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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.

Author information

1
Infectious Diseases Institute, Makerere University, Kampala, Uganda mlamorde@idi.co.ug.
2
Infectious Diseases Institute, Makerere University, Kampala, Uganda.
3
Department of Medicine, Makerere University College of Health Sciences, Kampala, Uganda.
4
Department of Molecular and Clinical Pharmacology, University of Liverpool, Liverpool, UK.
5
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.

Abstract

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

PMID:
25652748
DOI:
10.1093/jac/dku575
[Indexed for MEDLINE]

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