Protection of rhesus macaques from vaginal infection by vaginally delivered maraviroc, an inhibitor of HIV-1 entry via the CCR5 co-receptor

J Infect Dis. 2010 Sep 1;202(5):739-44. doi: 10.1086/655661.

Abstract

An effective vaginal microbicide could reduce human immunodeficiency virus type 1 (HIV-1) transmission to women. Among microbicide candidates in clinical development is Maraviroc (MVC), a small-molecule drug that binds the CCR5 co-receptor and impedes HIV-1 entry into cells. Delivered systemically, MVC reduces viral load in HIV-1-infected individuals, but its ability to prevent transmission is untested. We have now evaluated MVC as a vaginal microbicide with use of a stringent model that involves challenge of rhesus macaques with a high-dose of a CCR5-using virus, SHIV-162P3. Gel-formulated, prescription-grade MVC provided dose-dependent protection, half-maximally at 0.5 mM (0.25 mg/mL). The duration of protection was transient; the longer the delay between MVC application and virus challenge, the less protection (half life of approximately 4 h). As expected, MVC neither protected against challenge with a CXCR4-using virus, SHIV-KU1, nor exacerbated postinfection viremia. These findings validate MVC development as a vaginal microbicide for women and should guide clinical programs.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Administration, Intravaginal
  • Animals
  • Anti-HIV Agents* / administration & dosage
  • Anti-HIV Agents* / therapeutic use
  • Cyclohexanes* / administration & dosage
  • Cyclohexanes* / therapeutic use
  • Female
  • HIV Fusion Inhibitors
  • HIV Infections / prevention & control*
  • HIV Infections / virology
  • HIV-1 / drug effects
  • Humans
  • Macaca mulatta
  • Maraviroc
  • Receptors, CCR5 / metabolism*
  • Simian Acquired Immunodeficiency Syndrome / prevention & control*
  • Simian Immunodeficiency Virus / drug effects
  • Treatment Outcome
  • Triazoles* / administration & dosage
  • Triazoles* / therapeutic use
  • Vaginal Diseases / prevention & control*
  • Vaginal Diseases / virology
  • Virus Internalization / drug effects
  • Virus Replication / drug effects

Substances

  • Anti-HIV Agents
  • Cyclohexanes
  • HIV Fusion Inhibitors
  • Receptors, CCR5
  • Triazoles
  • Maraviroc