Hepatitis C virus (HCV) infection is the major cause of chronic liver disease leading to cirrhosis and hepatocellular carcinoma, which affects more than 170 million people worldwide.  Before the development of boceprevir, the standard of care treatment for chronic HCV infection was a combination of PEG-interferon (P) with oral ribovirin (R).  Although PR therapy is reasonably successful with the majority of genotypes, its efficacy against the genotype 1 and relapse patients is moderate, with only about 40% of the patients showing sustained virological response. Lack of effective methods to treat chronic HCV infections and patients relapsing from interferon therapy required the discovery of new drugs.  The nonstructural protein, NS3, is a serine protease that plays a significant role in HCV replication.  The NS3 protease has a shallow and solvent-exposed substrate binding region which presents a challenge for drug discovery.  In this presentation, we discuss the discovery and development of boceprevir, a novel, potent, selective, orally bioavailable NS3 protease inhibitor, which was the first direct acting antiviral marketed for HCV treatment.

Discovery and development of Boceprevir, an HCV NS3 protease inhibitor, for the treatment of hepatitis C infection

243rd National Meeting (2012)

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