Dosing & Uses
Dosage Forms & Strengths
glecaprevir/pibrentasvir
tablet
- 100mg/40mg
Chronic Hepatitis C
Indicated for patients with genotypes 1-6 without cirrhosis or with compensated cirrhosis
Treatment-experienced patients with genotype 1 previously treated with a regimen containing NS5A inhibitor or an NS3/4A protease inhibitor, but not both
3 tablets (ie, 300 mg/120 mg total dose) PO qDay
Treatment duration, treatment-naïve
- Genotypes 1-6, no cirrhosis or compensated cirrhosis (Child-Pugh A): 8 weeks
Treatment duration, treatment-experienced
-
No cirrhosis
- Genotype 1 and NS5A inhibitor without prior treatment with an NS3/4A protease inhibitor (PI): 16 weeks
- Genotype 1 and NS3/4A PI without prior treatment with an NS5A inhibitor: 12 weeks
- Genotypes 1, 2, 4, 5, or 6 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 8 weeks
- Genotype 3 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 16 weeks
-
Compensated cirrhosis (Child-Pugh A)
- Genotype 1 and NS5A inhibitor without prior treatment with an NS3/4A protease inhibitor (PI): 16 weeks
- Genotype 1 and NS3/4A PI without prior treatment with an NS5A inhibitor: 12 weeks
- Genotypes 1, 2, 4, 5, or 6 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 12 weeks
- Genotype 3 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 16 weeks
-
Liver or kidney transplant recipients
- Treatment duration is 12 weeks
- 16-week treatment duration recommended for genotype 1 (NS5A inhibitor-experienced without prior treatment with an NS3/4A protease inhibitor) or genotype 3 (treatment-experience with regimens containing [peg]interferon, ribavirin, and/or sofosbuvir, but no prior treatment experience with an HCV NS3/4A PI or NS5A inhibitor)
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-to-severe (Child-Pugh B or C): Contraindicated
- Patients with any history of prior hepatic decompensation: Contraindicated
Dosing Considerations
Test 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
Dosage Forms & Strengths
glecaprevir/pibrentasvir
tablet
- 100mg/40mg
oral pellets
- 50mg/20mg
Chronic Hepatitis C
Indicated for treatment-naïve children aged ≥3 years with chronic hepatitis C virus (HCV) genotypes 1-6 without cirrhosis or with compensated cirrhosis
Also indicated for treatment-experienced children aged ≥3 years 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 years: Safety and efficacy not established
3-11 years
- <20 kg: 150 mg/60 mg PO qDay (3 packets of oral pellets)
- 20 to <30 kg: 200 mg/80 mg PO qDay (4 packets of oral pellets)
- 30 to <45 kg: 250 mg/120 mg PO qDay (5 packets of oral pellets)
≥12 years or weight ≥45 kg
- 300 mg/120 mg (3 tablets) PO qDay OR
- Unable to swallow tablets: 300 mg/120 mg PO qDay (6 packets of oral pellets)
Treatment duration, treatment-naïve
- Genotypes 1-6, no cirrhosis or compensated cirrhosis (Child-Pugh A): 8 weeks
Treatment duration, treatment-experienced
-
No cirrhosis
- Genotype 1 and NS5A inhibitor without prior treatment with an NS3/4A protease inhibitor (PI): 16 weeks
- Genotype 1 and NS3/4A PI without prior treatment with an NS5A inhibitor: 12 weeks
- Genotypes 1, 2, 4, 5, or 6 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 8 weeks
- Genotype 3 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 16 weeks
-
Compensated cirrhosis (Child-Pugh A)
- Genotype 1 and NS5A inhibitor without prior treatment with an NS3/4A protease inhibitor (PI): 16 weeks
- Genotype 1 and NS3/4A PI without prior treatment with an NS5A inhibitor: 12 weeks
- Genotypes 1, 2, 4, 5, or 6 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 12 weeks
- Genotype 3 (prior treatment with simeprevir and sofosbuvir, or simeprevir, boceprevir, or telaprevir with pegylated interferon and ribavirin): 16 weeks
-
Liver or kidney transplant recipients
- Treatment duration is 12 weeks
- 16-week treatment duration recommended for genotype 1 (NS5A inhibitor-experienced without prior treatment with an NS3/4A protease inhibitor) or genotype 3 (treatment-experience with regimens containing [peg]interferon, ribavirin, and/or sofosbuvir, but no prior treatment experience with an HCV NS3/4A PI or NS5A inhibitor)
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-to-severe (Child-Pugh B or C): Contraindicated
- Patients with any history of prior hepatic decompensation: Contraindicated
Dosing Considerations
Test 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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- elagolix
glecaprevir/pibrentasvir will increase the level or effect of elagolix by Other (see comment). Contraindicated. Concomitant use of elagolix and strong OATP1B1 inhibitors is contraindicated.
- rifampin
rifampin will decrease the level or effect of glecaprevir/pibrentasvir by increasing metabolism. Contraindicated. Coadministration of rifampin (a strong CYP3A4 and P-gp inducer) with glecaprevir/pibrentasvir significantly decreased glecaprevir/pibrentasvir plasma concentrations and AUC. Potential for loss of therapeutic effect.
Serious - Use Alternative (33)
- apalutamide
apalutamide will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- atazanavir
atazanavir will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. In clinical trials, coadministration of atazanavir (an inhibitor of CYP3A4 and OATP1B1) with glecaprevir (a CYP3A4 and OATP1B1 substrate) increased risk for ALT elevations.
- atorvastatin
glecaprevir/pibrentasvir increases levels of atorvastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. Coadministration of glecaprevir/pibrentasvir with atorvastatin is not recommended.
- carbamazepine
carbamazepine will decrease the level or effect of glecaprevir/pibrentasvir by increasing metabolism. Avoid or Use Alternate Drug. Coadministration of carbamazepine (a strong CYP3A4 and P-gp inducer) with glecaprevir/pibrentasvir may significantly decrease glecaprevir/pibrentasvir plasma concentrations and AUC. Potential for loss of therapeutic effect.
carbamazepine will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - colchicine
glecaprevir/pibrentasvir will increase the level or effect of colchicine by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Avoid use of colchicine with P-gp inhibitors. If coadministration is necessary, decrease colchicine dose or frequency as recommended in prescribing information. Use of any colchicine product in conjunction with P-gp inhibitors is contraindicated in patients with renal or hepatic impairment.
- cyclosporine
cyclosporine will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Avoid or Use Alternate Drug. Coadministration of cyclosporine (a moderate CYP3A4 inhibitor and P-gp inhibitor) with glecaprevir (CYP3A4 and P-gp substrate) and pibrentasvir (P-gp substrate) is not recommended if cyclosporine dose exceeds 100 mg/day.
- darunavir
darunavir will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glecaprevir/pibrentasvir with darunavir (P-gp and a strong CYP3A4 inhibitor).
- efavirenz
efavirenz will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of efavirenz (a strong CYP3A4 inducer) with glecaprevir/pibrentasvir may significantly decrease glecaprevir/pibrentasvir plasma concentrations and AUC. Potential for loss of therapeutic effect.
- enzalutamide
enzalutamide will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- fexinidazole
fexinidazole will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- ivosidenib
ivosidenib will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- lasmiditan
lasmiditan increases levels of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- leniolisib
leniolisib will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- lopinavir
lopinavir will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glecaprevir/pibrentasvir with lopinavir (P-gp and a strong CYP3A4 inhibitor).
- lovastatin
glecaprevir/pibrentasvir increases levels of lovastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. Coadministration of glecaprevir/pibrentasvir with lovastatin is not recommended.
- nirmatrelvir
nirmatrelvir will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Glecaprevir/pibrentasvir serum concentrations may be increased owing to P-gp, BCRP and OATP1B inhibition by ritonavir.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Glecaprevir/pibrentasvir serum concentrations may be increased owing to P-gp, BCRP and OATP1B inhibition by ritonavir.
- phenytoin
phenytoin will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- primidone
primidone will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- repotrectinib
glecaprevir/pibrentasvir will increase the level or effect of repotrectinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- revefenacin
glecaprevir/pibrentasvir increases levels of revefenacin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 and OATP1B3 transport inhibitors may increase systemic exposure of revefenacin's active metabolite. Coadministration not recommended.
- rifampin
rifampin will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- rimegepant
glecaprevir/pibrentasvir will increase the level or effect of rimegepant by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- ritonavir
ritonavir will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration of glecaprevir/pibrentasvir with ritonavir (P-gp and a strong CYP3A4 inhibitor).
- simvastatin
glecaprevir/pibrentasvir increases levels of simvastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. Coadministration of glecaprevir/pibrentasvir with simvastatin is not recommended.
- sotorasib
sotorasib will decrease the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
- St John's Wort
St John's Wort will decrease the level or effect of glecaprevir/pibrentasvir by increasing metabolism. Avoid or Use Alternate Drug. Coadministration of St John's wort (a strong CYP3A4 and P-gp inducer) with glecaprevir/pibrentasvir may significantly decrease glecaprevir/pibrentasvir plasma concentrations and AUC. Potential for loss of therapeutic effect.
- sulbactam/durlobactam
glecaprevir/pibrentasvir will increase the level or effect of sulbactam/durlobactam by Other (see comment). Avoid or Use Alternate Drug. Sulbactam is predicted to have active secretion by OATP1 as a significant portion of total clearance; therefore, inhibition of OAT1 may increase sulbactam plasma concentrations
- tepotinib
tepotinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
- trofinetide
trofinetide will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Avoid or Use Alternate Drug. Trofinetide (an OATP131 and OATP13B inhibitor) may increase plasma levels of OATP131 or OATP13B substrates. Avoid coadministration with sensitive substrates.
- tucatinib
tucatinib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- voxelotor
voxelotor will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
- zavegepant intranasal
glecaprevir/pibrentasvir will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
Monitor Closely (202)
- abiraterone
abiraterone will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- afatinib
afatinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of afatinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. - aliskiren
glecaprevir/pibrentasvir will increase the level or effect of aliskiren by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
- alvimopan
glecaprevir/pibrentasvir will increase the level or effect of alvimopan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
- ambrisentan
glecaprevir/pibrentasvir will increase the level or effect of ambrisentan by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
glecaprevir/pibrentasvir will increase the level or effect of ambrisentan by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. - amiodarone
amiodarone will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of amiodarone by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. - amitriptyline
glecaprevir/pibrentasvir will increase the level or effect of amitriptyline by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
- amobarbital
amobarbital will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- apalutamide
apalutamide will decrease the level or effect of glecaprevir/pibrentasvir by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces OATP1B1 and may decrease systemic exposure of drugs that are OATP1B1 substrates.
- apixaban
glecaprevir/pibrentasvir will increase the level or effect of apixaban by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
- atogepant
glecaprevir/pibrentasvir will increase the level or effect of atogepant by Other (see comment). Modify Therapy/Monitor Closely. Recommended dosage of atogepant (an OATP1B1 substrate) with concomitant use of OATP inhibitors is 10 mg or 30 mg qDay.
- azithromycin
azithromycin will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- belzutifan
belzutifan will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- bendamustine
glecaprevir/pibrentasvir will increase the level or effect of bendamustine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
- berotralstat
glecaprevir/pibrentasvir increases levels of berotralstat by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Reduced berotralstat dose to 110 mg/day when coadministered with P-gp inhibitors.
berotralstat will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered. - bosentan
bosentan will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
glecaprevir/pibrentasvir will increase the level or effect of bosentan by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3 - budesonide
glecaprevir/pibrentasvir will increase the level or effect of budesonide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- butabarbital
butabarbital will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- butalbital
butalbital will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- carfilzomib
glecaprevir/pibrentasvir will increase the level or effect of carfilzomib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- carvedilol
carvedilol will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of carvedilol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - caspofungin
caspofungin will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
- cenobamate
cenobamate will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- cetirizine
glecaprevir/pibrentasvir will increase the level or effect of cetirizine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- cimetidine
glecaprevir/pibrentasvir will increase the level or effect of cimetidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ciprofloxacin
glecaprevir/pibrentasvir will increase the level or effect of ciprofloxacin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- clarithromycin
clarithromycin will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- clotrimazole
clotrimazole will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
- cobicistat
cobicistat will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- conivaptan
conivaptan will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- crizotinib
crizotinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- dabigatran
glecaprevir/pibrentasvir will increase the level or effect of dabigatran by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- dabrafenib
dabrafenib will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
glecaprevir/pibrentasvir will increase the level or effect of dabrafenib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - dasabuvir
glecaprevir/pibrentasvir will increase the level or effect of dasabuvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- daunorubicin
glecaprevir/pibrentasvir will increase the level or effect of daunorubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of daunorubicin by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - desloratadine
glecaprevir/pibrentasvir will increase the level or effect of desloratadine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- dexamethasone
dexamethasone will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
glecaprevir/pibrentasvir will increase the level or effect of dexamethasone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - digoxin
glecaprevir/pibrentasvir will increase the level or effect of digoxin by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Measure serum digoxin concentrations before initiating glecaprevir/pibrentasvir. To reduce digoxin concentrations, decrease the dose by ~50% or by modifying the dosing frequency and continue monitoring.
- diltiazem
glecaprevir/pibrentasvir will increase the level or effect of diltiazem by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- dipyridamole
dipyridamole will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
dipyridamole will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.
glecaprevir/pibrentasvir will increase the level or effect of dipyridamole by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - docetaxel
glecaprevir/pibrentasvir will increase the level or effect of docetaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- doxorubicin
glecaprevir/pibrentasvir will increase the level or effect of doxorubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of doxorubicin by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - dronedarone
dronedarone will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- duvelisib
glecaprevir/pibrentasvir will increase the level or effect of duvelisib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- edoxaban
glecaprevir/pibrentasvir will increase the level or effect of edoxaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- elagolix
elagolix will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
elagolix decreases levels of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed. - elbasvir/grazoprevir
glecaprevir/pibrentasvir will increase the level or effect of elbasvir/grazoprevir by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
- eletriptan
glecaprevir/pibrentasvir will increase the level or effect of eletriptan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- eliglustat
eliglustat will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- eltrombopag
eltrombopag will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Monitor for glecaprevir/pibrentasvir adverse effects if coadministered with drugs that are OATP1B1 and BCRP inhibitor
- eluxadoline
eluxadoline will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir is an OATP1B1 inhibitor, BCRP substrate and inhibitor, and glecaprevir is a OAT1B1/3 substrate. Eluxadoline is an OATP1B1 substrate and BCRP inhibitor. Glecaprevir/pibrentasvir may decrease the therapeutic effects of eluxadoline. Eluxadoline may increase the plasma levels of glecaprevir/pibrentasvir.
- enalapril
glecaprevir/pibrentasvir will increase the level or effect of enalapril by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
- encorafenib
encorafenib, glecaprevir/pibrentasvir. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
encorafenib will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a OATP1B1 and OATP1B3 inhibitor) may increase the concentration and toxicities of OATP1B1 and OATP1B3 substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates. - erythromycin base
erythromycin base will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of erythromycin base by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
glecaprevir/pibrentasvir will increase the level or effect of erythromycin base by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- estradiol
glecaprevir/pibrentasvir will increase the level or effect of estradiol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- etoposide
glecaprevir/pibrentasvir will increase the level or effect of etoposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- etravirine
etravirine will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
etravirine will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - everolimus
glecaprevir/pibrentasvir will increase the level or effect of everolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ezetimibe
glecaprevir/pibrentasvir will increase the level or effect of ezetimibe by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
- fedratinib
fedratinib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fentanyl
glecaprevir/pibrentasvir will increase the level or effect of fentanyl by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- fexofenadine
glecaprevir/pibrentasvir will increase the level or effect of fexofenadine by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
glecaprevir/pibrentasvir will increase the level or effect of fexofenadine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - flibanserin
flibanserin will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- fluvastatin
glecaprevir/pibrentasvir increases levels of fluvastatin by Other (see comment). Modify Therapy/Monitor Closely. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. Use lowest approved dose of fluvastatin. If a higher dose is needed, use the lowest necessary statin dose based on a risk/benefit assessment.
- fosamprenavir
fosamprenavir will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fosphenytoin
fosphenytoin will decrease the level or effect of glecaprevir/pibrentasvir by increasing metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 and P-gp with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
fosphenytoin will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - fostamatinib
fostamatinib will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of P-gp/BCRP substrate drugs. Monitor for toxicities of P-gp/BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib.
- fostemsavir
fostemsavir will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits OATP1B1/3 transporter. If possible, avoid coadministration or modify dose of OATP1B1/3 substrates coadministered with fostemsavir.
- gefitinib
gefitinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.
- gemfibrozil
gemfibrozil will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
- glyburide
glyburide will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
glecaprevir/pibrentasvir will increase the level or effect of glyburide by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates. - grapefruit
grapefruit will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- hydrocortisone
glecaprevir/pibrentasvir will increase the level or effect of hydrocortisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ibrutinib
ibrutinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- idarubicin
glecaprevir/pibrentasvir will increase the level or effect of idarubicin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- idelalisib
idelalisib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- imatinib
imatinib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of imatinib by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of OATP1B1/OATP1B3, P-gp and BCRP substrates. - indinavir
indinavir will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of indinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - irinotecan
glecaprevir/pibrentasvir will increase the level or effect of irinotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of irinotecan by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - irinotecan liposomal
glecaprevir/pibrentasvir will increase the level or effect of irinotecan liposomal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- isavuconazonium sulfate
isavuconazonium sulfate will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- isoniazid
isoniazid will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
istradefylline will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates. - itraconazole
itraconazole will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
itraconazole will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - ivacaftor
ivacaftor will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.
- ivermectin
glecaprevir/pibrentasvir will increase the level or effect of ivermectin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ketoconazole
ketoconazole will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lapatinib
lapatinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with P-gp/BCRP inhibitors.
glecaprevir/pibrentasvir will increase the level or effect of lapatinib by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates. - ledipasvir/sofosbuvir
ledipasvir/sofosbuvir will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of ledipasvir/sofosbuvir by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates. - leflunomide
glecaprevir/pibrentasvir will increase the level or effect of leflunomide by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- lenacapavir
lenacapavir will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- lenvatinib
glecaprevir/pibrentasvir will increase the level or effect of lenvatinib by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates.
- letermovir
glecaprevir/pibrentasvir increases levels of letermovir by decreasing metabolism. Use Caution/Monitor. Coadminstration of letermovir, an OATP1B1/3 substrate, with OATP1B1/3 inhibitors may increase letermovir plasma concentrations.
letermovir increases levels of glecaprevir/pibrentasvir by Other (see comment). Use Caution/Monitor. Comment: Letermovir, an OATP1B1/3 inhibitor may increase plasma concentrations of coadministered OATP1B1/3 substrates. - levoketoconazole
levoketoconazole will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lidocaine
glecaprevir/pibrentasvir will increase the level or effect of lidocaine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- linagliptin
glecaprevir/pibrentasvir will increase the level or effect of linagliptin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lomitapide
lomitapide will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lonafarnib
lonafarnib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.
- loperamide
glecaprevir/pibrentasvir will increase the level or effect of loperamide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lorlatinib
lorlatinib will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lovastatin
glecaprevir/pibrentasvir will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- maraviroc
glecaprevir/pibrentasvir will increase the level or effect of maraviroc by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- mefloquine
mefloquine will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of mefloquine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - methotrexate
glecaprevir/pibrentasvir will increase the level or effect of methotrexate by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of OATP1B1/OATP1B3, P-gp and BCRP substrates.
- methylprednisolone
glecaprevir/pibrentasvir will increase the level or effect of methylprednisolone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- metyrapone
metyrapone will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
- mifepristone
mifepristone will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mitomycin
glecaprevir/pibrentasvir will increase the level or effect of mitomycin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- mitotane
mitotane will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- mitoxantrone
glecaprevir/pibrentasvir will increase the level or effect of mitoxantrone by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- momelotinib
glecaprevir/pibrentasvir increases toxicity of momelotinib by Other (see comment). Use Caution/Monitor. Comment: OATP1B1/B3 inhibitor increases momelotinib (OATP1B1/B3 subtrate) plasma concentrations, which may increase the risk of adverse reactions with momelotinib.
- morphine
glecaprevir/pibrentasvir will increase the level or effect of morphine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nadolol
glecaprevir/pibrentasvir will increase the level or effect of nadolol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nafcillin
nafcillin will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- naldemedine
glecaprevir/pibrentasvir will increase the level or effect of naldemedine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nefazodone
nefazodone will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nelfinavir
nelfinavir will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
nelfinavir will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of nelfinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - nevirapine
nevirapine will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- nicardipine
nicardipine will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of nicardipine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - nilotinib
nilotinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - nintedanib
glecaprevir/pibrentasvir will increase the level or effect of nintedanib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nitrofurantoin
glecaprevir/pibrentasvir will increase the level or effect of nitrofurantoin by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- olmesartan
glecaprevir/pibrentasvir will increase the level or effect of olmesartan by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
- ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
glecaprevir/pibrentasvir will increase the level or effect of ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
- ondansetron
glecaprevir/pibrentasvir will increase the level or effect of ondansetron by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- osimertinib
osimertinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.
glecaprevir/pibrentasvir will increase the level or effect of osimertinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of osimertinib by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - oxcarbazepine
oxcarbazepine will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- paclitaxel
paclitaxel will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
glecaprevir/pibrentasvir will increase the level or effect of paclitaxel by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
glecaprevir/pibrentasvir will increase the level or effect of paclitaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - paclitaxel protein bound
glecaprevir/pibrentasvir will increase the level or effect of paclitaxel protein bound by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- paliperidone
paliperidone will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of paliperidone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - pantoprazole
pantoprazole will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with P-gp/BCRP inhibitors.
glecaprevir/pibrentasvir will increase the level or effect of pantoprazole by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates. - pazopanib
pazopanib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
glecaprevir/pibrentasvir will increase the level or effect of pazopanib by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates. - pentobarbital
pentobarbital will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- phenobarbital
phenobarbital will decrease the level or effect of glecaprevir/pibrentasvir by increasing metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 and P-gp with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
phenobarbital will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - pioglitazone
pioglitazone will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
- pitavastatin
glecaprevir/pibrentasvir increases levels of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. Use lowest approved dose of pitavastatin. If a higher dose is needed, use the lowest necessary statin dose based on a risk/benefit assessment.
- pomalidomide
glecaprevir/pibrentasvir will increase the level or effect of pomalidomide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ponatinib
ponatinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with P-gp/BCRP inhibitors.
- posaconazole
posaconazole will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of posaconazole by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - pravastatin
glecaprevir/pibrentasvir increases levels of pravastatin by Other (see comment). Modify Therapy/Monitor Closely. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. If coadministered, reduce pravastatin dose by 50%.
- prazosin
glecaprevir/pibrentasvir will increase the level or effect of prazosin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- prednisone
glecaprevir/pibrentasvir will decrease the level or effect of prednisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- pretomanid
pretomanid will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Use Caution/Monitor. Increase monitoring for drug-related adverse effects if pretomanid is coadministered with sensitive OATP1B3 substrates.
- progesterone, natural
progesterone, natural will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- propafenone
propafenone will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- propranolol
propranolol will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- quinidine
quinidine will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of quinidine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - quinine
quinine will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of quinine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - ranolazine
ranolazine will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of ranolazine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - regorafenib
regorafenib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.
- repaglinide
repaglinide will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
glecaprevir/pibrentasvir will increase the level or effect of repaglinide by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3 - rifabutin
rifabutin will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- rifapentine
rifapentine will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- rifaximin
glecaprevir/pibrentasvir will increase the level or effect of rifaximin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- riociguat
glecaprevir/pibrentasvir will increase the level or effect of riociguat by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates.
- risperidone
glecaprevir/pibrentasvir will increase the level or effect of risperidone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ritonavir
glecaprevir/pibrentasvir will increase the level or effect of ritonavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- rolapitant
rolapitant will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with P-gp/BCRP inhibitors.
- rosiglitazone
rosiglitazone will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
- rosuvastatin
glecaprevir/pibrentasvir increases levels of rosuvastatin by Other (see comment). Modify Therapy/Monitor Closely. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. If coadministered, do not exceed 10 mg/day of rosuvastatin.
- rucaparib
rucaparib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- safinamide
safinamide will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors.
- saquinavir
saquinavir will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
saquinavir will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of saquinavir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - sarecycline
sarecycline will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.
- saxagliptin
glecaprevir/pibrentasvir will increase the level or effect of saxagliptin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- secobarbital
secobarbital will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of drugs that induce CYP3A4 with glecaprevir/pibrentasvir may decrease glecaprevir/pibrentasvir plasma concentrations. Potential for loss of therapeutic effect.
- selexipag
glecaprevir/pibrentasvir will increase the level or effect of selexipag by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- silodosin
glecaprevir/pibrentasvir will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- sirolimus
glecaprevir/pibrentasvir will increase the level or effect of sirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- sitagliptin
glecaprevir/pibrentasvir will increase the level or effect of sitagliptin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- stiripentol
stiripentol, glecaprevir/pibrentasvir. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
stiripentol will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol. - sulfasalazine
glecaprevir/pibrentasvir will increase the level or effect of sulfasalazine by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- sunitinib
sunitinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with P-gp/BCRP inhibitors.
- suvorexant
suvorexant will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tacrolimus
tacrolimus will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
glecaprevir/pibrentasvir will increase the level or effect of tacrolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - talazoparib
glecaprevir/pibrentasvir will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- tamoxifen
tamoxifen will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tazemetostat
tazemetostat will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- telmisartan
telmisartan will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with OATP1B1/OATP1B3 inhibitors
glecaprevir/pibrentasvir will increase the level or effect of telmisartan by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3 - temsirolimus
glecaprevir/pibrentasvir will increase the level or effect of temsirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- teniposide
glecaprevir/pibrentasvir will increase the level or effect of teniposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tenofovir AF
glecaprevir/pibrentasvir will increase the level or effect of tenofovir AF by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- tenofovir DF
glecaprevir/pibrentasvir will increase the level or effect of tenofovir DF by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.
- testosterone
glecaprevir/pibrentasvir will increase the level or effect of testosterone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tipranavir
tipranavir will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tolvaptan
glecaprevir/pibrentasvir will increase the level or effect of tolvaptan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- topotecan
glecaprevir/pibrentasvir will increase the level or effect of topotecan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of topotecan by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - trabectedin
glecaprevir/pibrentasvir will increase the level or effect of trabectedin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tucatinib
tucatinib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
- ulipristal
ulipristal will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- vandetanib
vandetanib will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
vandetanib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with BCRP inhibitors. - velpatasvir
glecaprevir/pibrentasvir will increase the level or effect of velpatasvir by Other (see comment). Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of P-gp and BCRP substrates.
- vemurafenib
vemurafenib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with P-gp/BCRP inhibitors.
glecaprevir/pibrentasvir will increase the level or effect of vemurafenib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of vemurafenib by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates. - venetoclax
venetoclax will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - verapamil
verapamil will increase the level or effect of glecaprevir/pibrentasvir by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
glecaprevir/pibrentasvir will increase the level or effect of verapamil by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. - vinblastine
glecaprevir/pibrentasvir will increase the level or effect of vinblastine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
- vincristine
glecaprevir/pibrentasvir will increase the level or effect of vincristine by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
- voriconazole
voriconazole will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- voxilaprevir
glecaprevir/pibrentasvir will increase the level or effect of voxilaprevir by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.
Minor (6)
- acetazolamide
acetazolamide will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ribociclib
ribociclib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- voclosporin
voclosporin will increase the level or effect of glecaprevir/pibrentasvir by Other (see comment). Minor/Significance Unknown. Information suggests voclosporin (an OATP1B1 inhibitor) may increase in the concentration of OATP1B1 substrates is possible. Monitor for adverse reactions of OATP1B1 substrates when coadministered with voclosporin.
Adverse Effects
>10%
Headache (9-17%)
Fatigue (11-14%)
Nausea (6-12%)
1-10%
Diarrhea (3-7%)
Increased bilirubin, ≥2x ULN (3.5%)
Pruritus (7%)
Postmarketing Reports
Skin and SC tissue disorders: Angioedema
Hepatobiliary disorders: Hepatic decompensation, hepatic failure
Warnings
Black Box Warnings
Risk of hepatitis B virus reactivation in patients coinfected with HCV and HBV
- Test 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
Moderate or severe hepatic impairment (Child-Pugh B or C)
History of prior hepatic decompensation
Coadministration with atazanavir or rifampin
Cautions
Hepatitis B virus reactivation in patients coinfected with HCV/HBV may occur
Postmarketing cases of hepatic decompensation/failure, including those with fatal outcomes, have been reported
No dosage adjustment of required in people who inject drugs (PWID) or those who are on medication-assisted treatment (MAT) for opioid use disorder; safety and efficacy reported to be similar to those not reporting history of injection drug use
Hepatitis B Virus reactivation in HCV and HBV coinfection
- In patients with resolved HBV infection reappearance of HBsAg can occur
- Reactivation of HBV replication may be accompanied by hepatitis, ie, increase in aminotransferase levels and, in severe cases, increases in bilirubin levels, liver failure, and death can occur
- Test all patients for evidence of current or prior HBV infection by measuring HBsAg and anti-HBc before initiating HCV treatment
- In patients with serologic evidence of HBV infection, monitor for clinical and laboratory signs of hepatitis flare or HBV reactivation during HCV treatment and during post-treatment follow-up; initiate appropriate patient management for HBV infection as clinically indicated
Hepatic decompensation
- Majority of patients with severe outcomes had evidence of advanced liver disease with moderate or severe hepatic impairment (Child-Pugh B or C) prior to initiating therapy, including some patients reported as having compensated cirrhosis with mild liver impairment (Child-Pugh A) at baseline but with a prior decompensation event (i.e., prior history of ascites, variceal bleeding, encephalopathy)
- Patients with compensated cirrhosis (Child Pugh A) or evidence of advanced liver disease such as portal hypertension, perform hepatic laboratory testing as clinically indicated; and monitor for signs and symptoms of hepatic decompensation such as presence of jaundice, ascites, hepatic encephalopathy, and variceal hemorrhage; discontinue in patients who develop evidence of hepatic decompensation/failure
Drug interaction overview
-
Effects 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
-
Effects 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
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.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 hr (glecaprevir and pibrentasvir)
Peak plasma concentration: 597 ng/mL (glecaprevir); 110 ng/mL (pibrentasvir)
AUC: 4800 ng⋅hr/mL (glecaprevir); 1430 ng⋅hr/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
- Glecaprevir: Feces (92.7%); urine (0.7%)
- Pibrentasvir: Feces (96.6%)
Administration
Oral Pellet Preparation
Sprinkle oral pellets for the total daily dose on a small amount of soft food with low water content (eg, peanut butter, chocolate hazelnut spread, cream cheese, thick jam, or Greek yogurt) that will stick to a spoon and can be swallowed without chewing
Avoid liquids or foods that would drip or slide off the spoon as the drug may dissolve quickly and become less effective
Oral Administration
Tablets: Take with food at the same time once daily
Oral pellets
- Take together as one dose, with food, once daily
- Do not crush or chew
- Swallow within 15 minutes of preparation
Missed dose
- <18 hr from usual dosage time: Take dose as soon as possible; take next dose at the usual time
- >18 hr from usual dosage time: Do not to take missed dose; take next dose at the usual time
Storage
Tablets or pellets: Store at or below 30°C (86°F)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Mavyret oral - | 100-40 mg tablet |  | |
| Mavyret oral - | 50-20 mg pellet |  |
Copyright © 2010 First DataBank, Inc.
Formulary
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