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November 27, 2025
Brand Name :
Zepatier
Synonyms :
elbasvir/grazoprevir
Class :
HCV NS3/4A Protease Inhibitors, HCV NS5A Inhibitors
Dosage Forms & Strengths
Tablet
50mg/100mg
Dosage Forms & Strengths
Tablet
50mg/100mg
Refer adult dosing
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may decrease the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of elbasvir/grazoprevir
OATP1B1/1B3 (SLCO1B1/1B3) inhibitors increase the concentration of elbasvir and grazoprevir in the serum
OATP1B1/1B3 (SLCO1B1/1B3) inhibitors increase the concentration of elbasvir and grazoprevir in the serum
OATP1B1/1B3 (SLCO1B1/1B3) inhibitors increase the concentration of elbasvir and grazoprevir in the serum
OATP1B1/1B3 (SLCO1B1/1B3) inhibitors increase the concentration of elbasvir and grazoprevir in the serum
OATP1B1/1B3 (SLCO1B1/1B3) inhibitors increase the concentration of elbasvir and grazoprevir in the serum
may enhance the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may increase the hypoglycemic effect of direct-acting antiviral agents
may increase the hypoglycemic effect of direct-acting antiviral agents
may increase the hypoglycemic effect of direct-acting antiviral agents
may increase the hypoglycemic effect of direct-acting antiviral agents
may increase the hypoglycemic effect of direct-acting antiviral agents
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may decrease the anticoagulant effect of direct-acting antiviral agents
may decrease the anticoagulant effect of direct-acting antiviral agents
may decrease the anticoagulant effect of direct-acting antiviral agents
may decrease the anticoagulant effect of direct-acting antiviral agents
may decrease the anticoagulant effect of direct-acting antiviral agents
Actions and Spectrum:
elbasvir targets the NS5A protein, which is crucial in viral replication, assembly, and secretion. By inhibiting NS5A, elbasvir prevents the production of new infectious virus particles and slows down the progression of the infection.
grazoprevir targets the NS3/4A protease, essential for viral replication and maturation. By inhibiting NS3/4A, grazoprevir blocks the cleavage of viral proteins and prevents the formation of new infectious virus particles.
Combining elbasvir and grazoprevir has a synergistic effect in treating chronic HCV infection. The two medications target different stages of the viral life cycle and can prevent the emergence of drug-resistant virus strains.
elbasvir/grazoprevir has a broad spectrum of activity against all six major genotypes of the HCV virus. It effectively treats treatment-naive and treatment-experienced patients, including those with compensated cirrhosis and HIV coinfection.
Frequency defined
>10%
Adults
Headache, treatment-naïve (10-11%)
Fatigue, treatment-naïve (5-11%)
Pediatric
Headache (14%)
1-10%
Adults
Treatment-experienced
Depression (2%)
Diarrhea (1%)
Fatigue (2%)
Irritability (5%)
Abdominal pain (1%)
Treatment-experienced plus ribavirin
Depression (2%)
Arthralgia (8%)
Headache (4%)
Irritability (4%)
Dyspnea (4%)
Rash or pruritus (2%)
Fatigue (3%)
Abdominal pain (6%)
Anemia (2%)
Pediatric patients
Nausea (9%)
Post-marketing reports
Hepatic decomposition
Angioedema
Hepatic failure
Hepatitis B Virus reactivation:
Before therapy, check all patients for HBV infection. HBV reactivation has been recorded in HCV/HBV coinfected individuals taking HCV direct acting antivirals but not HBV antiviral medication.
Symptoms include fulminant hepatitis, hepatic failure, and death. Monitor HCV/HBV coinfected patients for hepatitis flare or HBV reactivation during and after HCV therapy. Clinically suggested HBV patient management
Contraindications:
Caution:
Pregnancy consideration: Insufficient data available
Lactation: Excretion of the drug in human breast milk is unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
Pharmacodynamics:
Pharmacokinetics:
Absorption
elbasvir is rapidly absorbed, with a peak plasma concentration occurring approximately 3 hours after oral administration. grazoprevir is slowly absorbed, with a peak plasma concentration occurring at approximately 2-3 hours after oral administration
Distribution
Both elbasvir and grazoprevir are highly protein-bound, with binding rates of approximately 99%. The volume of distribution for elbasvir is approximately 441 L, while the volume for grazoprevir is approximately 214 L
Metabolism
CYP3A4 and CYP2C8 enzymes primarily metabolize elbasvir.CYP3A4 and UGT1A1 enzymes primarily metabolize grazoprevir
Elimination and excretion
The elimination half-life for elbasvir is approximately 24 hours. The elimination half-life for grazoprevir is approximately 31 hours. Both elbasvir and grazoprevir are primarily eliminated via the fecal route, with only small amounts excreted in the urine.
Administration:
Oral administration:
Take it with or without food
Storage:
Storage at 20-25°C (68-77°F); excursions allowed 15-30°C (59-86°F)
Patient information leaflet
Generic Name: elbasvir/grazoprevir
Pronounced: [ ELB-as-vir-and-graz-OH-pre-vir ]
Why do we use elbasvir/grazoprevir?