CCR5 antagonism in HIV infection: current concepts and future opportunities. Review uri icon



  • CCR5 antagonists inhibit HIV-1 entry by blocking the interaction of HIV-1 with the CCR5 cellular receptor. In patients with established HIV-1 infection, some viral strains use an alternative coreceptor for HIV-1 entry, CXCR4; CCR5 antagonists are not effective in patients harboring these viral strains. Coreceptor tropism testing of viral strains in an individual patient is necessary prior to treating with a CCR5 antagonist. There is one CCR5 antagonist, maraviroc, that is FDA-approved for treatment of HIV-1 infection. This drug is used most commonly for the treatment of HIV-1 infection in patients who have failed other antiretroviral regimens. In addition to virologic effects, CCR5 antagonists are under investigation for immune-modulating effects and for HIV-1 prevention. Ongoing research will further elucidate the role of CCR5 antagonists in combating HIV disease.

publication date

  • October 27, 2011



  • CCR5 Receptor Antagonists
  • Cyclohexanes
  • HIV Infections
  • HIV-1
  • Triazoles


PubMed Central ID

  • PMC3298858

Scopus Document Identifier

  • 84855928248

Digital Object Identifier (DOI)

  • 10.1146/annurev-med-052010-145454

PubMed ID

  • 22034870

Additional Document Info


  • 63