Products
Grazoprevir was approved in many countries in 2015 as film-coated tablets in fixed combination with the NS5A inhibitor elbasvir (Zepatier).
Structure and properties
Grazoprevir (C38H52N6O10S, Mr = 784.9 g/mol)
Effects
Grazoprevir has antiviral properties. The effects are due to inhibition of HCV protease, which converts the viral polyprotein into the active proteins. The protease plays an important role in viral replication. Grazoprevir has a long half-life of 31 hours.
Indications
For the treatment of chronic hepatitis C (genotype 1 or 4).
Dosage
According to the SmPC. Tablets are taken once daily, regardless of meals. The duration of treatment is 12 or 16 weeks.
Contraindications
For complete precautions, see the drug label.
Interactions
Grazoprevir is a substrate of OATP1B1/3, CYP3A4, and P-glycoprotein.
Adverse effects
The most common potential adverse effects of the fixed combination include fatigue, headache, and nausea.
