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Published on: February 1, 2017
Development of boceprevir: a first-in-class direct antiviral treatment for chronic hepatitis C infection
Daria J Hazuda1, Margaret Burroughs, Anita Y M Howe
1Merck Research Laboratories, West Point, Pennsylvania 19486, USA. Daria_hazuda@merck.com
Abstract:
The identification of hepatitis C virus (HCV) as the causative agent of non-A and non-B hepatitis, over 20 years ago, fueled an intensive effort to develop direct-acting antivirals targeting the viral polymerase and protease, two key proteins critical for HCV replication. However, it took more than two decades for these efforts to be realized with boceprevir, one of the two HCV protease inhibitors approved for treatment of HCV infection in 2011. The development of boceprevir is a major advancement in the ability to treat HCV infection and a significant step toward the long-term goal of eradicating chronic HCV infection. Both as a first-in-class agent and an entirely new modality for treating HCV infection, many challenges were encountered during the discovery and development of this compound. The lessons learned in overcoming these obstacles offer insights and pave the way for the newly emerging field of HCV antiviral therapeutics. This paper will describe the discovery and development of a first-in-class direct antiviral treatment for chronic hepatitis C infection, boceprevir, marketed around the world as Victrelis™.
Insights
Boceprevir, a direct-acting antiviral, was developed to target hepatitis C virus (HCV) protease. This breakthrough treatment offers a new modality for managing chronic HCV infection.
Area of Science:
- Hepatology
- Virology
- Drug Discovery
Background:
- Hepatitis C virus (HCV) identified as cause of non-A, non-B hepatitis over 20 years ago.
- Intensive research focused on direct-acting antivirals targeting viral polymerase and protease.
- Over two decades of effort led to the development of HCV protease inhibitors.
Purpose of the Study:
- Describe the discovery and development of boceprevir.
- Highlight boceprevir as a first-in-class direct antiviral treatment for chronic hepatitis C.
- Discuss challenges and lessons learned in developing novel HCV therapeutics.
Main Methods:
- Targeted development of direct-acting antivirals.
- Focus on inhibiting key viral proteins: polymerase and protease.
- Clinical trials and regulatory approval processes for boceprevir.
Main Results:
- Boceprevir approved in 2011 as one of the first HCV protease inhibitors.
- Represents a major advancement in treating HCV infection.
- Paved the way for new HCV antiviral therapeutics.
Conclusions:
- Boceprevir's development signifies a milestone in HCV treatment.
- Lessons from its discovery inform future antiviral drug development.
- Offers a new therapeutic modality for chronic HCV infection, aiding eradication efforts.
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