Boceprevir

The antiviral agent boceprevir is a protease inhibitor that covalently and reversibly binds to the catalytic site (Ser139) of hepatitis C virus (HCV) nonstructural protein 3/4A (NS3/4A), a serine protease that is essential for viral replication (Ki = 14nM) by cleaving the virally encoded polyprotein into mature proteins like NS4A, NS4B, NS5A and NS5B. It inhibits the NS3/4A protease in an in vitro HCV replicon system with an EC50 value of 200 nM.Boceprevir has been identified as a potential inhibitor of SARS-CoV-2 responsible for COVID-19. It inhibits SARS-CoV-2 viral replication by targeting the viral main protease Mpro (IC50 = 4.13µM).