Rexahn Pharmaceuticals, Inc. (NYSE MKT: RNN), a clinical stage
biopharmaceutical company developing potential best-in-class oncology
therapies, today announced the on-line publication of preclinical
results for RX-3117 in a peer reviewed medical journal, Investigational
New Drugs, in an article titled, "Metabolism, mechanism
of action and sensitivity profile of fluorocyclopentenylcytosine
(RX-3117; TV-1360)". Investigational New Drugs is an
interdisciplinary journal presenting the latest investigations and
discussions of critical questions appropriate to the entire field of new
anticancer drug development.
Peter D. Suzdak, Ph.D., Rexahn's Chief Executive Officer, commented,
"The broad spectrum of anti-tumor activity against human cancer cell
lines, oral bioavailability in cancer patients, and improved preclinical
and clinical safety profile suggest that RX-3117 may represent a major
advance in the treatment of solid cancer tumors. Rexahn anticipates
initiating a Phase I clinical study in cancer patients with solid tumors
in the fourth quarter of 2013."
The published study characterized the broad spectrum of potent
anti-tumor effects of RX-3117 against 50 different human cancer cell
lines (including colon, lung, renal and pancreas) and its unique
mechanism of activation in cancer cells. In addition, RX-3117 was shown
to be effective in gemcitabine resistant human cancer cell lines.
Although RX-3117 shares some properties with other nucleoside compounds
such as gemcitabine, its cytotoxicity profile, metabolism and mechanism
of action make it distinct and potentially clinically superior to
existing nucleoside compounds.
Prof. Dr. Godefridus J. (Frits) Peters, Head Laboratory Medical
Oncology, VU University Medical Center, Amsterdam, The Netherlands, and
lead author of the published results, commented, "RX-3117 is an exciting
new nucleoside analog with unique properties both regarding its
mechanism of action and its pharmacology. Its excellent oral
bioavailability fits very well with the current tendency to give
anticancer drugs orally. Its mechanism of action gives several leads for
future combination therapies with different drugs."
RX-3117 is a novel small molecule nucleoside compound that is
incorporated into DNA or RNA of cancer cells and inhibits both DNA and
RNA synthesis which induces apoptotic cell death of tumor cells. RX-3117
also mediates the down-regulation 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, in human cancer cell lines
made resistant to the anti-tumor effects of gemcitabine, RX-3117 still
retains its full anti-tumor activity.
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 34-58% 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.
The Investigational New Drug (IND) application for RX-3117 filed in July
2013 has now cleared the 30 day review period by the US Food and Drug
Administration (FDA). Rexahn expects to initiate a Phase I clinical
trial in cancer patients during the fourth quarter of 2013.
Additionally, Rexahn will be exploring potential partnering
opportunities with oncology focused pharmaceutical companies.
About Prof. Dr. Godefridus J. (Frits) Peters
Dr. Peters is head of the Laboratory Medical Oncology of the VU
University Medical Center in Amsterdam (the Netherlands). The research
of Prof. Peters is focused on translation of preclinical pharmacology of
anticancer agents to the clinic. Dr. Peters has published more than 500
peer reviewed articles, review chapters and abstracts in high profile
scientific journals. Drug classes studied include antifolates, other
antimetabolites, platinum analogs, topoisomerase inhibitors, taxanes and
more recently anti-signalling protein kinase inhibitors. He is/was a
member of 20 editorial boards, was founder and first president of the
Purine and Pyrimidine Society, and is chair of the EORTC-Pharmacology
and Molecular Mechanisms Group.
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.
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 future
operations and products 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 marketing success of Rexahn's licensees or sublicensees;
the success 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.
The Trout Group LLC
Tricia Truehart, 646-378-2953