Rilpivirine: a new addition to the anti-HIV-1 armamentarium

Drugs Today (Barc). 2011 Jan;47(1):5-15. doi: 10.1358/dot.2011.47.1.1583188.

Abstract

HIV has shifted from an acute illness to a chronic condition that can be successfully managed long-term with combination antiretroviral therapy. Rilpivirine (TMC-278) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that is positioned to become an importation therapy option for HIV-1-infected patients, particularly for those that are naive to therapy. In phase III studies this agent demonstrated similar virologic and immunologic efficacy compared to a current standard of care, efavirenz, while causing less adverse events. A higher proportion of rilpivirine-treated patients did experience virologic failure, however, and providers will need to weigh this risk with the improved tolerability of rilpivirine. In vitro studies have demonstrated that rilpivirine, as a diarylpyrimidine NNRTI with greater flexibility, has a higher genetic barrier to resistance when compared to first-generation NNRTI agents. Longer-term clinical data will be necessary to better understand rilpivirine's durability and activity against viral resistance in patients. Rilpivirine will be available as a stand-alone agent and will also be coformulated with tenofovir and emtricitabine to create a safe and effective antiretroviral regimen that can be administered as a single daily-dosed tablet.

Publication types

  • Review

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy*
  • Anti-HIV Agents / therapeutic use*
  • Clinical Trials as Topic
  • Drug Resistance, Viral
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • HIV-1 / drug effects*
  • Humans
  • Nitriles / adverse effects
  • Nitriles / pharmacokinetics
  • Nitriles / pharmacology
  • Nitriles / therapeutic use*
  • Pyrimidines / adverse effects
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use*
  • Rilpivirine

Substances

  • Anti-HIV Agents
  • Nitriles
  • Pyrimidines
  • HIV Reverse Transcriptase
  • Rilpivirine