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Grazoprevir is an antiviral and NS3/4A protease inhibitor used to treat hepatitis C infections. HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients.
- Mechanism
- Curator reviewed
Grazoprevir is a second generation NS3/4a protease inhibitor used to inhibit viral HCV replication. NS3/4a protease is an integral part of viral replication and mediates the cleavage the virally encoded polyprotein to mature proteins (NS3, NS4A, NS4B, NS5A and NS5B). Grazoprevir inhibits the NS3/4protease enzymes of HCV genotype 1a, 1B, and 4 with IC50 values of 7pM, 4pM, and 62pM, respectively.
- Primary indication
- Grazoprevir is indicated in combination with DB11574 (as the fixed dose combination product Zepatier) with or without DB00811 for treatment of chronic HCV genotypes 1a, 1b, or 4 infection in adults.Curator reviewed · 4 structured indications
- Formula / weight
- C38H50N6O9S · 766.903 g/mol (avg)
- First approval
- Canada, 2016 · United States, 2016 · European Union, 2016
- Code names
- MK-5172
- Brand names
- Zepatier
Resolves to
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Which drugs share a target with Grazoprevir, and which of those have an active Phase 3 trial?