Update on rilpivirine: a new potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV replication

Ann Med. 2013 May;45(3):236-41. doi: 10.3109/07853890.2012.732704. Epub 2012 Nov 17.

Abstract

Introduction: A combination of antiretroviral drugs (ARVs) is necessary to achieve sustained virologic suppression of HIV viral load (< 50 copies/mL). Rilpivirine (RPV) is a potent new non-nucleoside reverse transcriptase inhibitor (NNRTI) that has the potential to be part of effective ARV combinations. Here, we review currently available data on RPV from the standpoint of virologic suppression and efficacy, drug-drug interactions safety, and resistance.

Areas covered: This review presents data on the results of clinical trials involving RPV. The topics considered include antiviral potency, dosing, clinical utility, drug resistance, toxicity profile, and pharmacokinetics.

Expert opinion: RPV is a potent new addition to the antiretroviral family of drugs for use in combination therapy in previously untreated HIV-infected patients. However, caution needs to be exercised in administration of RPV to patients who initiated therapy with viral loads > 100,000 viral RNA copies/mL.

Publication types

  • Review

MeSH terms

  • Alanine Transaminase / blood
  • CD4 Lymphocyte Count
  • Cholesterol / blood
  • Clinical Trials as Topic
  • Creatinine / blood
  • Dose-Response Relationship, Drug
  • Drug Eruptions
  • Drug Interactions
  • Drug Resistance, Viral / genetics
  • Drug Therapy, Combination
  • Electrocardiography
  • HIV Infections / drug therapy
  • HIV Reverse Transcriptase / antagonists & inhibitors
  • Humans
  • Nitriles / pharmacology*
  • Pyrimidines / pharmacology*
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Rilpivirine
  • Viral Load

Substances

  • Nitriles
  • Pyrimidines
  • Reverse Transcriptase Inhibitors
  • Cholesterol
  • Creatinine
  • Alanine Transaminase
  • HIV Reverse Transcriptase
  • Rilpivirine