title: Maraviroc: pharmacokinetics and drug interactions.
abstract: Maraviroc is a potent selective CCR5 antagonist and is the first of this new class of oral agents to be approved for the treatment of CCR5-tropic HIV type-1. Maraviroc is extensively metabolized by CYP3A4, with renal clearance accounting for approximately 23% of total clearance. The half-life of maraviroc is approximately 16 h. Maraviroc does not inhibit any of the major CYP450 enzymes at clinically relevant doses and it has not shown any clinically relevant effects on plasma concentrations of other agents; hence, no dose adjustments of coadministered agents are required. Maraviroc exposure is altered by agents that modulate the activity of CYP3A4 and, in some circumstances, maraviroc dose adjustment is necessary. This article aims to review all pharmacokinetic and drug interaction data available for maraviroc, and to provide a comprehensive summary of the dose adjustment recommendations for maraviroc when coadministered with agents from all classes of antiretroviral therapy as well as other commonly coadministered agents.
authors.affiliation: Pfizer Global Research and Development, Sandwich, UK.
authors.forename: Samantha
authors.initials: S
authors.lastname: Abel
authors.forename: David J
authors.initials: DJ
authors.lastname: Back
authors.forename: Manoli
authors.initials: M
authors.lastname: Vourvahis
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000378:metabolism; D065100:CCR5 Receptor Antagonists; D002986:Clinical Trials as Topic; D003510:Cyclohexanes / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D005260:Female; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008297:Male; D000077592:Maraviroc; D008875:Middle Aged; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000378:metabolism; D014230:Triazoles / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; D065100:CCR5 Receptor Antagonists; D003510:Cyclohexanes; D018894:Reverse Transcriptase Inhibitors; D014230:Triazoles; D000077592:Maraviroc