Rilpivirine, emtricitabine and tenofovir alafenamide: single-tablet combination for the treatment of HIV-1 infection in selected patients

Expert Rev Anti Infect Ther. 2016 Dec;14(12):1113-1126. doi: 10.1080/14787210.2016.1255551.

Abstract

Co-formulated rilpivirine, emtricitabine and tenofovir alafenamide (RPV/F/TAF) is the 6th single-tablet combination antiretroviral medication approved within the past decade for the treatment of HIV-1 infection. It was approved based on positive bioequivalence studies with already approved drugs with its component compounds, RPV and the single tablet regimen- elvitegravir, cobicistat, F/TAF. Areas covered: This article reviews the chemical, pharmacodynamic and pharmacokinetic properties, key drug interactions, and the efficacy, safety, tolerability and optimal clinical uses of the medication and/or its components in different patient populations. The article incorporates pre-clinical and clinical trial data available from Google, Google scholar, PubMed database, conference abstracts as well as US FDA approved drug prescribing information up till September 30, 2016. Expert commentary: RPV/F/TAF is a once-daily administered, well tolerated, and effective antiretroviral regimen that should be taken with a meal. Desirable properties include less neuropsychiatric toxicity than 1st generation non-nucleoside reverse transcriptase inhibitors, better bone and renal safety than tenofovir disoproxil fumarate containing regimens and it may be used in individuals with a creatinine clearance >30 mL/min. A five-year future view of the role of oral antiretroviral drug therapy as well as evolving treatment options for HIV-infected patients are also discussed in the article.

Keywords: Antiviral drug; Complera®/Eviplera®; Odefsey®; emtricitabine; reverse transcriptase; tenofovir alafenamide (TAF); tenofovir disoproxil fumarate(TDF).

Publication types

  • Review

MeSH terms

  • Adenine / administration & dosage
  • Adenine / adverse effects
  • Adenine / analogs & derivatives*
  • Adenine / pharmacokinetics
  • Adenine / therapeutic use
  • Administration, Oral
  • Alanine
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / adverse effects
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / therapeutic use*
  • Biological Availability
  • Clinical Trials as Topic
  • Drug Administration Schedule
  • Drug Combinations
  • Emtricitabine / administration & dosage
  • Emtricitabine / adverse effects
  • Emtricitabine / pharmacokinetics
  • Emtricitabine / therapeutic use*
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • Humans
  • Rilpivirine / administration & dosage
  • Rilpivirine / adverse effects
  • Rilpivirine / pharmacokinetics
  • Rilpivirine / therapeutic use*
  • Tablets
  • Tenofovir / analogs & derivatives
  • Therapeutic Equivalency
  • Viral Load / drug effects

Substances

  • Anti-HIV Agents
  • Drug Combinations
  • Tablets
  • Tenofovir
  • tenofovir alafenamide
  • Rilpivirine
  • Emtricitabine
  • Adenine
  • Alanine