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

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

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Infectious Diseases Institute, Makerere University, Kampala, Uganda
Infectious Diseases Institute, Makerere University, Kampala, Uganda.
Department of Medicine, Makerere University College of Health Sciences, Kampala, Uganda.
Department of Molecular and Clinical Pharmacology, University of Liverpool, Liverpool, UK.
Department of Global Health, Northwestern University, Chicago, IL, USA Department of Pharmacology and Therapeutics, Trinity College Dublin, Dublin, Ireland GUIDE Clinic, St James's Hospital, Dublin, Ireland.



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.


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.


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.


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.


Complera; food–drug interactions; sub-Saharan Africa

[Indexed for MEDLINE]

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