Approximately 3% (170 million) of the world's population are infected with hepatitis C virus (HCV).  Greater than 350,000 deaths per year are attributed to HCV related illnesses.  The current optimal therapy consists of pegylated interferon (IFN), ribavirin and one of two approved small molecule, direct acting antiviral (DAA), HCV protease inhibitors.  A considerable amount of preclinical and clinical research aimed at achieving shorter duration of treatment, improved tolerability, or Peg-IFN alfa free combination regimens is ongoing in the rapidly evolving, global effort to address this disease.  This presentation will describe the discovery and preclinical profile of BMS-791325, an allosteric inhibitor of HCV NS5B replicase, which is currently in Phase II clinical trials designed to explore its use in combination therapy against HCV.  BMS-791325 is a potent inhibitor of both 1a and 1b HCV virus in replicon studies and displayed pharmacokinetics in three species which supported advancement to clinical studies.

Discovery of BMS-791325, an allosteric NS5B replicase inhibitor for the treatment of Hepatitis C

243rd National Meeting (2012)

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