elbasvir and grazoprevir

ATC code

J05AP54

Therapeutic class

Systemic antivirals and immunoprophylaxis · Oral NS5A/NS3-4A combination for HCV

Forms

Elbasvir 50 mg/grazoprevir 100 mg tablet

Brand names

Zepatier (US)

Overall confidence

high

Regulatory sources consulted

Approved indications

Treatment of chronic genotype 1 or 4 HCV infection in adults and pediatric patients aged at least 12 years or weighing at least 30 kg.

Contraindications

Absolute

Moderate or severe hepatic impairment.
Use of OATP1B1/3 inhibitors or strong CYP3A inducers.
History of hepatic decompensation.
Concomitant efavirenz.

Clinical warnings

Assess HBV before starting because of reactivation risk during or after treatment. — DailyMed, set_id 164dc02a-9180-426a-b8b5-04ab39d2bbd4
Major warning · It may cause late ALT elevations; monitor liver tests before treatment, at week 8, and as indicated. — DailyMed, set_id 164dc02a-9180-426a-b8b5-04ab39d2bbd4
Major warning · For genotype 1a, test NS5A polymorphisms at positions 28, 30, 31, or 93 before treatment to select duration and ribavirin use. — DailyMed, set_id 164dc02a-9180-426a-b8b5-04ab39d2bbd4

Drug interactions

ModerateRifampicin, carbamazepine, phenytoin, or St John’s wort
Mechanism: They reduce exposure and antiviral efficacy.
Recommendation: Do not combine.
DailyMed, set_id 164dc02a-9180-426a-b8b5-04ab39d2bbd4
ModerateVitamin K antagonists and antidiabetic agents
Mechanism: Improved hepatic function after HCV clearance may change INR or glycemic control.
Recommendation: Closely monitor INR or glucose and adjust concomitant treatment when needed.
DailyMed, set_id 164dc02a-9180-426a-b8b5-04ab39d2bbd4

Adverse events

Common (≥1%)

Fatigue, headache, and nausea

Rare but serious

HBV reactivation and severe hepatotoxicity

Pregnancy and lactation

Avoid during pregnancy if ribavirin is used; without ribavirin, use only if benefit justifies risk. Decide on breastfeeding according to benefit and risk.

Recent literature (PubMed)

Elbasvir and grazoprevir for the treatment of hepatitis C.
Wang SJ, et al. · Expert Rev Anti Infect Ther · 2021 · Relevance 1/5
Introduction: Hepatitis C is one of the leading causes of chronic liver disease. The direct-acting-antivirals has revolutionized the chronic hepatitis C treatment. DAAs can achieve a sustained virological response rate >95% in different populations.Area covered: This review summarizes the pharmacokinetics, pharmacodynamics, efficacy, and safety of Elbasvir/Grazoprevir (EBR/GZR).Expert opinion: EBR/GZR is a combination of NS5A and NS3/4A inhibitors. The performance in the EBR/GZR combination's safety and tolerability is appreciated in clinical treatment. EBR/GZR also has a higher barrier to resistance-associated substitutions. Based on clinical trials and real-world experience, elbasvir/grazoprevir is effective in the HCV GT1, 4 infections.