GS-9451 has been identified as a specific HCV NS3 protease inhibitor and is currently in phase 2 clinical development for the treatment of chronic genotype 1 (GT1) HCV infection.  It has an in vitro EC50 ranging from 7-10 nM in both HCV 1a and 1b replicon assays and is highly selective (> 20000-fold) over all tested mammalian proteases.  It exhibited .good aqueous solubility and excellent pharmacokinetic properties in animal model studies.  We will discuss the SAR and pharmacokinetic optimizations that lead to the discovery of GS-9451.

Discovery of the novel HCV NS3 protease inhibitor, GS-9451

242nd National Meeting (2011)

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