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Pharmasset Nominates PSI-7851 as a Lead Development Candidate for the Treatment of Chronic Hepatitis C
Date:5/19/2008

- IND or foreign regulatory equivalent filing anticipated in 1Q 2009 -

PRINCETON, N.J., May 19 /PRNewswire-FirstCall/ -- Pharmasset, Inc. (Nasdaq: VRUS) has nominated PSI-7851 as a lead development candidate for the treatment of chronic hepatitis C virus (HCV). PSI-7851 is a proprietary nucleotide analogue polymerase inhibitor of HCV that is being advanced into Good Laboratory Practice (GLP) animal toxicity studies required for submission of an Investigational New Drug (IND) application with the FDA or an equivalent foreign regulatory filing. PSI-7851 has demonstrated in vitro potency that is approximately 15- to 20-fold greater than the in vitro potency of R7128, a nucleoside analog polymerase inhibitor of HCV that Pharmasset is developing through its collaboration with Roche.

"Our in-house research team has, once again, discovered a new potential product candidate for the treatment of chronic HCV," stated Dr. Michael Otto, Pharmasset's Chief Scientific Officer. "Our goal continues to be the identification of anti-HCV compounds with improved potency, equivalent or improved safety and oral bioavailability. In addition, we have focused on increasing intrahepatic triphosphate levels, which may lead to a higher level of active drug in the liver. We anticipate completing the required animal toxicity studies and filing an IND in the first quarter of 2009."

Nucleotide analogs have shown the ability to deliver higher levels of the active triphosphate form of the drug into infected cells. PSI-7851 has demonstrated in vitro anti-HCV activity with EC90 values of 0.31 +/- 0.12 uM, which is approximately 15- to 20-fold more potent than the active metabolite of R7128, PSI-6130. In vitro studies of PSI-7851 have not shown evidence o
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SOURCE Pharmasset, Inc.
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3. Pharmasset Commences Dosing in 28-Day Combination Study of R7128 with Pegasys(R) plus Copegus(R) for Hepatitis C
4. Pharmasset Announces Clevudine and R7128 Presentations at HEP-DART
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