Boceprevir

Boceprevir

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Systematic (IUPAC) name
(1R,2S,5S)-N-[(2Ξ)-4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)]- 3-{(2S)-2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl}- 6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
Identifiers
CAS Number	394730-60-0
ATC code	none
Chemical data
Formula	C27H45N5O5
Molar mass	g·mol−1

Boceprevir (INN) is a protease inhibitor being studied as a treatment for hepatitis C.

It was being developed by Schering-Plough and has since been absorbed into the Merck's new pipeline since its acquired Schering in 2009. As of 2008, it is in phase II clinical trials (SPRINT-1 trial).

Phase 2 study results of Boceprivir were announced at the 44th annual meeting of the European Association for the Study of the Liver in Copenhagen in April, 2009. When used in combination with peginterferon alfa-2b and ribavirin, boceprivir use resulted in significantly higher sustained viral response (SVR) rates in the most difficult-to-treat patients with genotype 1.

The phase 2 trial compared 3 different regimens: 4 weeks of peginterferon alfa-2b (1.5 micrograms/kg once weekly) plus ribavirin (800 to 1400 mg daily based on patient weight) followed by boceprevir (800 mg 3 times a day in addition to peginterferon and ribavirin) for 24 weeks or 44 weeks; boceprevir in combination with peginterferon alfa-2b plus ribavirin as above for 28 or 48 weeks (triple therapy); and peginterferon alfa-2b plus low-dose ribavirin (400 to 1000 mg/day) and boceprevir for 48 weeks.

The patients enrolled in the SPRINT-1 study were among the most difficult to treat, and were comprised exclusively of those with genotype 1. (The patients were all treatment naive.) Additionally, many of the patients had other difficult-to-treat indices, including cirrhosis (6-9%), high viral load (90%) and African-American ancestry (14-17%). An SVR after 24 weeks off of therapy of 75% was achieved in the group treated for 48 weeks with 4 weeks of lead-in therapy with peginterferon alfa-2b plus ribavirin followed by the addition of boceprivir. This represents a near doubling of the rate of SVR compared to standard therapy without boceprivir in this group.

Anemia was the most common adverse event. It occurred in half of the patients who received boceprivir and by about a third of the patients taking peginterferon alfa-2b plus ribavirin at the standard dose.

The lead investigator of the study was Dr. Paul Kwo, associate professor of medicine at the School of Medicine, Indiana University, in Indianapolis, Indiana, USA.