Dosing & Uses
Dosage Forms & Strengths
tablet
- 150mg
- 300mg
oral solution
- 20mg/mL
HIV-1 Infection
Indicated for combination antiretroviral treatment of CCR5-tropic HIV-1 in patients who have viral replication and HIV-1 strains resistant to multiple antiretroviral agents
Recommended dosage differs based on concomitant medications owing to drug interactions; examples are listed below (ie, not an exhaustive list)
Noninteracting concomitant medications
- 300 mg PO BID
- Noninteracting drugs include: tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, and enfuvirtide
- Also, all other medications that are not potent CYP3A inhibitors or inducers
Potent CYP3A inhibitors (with or without a potent CYP3A inducer)
- 150 mg PO BID
- Potent CYP3A inhibitors include: protease inhibitors (except tipranavir/ritonavir), delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors (eg, nefazodone, telithromycin)
Potent CYP3A inducers (without a potent CYP3A inhibitor)
- 600 mg PO BID
- Potent CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin
Renal Impairment
Patients with severe impairment or ESRD on hemodialysis who are also taking potent CYP3A inhibitors or inducers: Contraindicated
Renal impairment in patients taking noninteracting concomitant medications
- No dosage change required (ie, may continue on maraviroc 300 mg BID), unless postural hypotension experienced, then reduce dose to 150 mg BID
Hepatic Impairment
Mild to moderate impairment: Maraviroc concentrations increased but dose adjustment not recommended; monitor
Moderate impairment and strong CYP 3A4 inhibitor: Use caution; monitor closely for adverse reactions
Maraviroc concentrations are higher when 150 mg BID is administered in patients with moderate hepatic impairment who are taking a potent CYP3A inhibitor compared with 300 mg BID without a CYP3A inhibitor
Severe impairment: Not studied
Dosing Considerations
Limitations of use: Not recommended in patients with dual/mixed- or CXCR4-tropic HIV-1
Testing before initiating
- Test all patients for CCR5 tropism using a highly sensitive tropism assay
- Maraviroc is recommended for patients with only CCR5-tropic HIV-1 infection
- Outgrowth of pre-existing low-level CXCR4- or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on maraviroc
- Monitor ALT, AST, and bilirubin prior to initiating, and periodically during treatment
Dosage Forms & Strengths
tablet
- 25mg
- 75mg
- 150mg
- 300mg
oral solution
- 20mg/mL
HIV-1 Infection
Indicated for combination antiretroviral treatment for the treatment of only CCR5-tropic HIV-1 infection in patients aged ≥2 years who weigh at least 10 kg
<2 years: Safety and efficacy not established
≥16 years: As in adults
Recommended dosage differs based on concomitant medications owing to drug interactions; examples are listed below (ie, not an exhaustive list)
Noninteracting concomitant medications
- <30 kg: Not recommended
- ≥30 kg: 300 mg PO BID
- Noninteracting drugs include: tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, and enfuvirtide
- Also, all other medications that are not potent CYP3A inhibitors or inducers
Potent CYP3A inhibitors (with or without a potent CYP3A inducer)
- 10 kg to <20 kg: 50 mg PO BID
- 20 kg to <30 kg: 75 mg (tablet) or 80 mg (oral solution) PO BID
- 30 kg to <40 kg: 100 mg PO BID
- ≥40 kg: 150 mg PO BID
- Potent CYP3A inhibitors include: protease inhibitors (except tipranavir/ritonavir), delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors (eg, nefazodone, telithromycin)
Potent CYP3A inducers (without a potent CYP3A inhibitor)
- Maraviroc is NOT recommended for children taking potent CYP3A inducers
- Potent CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin
Renal Impairment
Mild-to-moderate (CrCl 30-80 mL/min): Data are not available to recommend specific doses in children
Patients with severe impairment or ESRD on hemodialysis who are also taking potent CYP3A inhibitors or inducers: Contraindicated
Dosing Considerations
Limitations of use: Not recommended in patients with dual/mixed- or CXCR4-tropic HIV-1
Testing before initiating
- Test all patients for CCR5 tropism using a highly sensitive tropism assay
- Maraviroc is recommended for patients with only CCR5-tropic HIV-1 infection
- Outgrowth of pre-existing low-level CXCR4- or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on maraviroc
- Monitor ALT, AST, and bilirubin prior to initiating, and periodically during treatment
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Upper respiratory infections (20%)
Arthritis and musculoskeletal S/S (15%)
Cough (13%)
Pyrexia (12%)
Rash (11%)
Fever (13%)
2-10%
Dizziness (9%)
Appetite disorder (8%)
Herpes infection (8%)
Bronchitis (7%)
Sinusitis (7%)
Constipation (6%)
Apocrine and eccrine gland disorder (5%)
Paresthesia/dysesthesia (5%)
Renal/urinary disorder (3-5%)
Depression (4%)
Disturbed consciousness (4%)
Periph neuropathies (4%)
Pruritus (4%)
Sensory abnormalities (4%)
Folliculitis (3%)
Hypertension (3%)
Lipodystrophy (3%)
Muscle pain (3%)
Influenza (2%)
Pneumonia (2%)
Condyloma acuminata
Dermatitis/eczema
Dyspepsia
GI pain
Stomatitis/ulceration
<2% (critical ADRs)
CBN
Cardiac disorder
CVA
Hepatic cirrhosis
Hepatic failure
Neoplasms
C. difficile colitis
Viral meningitis
Pneumonia
Septic shock
Myositis
Osteonecrosis
Rhabdomyolysis
Warnings
Black Box Warnings
Hepatotoxicity reported; may be preceded by systemic allergic reaction (eg, pruritic rash, eosinophilia, elevated IgE)
Immediately evaluate if signs or symptoms of hepatitis or allergic reaction occur
Contraindications
Hypersensitivity
Severe renal impairment or end-stage renal disease (CrCl <30 mL/min) in patients taking potent CYP3A4 inhibitors or inducers
Cautions
Risks of hepatotoxicity
Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs
Autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) reported in the setting of immune reconstitution, however, the time to onset is more variable, and can occur many months after initiation of treatment
Do not use in treatment-naïve patients; more likely to experienced virologic failure and developed lamivudine resistance compared to efavirenz
Tropism testing with a highly sensitive tropism assay is required for the appropriate use
Evaluate if signs/symptoms of hepatitis, increase LFTs, or rash develop
Preexisting liver dysfunction or viral hepatitis B or C coinfection
Patient history of increased risk for cardiovascular events
History of postural hypotension or concomitant use of blood pressure lowering medication
Caution in renal and hepatic impairment; postural hypotension reported in patients with renal impairment
Monitor for developing infections
When administering to patients with pre-existing liver dysfunction or who are co-infected with hepatitis B and/or C virus, additional monitoring may be warranted
Cardiovascular adverse events triggered by postural hypotension’ additional monitoring may be warranted
Antiretroviral Pregnancy Registry has been established.to monitor maternal-fetal outcomes of pregnant women; register patients by calling 1-800-258-4263
Drug interaction overview
- Drug is metabolized by CYP3A, and is also a substrate for P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP)1B1, and multidrug resistance-associated protein (MRP)2; pharmacokinetics of maraviroc are likely to be modulated by inhibitors and inducers of CYP3A and P-gp, and may be modulated by inhibitors of OATP1B1 and MRP2; therefore, dosage adjustment may be required when maraviroc is coadministered with those drugs
Pregnancy & Lactation
Pregnancy: Limited data on pregnancy from the APR and case reports are not sufficient to inform a drug-associated risk of birth defects and miscarriage; n animal reproduction studies, no evidence of adverse developmental outcomes observed with maraviroc
Lactation: Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in United States not breastfeed their infants to avoid risking postnatal transmission of HIV-1 infection
There are no data on presence of maraviroc in human milk, effects on breastfed infant, or effects on milk production; when administered to lactating rats, maraviroc was present in milk; because of potential for (1) HIV transmission (in HIV-negative infants), (2) developing viral resistance (in HIV-positive infants), and (3) serious adverse reactions in a breastfed infant similar to those seen in adults, instruct mothers not to breastfeed if they are receiving therapy
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Selective antagonist of the interaction between human CCR5 and HIV-1 gp120; blocking this interaction prevents CCR5-tropic HIV-1 entry into cells
Absorption
Bioavailability: 23-33%
Peak plasma time: 0.5-4 hr
Peak plasma concentration: 333 ng/mL (330 mg BID)
Distribution
Protein bound: 76%
Vd: 194 L
Metabolism
Metabolized by cytochrome P450 system, with CYP3A as major enzyme of metabolism
Elimination
Half-life: 14-18 hr
Excretion: 76% (feces); 20% (urine)
Administration
Oral Administration
Tablets and oral solution are taken twice daily
May take with or without food
Must be given in combination with other antiretroviral medications
The recommended dosage of maraviroc differs based on concomitant medications owing to drug interactions
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Patient Handout
Formulary
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