Effect of food on rilpivirine/emtricitabine/tenofovir disoproxil fumarate, an antiretroviral single-tablet regimen for the treatment of HIV infection

摘要: The effect of food on rilpivirine/emtricitabine/tenofovir disoproxil fumarate single-tablet regimen (STR) was evaluated in healthy subjects. Subjects (N = 24) received (25/200/300 mg) under fasted or fed conditions (light [390 kcal, 12 g fat]; standard [540 21 fat]) followed by pharmacokinetic (PK) sampling. 90% confidence interval (CI) the geometric mean ratio for rilpivirine, emtricitabine, tenofovir exposure estimated versus dosing and light meal, with equivalence boundaries 80 - 125%. Safety assessed throughout study. Twenty-three subjects completed study; one discontinued due to protocol violation. Adverse events were mild moderate. Emtricitabine PK unaffected. Tenofovir AUCinf 38% 28% higher, respectively, meal fasted. Rilpivirine Cmax 16% 26% higher a standard, 9% 34% Compared lower limit rilpivirine AUClast when taken narrowly below bounds (79.9 79.2, respectively), above (129). Rilpivirine/emtricitabine/tenofovir should be administered food, which can meal.