Grazoprevir

Molecular Formula: C38H50N6O9S Molecular Weight: 766.9 Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively) . Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.