Maraviroc: a new CCR5 antagonist

Expert Rev Anti Infect Ther. 2009 Feb;7(1):9-19. doi: 10.1586/14787210.7.1.9.


Maraviroc is a small molecule and a member of a new class of antiretroviral compounds known as CCR5 antagonists, which block R5-tropic HIV entry into CD4 cells. HIV entry into the cell requires binding to a CD4 molecule and, in the majority of cases, to a coreceptor, either chemokine coreceptor 4 (CXCR4) or 5 (CCR5). In August 2007, the US FDA approved maraviroc for use in combination with other antiretroviral agents for treatment-experienced adults infected with CCR5-tropic HIV-1 only and who have evidence of viral replication. Maraviroc prevents the virus from entering uninfected cells by blocking the CCR5 coreceptor. Maraviroc has two dose formulations (150- and 300-mg tablets) and can be taken with or without food. The dosing recommendations are based on concomitant medications due to drug interactions. It is excreted primarily in the feces, with approximately 25% via urine. The safety and efficacy of maraviroc have not been established in pregnant women or pediatric patients. Maraviroc has been shown to achieve an undetectable HIV-1 RNA level in clinically advanced, class 3 antiretroviral treatment-experienced adults with evidence of CCR5-tropic HIV-1 replication despite ongoing antiretroviral therapy. It is generally well tolerated and its development is responding to a desperate need for new classes of antiretroviral agents that can target novel steps of the HIV lifecycle and do not share crossresistance with currently available therapy.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents* / administration & dosage
  • Anti-HIV Agents* / adverse effects
  • Anti-HIV Agents* / chemistry
  • Anti-HIV Agents* / therapeutic use
  • CCR5 Receptor Antagonists*
  • Child
  • Clinical Trials as Topic
  • Cyclohexanes* / administration & dosage
  • Cyclohexanes* / adverse effects
  • Cyclohexanes* / chemistry
  • Cyclohexanes* / therapeutic use
  • Female
  • HIV Fusion Inhibitors* / administration & dosage
  • HIV Fusion Inhibitors* / adverse effects
  • HIV Fusion Inhibitors* / chemistry
  • HIV Fusion Inhibitors* / therapeutic use
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV-1 / drug effects*
  • Humans
  • Male
  • Maraviroc
  • Pregnancy
  • Treatment Outcome
  • Triazoles* / administration & dosage
  • Triazoles* / adverse effects
  • Triazoles* / chemistry
  • Triazoles* / therapeutic use


  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Cyclohexanes
  • HIV Fusion Inhibitors
  • Triazoles
  • Maraviroc