Glecaprevir/Pibrentasvir
Mechanism :
Glecaprevir is an inhibitor of hepatitis C virus (HCV) NS3/4A protease, necessary for the proteolytic cleavage of the HCV-encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication.
Pibrentasvir is an inhibitor of HCV NS5A, essential for viral RNA replication and virion assembly.
Indication :
- Treatment naive chronic hepatitis C virus (HCV) genotype 1, 2, 3, 4, 5, or 6 infection in adolescents 12 years and older or weighing at least 45 kg.
- Treatment experienced HCV genotype 1
Contraindications :
Severe hepatic impairment (Child-Pugh class C); coadministration with atazanavir or rifampin.
Hypersensitivity to glecaprevir, pibrentasvir, or any component of the formulation; coadministration with atorvastatin, dabigatran, ethinyl estradiol, or simvastatin.
Dosing :
Available as 100 mg/40 mg tablet.
12 years and older or weighing at least 45 kilograms (kg):
3 tablets PO OD.
Adverse Effect :
Headache, fatigue, nausea, pruritus, diarrhea, hyperbilirubinemia.
Interaction :
Rifampin: Decreases the level or effect of glecaprevir/pibrentasvir by increasing metabolism.
Statins: Glecaprevir/pibrentasvir increases levels of statins.
Carbamazepine: Decreases the level or effect of glecaprevir/pibrentasvir by increasing metabolism.
Efavirenz: Decreases the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism.
Ritonavir: Increases the level or effect of glecaprevir/pibrentasvir by decreasing metabolism.
Hepatic Dose :
Mild hepatic impairment: No dosage adjustment is required.
Moderate and severe hepatic impairment: Use is contraindicated.