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Effect of food on rilpivirine/emtricitabine/tenofovir disoproxil fumarate, an antiretroviral single‐tablet regimen for the treatment of HIV infection
Author(s) -
Custodio Joseph M.,
Yin Xiang,
Hepner Mischa,
Ling Kah Hiing J.,
Cheng Andrew,
Kearney Brian P.,
Ramanathan Srinivasan
Publication year - 2014
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/jcph.210
Subject(s) - rilpivirine , emtricitabine , medicine , tenofovir , cmax , pharmacokinetics , pharmacology , human immunodeficiency virus (hiv) , virology , viral load , antiretroviral therapy
The effect of food on rilpivirine/emtricitabine/tenofovir disoproxil fumarate single‐tablet regimen (STR) was evaluated in healthy subjects. Subjects (N = 24) received rilpivirine/emtricitabine/tenofovir disoproxil fumarate (25/200/300 mg) under fasted or fed conditions (light [390 kcal, 12 g fat]; standard [540 kcal, 21 g fat]) followed by pharmacokinetic (PK) sampling. The 90% confidence interval (CI) of the geometric mean ratio for rilpivirine, emtricitabine, tenofovir exposure was estimated for fed versus fasted dosing and light versus standard meal, with equivalence boundaries of 80 − 125%. Safety was assessed throughout study. Twenty‐three subjects completed the study; one discontinued due to protocol violation. Adverse events were mild to moderate. Emtricitabine PK was unaffected. Tenofovir AUC inf was 38% and 28% higher, respectively, with standard and light meal versus fasted. Rilpivirine AUC inf and C max were 16% and 26% higher with a standard, and 9% and 34% with a light meal, respectively, versus fasted. Compared to standard meal, the lower limit of rilpivirine AUC last and AUC inf when taken with the light meal were narrowly below the equivalence bounds (79.9 and 79.2, respectively), rilpivirine C max was narrowly above (129). Rilpivirine/emtricitabine/tenofovir disoproxil fumarate should be administered with food, which can be a standard or light meal.