Rexahn Pharmaceuticals Announces Publication of Preclinical Data for RX-3117 Demonstrating Effectiveness Against Gemcitabine ...
January 06 2015 - 9:00AM
Rexahn Pharmaceuticals, Inc. (NYSE MKT:RNN), a clinical stage
biopharmaceutical company developing best-in-class therapeutics for
the treatment of cancer, today announced the online publication of
preclinical results for RX-3117 in the peer reviewed medical
journal, Anticancer Research, in an article titled, "A Novel
Cytidine Analog, RX-3117, Shows Potent Efficacy in Xenograft
Models, Even in Tumors that are Resistant to Gemcitabine". The
article was coauthored by Dr. G.J. Peters of the VU University of
The Netherlands and Rexahn scientists.
In this study, the efficacy of orally administered RX-3117 was
examined in nine different human tumor Xenograft models that had
differing degrees of resistance to gemcitabine. In the four high
gemcitabine resistant models gemcitabine treatment resulted in 0%
to 30% tumor growth inhibition, whereas oral treatment with RX-3117
induced tumor growth inhibition between 62% to 100%. RX-3117 was
also evaluated in a primary low passage Champions Tumorgraft™ model
derived from biopsy samples from pancreatic cancer patients with
known resistance to gemcitabine. In this model, RX-3117 produced a
76% inhibition of tumor growth, as compared to gemcitabine which
had tumor growth inhibition of 38%.
Dr. Staffan Eriksson, MD, PhD, Professor, Department of Anatomy,
Physiology and Biochemistry at The Swedish University of
Agricultural Sciences commented, "The Champions Tumorgraft™ model
used cancer cells, and their microenvironment, taken from
individual cancer patients and then transplanted directly into a
mouse Xenograft model, making the results potentially more
predictive for the outcome of clinical trials. The fact that
RX-3117 was active against cells partially resistant to gemcitabine
makes these results very promising for future drug development
efforts which may be of great benefit to many cancer patients."
Peter D. Suzdak, Ph.D., Rexahn's Chief Executive Officer,
commented, "The ability of RX-3117 to inhibit the growth of
gemcitabine resistant human cancers cells is very exciting.
Moreover, the pronounced anti-tumor effects of RX-3117 in the
Champions Tumorgraft™ model are of particular importance because
the cancer cells used in this model are derived directly from
biopsies taken from pancreatic cancer patients who have shown
gemcitabine resistance. Resistance to the anti-cancer effects of
gemcitabine represents a major clinical issue in the treatment of
cancer patients. Up to 40% of cancer patients receiving one or more
cycles of gemcitabine rapidly become resistant to its anti-cancer
activity. Based on study results to date, both preclinical and
clinical, we believe RX-3117 holds the potential to be used for the
treatment of tumors that do not respond to gemcitabine."
About RX-3117
RX-3117 is a novel small molecule anti-metabolite that is
incorporated into DNA or RNA of cells and inhibits both DNA and RNA
synthesis which induces apoptotic cell death of tumor cells.
RX-3117 also mediates the downregulation of DNA methyltransferase 1
(DNMT1), an enzyme responsible for the methylation of cytosine
residues on newly synthesized DNA and also a target for anticancer
therapies. Preclinical studies have shown RX-3117 to be effective
in both inhibiting the growth of various human cancer xenograft
models, including colon, lung, renal and pancreas, as well as
overcoming chemotherapeutic drug resistance.
RX-3117 has demonstrated a broad spectrum anti-tumor activity
against 50 different human cancer cell lines and efficacy in 12
different mouse xenograft models. The efficacy in the mouse
xenograft models was superior to that of gemcitabine. In addition,
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, Rexahn 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
RX-3117 demonstrated an oral bioavailability of 56% and a plasma
half-life (T1/2) of 14 hours. In addition, RX-3117 was safe and
well tolerated in all subjects throughout the dose range
tested.
Rexahn initiated a Phase Ib clinical trial of RX-3117 in cancer
patients with solid tumors in January 2014. The Phase Ib clinical
trial is a multi-center dose-escalation study that will evaluate
the safety, tolerability, dose-limiting toxicities and maximum
tolerated dose (MTD) of RX-3117 in patients with solid tumors.
Secondary endpoints will include characterizing the pharmacokinetic
profile of RX-3117 and evaluating the preliminary anti-tumor
effects of RX-3117. Patient enrollment has been completed in five
dose groups (30, 60, 100, 150 and 200 mg) and patients are now
enrolling for the sixth dose group (500 mg). The MTD of RX-3117 has
not yet been achieved. The Company expects to complete patient
enrollment of the RX-3117 Phase Ib clinical trial early in
2015.
About Rexahn Pharmaceuticals, Inc.
Rexahn Pharmaceuticals is a clinical stage biopharmaceutical
company dedicated to developing best-in-class therapeutics for the
treatment of cancer. Rexahn currently has three clinical stage
oncology candidates, Archexin®, RX-3117 and SupinoxinTM (RX-5902)
and a robust pipeline of preclinical compounds to treat multiple
types of cancer. Rexahn has also developed proprietary drug
discovery platform technologies in the areas of Nano-Polymer-Drug
Conjugate Systems (NPDCS), nano-medicines, 3D-GOLD, and TIMES. For
more information, please visit www.rexahn.com.
Safe Harbor
To the extent any statements made in this press release deal
with information that is not historical, these are forward-looking
statements under the Private Securities Litigation Reform Act of
1995. Such statements include, but are not limited to, statements
about Rexahn's plans, objectives, expectations and intentions with
respect to cash flow requirements, future operations and products,
enrollments in clinical trials, the path of clinical trials and
development activities, and other statements identified by words
such as "will," "potential," "could," "can," "believe," "intends,"
"continue," "plans," "expects," "anticipates," "estimates," "may,"
other words of similar meaning or the use of future dates.
Forward-looking statements by their nature address matters that
are, to different degrees, uncertain. Uncertainties and risks may
cause Rexahn's actual results to be materially different than those
expressed in or implied by Rexahn's forward-looking statements. For
Rexahn, particular uncertainties and risks include, among others,
the difficulty of developing pharmaceutical products, obtaining
regulatory and other approvals and achieving market acceptance; the
success and design of clinical testing; and Rexahn's need for and
ability to obtain additional financing. More detailed information
on these and additional factors that could affect Rexahn's actual
results are described in Rexahn's filings with the Securities and
Exchange Commission, including its most recent annual report on
Form 10-K and subsequent quarterly reports on Form 10-Q. All
forward-looking statements in this news release speak only as of
the date of this news release. Rexahn undertakes no obligation to
update or revise any forward-looking statement, whether as a result
of new information, future events or otherwise.
CONTACT: The Trout Group LLC
Tricia Truehart
(646) 378-2953
ttruehart@troutgroup.com