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Pharmacopeia Initiates Phase 2 Hypertension Study with PS433540 (DARA)
Date:9/17/2007

First internal candidate to enter Phase 2 clinical development

PRINCETON, N.J., Sept. 17 /PRNewswire-FirstCall/ -- Pharmacopeia (Nasdaq: PCOP), an innovator in the discovery and development of novel small molecule therapeutics, today announced the initiation of a Phase 2a 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 proven 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. Preclinical studies have shown that PS433540 is highly selective 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 are considerable preclinical and initial clinical 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.

The objective of the Phase 2a randomized, double-blind, placebo- controlled, parallel-group study is to evaluate the compound's safety and efficacy in subjects with Stage I and Stage II hypertension. This multi- center trial is expected to enroll 170 subjects. After a lead-in period, patients will be randomized into three study arms (placebo and two active arms
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