Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: a systematic review

Antivir Ther. 2012;17(8):1495-502. doi: 10.3851/IMP2254. Epub 2012 Aug 10.

Abstract

Rilpivirine (RPV) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). It remains active against HIV strains harbouring mutations that affect first-generation agents. RPV is dosed once daily with food and has been coformulated into a single tablet containing tenofovir and emtricitabine. Two Phase III studies of treatment-naive patients found RPV and efavirenz to have similar safety and efficacy. However, suboptimal virological suppression with RPV occurred more commonly in patients with higher baseline viral loads (>100,000 copies/ml). The most common mutation that emerged during RPV therapy was E138K, which often occurred in combination with M184I. E138K is likely to cause cross-resistance to other NNRTIs thereby limiting the further utilization of this class.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review
  • Systematic Review

MeSH terms

  • Alkynes
  • Anti-HIV Agents / adverse effects
  • Anti-HIV Agents / pharmacology
  • Anti-HIV Agents / therapeutic use*
  • Benzoxazines / adverse effects
  • Benzoxazines / therapeutic use
  • Clinical Trials as Topic
  • Cyclopropanes
  • Drug Interactions
  • Drug Resistance, Viral
  • Drug Substitution
  • HIV Infections / drug therapy*
  • HIV-1*
  • Humans
  • Nitriles / adverse effects
  • Nitriles / pharmacology
  • Nitriles / therapeutic use*
  • Pyrimidines / adverse effects
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use*
  • Reverse Transcriptase Inhibitors / adverse effects
  • Reverse Transcriptase Inhibitors / pharmacology
  • Reverse Transcriptase Inhibitors / therapeutic use*
  • Rilpivirine

Substances

  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Nitriles
  • Pyrimidines
  • Reverse Transcriptase Inhibitors
  • Rilpivirine
  • efavirenz