Selzentry
Classes
HIV-1 Entry Inhibitors/Fusion Inhibitors
Administration
May be administered without regard to meals.
Swallow tablets whole. Do not chew.
Administer oral solution using the manufacturer provided press-in bottle adapter and oral dosing syringe.
Adverse Reactions
new primary malignancy / Delayed / 0-3.0
thrombosis / Delayed / 0-2.0
cirrhosis / Delayed / 0-2.0
hepatic failure / Delayed / 0-2.0
heart failure / Delayed / 0-2.0
visual impairment / Early / 0-2.0
seizures / Delayed / 0-2.0
stroke / Early / 0-2.0
rhabdomyolysis / Delayed / 0-2.0
osteonecrosis / Delayed / 0-2.0
myocardial infarction / Delayed / 0.8-1.3
Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) / Delayed / Incidence not known
hepatotoxicity / Delayed / Incidence not known
toxic epidermal necrolysis / Delayed / Incidence not known
Stevens-Johnson syndrome / Delayed / Incidence not known
anemia / Delayed / 0-8.0
constipation / Delayed / 6.0-6.0
hyperamylasemia / Delayed / 4.3-5.7
neutropenia / Delayed / 4.3-5.7
hyperbilirubinemia / Delayed / 5.5-5.5
elevated hepatic enzymes / Delayed / 2.6-4.8
depression / Delayed / 4.0-4.0
peripheral neuropathy / Delayed / 4.0-4.0
dyspnea / Early / 4.0-4.0
lipodystrophy / Delayed / 3.0-4.0
hypertension / Early / 3.0-3.0
memory impairment / Delayed / 3.0-3.0
ejaculation dysfunction / Delayed / 3.0-3.0
jaundice / Delayed / 0-2.0
angina / Early / 0-2.0
meningitis / Delayed / 0-2.0
pseudomembranous colitis / Delayed / 0-2.0
erythema / Early / 2.0-2.0
conjunctivitis / Delayed / 2.0-2.0
ocular infection / Delayed / 2.0-2.0
orthostatic hypotension / Delayed / 0.5-0.5
hepatitis / Delayed / Incidence not known
eosinophilia / Delayed / Incidence not known
candidiasis / Delayed / Incidence not known
edema / Delayed / Incidence not known
infection / Delayed / 55.0-55.0
cough / Delayed / 14.0-14.0
fever / Early / 13.0-13.0
vomiting / Early / 12.0-12.0
rash / Early / 11.0-11.0
flatulence / Early / 10.0-10.0
dizziness / Early / 3.0-9.0
insomnia / Early / 8.0-8.0
sinusitis / Delayed / 7.0-7.0
arthralgia / Delayed / 6.0-7.0
paresthesias / Delayed / 4.0-5.0
dysesthesia / Delayed / 4.0-5.0
anxiety / Delayed / 4.0-4.0
nasal congestion / Early / 4.0-4.0
folliculitis / Delayed / 4.0-4.0
diarrhea / Early / 4.0-4.0
nausea / Early / 4.0-4.0
abdominal pain / Early / 4.0-4.0
pruritus / Rapid / 4.0-4.0
myalgia / Early / 3.0-3.0
acne vulgaris / Delayed / 3.0-3.0
tremor / Early / 0-2.0
influenza / Delayed / 2.0-2.0
alopecia / Delayed / 2.0-2.0
syncope / Early / Incidence not known
rhinitis / Early / Incidence not known
gynecomastia / Delayed / Incidence not known
Cushingoid features / Delayed / Incidence not known
Boxed Warning
Hepatotoxicity has been reported in patients receiving maraviroc, and evidence of a systemic allergic reaction (e.g., fever, serious rash, eosinophilia, or elevated IgE) prior to the development of hepatotoxicity may occur. These events have appeared approximately 1 month after starting therapy. However, cases of hepatitis have developed without allergic features and in patients without pre-existing hepatic impairment. Healthcare providers are advised to perform liver function tests before initiation therapy and at other points during treatment as clinically indicated. Instruct patients to discontinue maraviroc and seek immediate medical attention if signs or symptoms of hepatitis, allergic reaction, rash with fever, or other systemic symptoms develop; delaying treatment discontinuation may result in life-threatening reactions. Patients with moderate hepatic impairment who are receiving a concomitant potent CYP3A4 inhibitor should be monitored closely for adverse events as maraviroc concentrations are higher when 150 mg PO twice daily is administered with a potent CYP3A4 inhibitor as compared to 300 mg PO twice daily without a CYP3A4 inhibitor. Of note, maraviroc has not been studied in patients with severe hepatic disease, including patients with hepatitis and HIV coinfection; therefore, it is recommended to administer maraviroc cautiously to patients with pre-existing liver dysfunction. Patients presenting with HIV infection should be screened for hepatitis B virus (HBV) to assure appropriate treatment. Patients with hepatitis B and HIV coinfection should be started on a fully suppressive antiretroviral (ARV) regimen with activity against both viruses (regardless of CD4 counts and HBV DNA concentrations). HIV treatment guidelines recommend these patients receive an ARV regimen that contains a dual NRTI backbone of tenofovir alafenamide or tenofovir disoproxil fumarate with either emtricitabine or lamivudine. If tenofovir cannot be used, entecavir should be used in combination with a fully suppressive ARV regimen (note: entecavir should not be considered part of the ARV regimen). Avoid using single-drug therapy to treat HBV (i.e., lamivudine, emtricitabine, tenofovir, or entecavir as the only active agent) as this may result in HIV resistant strains. Further, HBV treatment regimens that include adefovir or telbivudine should also be avoided, as these regimens are associated with a higher incidence of toxicities and increased rates of HBV treatment failure. Most patients with coinfection should continue treatment indefinitely with the goal of maximal HIV suppression and prevention of HBV relapse. If treatment must be discontinued, monitor transaminase concentrations every 6 weeks for the first 3 months, and every 3 to 6 months thereafter. For patients who refuse a fully suppressive ARV regimen, but still requires treatment for HBV, consider 48 weeks of peginterferon alfa; do not administer HIV-active medications in the absence of a fully suppressive ARV regimen. Instruct patients with coinfection to avoid consuming alcohol, and offer vaccinations against hepatitis A and hepatitis B as appropriate. [46638] [33473] [34362]
Common Brand Names
Selzentry
Dea Class
Rx
Description
Entry inhibitor
Used for treatment of CCR5-tropic human immunodeficiency virus (HIV) infection in combination with other antiretroviral agents
Tropism assay of the HIV strain required prior to treatment
Dosage And Indications
300 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
150 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
600 mg PO twice daily. NOTE: Drug interaction examples include carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin.
300 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
200 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
150 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
150 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
100 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
75 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
50 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
Use not recommended. NOTE: Drug interaction examples include carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin.
300 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
150 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
600 mg PO twice daily. NOTE: Drug interaction examples include carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin.
300 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
200 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
150 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
100 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
40 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
30 mg PO twice daily. NOTE: Concomitant drugs that do not require a dosage change include dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir with ritonavir.
150 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
100 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
80 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
50 mg PO twice daily. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
Use not recommended. NOTE: Drug interaction examples include clarithromycin, cobicistat, elvitegravir with ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir with ritonavir), and telithromycin.
Use not recommended. NOTE: Drug interaction examples include carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin.
The US Public Health Service guidelines suggest maraviroc 300 mg PO twice daily in combination with one of the following backbones (in order of preference) as acceptable alternative regimens for HIV post-exposure prophylaxis (PEP): tenofovir plus emtricitabine; tenofovir plus lamivudine; zidovudine plus lamivudine; zidovudine plus emtricitabine. Prior to administering a maraviroc containing regimen, the US Public Health Service and the New York State Department of Health AIDS Institute (NYSDOH AI) recommend consultation with a clinician experienced in the management of PEP. This recommendation is due to the drugs lack of activity against potential CXCR4 tropic virus. According to PEP guidelines, individuals potentially exposed to HIV should receive a 3-drug regimen for a total of 28 days; however if tolerability is a concern, use of a 2-drug regimen may be considered and is preferred to prophylaxis discontinuation. Begin prophylaxis as soon as possible, ideally within 2 hours of exposure. If initiation of prophylaxis is delayed (beyond 36 hours or 72 hours after exposure), efficacy of the antiretroviral regimen may be diminished and treatment should be determined on a case-by-case basis. Exposures for which PEP is indicated include: skin puncture by a sharp object that has been contaminated with blood, body fluid, or other infectious material; bite from a patient with visible bleeding in the mouth which causes bleeding by the exposed worker; splash of blood, body fluid, or other infectious material onto the workers mouth, nose, or eyes; exposure of blood, body fluid, or other infectious material on a workers non-intact skin (i.e., open wound, chapped skin, abrasion, dermatitis).
†Indicates off-label use
Dosing Considerations
Specific guidelines for dosage adjustments in hepatic impairment are not available; however, because maraviroc is metabolized by the liver, concentrations are likely to be increased in such patients; use with caution and monitor patients frequently. In adult patients, maraviroc concentrations are higher when the 150 mg PO twice daily dose is administered with a potent CYP3A4 inhibitor as compared to the administration of the 300 mg PO twice daily dose without a CYP3A4 inhibitor; closely monitor patients with moderate hepatic impairment also receiving a concomitant potent CYP3A4 inhibitor for adverse events. Maraviroc has not been studied in patients with severe hepatic impairment or pediatric patients with any degree of hepatic impairment.
Renal ImpairmentAdult patients
In combination with strong CYP3A inhibitors with or without a CYP3A inducer:
CrCl 30 mL/minute or more: No dosage adjustment needed; 150 mg PO twice daily.
CrCl less than 30 mL/minute: Use is contraindicated.
In combination with strong CYP3A inducers without a strong CYP3A inhibitor:
CrCl 30 mL/minute or more: No dosage adjustment needed; 600 mg PO twice daily.
CrCl less than 30 mL/minute: Use is contraindicated.
For patients taking a medication regimen that does NOT include any strong CYP3A inducers or inhibitors:
CrCl 30 mL/minute or more: No dosage adjustment needed; 300 mg PO twice daily.
CrCl less than 30 mL/minute: No dosage adjustment is needed; however, in patients with symptoms of postural hypotension, reduce the dose to 150 mg PO twice daily.
Pediatric patients
Data are unavailable to recommend specific doses of maraviroc in pediatric patients with mild or moderate renal impairment. Maraviroc is contraindicated in pediatric patients with severe renal impairment or end-stage renal disease on regular hemodialysis who are receiving potent CYP3A inhibitors or inducers.
Hemodialysis
For adult patients taking a medication regimen that does NOT include any CYP3A inducers or inhibitors, normal doses of 300 mg PO twice daily should be used; however, in patients with any symptoms of postural hypotension, reduce the dose to 150 mg PO twice daily. Data are not available and use is contraindicated in patients taking concomitant CYP3A4 inducers or inhibitors.
Drug Interactions
Abrocitinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with abrocitinib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; abrocitinib is a P-gp inhibitor.
Adagrasib: (Major) Reduce the dose of maraviroc when coadministration with adagrasib is necessary, regardless of whether the patient is receiving a concomitant strong CYP3A inducer. The effect of adagrasib on maraviroc exposure is expected to exceed that of the inducer and overall, increased maraviroc concentrations are expected. Coadministration of maraviroc with adagrasib is contraindicated in patients with CrCl less than 30 mL/min. Recommendations for reducing the maraviroc dose when administered with adagrasib (with or without a concomitant CYP3A inducer) are: adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily. Maraviroc is a sensitive CYP3A and P-gp substrate and adagrasib is a strong CYP3A and P-gp inhibitor. Coadministration with strong CYP3A inhibitors may result in increased maraviroc concentrations.
Adefovir: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and adefovir as increased maraviroc concentrations may occur. Maraviroc is a substrate of multidrug resistance-associated protein (MRP2); adefovir is an inhibitor of MRP2. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Aldesleukin, IL-2: (Minor) Use caution if coadministration of maraviroc with aldesleukin is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and aldesleukin is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amiodarone: (Moderate) Use caution if coadministration of maraviroc with amiodarone is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A4/P-glycoprotein (P-gp) substrate and amiodarone is a CYP3A4/P-gp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amlodipine: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amlodipine; Atorvastatin: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amlodipine; Benazepril: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amlodipine; Celecoxib: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amlodipine; Olmesartan: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amlodipine; Valsartan: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amlodipine; Valsartan; Hydrochlorothiazide, HCTZ: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Amoxicillin; Clarithromycin; Omeprazole: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with clarithromycin (a strong CYP3A4 inhibitor and P-gp/OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with clarithromycin (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Apalutamide: (Major) Increase the adult maraviroc dose to 600 mg PO twice daily if coadministration with apalutamide is necessary without a concomitant strong CYP3A4 inhibitor, as maraviroc concentrations may be expected to decrease. Coadministration of maraviroc and apalutamide is contraindicated in patients with CrCL less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with apalutamide without a strong CYP3A inhibitor is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected. Maraviroc is a CYP3A4 substrate and apalutamide is a strong CYP3A4 inducer.
Aprepitant, Fosaprepitant: (Moderate) Use caution if maraviroc and aprepitant, fosaprepitant are used concurrently and monitor for an increase in maraviroc-related adverse effects for several days after administration of a multi-day aprepitant regimen. Maraviroc is a CYP3A substrate. Aprepitant, when administered as a 3-day oral regimen (125 mg/80 mg/80 mg), is a moderate CYP3A4 inhibitor and inducer and may increase plasma concentrations of maraviroc. For example, a 5-day oral aprepitant regimen increased the AUC of another CYP3A4 substrate, midazolam (single dose), by 2.3-fold on day 1 and by 3.3-fold on day 5. After a 3-day oral aprepitant regimen, the AUC of midazolam (given on days 1, 4, 8, and 15) increased by 25% on day 4, and then decreased by 19% and 4% on days 8 and 15, respectively. As a single 125 mg or 40 mg oral dose, the inhibitory effect of aprepitant on CYP3A4 is weak, with the AUC of midazolam increased by 1.5-fold and 1.2-fold, respectively. After administration, fosaprepitant is rapidly converted to aprepitant and shares many of the same drug interactions. However, as a single 150 mg intravenous dose, fosaprepitant only weakly inhibits CYP3A4 for a duration of 2 days; there is no evidence of CYP3A4 induction. Fosaprepitant 150 mg IV as a single dose increased the AUC of midazolam (given on days 1 and 4) by approximately 1.8-fold on day 1; there was no effect on day 4. Less than a 2-fold increase in the midazolam AUC is not considered clinically important.
Armodafinil: (Minor) Use caution if coadministration of maraviroc with armodafinil is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and armodafinil is a weak CYP3A4 inducer. Monitor for a decrease in efficacy with concomitant use.
Atazanavir: (Major) Coadministration of maraviroc, a CYP3A and OATP1B1 substrate, with atazanavir, a strong CYP3A4 inhibitor and in vitro inhibitor of OATP1B1, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with atazanavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Atazanavir; Cobicistat: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with cobicistat (a CYP3A4, P-gp, OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with cobicistat; coadministration is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with cobicistat (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended. (Major) Coadministration of maraviroc, a CYP3A and OATP1B1 substrate, with atazanavir, a strong CYP3A4 inhibitor and in vitro inhibitor of OATP1B1, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with atazanavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Berotralstat: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with berotralstat is necessary. Maraviroc is a P-gp substrate and a sensitive CYP3A substrate; berotralstat is a P-gp inhibitor and a moderate CYP3A4 inhibitor. Coadministration with moderate CYP3A4 inhibitors may result in increased maraviroc concentrations.
Bexarotene: (Moderate) Use caution if coadministration of maraviroc with bexarotene is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and bexarotene is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Brigatinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with brigatinib is necessary. Concurrent use may increase the plasma concentrations of maraviroc. Maraviroc is a P-glycoprotein (P-gp) substrate; brigatinib is a P-gp inhibitor.
Cabozantinib: (Minor) Monitor for an increase in maraviroc-related adverse reactions if coadministration with cabozantinib is necessary; a dose adjustment of maraviroc may be necessary. Maraviroc is a P-glycoprotein (P-gp) substrate. Cabozantinib is a P-gp inhibitor and has the potential to increase plasma concentrations of P-gp substrates; however, the clinical relevance of this finding is unknown.
Cannabidiol: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with cannabidiol is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; cannabidiol is a P-gp inhibitor.
Capmatinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with capmatinib is necessary. Maraviroc is a P-glycoprotein (P-gp) substrate and capmatinib is a P-gp inhibitor. Concomitant use may increase maraviroc exposure.
Carbamazepine: (Major) Coadministration of maraviroc, a CYP3A/P-glycoprotein (P-gp) substrate, and carbamazepine, a strong CYP3A inducer and P-gp inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with carbamazepine without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and carbamazepine is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Carvedilol: (Moderate) Increased concentrations of maraviroc may occur if it is coadministered with carvedilol; exercise caution. Carvedilol is a P-glycoprotein (P-gp) inhibitor and maraviroc is a P-gp substrate.
Ceritinib: (Major) Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors such as ceritinib; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCL less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with ceritinib (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended. The AUC of maraviroc was increased by up to approximately 10-fold in the presence of strong CYP3A4 inhibitors.
Chloramphenicol: (Major) Coadministration of maraviroc, a CYP3A substrate, with chloramphenicol, a strong CYP3A4 inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; also, coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with chloramphenicol (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Cidofovir: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and cidofovir as increased maraviroc concentrations may occur. Maraviroc is a substrate of multidrug resistance-associated protein (MRP2); cidofovir is an inhibitor of MRP2. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Cimetidine: (Minor) Use caution if coadministration of maraviroc with cimetidine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and cimetidine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Ciprofloxacin: (Minor) Use caution if coadministration of maraviroc with ciprofloxacin is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and ciprofloxacin is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Clarithromycin: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with clarithromycin (a strong CYP3A4 inhibitor and P-gp/OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with clarithromycin (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Clobazam: (Minor) Use caution if coadministration of maraviroc with clobazam is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and clobazam is a weak CYP3A4 inducer. Monitor for a decrease in efficacy with concomitant use.
Cobicistat: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with cobicistat (a CYP3A4, P-gp, OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with cobicistat; coadministration is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with cobicistat (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Conivaptan: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with conivaptan is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a CYP3A and P-gp substrate and conivaptan is a moderate CYP3A and P-gp inhibitor.
Crizotinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if concomitant use with crizotinib is necessary. Maraviroc is a sensitive CYP3A substrate and crizotinib is a moderate CYP3A4 inhibitor. Coadministration with moderate CYP3A4 inhibitors may result in increased maraviroc concentrations.
Cyclosporine: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and cyclosporine as increased maraviroc concentrations may occur. Maraviroc is a substrate of CYP3A, P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP1B), and multidrug resistance-associated protein (MRP2). Cyclosporine is a CYP3A4, P-gp, OATP1B1, and MRP2 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Dabrafenib: (Major) The concomitant use of dabrafenib and maraviroc may lead to decreased maraviroc concentrations and loss of efficacy. Use of an alternative agent is recommended. If concomitant use of these agents together is unavoidable, monitor patients for loss of maraviroc efficacy. Dabrafenib is a moderate CYP3A4 inducer and maraviroc is a sensitive CYP3A4 substrate. Concomitant use of dabrafenib with a single dose of another sensitive CYP3A4 substrate decreased the AUC value of the sensitive CYP3A4 substrate by 65%.
Daclatasvir: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and daclatasvir as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp) and organic anion-transporting polypeptide (OATP1B1); daclatasvir is an inhibitor of P-gp and OATP1B1. The effects of these transporters on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Danazol: (Moderate) Use caution if coadministration of maraviroc with danazol is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and danazol is a CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Darolutamide: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with darolutamide is necessary. Concurrent use may increase the plasma concentrations of maraviroc. Maraviroc is an OATP1B1 substrate; darolutamide is an OATP1B1 inhibitor.
Darunavir: (Major) Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors such as darunavir; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCL less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with darunavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Darunavir; Cobicistat: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with cobicistat (a CYP3A4, P-gp, OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with cobicistat; coadministration is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with cobicistat (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended. (Major) Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors such as darunavir; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCL less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with darunavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with cobicistat (a CYP3A4, P-gp, OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with cobicistat; coadministration is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with cobicistat (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended. (Major) Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors such as darunavir; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCL less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with darunavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Deferasirox: (Moderate) Use caution if coadministration of maraviroc with deferasirox is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and deferasirox is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Delavirdine: (Major) Coadministration of maraviroc, a CYP3A substrate, with delavirdine, a strong CYP3A4 inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with delavirdine (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Dextromethorphan; Quinidine: (Moderate) Use caution and careful monitoring with the coadministration of maraviroc and quinidine as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); quinidine is an inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Diltiazem: (Moderate) Monitor for an increase in maraviroc adverse effects with concomitant use of diltiazem due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and diltiazem is a CYP3A4 inhibitor.
Dronedarone: (Moderate) Use caution if coadministration of maraviroc with dronedarone is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A and P-glycoprotein (P-gp) substrate and dronedarone is a CYP3A4/P-gp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Duvelisib: (Moderate) Monitor for increased toxicity of maraviroc if coadministered with duvelisib. Coadministration may increase the exposure of maraviroc. Maraviroc is a sensitive CYP3A substrate; duvelisib is a moderate CYP3A inhibitor.
Efavirenz: (Major) Coadministration of maraviroc, a CYP3A substrate, and efavirenz, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor, significantly decreases maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with efavirenz without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and efavirenz is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Efavirenz; Emtricitabine; Tenofovir Disoproxil Fumarate: (Major) Coadministration of maraviroc, a CYP3A substrate, and efavirenz, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor, significantly decreases maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with efavirenz without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and efavirenz is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate: (Major) Coadministration of maraviroc, a CYP3A substrate, and efavirenz, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor, significantly decreases maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with efavirenz without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and efavirenz is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Elacestrant: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with elacestrant is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; elacestrant is a P-gp inhibitor.
Elbasvir; Grazoprevir: (Minor) Use caution if coadministration of maraviroc with grazoprevir is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and grazoprevir is a weak CYP3A inhibitor. Monitor for an increase in adverse effects with concomitant use.
Elexacaftor; tezacaftor; ivacaftor: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with elexacaftor is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is an OATP1B1 substrate; elexacaftor is an OATP1B1 inhibitor. (Minor) Use caution if coadministration of maraviroc with ivacaftor is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A and P-glycoprotein (Pgp) substrate and ivacaftor is a weak CYP3A4/Pgp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Eliglustat: (Moderate) Use caution and closely monitor for increased adverse effects with the coadministration of maraviroc and eliglustat as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); eliglustat is an inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Eltrombopag: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and eltrombopag as increased maraviroc concentrations may occur. Maraviroc is a substrate of organic anion-transporting polypeptide (OATP1B1); eltrombopag is an inhibitor of OATP1B1. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with cobicistat (a CYP3A4, P-gp, OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with cobicistat; coadministration is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with cobicistat (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended. (Major) Coadministration of maraviroc, a CYP3A substrate, with elvitegravir boosted with ritonavir, a strong CYP3A4 inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with elvitegravir boosted with ritonavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with cobicistat (a CYP3A4, P-gp, OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with cobicistat; coadministration is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with cobicistat (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended. (Major) Coadministration of maraviroc, a CYP3A substrate, with elvitegravir boosted with ritonavir, a strong CYP3A4 inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with elvitegravir boosted with ritonavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Enasidenib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with enasidenib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp and OATP1B1 substrate; enasidenib is a P-gp and OATP1B1 inhibitor.
Encorafenib: (Moderate) Coadministration of encorafenib with maraviroc may result in increased toxicity or decreased efficacy of maraviroc. Maraviroc is a sensitive CYP3A4 substrate. In vitro studies with encorafenib showed time-dependent inhibition of CYP3A4 and induction of CYP3A4. The clinical relevance of the in vivo effect of encorafenib on CYP3A4 is not established. Additionally, maraviroc is an OATP1B1 substrate and encorafenib is an OATP1B1 inhibitor. Monitor for an increase in maraviroc-related adverse reactions if these medications are used together.
Enzalutamide: (Major) Coadministration of maraviroc, a CYP3A substrate, and enzalutamide, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with enzalutamide without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and enzalutamide is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Erythromycin: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and eythromycin as increased maraviroc concentrations may occur. Maraviroc is a substrate of CYP3A, P-glycoprotein (P-gp), and organic anion-transporting polypeptide (OATP1B). Erythromycin is a CYP3A4, P-gp, and OATP1B1 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Eslicarbazepine: (Moderate) Use caution if coadministration of maraviroc with eslicarbazepine is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and eslicarbazepine is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Etravirine: (Major) Coadministration of maraviroc, a CYP3A substrate, and etravirine, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor significantly decreases maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with etravirine without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and etravirine is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Felbamate: (Minor) Use caution if coadministration of maraviroc with felbamate is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and felbamate is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Flibanserin: (Moderate) Use caution and closely monitor for increased adverse effects with the coadministration of maraviroc and flibanserin as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); flibanserin is an inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Fluconazole: (Moderate) Use caution if coadministration of maraviroc with fluconazole is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and fluconazole is a CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Fluoxetine: (Minor) Use caution if coadministration of maraviroc with fluoxetine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and fluoxetine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Flutamide: (Moderate) Use caution if coadministration of maraviroc with flutamide is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate. Flutamide is an inducer of CYP3A4 in vitro but the clinical significance of this finding is unknown. Monitor for a decrease in maraviroc efficacy with concomitant use.
Fosamprenavir: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with fosamprenavir is necessary. Maraviroc is a sensitive CYP3A substrate and fosamprenavir is a moderate CYP3A inhibitor. Coadministration with moderate CYP3A inhibitors may result in increased maraviroc concentrations.
Fosphenytoin: (Major) Coadministration of maraviroc, a CYP3A substrate, and fosphenytoin, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with fosphenytoin without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and fosphenytoin is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Fostamatinib: (Moderate) Monitor for maraviroc toxicities that may require maraviroc dose reduction if given concurrently with fostamatinib. Concomitant use of fostamatinib with a P-gp substrate may increase the concentration of the P-gp substrate. Fostamatinib is a P-gp inhibitor; maraviroc is a substrate for P-gp. Coadministration of fostamatinib with another P-gp substrate increased the P-gp substrate AUC by 37% and Cmax by 70%.
Furosemide: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and furosemide as increased maraviroc concentrations may occur. Maraviroc is a substrate of multidrug resistance-associated protein (MRP2); furosemide is an inhibitor of MRP2. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Futibatinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with futibatinib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; futibatinib is a P-gp inhibitor.
Gemfibrozil: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and gemfibrozil as increased maraviroc concentrations may occur. Maraviroc is a substrate of organic anion-transporting polypeptide (OATP1B1); gemfibrozil is an inhibitor of OATP1B1. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Gilteritinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with gilteritinib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; gilteritinib is a P-gp inhibitor.
Glecaprevir; Pibrentasvir: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and glecaprevir as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp) and organic anion-transporting polypeptide (OATP1B1); glecaprevir is an inhibitor of P-gp and OATP1B1. The effects of these transporters on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible. (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and pibrentasvir as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp) and organic anion-transporting polypeptide (OATP1B1); pibrentasvir is an inhibitor of P-gp and OATP1B1. The effects of these transporters on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Grapefruit juice: (Major) Advise patients to avoid grapefruit and grapefruit juice during maraviroc therapy. Coadministration of maraviroc, a CYP3A substrate, with grapefruit juice, a strong CYP3A4 inhibitor, may result in increased maraviroc concentrations and increased side effects. Reduce the dose of maraviroc when it is used with other strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/minute.
Idelalisib: (Major) Coadministration of idelalisib, a strong CYP3A4 inhibitor, and maraviroc, a CYP3A4 substrate, may result in elevated maraviroc concentrations. According to the manufacturer of idelalisib, concomitant use of idelalisib and CYP3A substrates should be avoided. The AUC of a sensitive CYP3A substrate was increased 5.4-fold when coadministered with idelalisib. According to the manufacturer of maraviroc, a reduced adult maraviroc dose of 150 mg PO twice daily is recommended when it is administered in the presence of a CYP3A inhibitor, with or without a concomitant CYP3A inducer. Coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Dose recommendations in pediatrics are: 150 mg PO twice daily for children weighing 40 kg or more, 100 mg PO twice daily for children weighing 30 to 39 kg, 75 mg PO twice daily (or 80 mg PO twice daily for solution) for children weighing 20 to 29 kg, 50 mg PO twice daily for children weighing 10 to 19 kg, and use is not recommended in children weighing 2 to 9 kg.
Imatinib: (Moderate) Use caution if coadministration of maraviroc with imatinib is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and imatinib is a CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Indinavir: (Major) Coadministration of maraviroc, a CYP3A substrate, with indinavir, a strong CYP3A4 inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with indinavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Isavuconazonium: (Moderate) Use caution if coadministration of maraviroc with isavuconazonium is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A/P-glycoprotein (P-gp) substrate and isavuconazole, the active moiety of isavuconazonium, is a CYP3A4/P-gp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Isoniazid, INH; Pyrazinamide, PZA; Rifampin: (Major) Coadministration of maraviroc, a CYP3A/P-glycoprotein (P-gp) substrate, and rifampin, a strong CYP3A inducer and P-gp inducer, without a concomitant strong CYP3A inhibitor significantly decreases maraviroc concentrations. Consider using rifabutin instead of rifampin in patients receiving maraviroc. However, if rifampin must be used, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with rifampin without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and rifampin is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Isoniazid, INH; Rifampin: (Major) Coadministration of maraviroc, a CYP3A/P-glycoprotein (P-gp) substrate, and rifampin, a strong CYP3A inducer and P-gp inducer, without a concomitant strong CYP3A inhibitor significantly decreases maraviroc concentrations. Consider using rifabutin instead of rifampin in patients receiving maraviroc. However, if rifampin must be used, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with rifampin without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and rifampin is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Itraconazole: (Major) Reduce the dose of maraviroc when coadministered with itraconazole; coadministration is contraindicated in patients with CrCl less than 30 mL/min. Coadministration of maraviroc, a CYP3A/P-gp substrate, with itraconazole, a strong CYP3A4 inhibitor and P-gp inhibitor, may result in increased maraviroc concentrations. Maraviroc dosage adjustments are as follows when administered with itraconazole (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Ivacaftor: (Minor) Use caution if coadministration of maraviroc with ivacaftor is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A and P-glycoprotein (Pgp) substrate and ivacaftor is a weak CYP3A4/Pgp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Ketoconazole: (Major) Reduce the dose of maraviroc when coadministration with ketoconazole is necessary, regardless of whether the patient is receiving a concomitant strong CYP3A4 inducer. The effect of ketoconazole on maraviroc exposure is expected to exceed that of the inducer and overall, increased maraviroc concentrations are expected. Coadministration of maraviroc with ketoconazole is contraindicated in patients with CrCl less than 30 mL/minute. Recommendations for reducing the maraviroc dose when administered with ketoconazole (with or without a concomitant CYP3A inducer) are: adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily. Maraviroc is a sensitive CYP3A substrate and ketoconazole is a strong CYP3A inhibitor. Coadministration with strong CYP3A4 inhibitors may result in increased maraviroc concentrations.
Lansoprazole; Amoxicillin; Clarithromycin: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with clarithromycin (a strong CYP3A4 inhibitor and P-gp/OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with clarithromycin (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Lapatinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with lapatinib is necessary. Maraviroc is a P-glycoprotein (P-gp) substrate and lapatinib is a P-gp inhibitor. Concomitant use may increase maraviroc exposure.
Lasmiditan: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with lasmiditan is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; lasmiditan is a P-gp inhibitor.
Ledipasvir; Sofosbuvir: (Minor) Use caution and closely monitor for increased adverse effects with the coadministration of maraviroc and ledipasvir as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); ledipasvir is a weak inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Leflunomide: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and leflunomide as increased maraviroc concentrations may occur. Maraviroc is a substrate of organic anion-transporting polypeptide (OATP1B1); leflunomide is an inhibitor of OATP1B1. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Lenacapavir: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with lenacapavir is necessary. Maraviroc is a CYP3A and P-gp substrate and lenacapavir is a moderate CYP3A and P-gp inhibitor. Coadministration with moderate CYP3A inhibitors may result in increased maraviroc concentrations.
Leniolisib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with leniolisib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is an OATP1B1 substrate; leniolisib is an OATP1B1 inhibitor.
Lesinurad: (Minor) Use caution if coadministration of maraviroc with lesinurad is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and lesinurad is a weak CYP3A4 inducer. Monitor for a decrease in efficacy with concomitant use.
Lesinurad; Allopurinol: (Minor) Use caution if coadministration of maraviroc with lesinurad is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and lesinurad is a weak CYP3A4 inducer. Monitor for a decrease in efficacy with concomitant use.
Letermovir: (Moderate) Administering letermovir with maraviroc may increase maraviroc concentration and risk for adverse events. In patients also receiving cyclosporine, reduce maraviroc adult dose to 150 mg twice daily (weight based dose reductions also recommended for pediatric patients), because the magnitude of the interaction may be amplified. In patients with severe renal impairment, use of maraviroc with both letermovir and cyclosporine is contraindicated. Maraviroc is primarily metabolized by CYP3A4 and is a substrate of organic anion-transporting polypeptide (OATP1B). Letermovir is a moderate CYP3A4 and OATP1B1 inhibitor; however, when given with cyclosporine, the combined effect on CYP3A4 substrates may be similar to a strong CYP3A4 inhibitor.
Levamlodipine: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Levoketoconazole: (Major) Reduce the dose of maraviroc when coadministration with ketoconazole is necessary, regardless of whether the patient is receiving a concomitant strong CYP3A4 inducer. The effect of ketoconazole on maraviroc exposure is expected to exceed that of the inducer and overall, increased maraviroc concentrations are expected. Coadministration of maraviroc with ketoconazole is contraindicated in patients with CrCl less than 30 mL/minute. Recommendations for reducing the maraviroc dose when administered with ketoconazole (with or without a concomitant CYP3A inducer) are: adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily. Maraviroc is a sensitive CYP3A substrate and ketoconazole is a strong CYP3A inhibitor. Coadministration with strong CYP3A4 inhibitors may result in increased maraviroc concentrations.
Lomitapide: (Moderate) Concomitant use of lomitapide and maraviroc may result in increased serum concentrations of maraviroc. According to the manufacturer of lomitapide, dose reduction of maraviroc should be considered during concurrent use. Lomitapide is an inhibitor of P-glycoprotein (P-gp) and maraviroc is a P-gp substrate.
Lonafarnib: (Major) Reduce the dose of maraviroc when coadministration with lonafarnib is necessary, regardless of whether the patient is receiving a concomitant strong CYP3A inducer. The effect of lonafarnib on maraviroc exposure is expected to exceed that of the inducer and overall, increased maraviroc concentrations are expected. Coadministration of maraviroc with lonafarnib is contraindicated in patients with CrCl less than 30 mL/min. Recommendations for reducing the maraviroc dose when administered with lonafarnib (with or without a concomitant CYP3A inducer) are: adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily. Maraviroc is a sensitive CYP3A and P-gp substrate and lonafarnib is a strong CYP3A and P-gp inhibitor.
Lopinavir; Ritonavir: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, MRP2) with ritonavir (a strong CYP3A4 inhibitor and P-gp/MRP2 inhibitor) has been reported to significantly increase maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with ritonavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended. (Major) Coadministration of maraviroc, a substrate of organic anion-transporting polypeptide (OATP1B1), with lopinavir, a OATP1B1 inhibitor, has been reported to increase maraviroc exposure. Adjust the maraviroc dosage as follows when administered with lopinavir; ritonavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Lorlatinib: (Moderate) Monitor for a decrease in the efficacy of maraviroc if coadministration with lorlatinib is necessary. Maraviroc is a CYP3A4 substrate and a P-glycoprotein (P-gp) substrate. Lorlatinib is a moderate CYP3A4 inducer as well as a P-gp inducer.
Lumacaftor; Ivacaftor: (Major) Coadministration of maraviroc, a CYP3A substrate, and lumacaftor; ivacaftor, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with lumacaftor; ivacaftor without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and lumacaftor; ivacaftor is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Lumacaftor; Ivacaftor: (Minor) Use caution if coadministration of maraviroc with ivacaftor is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A and P-glycoprotein (Pgp) substrate and ivacaftor is a weak CYP3A4/Pgp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Maribavir: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with maribavir is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; maribavir is a P-gp inhibitor.
Mavacamten: (Major) Increase the adult dose of maraviroc to 600 mg PO twice daily when coadministered with mavacamten without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and mavacamten is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, the concomitant use of maraviroc with mavacamten without also taking a strong CYP3A inhibitor is not recommended. If the adult or pediatric patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of mavacamten; overall, increased maraviroc concentrations are expected (see recommended dose adjustments for use of maraviroc with the strong inhibitor). Maraviroc is a sensitive CYP3A substrate and mavacamten is a moderate CYP3A inducer.
Mefloquine: (Moderate) Use caution and closely monitor for increased adverse effects with the coadministration of maraviroc and mefloquine as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); mefloquine is an inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Midostaurin: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with midostaurin is necessary. Concurrent use may increase the plasma concentrations of maraviroc. Maraviroc is an OATP1B1 substrate; midostaurin is an OATP1B1 inhibitor.
Mifepristone: (Moderate) Use caution if coadministration of maraviroc with mifepristone is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A/P-glycoprotein (P-gp) substrate and mifepristone is a CYP3A4/P-gp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Mitapivat: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with mitapivat is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; mitapivat is a P-gp inhibitor.
Modafinil: (Moderate) Use caution if coadministration of maraviroc with modafinil is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and modafinil is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Nafcillin: (Moderate) Use caution if coadministration of maraviroc with nafcillin is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and nafcillin is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Nefazodone: (Major) Coadministration of maraviroc, a CYP3A substrate, with nefazodone, a strong CYP3A4 inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with nefazodone (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Nelfinavir: (Major) Coadministration of maraviroc, a CYP3A/P-gp substrate, with nelfinavir, a strong CYP3A4 inhibitor and P-gp inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with nelfinavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Neratinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with neratinib is necessary. Concurrent use may increase the plasma concentrations of maraviroc. Maraviroc is a P-glycoprotein (P-gp) substrate; neratinib is a P-gp inhibitor.
Netupitant, Fosnetupitant; Palonosetron: (Moderate) Use caution if coadministration of maraviroc with netupitant is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and netupitant is a CYP3A4 inhibitor; the inhibitory effect on CYP3A4 can last for multiple days. Monitor for an increase in adverse effects with concomitant use.
Nicardipine: (Moderate) Monitor for an increase in adverse effects with concomitant use of maraviroc and nicardipine due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A and nicardipine is a CYP3A4 inhibitor.
Nifedipine: (Minor) Use caution and careful monitoring with the coadministration of maraviroc and nifedipine as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (Pgp); nifedipine is a mild inhibitor of Pgp. The effects of Pgp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Nirmatrelvir; Ritonavir: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, MRP2) with ritonavir (a strong CYP3A4 inhibitor and P-gp/MRP2 inhibitor) has been reported to significantly increase maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with ritonavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Olanzapine; Fluoxetine: (Minor) Use caution if coadministration of maraviroc with fluoxetine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and fluoxetine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Olmesartan; Amlodipine; Hydrochlorothiazide, HCTZ: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Omeprazole; Amoxicillin; Rifabutin: (Moderate) Use caution if coadministration of maraviroc with rifabutin is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and rifabutin is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Oritavancin: (Minor) Use caution if coadministration of maraviroc with oritavancin is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and oritavancin is a weak CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Osimertinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with osimertinib is necessary. Maraviroc is a P-glycoprotein (P-gp) substrate and osimertinib is a P-gp inhibitor. Concomitant use may increase maraviroc exposure.
Oxcarbazepine: (Moderate) Use caution if coadministration of maraviroc with oxcarbazepine is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and oxcarbazepine is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Pacritinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with pacritinib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; pacritinib is a P-gp inhibitor.
Pazopanib: (Minor) Use caution if coadministration of maraviroc with pazopanib is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and pazopanib is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Perampanel: (Minor) Use caution if coadministration of maraviroc with perampanel is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and perampanel is a weak CYP3A4 inducer. Monitor for a decrease in efficacy with concomitant use.
Perindopril; Amlodipine: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Pexidartinib: (Moderate) Be aware of the potential for decreased plasma concentrations of maraviroc if coadministration with pexidartinib is necessary, leading to a reduction of antiretroviral efficacy and the potential development of viral resistance. Maraviroc is a sensitive CYP3A4 substrate and pexidartinib is a moderate CYP3A4 inducer.
Phenobarbital: (Major) Coadministration of maraviroc, a CYP3A/P-glycoprotein (P-gp) substrate, and phenobarbital, a strong CYP3A inducer and P-gp inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with phenobarbital without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and phenobarbital is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Phenobarbital; Hyoscyamine; Atropine; Scopolamine: (Major) Coadministration of maraviroc, a CYP3A/P-glycoprotein (P-gp) substrate, and phenobarbital, a strong CYP3A inducer and P-gp inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with phenobarbital without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and phenobarbital is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Phentermine; Topiramate: (Minor) Use caution if coadministration of maraviroc with topiramate is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and topiramate is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Phenytoin: (Major) Coadministration of maraviroc, a CYP3A substrate, and phenytoin, a strong CYP3A inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with phenytoin without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and phenytoin is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Pirfenidone: (Minor) Use caution and closely monitor for increased adverse effects with the coadministration of maraviroc and pirfenidone as increased maraviroc concentrations may occur. Maraviroc is a substrate of CYP3A and P-glycoprotein (P-gp); pirfenidone is a weak inhibitor of CYP3A4 and P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Pirtobrutinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with pirtobrutinib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; pirtobrutinib is a P-gp inhibitor.
Posaconazole: (Major) Coadministration of maraviroc, a CYP3A/P-gp substrate, with posaconazole, a strong CYP3A4 inhibitor and P-gp inhibitor, may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with posaconazole (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Pretomanid: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with pretomanid is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; pretomanid is a P-gp inhibitor.
Primidone: (Major) Coadministration of maraviroc, a CYP3A/P-glycoprotein (P-gp) substrate, and primidone, a strong CYP3A inducer and P-gp inducer, without a concomitant strong CYP3A inhibitor may decrease maraviroc concentrations, therefore, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with primidone without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and primidone is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Probenecid: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and probenecid as increased maraviroc concentrations may occur. Maraviroc is a substrate of multidrug resistance-associated protein (MRP2); probenecid is an inhibitor of MRP2. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Probenecid; Colchicine: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and probenecid as increased maraviroc concentrations may occur. Maraviroc is a substrate of multidrug resistance-associated protein (MRP2); probenecid is an inhibitor of MRP2. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Propafenone: (Moderate) Use caution and careful monitoring with the coadministration of maraviroc and propafenone as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); propafenone is an inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Quinidine: (Moderate) Use caution and careful monitoring with the coadministration of maraviroc and quinidine as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); quinidine is an inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Quinine: (Moderate) Use caution if coadministration of maraviroc with quinine is necessary as altered maraviroc concentrations may occur. Maraviroc is a substrate of CYP3A; quinine is an inhibitor and inducer of CYP3A4. Monitor for decreased efficacy and/or an increase in adverse effects with concomitant use.
Ranolazine: (Moderate) Use caution and careful monitoring with the coadministration of maraviroc and ranolazine as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp) and CYP3A; ranolazine is an inhibitor of P-gp and a weak in vitro inhibitor of CYP3A. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Ribociclib: (Major) Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors such as ribociclib; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCL less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with ribociclib (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Ribociclib; Letrozole: (Major) Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors such as ribociclib; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCL less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with ribociclib (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Rifabutin: (Moderate) Use caution if coadministration of maraviroc with rifabutin is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and rifabutin is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Rifampin: (Major) Coadministration of maraviroc, a CYP3A/P-glycoprotein (P-gp) substrate, and rifampin, a strong CYP3A inducer and P-gp inducer, without a concomitant strong CYP3A inhibitor significantly decreases maraviroc concentrations. Consider using rifabutin instead of rifampin in patients receiving maraviroc. However, if rifampin must be used, the adult maraviroc dose should be increased to 600 mg PO twice daily when coadministered with rifampin without a concomitant strong CYP3A inhibitor. Coadministration of maraviroc and rifampin is contraindicated in patients with CrCl less than 30 mL/min. For pediatric patients, concomitant use of maraviroc with a strong CYP3A inducer, without a strong CYP3A inhibitor, is not recommended. If the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected.
Rifapentine: (Major) The HIV guidelines recommend avoiding coadministration of maraviroc and rifapentine as decreased concentrations of maraviroc are expected. Maraviroc is a substrate of CYP3A and rifapentine is a CYP3A4 inducer. However, if the patient's medication regimen also contains a strong CYP3A inhibitor, the CYP3A inhibitor's actions are expected to exceed that of the inducer; overall, increased maraviroc concentrations are expected. Monitor for decreased efficacy if coadministration is necessary.
Ritlecitinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with ritlecitinib is necessary. Maraviroc is a sensitive CYP3A substrate and ritlecitinib is a moderate CYP3A inhibitor. Coadministration with moderate CYP3A inhibitors may result in increased maraviroc concentrations.
Ritonavir: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, MRP2) with ritonavir (a strong CYP3A4 inhibitor and P-gp/MRP2 inhibitor) has been reported to significantly increase maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with ritonavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Rolapitant: (Moderate) Use caution and closely monitor for increased adverse effects with the coadministration of maraviroc and rolapitant as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); rolapitant is an inhibitor of P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Saquinavir: (Major) Coadministration of maraviroc, a CYP3A/P-gp substrate, with saquinavir, a strong CYP3A4 inhibitor and P-gp inhibitor, has been reported to increase maraviroc concentrations by 9.8-fold. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with saquinavir (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Selpercatinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with selpercatinib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; selpercatinib is a P-gp inhibitor.
Sodium Phenylbutyrate; Taurursodiol: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with taurursodiol is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; taurursodiol is a P-gp inhibitor.
Sofosbuvir; Velpatasvir: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and velpatasvir as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp) and organic anion-transporting polypeptide (OATP1B1); velpatasvir is an inhibitor of P-gp and OATP1B1. The effects of these transporters on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Sofosbuvir; Velpatasvir; Voxilaprevir: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and velpatasvir as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp) and organic anion-transporting polypeptide (OATP1B1); velpatasvir is an inhibitor of P-gp and OATP1B1. The effects of these transporters on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible. (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and voxilaprevir as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp) and organic anion-transporting polypeptide (OATP1B1); voxilaprevir is an inhibitor of P-gp and OATP1B1. The effects of these transporters on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Sorafenib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with sorafenib is necessary. Maraviroc is a P-glycoprotein (P-gp) substrate. Sorafenib inhibits P-gp in vitro and may increase the concentrations of concomitantly administered drugs that are P-gp substrates.
Sotorasib: (Major) Avoid concurrent use of sotorasib and maraviroc due to unpredictable effects. Coadministration may alter the exposure of maraviroc resulting in decreased efficacy or increased toxicity. Maraviroc is a CYP3A4 and P-gp substrate; sotorasib is a moderate CYP3A4 inducer and P-gp inhibitor.
Sparsentan: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with sparsentan is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; sparsentan is a P-gp inhibitor.
St. John's Wort, Hypericum perforatum: (Major) Concomitant use of maraviroc and St. John's wort, Hypericum perforatum or products containing St. John's wort is not recommended. St. John's wort is expected to substantially decrease maraviroc concentrations; reductions in plasma concentrations could lead to HIV treatment failures or the development of viral-resistance. St. John's wort in all forms, including teas, should be avoided in HIV-infected patients treated with maraviroc.
Stiripentol: (Moderate) Consider a dose adjustment of maraviroc when coadministered with stiripentol. Coadministration may alter plasma concentrations of maraviroc resulting in an increased risk of adverse reactions and/or decreased efficacy. Maraviroc is a sensitive CYP3A4 substrate. In vitro data predicts inhibition or induction of CYP3A4 by stiripentol potentially resulting in clinically significant interactions.
Tacrolimus: (Minor) Use caution and careful monitoring with the coadministration of maraviroc and tacrolimus as increased maraviroc concentrations may occur. Maraviroc is a substrate of P-glycoprotein (P-gp); tacrolimus may be an inhibitor of P-gp. Conflicting data exist regarding any interaction between tacrolimus and P-gp. The effects of P-gp on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Telmisartan; Amlodipine: (Minor) Use caution if coadministration of maraviroc with amlodipine is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and amlodipine is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Temsirolimus: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with temsirolimus is necessary; a dose adjustment of maraviroc may be necessary. Maraviroc is a P-glycoprotein (P-gp) substrate and temsirolimus is a P-gp inhibitor. Concomitant use is likely to lead to increased concentrations of maraviroc.
Tepotinib: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with tepotinib is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp substrate; tepotinib is a P-gp inhibitor.
Teriflunomide: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and teriflunomide as increased maraviroc concentrations may occur. Maraviroc is a substrate of organic anion-transporting polypeptide (OATP1B1); teriflunomide is an inhibitor of OATP1B1. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Tezacaftor; Ivacaftor: (Minor) Use caution if coadministration of maraviroc with ivacaftor is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A and P-glycoprotein (Pgp) substrate and ivacaftor is a weak CYP3A4/Pgp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Ticagrelor: (Minor) Use caution if coadministration of maraviroc with ticagrelor is necessary due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A4 and P-glycoprotein substrate (P-gp) and ticagrelor is a weak CYP3A4 and P-gp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Topiramate: (Minor) Use caution if coadministration of maraviroc with topiramate is necessary, due to a possible decrease in maraviroc exposure. Maraviroc is a CYP3A substrate and topiramate is a CYP3A4 inducer. Monitor for a decrease in maraviroc efficacy with concomitant use.
Trandolapril; Verapamil: (Moderate) Use caution if coadministration of maraviroc with verapamil is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A4/P-glycoprotein (P-gp) substrate and verapamil is a CYP3A4/P-gp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Trofinetide: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with trofinetide is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is an OATP1B1 substrate; trofinetide is an OATP1B1 inhibitor.
Tucatinib: (Major) Reduce the dose of maraviroc when coadministered with tucatinib; coadministration is contraindicated in patients with CrCl less than 30 mL/minute. Coadministration of maraviroc, a CYP3A/P-gp substrate, with tucatinib, a strong CYP3A4 inhibitor and P-gp inhibitor, may result in increased maraviroc concentrations. Maraviroc dosage adjustments are as follows when administered with tucatinib (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Valproic Acid, Divalproex Sodium: (Minor) Use caution and closely monitor for decreased efficacy and/or increased adverse effects with the coadministration of maraviroc and valproic acid as altered maraviroc concentrations may occur. Maraviroc is a substrate of CYP3A and P-glycoprotein (P-gp); valproic acid is a weak CYP3A4 inhibitor/inducer, as well as a weak P-gp inducer. The effects of P-gp on the concentrations of maraviroc are unknown, although a decrease in concentrations and thus, decreased efficacy, are possible.
Vemurafenib: (Moderate) Concomitant use of vemurafenib and maraviroc may result in altered concentrations of maraviroc. Vemurafenib is an inhibitor of P-glycoprotein (P-gp) and a weak inducer of CYP3A4. Maraviroc is a substrate of P-gp and CYP3A4. Use caution and monitor patients for toxicity and efficacy.
Verapamil: (Moderate) Use caution if coadministration of maraviroc with verapamil is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A4/P-glycoprotein (P-gp) substrate and verapamil is a CYP3A4/P-gp inhibitor. Monitor for an increase in adverse effects with concomitant use.
Voclosporin: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with voclosporin is necessary. Concomitant use may increase maraviroc exposure. Maraviroc is a P-gp and OATP1B1 substrate; voclosporin is a P-gp and OATP1B1 inhibitor.
Vonoprazan; Amoxicillin; Clarithromycin: (Major) Coadministration of maraviroc (a substrate of CYP3A, P-gp, and OATP1B1) with clarithromycin (a strong CYP3A4 inhibitor and P-gp/OATP1B1 inhibitor) may result in increased maraviroc concentrations. Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCl less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with clarithromycin (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Voriconazole: (Major) Reduce the dose of maraviroc when coadministered with strong CYP3A inhibitors such as voriconazole; coadministration of maraviroc with strong CYP3A inhibitors is contraindicated in patients with CrCL less than 30 mL/min. Adjust the maraviroc dosage as follows when administered with voriconazole (with or without a concomitant CYP3A inducer): adults and children weighing 40 kg or more: 150 mg PO twice daily; children weighing 30 to 39 kg: 100 mg PO twice daily; children weighing 20 to 29 kg: 75 mg PO twice daily (or 80 mg PO twice daily for solution); children weighing 10 to 19 kg: 50 mg PO twice daily; children weighing 2 to 9 kg: use not recommended.
Voxelotor: (Moderate) Monitor for an increase in maraviroc-related adverse reactions if coadministration with voxelotor is necessary. Maraviroc is a sensitive CYP3A substrate and voxelotor is a moderate CYP3A inhibitor. Coadministration with moderate CYP3A inhibitors may result in increased maraviroc concentrations.
Zafirlukast: (Minor) Use caution if coadministration of maraviroc with zafirlukast is necessary, due to a possible increase in maraviroc exposure. Maraviroc is a CYP3A substrate and zafirlukast is a weak CYP3A4 inhibitor. Monitor for an increase in adverse effects with concomitant use.
Zonisamide: (Minor) Zonisamide is a weak inhibitor of P-glycoprotein (P-gp), and maraviroc is a substrate of P-gp. There is theoretical potential for zonisamide to affect the pharmacokinetics of drugs that are P-gp substrates. Use caution when starting or stopping zonisamide or changing the zonisamide dosage in patients also receiving drugs which are P-gp substrates.
How Supplied
Maraviroc/Selzentry Oral Sol: 1mL, 20mg
Maraviroc/Selzentry Oral Tab: 25mg, 75mg, 150mg, 300mg
Maximum Dosage
600 mg/day PO; 1,200 mg/day PO if taking a potent or moderate CYP3A inducer; 300 mg/day PO if taking a potent CYP3A inhibitor.
Geriatric600 mg/day PO; 1,200 mg/day PO if taking a potent or moderate CYP3A inducer; 300 mg/day PO if taking a potent CYP3A inhibitor.
Adolescentsweighing 40 kg or more: 600 mg/day PO; 300 mg/day PO if taking a potent CYP3A inhibitor; use not recommended with potent or moderate CYP3A inducers.
weighing 30 to 39 kg: 600 mg/day PO; 200 mg/day PO if taking a potent CYP3A inhibitor; use not recommended with potent or moderate CYP3A inducers.
weighing 40 kg or more: 600 mg/day PO; 300 mg/day PO if taking a potent CYP3A inhibitor; use not recommended with potent or moderate CYP3A inducers.
weighing 30 to 39 kg: 600 mg/day PO; 200 mg/day PO if taking a potent CYP3A inhibitor; use not recommended with potent or moderate CYP3A inducers.
weighing 20 to 29 kg: 400 mg/day PO; 150 mg/day PO for tablets and 160 mg/day PO for solution if taking a potent CYP3A inhibitor; use not recommended with potent or moderate CYP3A inducers.
weighing 14 to 19 kg: 400 mg/day PO; 100 mg/day PO if taking a potent CYP3A inhibitor; use not recommended with potent or moderate CYP3A inducers.
weighing 10 to 13 kg: 300 mg/day PO; 100 mg/day PO if taking a potent CYP3A inhibitor; use not recommended with potent or moderate CYP3A inducers.
weighing 6 to 9 kg: 200 mg/day PO for solution; use not recommended with potent or moderate CYP3A inducers or potent CYP3A inhibitors.
weighing 6 to 9 kg: 200 mg/day PO for solution; use not recommended with potent or moderate CYP3A inducers or potent CYP3A inhibitors.
weighing 4 to 5 kg: 80 mg/day for solution; use not recommended with potent or moderate CYP3A inducers or potent CYP3A inhibitors.
weighing 2 to 3 kg: 60 mg/day for solution; use not recommended with potent or moderate CYP3A inducers or potent CYP3A inhibitors.
weighing 4 to 5 kg: 80 mg/day for solution; use not recommended with potent or moderate CYP3A inducers or potent CYP3A inhibitors.
weighing 2 to 3 kg: 60 mg/day for solution; use not recommended with potent or moderate CYP3A inducers or potent CYP3A inhibitors.
Mechanism Of Action
Maraviroc interferes with the entry of HIV-1 into host cells by inhibiting the fusion of the virus and cell membranes. In order for HIV-1 to enter and infect a human cell, the viral surface glycoprotein gp120 binds to the host CD4+ cell receptor, along with a chemokine co-receptor CCR5 or CXCR4 (both expressed on lymphocytes and mononuclear cells). Then, the viral transmembrane glycoprotein gp41 undergoes a conformational change facilitating the fusion of cellular and viral membranes. Maraviroc blocks the CCR5 receptor and prevents the functional viral envelope protein-co-receptor interaction required for membrane fusion and subsequent viral entry into target cells.
Maraviroc is only effective at reducing viral load in patients with CCR5-tropic HIV strains; it is not effective against viruses targeting the CXCR4 co-receptor (i.e., CXCR4-tropic HIV) and has a limited effect against viruses with the ability to target both receptors (i.e., dual-tropic HIV). CXCR4-tropic and dual-tropic HIV strains are common in patients with HIV for several years. Because the target population for maraviroc is treatment-experienced patients, who have likely been infected with HIV for several years, tropism assay of the HIV strain is necessary prior to treatment. In the majority of cases, treatment failure on maraviroc was associated with the detection of CXCR4-using (i.e., CXCR4- or dual-tropic) virus which was not detected by the tropism assay prior to treatment. CXCR4-using virus was detected at failure in approximately 55% of patients who failed treatment on maraviroc, as compared to 9% who experienced treatment failure in the placebo arm. To investigate the likely origin of the on-treatment CXCR4-using virus, a detailed clonal analysis was conducted on viruses from 20 representative subjects (16 subjects from the maraviroc arms and 4 subjects from the placebo arm) in whom CXCR4-using virus was detected at treatment failure. From an analysis of amino acid sequence differences and phylogenetic data, CXCR4-using virus in these subjects emerged from a low level of pre-existing CXCR4-using virus not detected by the tropism assay (which is population-based) prior to treatment rather than from a co-receptor switch from CCR5-tropic virus to CXCR4-using virus resulting from a mutation in the virus.
Pharmacokinetics
Maraviroc is administered orally. It is bound (approximately 76%) to human plasma proteins, and shows moderate affinity for albumin and alpha-1 acid glycoprotein. After a single 300 mg dose of 14C-maraviroc, maraviroc is the major circulating component (approximately 42% drug related radioactivity) and the most significant circulating metabolite is a secondary amine (approximately 22% radioactivity) formed by N-dealkylation; this metabolite has no significant pharmacological activity. The terminal half-life following oral dosing to steady-state in healthy subjects was 14 to 18 hours. Maraviroc was the major component present in urine (mean of 8% dose) and feces (mean of 25% dose); the remainder was excreted as metabolites.
Affected cytochrome P450 isoenzymes and drug transporters: CYP3A, CYP2D6, P-gp, OATP1B1, MRP2
Maraviroc is a substrate of CYP3A, P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP1B1), and multidrug resistance-associated protein (MRP2). The pharmacokinetic parameters of maraviroc are likely to be modulated by inhibitors and inducers of CYP3A4 and P-gp, and may be modulated by inhibitors of OATP1B1 and MRP2. The recommended dose of maraviroc differs based on concurrently administered medications and their influence on CYP3A. Carefully asses each medications' potential for CYP3A influence prior to coadministration, and adjust the maraviroc dose accordingly. Based on in vitro data, maraviroc is unlikely to inhibit the actions of CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, or CYP3A enzymes. In addition, maraviroc does not inhibit the CYP2D6 enzyme in vitro until concentrations are more than 100 microM, which correlate with low or normal doses (i.e., 150 mg or 300 mg twice daily); there is potential inhibition at higher doses (i.e., 600 mg twice daily). In vitro studies suggest that maraviroc could inhibit P-gp in the gut; however, it did not significantly affect the pharmacokinetics of digoxin in vivo, suggesting maraviroc may not significantly inhibit or induce P-gp clinically. Maraviroc does not inhibit the uptake of OATP1B1 or the export of MRP2.
The absolute bioavailability is 23% for maraviroc 100 mg and is predicted to be 33% for maraviroc 300 mg. In volunteers without HIV, peak plasma concentrations were attained 0.5 to 4 hours after single oral doses of 1 to 1,200 mg. The pharmacokinetics are not dose-proportional over the dose range. Administration of a 300 mg tablet with a high-fat breakfast reduced the Cmax and AUC by 33% in healthy volunteers; coadministration of 75 mg of the oral solution with a high-fat breakfast reduced the AUC by 73%. There were no food restrictions in the studies that demonstrated the efficacy and safety; therefore, maraviroc can be administered with or without food. In healthy volunteers receiving 300 mg twice daily, the Cmax was 888 ng/mL, the Cmin was 43.1 ng/mL, and the AUC12 was 2,908 ng x hour/mL. In asymptomatic HIV patients receiving 300 mg twice daily in phase 2 trials, the Cmax was 618 ng/mL, the Cmin was 33.6 ng/mL, and the AUC12 was 2,550 ng x hour/mL. In treatment-experienced HIV patients receiving 300 mg twice daily, the Cmax was 266 ng/mL, the Cmin was 37.2 ng/mL, and the AUC12 was 1,513 ng x hour/mL. In treatment-experienced HIV patients receiving 150 mg twice daily with a CYP3A4 inhibitor, the Cmax was 332 ng/mL, the Cmin was 101 ng/mL, and the AUC12 was 2,463 ng x hour/mL. In treatment-naive HIV patients receiving 300 mg twice daily, the Cmax was 287 ng/mL, the Cmin was 60 ng/mL, and the AUC12 was 1,865 ng x hour/mL.
Pregnancy And Lactation
Antiretroviral therapy should be provided to all patients during pregnancy, regardless of HIV RNA concentrations or CD4 cell count. Using highly active antiretroviral combination therapy (HAART) to maximally suppress viral replication is the most effective strategy to prevent the development of resistance and to minimize the risk of perinatal transmission. Begin HAART as soon as pregnancy is recognized, or HIV is diagnosed. Data regarding administration of maraviroc during pregnancy are too limited to rule out any potential association with birth defects (i.e., 30 first trimester exposures); therefore, maraviroc-containing regimens should not be initiated in pregnant patients. However, it may be appropriate to continue use of the drug in some virally suppressed pregnant patients. Regular laboratory monitoring is recommended to determine antiretroviral efficacy. Monitor CD4 counts at the initial visit. Patients who have been on HAART for at least 2 years and have consistent viral suppression and CD4 counts consistently greater than 300 cells/mm3 do not need CD4 counts monitored after the initial visit during the pregnancy. However, CD4 counts should be monitored every 3 months during pregnancy for patients on HAART less than 2 years, patients with CD4 count less than 300 cells/mm3, or patients with inconsistent adherence or detectable viral loads. Monitor plasma HIV RNA at the initial visit (with review of prior levels), 2 to 4 weeks after initiating or changing therapy, monthly until undetectable, and then at least every 3 months during pregnancy. Viral load should also be assessed at approximately 36 weeks gestation, or within 4 weeks of delivery, to inform decisions regarding mode of delivery and optimal treatment for newborns. Patients whose HIV RNA levels are above the threshold for resistance testing (usually greater than 500 copies/mL but may be possible for levels greater than 200 copies/mL in some laboratories) should undergo antiretroviral resistance testing (genotypic testing, and if indicated, phenotypic testing). Resistance testing should be conducted before starting therapy in treatment-naive patients who have not been previously tested, starting therapy in treatment-experienced patients (including those who have received pre-exposure prophylaxis), modifying therapy in patients who become pregnant while receiving treatment, or modifying therapy in patients who have suboptimal virologic response to treatment that was started during pregnancy. DO NOT delay initiation of antiretroviral therapy while waiting on the results of resistance testing; treatment regimens can be modified, if necessary, once the testing results are known. First trimester ultrasound is recommended to confirm gestational age and provide an accurate estimation of gestational age at delivery. A second trimester ultrasound can be used for both anatomical survey and determination of gestational age in those patients not seen until later in gestation. Perform standard glucose screening in patients receiving antiretroviral therapy at 24 to 28 weeks gestation, although it should be noted that some experts would perform earlier screening with ongoing chronic protease inhibitor-based therapy initiated prior to pregnancy, similar to recommendations for patients with high-risk factors for glucose intolerance. Liver function testing is recommended within 2 to 4 weeks after initiating or changing antiretroviral therapy, and approximately every 3 months thereafter during pregnancy (or as needed). All pregnant patients should be counseled about the importance of adherence to their antiretroviral regimen to reduce the potential for development of resistance and perinatal transmission. It is strongly recommended that antiretroviral therapy, once initiated, not be discontinued. If a patient decides to discontinue therapy, a consultation with an HIV specialist is recommended. There is a pregnancy exposure registry that monitors outcomes in pregnant patients exposed to maraviroc; information about the registry can be obtained at www.apregistry.com or by calling 1-800-258-4263.
HIV treatment guidelines recommend clinicians provide mothers with evidence-based, patient-centered counseling to support shared decision-making regarding infant feeding. Inform patients that use of replacement feeding (i.e., formula or banked pasteurized donor human milk) eliminates the risk of HIV transmission; thus, replacement feeding is recommended for use when mothers with HIV are not on antiretroviral therapy (ART) or do not have suppressed viral load during pregnancy, as well as at delivery. For patients on ART who have achieved and maintained viral suppression during pregnancy (at minimum throughout the third trimester) and postpartum, the transmission risk from breast-feeding is less than 1%, but not zero. Virologically suppressed mothers who choose to breast-feed should be supported in this decision. If breast-feeding is chosen, counsel the patient about the importance of adherence to therapy and recommend that the infant be exclusively breast-fed for up to 6 months of age, as exclusive breast-feeding has been associated with a lower rate of HIV transmission as compared to mixed feeding (i.e., breast milk and formula). Promptly identify and treat mastitis, thrush, and cracked or bleeding nipples, as these conditions may increase the risk of HIV transmission through breast-feeding. Breast-fed infants should undergo immediate diagnostic and virologic HIV testing. Testing should continue throughout breast-feeding and up to 6 months after cessation of breast-feeding. For expert consultation, healthcare workers may contact the Perinatal HIV Hotline (888-448-8765). There are limited data regarding maraviroc use during breast-feeding, and excretion into human breast milk is unknown. Antiretroviral medications whose passage into human breast milk have been evaluated include nevirapine, zidovudine, lamivudine, and nelfinavir.