grazoprevir

J05AP11

Forms & Strengths

Adult Dosing

Chronic hepatitis C genotype 1 or 4 infection: One tablet (elbasvir 50 mg / grazoprevir 100 mg) orally once daily with or without food for 12 weeks
Genotype 1a infection with baseline NS3 resistance-associated polymorphisms: Add weight-based ribavirin and extend duration to 16 weeks
Genotype 4 infection with baseline failure risks or prior treatment failure: Add ribavirin or extend duration based on specific patient factors

Pediatric Dosing

Safety and efficacy have not been established in pediatric patients less than 18 years of age

Indications

Treatment of chronic hepatitis C virus (HCV) genotype 1 or 4 infection in adults
Used in combination with elbasvir, with or without ribavirin

Mechanism of Action

HCV NS3/4A protease inhibitor that prevents viral replication by blocking the cleavage of the HCV encoded polyprotein

Contraindications

Moderate to severe hepatic impairment (Child-Pugh B or C)
History of hepatic decompensation
Co-administration with strong CYP3A inducers (e.g., efavirenz, rifampin, St. John's wort)
Co-administration with OATP1B1/3 inhibitors that significantly increase plasma concentrations (e.g., atazanavir, darunavir, lopinavir, saquinavir, tipranavir, cyclosporine)

Adverse Reactions

Fatigue
Headache
Nausea
Pruritus
Insomnia
Elevated ALT/AST (transient hepatic enzyme elevations, typically occurring around week 4 of therapy)

Drug Interactions

Strong CYP3A inducers (e.g., carbamazepine, phenytoin, rifampin, St. John's wort) significantly decrease grazoprevir plasma concentrations and therapeutic efficacy
OATP1B1/3 inhibitors (e.g., cyclosporine) significantly increase grazoprevir plasma concentrations, raising the risk of ALT elevations
Statins (e.g., atorvastatin, rosuvastatin): grazoprevir increases exposure, potentially increasing the risk of myopathy or rhabdomyolysis
Tacrolimus: co-administration may increase blood concentrations of tacrolimus

Curated Content: Needs Vetting Before Put to Clinical Use