CCR5 antagonism in HIV infection: current concepts and future opportunities.
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.
Division of Infectious Diseases, Weill Medical College of Cornell University, New York, New York 10065, USA. tiw2001@med.cornell.edu
Timothy J
TJ
Wilkin
Roy M
RM
Gulick
D065100:CCR5 Receptor Antagonists; D003510:Cyclohexanes / Q000627:therapeutic use*; D055808:Drug Discovery / Q000639:trends; D023581:HIV Fusion Inhibitors / Q000627:therapeutic use; D015658:HIV Infections / Q000517:prevention & control* / Q000821:virology*; D015497:HIV-1 / Q000378:metabolism*; D006801:Humans; D000077592:Maraviroc; D019713:Receptors, CCR5 / Q000378:metabolism; D014230:Triazoles / Q000627:therapeutic use*
D065100:CCR5 Receptor Antagonists; D003510:Cyclohexanes; D023581:HIV Fusion Inhibitors; D019713:Receptors, CCR5; D014230:Triazoles; D000077592:Maraviroc