dated as of November 6, 2015, by and between 
Rexahn Pharmaceuticals, Inc. and the purchasers identified on the signature pages thereto, 
filed as Exhibit 10.1 to the Company’s Current Report on Form 8-K filed on November 6, 
2015, is incorporated herein by reference. 

Form of Securities Purchase Agreement, dated as of February 26, 2016, by and between 
Rexahn Pharmaceuticals, Inc. and the purchasers identified on the signature pages thereto, 
filed as Exhibit 10.1 to the Company’s Current Report on Form 8-K filed on February 26, 
2016, is incorporated herein by reference. 

Form of Securities Purchase Agreement, dated as of September 14, 2016, by and between 
Rexahn Pharmaceuticals, Inc. and the purchasers identified on the signature pages thereto, 
filed as Exhibit 10.1 to the Company’s Current Report on Form 8-K filed on September 14, 
2016, is incorporated herein by reference. 

At Market Issuance Sales Agreement, dated as of March 16, 2015, by and between Rexahn 
Pharmaceuticals, Inc. and MLV & Co. LLC, filed as Exhibit 10.18 to the Company’s Annual 
Report on Form 10-K for the year ended December 31, 2014, is incorporated herein by 
reference. 

Statement Regarding the Computation of Ratio of Earnings to Combined Fixed Charges and 
Preferred Stock Dividends 

Consent of Baker Tilly Virchow Krause, LLP, independent registered public accounting firm   

Power of Attorney 

Certification of Chief Executive Officer Pursuant to Rule 13a-14(a) or Rule 15d-14(a) 

Certification of Chief Financial Officer Pursuant to Rule 13a-14(a) or Rule 15d-14(a) 

Certification of Chief Executive Officer of Periodic Report Pursuant to 18 U.S.C. 
Section 1350 

Certification of Chief Financial Officer of Periodic Report Pursuant to 18 U.S.C. 
Section 1350 

101.INS 

XBRL Instance Document 

101.SCH 

XBRL Taxonomy Extension Schema 

101.CAL  XBRL Taxonomy Calculation Linkbase 

101.DEF 

XBRL Taxonomy Definition Linkbase 

101.LAB  XBRL Taxonomy Label Linkbase 

101.PRE 

XBRL Taxonomy Presentation Linkbase 

*Indicates management contract or compensatory plan or arrangement 

 
 
 
 
ORPORATE INFORMATION    
      CCCCORPORATE INFORMATION
ORPORATE INFORMATION
ORPORATE INFORMATION

BOARD OF DIRECTORS    
BOARD OF DIRECTORS
BOARD OF DIRECTORS
BOARD OF DIRECTORS

CORPORATE HEADQUARTERSRSRSRS    
CORPORATE HEADQUARTE
CORPORATE HEADQUARTE
CORPORATE HEADQUARTE

Peter Brandt, Chairman 
Former President and Chief Executive 
Officer,  
Noven Pharmaceuticals 

Chang H. Ahn, Ph.D. Chairman Emeritus 
Chief Scientist,  
Rexahn Pharmaceuticals 

Charles Beever, Director 
Former Vice President,  
PwC Strategy& 

Mark Carthy, Director 
Managing Partner,  
Orion Equity Partners 

Kwang Soo Cheong, Ph.D. Director 
Associate Professor,  
Johns Hopkins University 

Richard J. Rodgers, Director 
Former Executive Vice President and Chief 
Financial Officer, TESARO 

Peter D. Suzdak, Ph.D. Director 
Chief Executive Officer,  
Rexahn Pharmaceuticals, Inc. 

EXECUTIVE OFFICERS    
EXECUTIVE OFFICERS
EXECUTIVE OFFICERS
EXECUTIVE OFFICERS

Peter D. Suzdak, Ph.D. 
Chief Executive Officer 

Tae Heum (Ted) Jeong, D. Mgt.  
Sr. Vice President, Chief Financial Officer 
and Secretary 

Ely Benaim, M.D. 
Chief Medical Officer 

Lisa Nolan, Ph.D. 
Chief Business Officer 

Rexahn Pharmaceuticals, Inc. 
15245 Shady Grove Road, Suite 455 
Rockville, MD 20850 
Phone: 240-268-5300 
www.rexahn.com 

TRANSFER AGENT    
TRANSFER AGENT
TRANSFER AGENT
TRANSFER AGENT

Olde Monmouth Stock Transfer Co., Inc. 
Matthew J. Troster  
200 Memorial Parkway 
Atlantic Highlands, NJ  07716 
Phone: 732-872-2727 

LEGAL COUNSEL    
LEGAL COUNSEL
LEGAL COUNSEL
LEGAL COUNSEL

Hogan Lovells US LLP 
100 International Drive, Suite 2000 
Baltimore, MD 21202 

INDEPENDENT REGISTER
INDEPENDENT REGISTEREDEDEDED    
INDEPENDENT REGISTER
INDEPENDENT REGISTER
PUBLIC ACCOUNTING FIRMRMRMRM        
PUBLIC ACCOUNTING FI
PUBLIC ACCOUNTING FI
PUBLIC ACCOUNTING FI

Baker Tilly Virchow Krause, LLP 
2609 Keiser Blvd 
Wyomissing, PA 19610-3338 

SECURITIES INFORMATIONONONON    
SECURITIES INFORMATI
SECURITIES INFORMATI
SECURITIES INFORMATI

TRADING MARKET: NYSE MKT 
SYMBOL: RNN 

FOR INVESTOR RELATIONS INQUIRIES OR 
TO REQUEST ADDITIONAL COPIES OF THIS 
ANNUAL REPORT, CONTACT: 

LifeSci Advisors, LLC 
Matthew P. Duffy 
(212)-915-0685 
matthew@lifesciadvisors.com 

Stockholders may obtain a copy of any 
exhibit to our Form 10-K free of charge by 
writing to the company at our corporate 
headquarters address above.