Reviews of anti-infective agents: maraviroc: the first of a new class of antiretroviral agents.
Maraviroc is the first US Food and Drug Administration-approved drug from a new class of antiretroviral agents that targets a host protein, the chemokine receptor CCR5, rather than a viral target. Binding of maraviroc to this cell-surface protein results in blocking human immunodeficiency virus type 1 (HIV-1) attachment to the coreceptor and prevents the virus from entering CD4+ cells. In this review, we include the details of the discoveries that led to the development of this drug. The drug's pharmacology, including pharmacokinetics and drug interactions, is discussed, as are the clinical efficacy studies that led to licensure. HIV-1 mechanisms of resistance to maraviroc, assays to determine viral coreceptor use (tropism), drug safety, and clinical use of maraviroc are discussed at length.
Wayne State University, Detroit, Michigan, USA. rmacarthur@med.wayne.edu
Rodger D
RD
MacArthur
Richard M
RM
Novak
D019380:Anti-HIV Agents / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D001681:Biological Assay; D065100:CCR5 Receptor Antagonists; D015496:CD4-Positive T-Lymphocytes / Q000378:metabolism / Q000821:virology; D002986:Clinical Trials as Topic; D003510:Cyclohexanes / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D051544:Cytochrome P-450 CYP3A / Q000187:drug effects / Q000378:metabolism; D004347:Drug Interactions; D024882:Drug Resistance, Viral / Q000502:physiology; D015658:HIV Infections / Q000188:drug therapy* / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D000077592:Maraviroc; D019713:Receptors, CCR5 / Q000378:metabolism; D014230:Triazoles / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D018523:Tropism; D053586:Virus Internalization
D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D003510:Cyclohexanes; D019713:Receptors, CCR5; D014230:Triazoles; D051544:Cytochrome P-450 CYP3A; D000077592:Maraviroc