Maraviroc
SELZENTRY
What it isCCR5 antagonist blocking viral entry; CCR5-tropic HIV.
Why this oneIt blocks a host receptor rather than a viral enzyme, so resistance pathways differ entirely.
What limits itA tropism assay is required first, and it fails against CXCR4-tropic virus. Hepatotoxicity; CYP3A4-dependent.
FDA-approved for
- CCR5-tropic HIV-1 infection (2007)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 (CCR5-tropic) + potent CYP3A inhibitors (with/without inducer) | Adult | 150 mg BID | 150 mg BID | 150 mg BID |
| HIV-1 (CCR5-tropic) + non-interacting meds (NRTIs, tipranavir/rtv, nevirapine, raltegravir, dolutegravir) | Adult | 300 mg BID | 300 mg BID | 300 mg BID |
| HIV-1 (CCR5-tropic) + potent/moderate CYP3A inducers (efavirenz, rifampin, etc.) | Adult | 600 mg BID | 600 mg BID | 600 mg BID |
| HIV-1 (CCR5-tropic), weight-based; not to exceed adult dose | Peds ≥2 yr, ≥10 kg | 50–150 mg BID by weight & concomitant meds | per weight/concomitant meds | 300 mg BID |
Renal Adjust by CrCl and concomitant meds; contraindicated in severe impairment/ESRD (CrCl <30) on potent CYP3A inhibitors or inducers; reduce to 150 mg BID if postural hypotension.
Hepatic Concentrations may increase; monitor closely (esp. moderate impairment on potent CYP3A inhibitor); not studied in severe impairment.
Dose depends on concomitant CYP3A inhibitors/inducers.
Instructions
- Test all patients for CCR5 tropism before starting.
- Must be given with other antiretrovirals.
- Take with or without food.
- If unable to swallow tablets, use oral solution.
Contraindications
- Severe renal impairment or ESRD (CrCl <30 mL/min) while taking potent CYP3A inhibitors or inducers.
Cautions
- Hepatotoxicity with allergic features (life-threatening).
- Severe skin/hypersensitivity reactions (SJS, TEN, DRESS).
- Cardiovascular events; postural hypotension (esp. renal impairment).
- Immune reconstitution syndrome.
- Increased risk of infection and possible malignancy (CCR5 antagonism).
Adverse reactions
- URTI
- cough
- pyrexia
- rash
- dizziness/postural dizziness
- constipation
- herpes infection (treatment-experienced adults)
Pregnancy Limited human data; no adverse developmental effects in animals. Antiretroviral Pregnancy Registry 1-800-258-4263.
Lactation Do not breastfeed — risk of HIV-1 transmission; human-milk presence unknown (present in rat milk).
⚠ BOXED WARNING
- Hepatotoxicity
Cost, est. cash$10–$500/month
Generic entry2022
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Mechanism of action: Maraviroc ballicule
