What is the role of chemokine receptor antagonists in antiretroviral therapy of HIV infection?

Updated: Apr 18, 2019
  • Author: R Chris Rathbun, PharmD, BCPS (AQ-ID), AAHIVP; Chief Editor: John Bartlett, MD  more...
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Answer

In August 2007, maraviroc (Selzentry) was approved by the FDA and was the first medication in a novel class of antiretroviral agents termed chemokine receptor 5 (CCR5) antagonists. It joins the fusion inhibitor, enfuvirtide, as another type of agent under the general antiretroviral treatment class of HIV-entry inhibitors.

Maraviroc is a selective chemokine receptor antagonist (CRA). It is imperative to test all patients for CCR5 tropism using a highly sensitive tropism assay before initiating the drug. Outgrowth of pre-existing low-level CXCR4- or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on maraviroc. It blocks viral entry via CCR5 co-receptor into host cells, reduces viral load, and increases T-cell counts in CCR5-tropic HIV-1 (i.e., R5 virus). This agent is indicated for combination treatment with optimized background therapy in treatment-experienced adults infected with only R5 virus who have evidence of viral replication and have HIV-1 strains resistant to multiple antiretroviral agents. It is approved for children as young as 2 years old.


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