In vitro phenotypic susceptibility of HIV-2 clinical isolates to CCR5 inhibitors

Antimicrob Agents Chemother. 2012 Jan;56(1):137-9. doi: 10.1128/AAC.05313-11. Epub 2011 Nov 7.

Abstract

HIV-2 is naturally resistant to nonnucleoside reverse transcriptase inhibitors, to a fusion inhibitor, and to some of the protease inhibitors. Maraviroc is the first drug of the new anti-CCR5 drug class and is effective only on CCR5-tropic (R5) HIV-1. No previous studies concerning HIV-2 susceptibility to maraviroc have been reported yet. We developed a phenotypic maraviroc susceptibility test using a peripheral blood mononuclear cell (PBMC) model. We analyzed the maraviroc susceptibility of 13 R5 HIV-2, 2 X4R5 (dual) HIV-2, and 2 CXCR4-tropic (X4) HIV-2 clinical isolates. We also tested, with the same protocol, 1 X4 HIV-1 and 4 R5 HIV-1 clinical isolates. For the R5 HIV-2 clinical isolates, the 50% effective concentration (EC(50)) for maraviroc was 0.80 nM (interquartile range [IQR], 0.48 to 1.39 nM), similar to that observed for the R5 HIV-1 isolates. The median maximum percentage of inhibition in the R5 HIV-2 isolates was 93% (IQR, 84 to 98%), similar to that observed in the R5 HIV-1 isolates. As expected, both X4 HIV-1 and HIV-2 were highly resistant to maraviroc. Our study showed for the first time that maraviroc is active in vitro against R5 HIV-2. The new tools we developed will allow identification of HIV-2-infected patients eligible for CCR5 inhibitor use and management of virological failure when receiving a maraviroc-based regimen.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / pharmacology*
  • CCR5 Receptor Antagonists*
  • Cells, Cultured
  • Cyclohexanes / pharmacology*
  • Drug Resistance, Viral*
  • Female
  • Genotype
  • HIV Infections / drug therapy*
  • HIV Infections / metabolism
  • HIV Infections / virology
  • HIV-1 / drug effects*
  • HIV-1 / metabolism
  • HIV-2 / drug effects*
  • HIV-2 / metabolism
  • Humans
  • Inhibitory Concentration 50
  • Leukocytes, Mononuclear
  • Lymphocyte Activation / drug effects
  • Male
  • Maraviroc
  • Models, Biological
  • Phytohemagglutinins / pharmacology
  • Receptors, CCR5 / metabolism
  • Receptors, CXCR4 / antagonists & inhibitors
  • Receptors, CXCR4 / metabolism
  • Species Specificity
  • Triazoles / pharmacology*
  • Virus Replication / drug effects

Substances

  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • CXCR4 protein, human
  • Cyclohexanes
  • Phytohemagglutinins
  • Receptors, CCR5
  • Receptors, CXCR4
  • Triazoles
  • Maraviroc