Steady-state pharmacokinetics of rilpivirine under different meal conditions in HIV-1-infected Ugandan adults

J Antimicrob Chemother. 2015 May;70(5):1482-6. doi: 10.1093/jac/dku575. Epub 2015 Feb 3.


Objectives: To investigate the effect of food on the steady-state pharmacokinetics of rilpivirine when administered as a fixed-dose combination tablet containing tenofovir disoproxil fumarate, emtricitabine plus rilpivirine (TDF/FTC/RPV) in HIV-1-infected Ugandan patients.

Methods: This was an open-label, three-period, longitudinal pharmacokinetic study with patients serving as their own controls. Fifteen consenting and virologically suppressed HIV-1-infected adults were switched from an efavirenz-based regimen to TDF/FTC/RPV for 56 days. Enrolled patients underwent 24 h blood sampling with TDF/FTC/RPV dosing in the fasted state (day 42), with a low-fat meal (11 g of fat/353 kcal, day 49) and with a moderate-fat meal (19 g of fat/589 kcal, day 56; reference). A viral load assessment was performed on day 56.

Results: Rilpivirine AUC0-24 was significantly decreased by 16% (geometric mean ratio, 90% CI: 0.84, 0.73-0.96) during administration in the fasted state when compared with AUC0-24 during administration with a moderate-fat meal. Similarly, rilpivirine C24 was significantly decreased by 21% (0.79, 0.65-0.97) in the fasted state compared with a moderate-fat meal. Pharmacokinetic parameters were unchanged during administration with a low-fat meal, except for C24, which was significantly increased by 15% (1.15, 1.01-1.31) when compared with the moderate-fat meal. Rilpivirine Cmax was similar under the three meal conditions. Virological suppression was unchanged at the end of the study.

Conclusions: A food effect was observed for steady-state pharmacokinetic parameters of rilpivirine (AUC0-24 and C24) when TDF/FTC/RPV was administered in the fasted state compared with the moderate-fat meal. The TDF/FTC/RPV formulation can be administered with either a low-fat or moderate-fat meal.

Keywords: Complera; food–drug interactions; sub-Saharan Africa.

Publication types

  • Clinical Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / pharmacokinetics*
  • Diet / methods*
  • Drug Combinations
  • Emtricitabine / administration & dosage
  • Female
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV-1 / isolation & purification
  • Humans
  • Longitudinal Studies
  • Male
  • Middle Aged
  • Plasma / chemistry
  • Rilpivirine / administration & dosage
  • Rilpivirine / pharmacokinetics*
  • Tenofovir / administration & dosage
  • Uganda
  • Young Adult


  • Anti-HIV Agents
  • Drug Combinations
  • Tenofovir
  • Rilpivirine
  • Emtricitabine