maraviroc (Rx)

HIV-1 Infection

Indicated in combination with other antiretroviral agents for treatment of only CCR5-tropic human immunodeficiency virus type 1 (HIV-1) infection

General dosage recommendations

Administer PO BID

Must be given in combination with other antiretroviral medications

Recommended dose differs based on concomitant medications owing to drug interactions

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, dolutegravir, 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), elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, cobicistat, nefazodone, and telithromycin

Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)

• 600 mg PO BID
• Potent and moderate CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Dosage Modifications

Renal impairment

• Mild-to-moderate (CrCl 30-80 mL/min): No dosage adjustment required

• Severe (CrCl <30 mL/min)

  • Coadministered with potent CYP3A inhibitors: Contraindicated
  • Coadministered with noninteracting medications: No dose adjustment required
  • Coadministered with potent and moderate CYP3A inducers: Contraindicated

• ESRD on hemodialysis

  • Coadministered with potent CYP3A inhibitors: Contraindicated
  • Coadministered with noninteracting medications: Reduce to 300 mg qDay
  • Coadministered with potent and moderate CYP3A inducers: Contraindicated

Hepatic impairment

• Mild to moderate impairment: Serum 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 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
• Only indicated for patients with 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

HIV-1 Infection

Indicated in combination with other antiretroviral agents for treatment of only CCR5-tropic human immunodeficiency virus type 1 (HIV-1) infection in patients weighing at least 2 kg

General dosing recommendations

• Administer PO BID
• Must be given in combination with other antiretroviral medications
• Recommended dose differs based on concomitant medications owing to drug interactions

Aged 2 years and older weighing at least 10 kg (tablets)

• Noninteracting concomitant medications

  • 10 kg to <14 kg: 150 mg PO BID
  • 14 kg to <30 kg: 200 mg PO BID
  • ≥30 kg: 300 mg PO BID
  • Noninteracting drugs include:dolutegrative, 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 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), elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, nefazodone, and telithromycin

• Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)

  • Not recommended for children taking potent CYP3A inducers
  • Potent and moderate CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Pediatric patients weighing at least 2 kg (oral solution)

• Noninteracting concomitant medications

  • 2 kg to <4 kg: 30 mg (1.5 mL) PO BID
  • 4 kg to <6 kg: 40 mg (2 mL) PO BID
  • 6 kg to <10 kg: 100 mg (5 mL) PO BID
  • 10 kg to <14 kg: 150 mg (7.5 mL) PO BID
  • 14 kg to <30 kg: 200 mg (10 mL) PO BID
  • ≥30 kg: 300 mg (15 mL) PO BID

• Potent CYP3A inhibitors (with or without a potent CYP3A inducer)

  • 2 kg to <10 kg: Not recommended
  • 10 kg to <20 kg: 50 mg (2.5 mL) PO BID
  • 20 kg to <30 kg: 80 mg (4 mL) PO BID
  • 30 kg to <40 kg: 100 mg (5 mL) PO BID
  • ≥40 kg: 150 mg (7.5 mL) PO BID

• Potent CYP3A inducers (without a potent CYP3A inhibitor)

  • NOT recommended for children taking potent CYP3A inducers
  • Potent and moderate CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Dosage Modifications

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
• Only indicated for patients with 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