Glecaprevir + Pibrentasvir
Indications
Glecaprevir + Pibrentasvir is used for:
Chronic Hepatitis C
Adult Dose
Chronic Hepatitis C
Treatment-naïve adults and adolesents with chronic hepatitis C virus (HCV) genotypes 1-6 without cirrhosis or with compensated cirrhosis
Treatment-experienced patients with HCV genotype 1 who have been previously treated with a regimen containing either an NS5A inhibitor or an NS3/4A protease inhibitor, but not both
3 tablets (ie, 300 mg/120 mg total dose) PO once daily with food
Recommended duration for treatment-naïve patients
Genotypes 1-6, no cirrhosis: 8 wk
Genotypes 1-6, compensated cirrhosis (Child-Pugh A): 12 wk
Recommended duration for treatment-experienced patients
No cirrhosis
Genotype 1 and NS5A inhibitor prior treatment: 16 wk
Genotype 1 and NS3/4A protease inhibitor prior treatment: 12 wk
Genotypes 1, 2, 4, 5, or 6 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 8 wk
Genotype 3 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 16 wk
Compensated cirrhosis (Child-Pugh A)
Genotype 1 and NS5A inhibitor prior treatment: 16 wk
Genotype 1 and NS3/4A protease inhibitor prior treatment: 12 wk
Genotypes 1, 2, 4, 5, or 6 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 12 wk
Genotype 3 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 16 wk
Hepatic impairment
Mild (Child-Pugh A): No dosage adjustment required
Moderate (Child-Pugh B): Not recommended
Severe (Child-Pugh C): Contraindicated
Child Dose
Renal Dose
Renal impairment
Mild, moderate, or severe, including patients on dialysis: No dosage adjustment required
Administration
Take with food at the same time once daily
Contra Indications
Severe hepatic impairment (Child-Pugh C)
Coadministration with atazanavir or rifampin
Precautions
Hepatitis B virus reactivation in patients coinfected with HCV/HBV may occur
Pregnancy-Lactation
Pregnancy
No adequate human data are available to establish whether or not glecaprevir/pibrentasvir poses a risk to pregnancy outcomes
Lactation
Unknown if distributed in human breast milk
When administered to lactating rodents, glecaprevir and pibrentasvir were present in milk, without effect on growth and development observed in the nursing pups
Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition
Interactions
Coadministration is contraindicated with rifampin or atazanavir
Coadministration is not recommended with carbamazepine, efavirenz, or St John’s wort
Adverse Effects
Side effects of Glecaprevir + Pibrentasvir :
>10%
Headache (9-17%)
Fatigue (11-14%)
Nausea (6-12%)
1-10%
Diarrhea (3-7%)
Increased bilirubin, ≥2x ULN (3.5%)
Pruritus (7%)
Mechanism of Action
Glecaprevir: HCV NS3/4A protease inhibitor; 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: HCV NS5A inhibitor; essential for viral RNA replication and virion assembly