Drug reference

grazoprevir

NS3 protease inhibitor · Antiviral, Hepatitis C agent

NS3 protease inhibitorAntiviral, Hepatitis C agent

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

—

not curated

Top interactionssee all 12 →

Moderate Or Strong Cyp3a InducersContraindicatedTextbookHarrison 22e · unknown
Strong Cyp3a InhibitorsContraindicatedTextbookHarrison 22e · unknown
Hiv Protease InhibitorsSevereTextbookG&G 14e · p1241, p1242
Moderate Cyp3a InducersSevereTextbookG&G 14e · p1241, p1242

Mechanism

Grazoprevir is an inhibitor of the non-structural protein 3 (NS3) protease of the hepatitis C virus, which is crucial for viral polyprotein processing and replication.

Indications

HCV genotypes 1 and 4 (as part of fixed-dose combination with elbasvir)Patients with renal impairment (as part of fixed-dose combination with elbasvir, preferred treatment)Genotype 1a patients with preexisting NS5A RASs (as part of fixed-dose combination with elbasvir and ribavirin, extended duration)

Dosing

Adult: 100 mg (as part of fixed-dose combination with elbasvir) once daily
Renal adjustment: No specific adjustment needed, preferred treatment in renal impairment

Pharmacokinetics

Half-life

Approximately 30 h

Bioavailability

10%–40%

Protein binding

Extensively (~99%) bound

Metabolism

Substrate for CYP3A4

Excretion

Less than 1% renally eliminated

Contraindications

Advanced liver disease
Moderate or severe hepatic impairment (Child-Pugh B or C)
Concomitant use with HIV protease inhibitors (OATP1B1 inhibitors)
Concomitant use with moderate or strong CYP3A and P-gp inducers (including efavirenz)

Side effects

Common

HeadacheFatigueNausea

Serious

Liver function test elevations (with higher exposures)

Drug interactions

Moderate Or Strong Cyp3a Inducers

Contraindicated

Textbook

Potential for reduced plasma levels and loss of efficacy of grazoprevir.

Coadministration with moderate or strong CYP3A inducers is not recommended.

Source: Harrison 22e · unknown

Strong Cyp3a Inhibitors

Contraindicated

Textbook

Potential for increased plasma levels and adverse effects of grazoprevir.

Coadministration with strong CYP3A inhibitors is not recommended.

Source: Harrison 22e · unknown

Hiv Protease Inhibitors

Severe

Textbook

Increased grazoprevir exposures.

HIV protease inhibitors are not recommended for coadministration with GZR/EBR. Should not be used with OATP1B1 inhibitors.