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CCR5 antagonist Pregnancy: eMC §4.6: there are limited data from the use of maraviroc in pregnant women and the effect on human pregnancy is unknown; animal studies showed reproductive toxicity at high exposures. Maraviroc should be used during pregnancy only if the expected benefit justifies the potential risk to the foetus. It is unknown whether maraviroc is excreted in human milk (extensive excretion in animal milk) and a risk to the newborn/infant cannot be excluded; it is recommended that women living with HIV do not breast-feed their infants in order to avoid transmission of HIV. There are no data on effects on human fertility.

Maraviroc

Brand names: Celsentri

Maraviroc is an antiretroviral CCR5 antagonist used as part of combination therapy for HIV infection in patients with detectable CCR5-tropic virus.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 150 mg, 300 mg or 600 mg twice daily, chosen according to concomitant medicines: 150 mg twice daily with a potent CYP3A inhibitor (with or without a potent CYP3A inducer); 300 mg twice daily without potent CYP3A inhibitors or inducers; 600 mg twice daily with a potent CYP3A inducer without a potent CYP3A inhibitor
Route: Oral use - maraviroc can be taken with or without food
Frequency: Twice daily
eMC §4.2 (Maraviroc 150 mg film-coated tablets). Therapy should be initiated by a physician experienced in the management of HIV infection. BEFORE STARTING: it has to be confirmed that only CCR5-tropic HIV-1 is detectable (i.e. CXCR4 or dual/mixed tropic virus not detected) using an adequately validated and sensitive detection method on a newly drawn blood sample - viral tropism cannot be safely predicted by treatment history or from stored samples. The stated adult regimen applies to adults and adolescents weighing at least 30 kg. Many medicines have profound effects on maraviroc exposure through drug-drug interactions, so the SPC directs prescribers to Table 2 in §4.5 to determine the correct dose before prescribing. There are no data on reuse of maraviroc in patients who now have only CCR5-tropic virus but previously failed maraviroc (or another CCR5 antagonist) with CXCR4 or dual/mixed tropic virus, and no data on switching from another antiretroviral class in virologically suppressed patients - alternative treatment options should be considered. PAEDIATRIC (eMC §4.2, non per-kg so not captured as a structured paediatric dose): children and adolescents weighing less than 30 kg, or unable to reliably swallow the tablets, should be prescribed the oral solution (20 mg per mL) - refer to the separate SPC for maraviroc oral solution. For adolescents the SPC gives a weight-band table (30 to less than 40 kg, and at least 40 kg) derived from the corresponding adult dose: where the adult dose would be 150 mg twice daily, an adolescent 30 to <40 kg should receive the oral solution and one weighing at least 40 kg 150 mg twice daily; where the adult dose would be 300 mg twice daily, 300 mg twice daily in both weight bands; where the adult dose would be 600 mg twice daily, data to support these doses are lacking and maraviroc is NOT recommended in children taking concomitant interacting medicines that in adults would require 600 mg twice daily. Safety and efficacy in children younger than 2 years of age or weighing less than 10 kg has not been established and no data are available. There are no data to recommend a specific dose in paediatric patients with renal impairment or hepatic impairment, so maraviroc should be used with caution in that population. Verify any under-18 use against a children's formulary. ELDERLY: limited experience in patients over 65 years - use with caution. HEPATIC IMPAIRMENT: limited data in adults and none for children; use with caution. The eMC §4.5 interactions table was not captured in this bundle - the clinician must read it in the SPC before selecting a dose.

Dose adjustments

Renal

eMC §4.2: in adult patients with a creatinine clearance below 80 mL/min who are ALSO receiving potent CYP3A4 inhibitors, the dose interval should be adjusted to 150 mg once daily. Potent CYP3A4 inhibitors given as examples are ritonavir-boosted protease inhibitors (except tipranavir/ritonavir), cobicistat, itraconazole, voriconazole, clarithromycin, telithromycin, telaprevir and boceprevir. Use with caution in adults with severe renal impairment (CrCl <30 mL/min) receiving potent CYP3A4 inhibitors. No data are available to recommend a specific dose in paediatric patients with renal impairment. The US labelling goes further and contraindicates maraviroc in severe renal impairment or ESRD (CrCl <30 mL/min) when a potent CYP3A inhibitor or inducer is co-administered.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to the active substance or to peanut or soya or to any of the excipients (eMC §4.3)
  • The US labelling additionally lists a contraindication not present in the eMC §4.3 text: patients with severe renal impairment or end-stage renal disease (CrCl less than 30 mL/min) who are concomitantly taking potent CYP3A inhibitors or inducers (US label §4)

Side effects

  • Most frequently reported in the Phase 2b/3 studies and all common (>=1/100 to <1/10): nausea, diarrhoea, fatigue and headache (eMC §4.8)
  • Common: abdominal pain, flatulence, nausea; anorexia; depression, insomnia; asthenia; rash
  • Common: anaemia; alanine aminotransferase increased, aspartate aminotransferase increased
  • Uncommon: postural hypotension; seizures and seizure disorders; renal failure, proteinuria; myositis and blood creatine phosphokinase increased; hyperbilirubinaemia; pneumonia and oesophageal candidiasis
  • Rare/very rare: toxic hepatitis, hepatic failure, hepatic cirrhosis, hepatic failure with allergic features, angina pectoris, pancytopenia, granulocytopenia, Stevens-Johnson syndrome / toxic epidermal necrolysis. Delayed-type hypersensitivity reactions typically occur within 2-6 weeks of starting therapy and include rash, fever, eosinophilia and liver reactions

Interactions

  • eMC §4.2 states many medicines have profound effects on maraviroc exposure and directs prescribers to Table 2 of §4.5 to determine the dose - that §4.5 table was NOT captured in this bundle and must be consulted in the SPC
  • Potent CYP3A inhibitors (with or without a potent CYP3A inducer) increase maraviroc concentrations - eMC examples include ritonavir-boosted protease inhibitors (except tipranavir/ritonavir), cobicistat, itraconazole, voriconazole, clarithromycin, telithromycin, telaprevir and boceprevir; dose 150 mg twice daily
  • Potent and moderate CYP3A inducers without a potent CYP3A inhibitor decrease maraviroc concentrations - US label §7.1 lists carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin and rifampicin; dose 600 mg twice daily
  • Concomitant use of maraviroc and St John's wort (Hypericum perforatum) is not recommended - expected to substantially decrease maraviroc concentrations, risking loss of virologic response and resistance (US label §7.1)
  • Maraviroc is a CYP3A substrate and also a substrate for P-glycoprotein, OATP1B1 and MRP2, so inhibitors and inducers of these may modulate its pharmacokinetics and require a dosage adjustment (US label §7.1)

Clinical monograph

How it works

It binds the CCR5 co-receptor on the host cell surface, blocking the interaction with the viral envelope glycoprotein that CCR5-tropic HIV requires to enter the cell.

Prescribing in practice

  • A tropism test must confirm CCR5-tropic virus before use, because maraviroc is ineffective against CXCR4-tropic or dual/mixed-tropic HIV.
  • It is a CYP3A substrate, so the dose must be adjusted according to interacting drugs and current prescribing references.
  • Hepatotoxicity, sometimes preceded by allergic or systemic features, has been reported and warrants vigilance.

Monitoring

Monitor HIV viral load and CD4 count, and review liver function and for signs of hypersensitivity during treatment.

Counselling the patient

  • This medicine only works against a particular type of HIV, which is why a blood test is done first.
  • Take it consistently as part of your full HIV treatment.
  • Report any jaundice, abdominal pain or rash promptly.

Evidence & guidelines

Efficacy in treatment-experienced patients with CCR5-tropic HIV was shown in randomised controlled trials supporting its licensed use.

Reference: BHIVA; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.