1241946-89-3

Simeprevir is an orally bioavailable and potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A) protease (K_i = 0.36 nM), a serine protease essential for HCV replication. It inhibits HCV viral replication with an EC₅₀ value of 7.8 nM in Huh7 replicon cells using a luciferase-based assay. Simeprevir is effective against the HCV genotypes 1a and 1b in biochemical assays. In Huh7 replicon cells, it is synergistically effective when used in combination with IFN-α or NM-107 and has an additive effect when used with ribavirin . Formulations containing simeprevir have been used, alone or in combination with pegylated IFN-α and ribavirin, for the treatment of HCV.