Rexahn Initiates Phase Ib Clinical Trial of RX-3117 for Treatment of Solid Tumors
January 08 2014 - 7:00AM
Business Wire
RX-3117 has Shown Efficacy Against
Gemcitabine-Resistant Human Cancer Cell Lines and a Broad-Spectrum
of Anti-Cancer Activity
Rexahn Pharmaceuticals, Inc. (NYSE MKT: RNN) a clinical stage
biopharmaceutical company, announced today the initiation of a
Phase Ib clinical trial to study the safety and efficacy of RX-3117
in cancer patients with solid tumors.
RX-3117 is a next-generation cancer cell specific drug candidate
that possesses a broad spectrum of anticancer activity with reduced
side effects. In an exploratory Phase I clinical trial conducted in
Europe, RX-3117 demonstrated oral bioavailability, and safety and
tolerability in cancer patients with solid tumors. The compound has
also shown efficacy in human cancer cell lines resistant to
gemcitabine (one of the most widely used chemotherapy drugs on the
market today). Resistance to the anti-cancer effects of gemcitabine
represents a major clinical issue in the treatment of cancer
patients, as it has been estimated that up to 25% of cancer
patients receiving one or more cycles of gemcitabine rapidly become
resistant to its anti-cancer activity.
The Phase Ib trial is a multi-center dose-escalation study which
will evaluate the safety, tolerability, dose-limiting toxicities
and maximal 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.
The trial is expected to enroll up to 30 patients from multiple
sites in the United States. Patients will receive RX-3117 orally 3
times a week for 3 weeks followed by 1 week off, and will have the
ability to continue on the drug for up to 8 cycles of treatment.
The decision to enroll the next group of patients and escalate the
dose will be made after 1 cycle of treatment, based on safety and
tolerability. Patients will be assessed for tumor progression by CT
or MRI prior to the start of therapy and after every 2 cycles of
therapy. Rexahn expects to complete enrollment of patients by the
end of 2014, and data is expected in the first half of 2015.
“The initiation of this Phase I clinical trial of RX-3117
represents an important milestone for Rexahn,” added Peter D.
Suzdak, Ph.D., Rexahn’s Chief Executive Officer. “This compound is
exciting to work with, as it has a unique profile with demonstrated
activity against gemcitabine-resistant human cancer cells. We were
pleased to see reduced side effect liability and oral
bioavailability in cancer patients in our initial exploratory Phase
I clinical trial conducted in Europe, and we believe that RX-3117
may represent a significant advancement in the treatment of cancer
patients with solid tumors.”
Dr. Drew Rasco, MD, Clinical Investigator, South Texas
Accelerated Research Therapeutics in San Antonio, TX commented,
“Gemcitabine resistance represents a major problem in the treatment
of cancer patients with solid tumors. RX-3117 represents a very
interesting new approach for the treatment of cancer patients with
solid tumors who have become resistant to gemcitabine.”
About RX-3117
RX-3117 is a nucleoside analog that is activated
(phosphorylated) by Uridine Cytidine Kinase (UCK) and inhibits both
DNA and RNA synthesis which induces apoptotic cell death of tumor
cells. UCK is overexpressed in multiple human tumors, but has a
limited presence in normal tissues. This unique specificity for
cancer cells may lead to an improved safety profile in cancer
patients. RX-3117 also mediates the downregulation of DNA
methyltransferase 1 (DNMT1), which is an enzyme responsible for the
methylation of cytosine residues on newly synthesized DNA and is
also a key target for anti-cancer therapies. RX-3117 has broad
spectrum anti-tumor activity against 80 different human cancer cell
lines (including NSCLC, breast, ovarian, pancreas, colon, renal,
brain, bladder, cervical) and efficacy in 12 different mouse
xenograft models (including colorectal, non-small cell lung,
pancreatic and renal cell carcinoma) superior to that 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. The trial investigated the oral bioavailability, safety and
tolerability of RX-3117 in nine cancer patients with solid tumors.
Groups of three patients received single doses of RX-3117 and were
assessed for safety, tolerability and plasma exposure. In this
study, oral administration of RX-3117 demonstrated an oral
bioavailability of up to 56% and a plasma half-life (T1/2) of 14 –
21 hours. In addition, RX-3117 was safe and well tolerated in all
subjects throughout the dose range tested with no post-dose adverse
events, laboratory abnormalities or ECG changes emerging through 7
days of follow-up.
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 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 timing and success of clinical
testing; the timing of the conduct of clinical testing; the timing
of the receipt and disclosure of clinical data 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 LLCTricia Truehart,
646-378-2953ttruehart@troutgroup.com
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