glecaprevir/pibrentasvir (Rx)

Brand and Other Names:Mavyret
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

glecaprevir/pibrentasvir

tablet

  • 100mg/40mg

Chronic Hepatitis C

Indicated for

  • Treatment-naïve adults 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

Dose

  • 3 tablets (ie, 300 mg/120 mg total dose) PO once daily with food
  • Also see recommended duration

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

Dosage Modifications

Renal impairment

  • Mild, moderate, or severe, including patients on dialysis: No dosage adjustment required

Hepatic impairment

  • Mild (Child-Pugh A): No dosage adjustment required
  • Moderate (Child-Pugh B): Not recommended
  • Severe (Child-Pugh C): Contraindicated

Dosing Considerations

Test all patients for evidence of current or prior hepatitis B virus (HBV) infection by measuring hepatitis B surface antigen (HBsAg) and hepatitis B core antibody (anti-HBc) before initiating HCV treatment

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

and glecaprevir/pibrentasvir

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     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (9-17%)

            Fatigue (11-14%)

            Nausea (6-12%)

            1-10%

            Diarrhea (3-7%)

            Increased bilirubin, ≥2x ULN (3.5%)

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            Warnings

            Black Box Warnings

            Test patients for evidence of current or prior HBV infection by measuring HBsAg and anti-HBc before initiating treatment

            HBV reactivation has been reported in HCV/HBV-coinfected patients who were undergoing or had completed treatment with HCV direct-acting antivirals and were not receiving HBV antiviral therapy

            Some cases have resulted in fulminant hepatitis, hepatic failure, and death

            Monitor HCV/HBV-coinfected patients for hepatitis flare or HBV reactivation during HCV treatment and posttreatment follow up

            Initiate appropriate patient management for HBV infection as clinically indicated

            Contraindications

            Severe hepatic impairment (Child-Pugh C)

            Coadministration with atazanavir or rifampi

            Cautions

            Hepatitis B virus reactivation in patients coinfected with HCV/HBV may occur (see Black Box Warnings)

            Drug interaction overview

            • Mechanisms for the potential effect of glecaprevir/pibrentasvir on other drugs
              • Glecaprevir and pibrentasvir: Inhibit P-gp, BCRP, OATP1B1, and OATP1B3; coadministration of glecaprevir/pibrentasvir may increase plasma concentrations of substrates of these transporters
              • Glecaprevir and pibrentasvir: Weak inhibitors of CYP3A, CYP1A2, and UGT1A1; significant interactions are not expected when glecaprevir/pibrentasvir is coadministered with substrates of CYP3A, CYP1A2, CYP2C9, CYP2C19, CYP2D6, UGT1A1, or UGT1A4
            • Mechanisms for the potential effect of other drugs on glecaprevir/pibrentasvir
              • Glecaprevir and pibrentasvir: Substrates of P-gp and/or BCRP
              • Glecaprevir: Substrate of OATP1B1, OATP1B3, and CYP3A (secondary)
              • Coadministration of glecaprevir/pibrentasvir with drugs that inhibit hepatic P-gp, BCRP, or OATP1B1/3 may increase the plasma concentrations of glecaprevir and/or pibrentasvir
              • Coadministration of glecaprevir/pibrentasvir with drugs that induce P-gp/CYP3A may significantly decrease glecaprevir and pibrentasvir plasma concentrations, leading to reduced therapeutic effect
              • Coadministration is contraindicated with rifampin or atazanavir
              • Coadministration is not recommended with carbamazepine, efavirenz, or St John’s wort
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            Pregnancy

            Pregnancy

            No adequate human data are available to establish whether or not glecaprevir/pibrentasvir poses a risk to pregnancy outcomes

            Animal studies

            • No adverse developmental effects were observed when glecaprevir and pibrentasvir were administered separately during organogenesis at exposures up to 53 times (rats; glecaprevir) or 51 and 1.5 times (mice and rabbits, respectively; pibrentasvir) the human exposures at the recommended dose

            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

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            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

            Absorption

            Peak plasma time: 5.0 hr (glecaprevir and pibrentasvir)

            Peak plasma concentration: 597 ng/mL (glecaprevir); 110 ng/mL (pibrentasvir)

            AUC: 4800 ng·h/mL (glecaprevir); 1430 ng·h/mL (pibrentasvir)

            Distribution

            Protein bound: 97.5% (glecaprevir); >99.9% (pibrentasvir)

            Blood-to-plasma ratio: 0.57 (glecaprevir); 0.62 (pibrentasvir)

            Metabolism

            Glecaprevir is metabolized by CYP3A4 (secondary)

            Elimination

            Half-life: 6 hr (glecaprevir); 13 hr (pibrentasvir)

            Excretion: Feces (92.7%, glecaprevir; 96.6%, pibrentasvir); urine (0.7%, glecaprevir)

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            Administration

            Oral Administration

            Take with food

            Missed dose

            • <18 hr from the usual dosage time: Take the dose as soon as possible; take the next dose at the usual time
            • >18 hr from the usual dosage time: Do not to take the missed dose; take the next dose at the usual time

            Storage

            Store at or below 30°C (86°F)

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            Formulary

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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