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The discovery and development of boceprevir
1Montclair State University, Department of Chemistry and Biochemistry , 1 Normal Avenue Montclair NJ 07043 , USA +1 973 655 7204 ; +1 973 655 7772 ; rotellad@mail.montclair.edu.
Expert Opinion on Drug Discovery
|October 2, 2013
Summary
Boceprevir, the first direct-acting hepatitis C virus (HCV) agent, targets NS3 protease for viral replication. While effective, some patients don't achieve sustained viral response, and side effects like anemia occur.
Area of Science:
- Hepatology
- Virology
- Drug Discovery
Background:
- Boceprevir was the first direct-acting antiviral agent developed for hepatitis C virus (HCV) infection.
- It targets the viral NS3 protease, an enzyme critical for HCV replication.
- This peptidomimetic drug was optimized for oral bioavailability and combined with other agents to achieve sustained viral response in Genotype 1 HCV patients.
Purpose of the Study:
- To review the pre-clinical and clinical discovery of boceprevir.
- To discuss the role and function of its molecular target, NS3 protease.
- To outline the assays and clinical studies used to evaluate boceprevir's efficacy and safety.
Main Methods:
- Review of pre-clinical research and development.
- Analysis of in vitro efficacy assays.
- Examination of clinical trial data for safety and efficacy.
Main Results:
- Boceprevir demonstrated efficacy in achieving sustained viral response in Genotype 1 HCV patients when combined with ribavirin and peg interferon.
- The drug targets the essential NS3 protease enzyme.
- Clinical studies established its safety and efficacy profile.
Conclusions:
- Boceprevir marked a significant advancement as the first direct-acting anti-HCV therapy.
- Limitations include a 30% rate of non-response and 11% incidence of anemia/neutropenia.
- Ongoing research aims to develop improved therapeutic options for HCV.
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