Pharmacopeia
(Nasdaq: PCOP), an innovator in the discovery and development of novel
small molecule therapeutics, today announced the initiation of a Phase 1
clinical study of PS433540, the company's lead internal product candidate.
PS433540 is a Dual-Acting angiotensin and endothelin Receptor Antagonist
(DARA) that is being developed as a potential treatment for hypertension
and diabetic nephropathy. PS433540, the first and only DARA compound in
development, possesses two clinically validated mechanisms of action in a
single compound. The compound works by selectively blocking the action of
two potent vasoconstrictor and mitogenic agents, angiotensin II (AII) and
endothelin 1 (ET1), at their respective receptors. PS433540 is highly
selective (10,000- fold) for the AII receptor sub-type 1 and the ET
receptor sub-type A. As such PS433540 combines the properties of an
angiotensin receptor blocker (ARB) and an endothelin receptor antagonist
(ERA) in the same molecule. There is considerable preclinical data
suggesting that compared to either agent alone, simultaneously blocking the
actions of both AII and ET1 may provide significantly improved treatment
options for several cardiovascular diseases. In addition, studies to date
have demonstrated PS433540 to be safe and well tolerated in preclinical
studies with a pharmacokinetic profile consistent with an expected
once-daily oral dosing in humans.
"PS433540 is a first-in-class compound which, with its unique DARA
activity, could represent a significant advance in the treatment of
cardiovascular disease," said Rene Belder, M.D., Pharmacopeia's Vice
President of Clinical and Regulatory Affairs. "We are eager to complete
this initial clinical study and employ the results to design later-stage
trials to expedite the clinical development of this product candidate."
The objective of this randomized, placebo-controlled, dose-escalation
study is to evaluate the compound's preliminary safety and tolerability by
treating up to seven separate groups of healthy volunteers. Each group will
consist of eight people, with six individuals receiving the active DARA
compound and two receiving placebo. PS433540 doses administered to the
study subjects will increase for each successive group. In addition to
safety and tolerability, clinical investigators will also evaluate
dose-related pharmacokinetics.
"With the initiation of this trial, Pharmacopeia has achieved two of
its primary objectives," stated David Floyd, Ph.D., Executive Vice
President and Chief Scientific Officer of Pharmacopeia. "The first goal was
to successfully build an internal development capability to complement our
long-standing expertise in discovery. The second was to advance an internal
program into the clinic. Today, we have achieved both goals, and in doing
so, we have initiated a clinical program with a promising compound for the
potential treatment of hypertension and diabetic nephropathy."
ABOUT PHARMACOPEIA
Pharmacopeia is committed to discovering and developing novel
therapeutics to address significant medical needs. The Company has a broad
portfolio advancing towards clinical validation, both independently and
with partners. Pharmacopeia's most advanced internal program is a
dual-acting angiotensin and endothelin receptor antagonist (DARA) for
resistant hypertension and diabetic kidney disease for which a Phase 1
clinical trial is underway. Other internal proprietary programs address
immunoregulation. Four partnered programs are in active clinical trials: a
CXCR2 antagonist for chronic obstructive pulmonary disease (COPD), p38 MAP
kinase inhibitors for rheumatoid arthritis, an enzyme inhibitor for
oncology and a candidate for metabolic diseases. Four additional partnered
compounds are in preclinical development. Pharmacopeia's discovery,
development and commercialization partnerships are with leading
pharmaceutical companies including GlaxoSmithKline, Bristol-Myers Squibb,
Organon, Schering-Plough, Cephalon, Celgene, and Wyeth.
This press release, and oral statements made with respect to
information contained in this press release, constitute forward-looking
statements within the meaning of the Private Securities Litigation Reform
Act of 1995. Such forward-looking statements include those which express
plan, anticipation, intent, goal, contingency or future development and/or
otherwise are not statements of historical fact. These statements are based
upon management's current expectations and are subject to risks and
uncertainties, known and unknown, which could cause actual results and
developments to differ materially from those expressed or implied in such
statements. These forward- looking statements include, but are not limited
to, statements about the successful implementation of Pharmacopeia's
strategic plans, Pharmacopeia's plans to develop PS433540, a compound from
its DARA program, Pharmacopeia's Phase 1 clinical studies with respect to
PS433540, Pharmacopeia's ability to successfully perform under its
collaborations with Cephalon, GlaxoSmithKline, Organon and Wyeth,
Pharmacopeia's ability to build its pipeline of novel drug candidates
through its own internally-funded drug discovery programs, third party
collaborations and in-licensing, Pharmacopeia's ability to raise additional
capital, Pharmacopeia's expectations concerning the development priorities
of its collaborators, their ability to successfully develop compounds and
its receipt of milestones and royalties from the collaborations,
Pharmacopeia's anticipated operating results, financial condition,
liquidity and capital resources, Pharmacopeia's expectations concerning the
legal protections afforded by U.S. and international patent law,
Pharmacopeia's ability to pursue the development of new compounds and other
business matters without infringing the patent rights of others, additional
competition, and changes in economic conditions.
Further information about these and other relevant risks and
uncertainties may be found in Pharmacopeia's Reports on Form 8-K, 10-Q and
10-K filed with the U.S. Securities and Exchange Commission. Pharmacopeia
urges you to carefully review and consider the disclosures found in its
filings which are available in the SEC EDGAR database at sec
and from Pharmacopeia at pharmacopeia. All forward-looking
statements in this press release and oral statements made with respect to
information contained in this press release are qualified entirely by the
cautionary statements included in this press release and such filings.
These risks and uncertainties could cause actual results to differ
materially from results expressed or implied by such forward-looking
statements. These forward-looking statements speak only as of the date of
this press release. Pharmacopeia undertakes no obligation to (and expressly
disclaims any such obligation to) publicly update or revise the statements
made herein or the risk factors that may relate thereto whether as a result
of new information, future events, or otherwise.
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