title: Effects of a protein-rich drink or a standard meal on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine and tenofovir in healthy Japanese male subjects: a randomized, three-way crossover study.
abstract: This study investigated the effects of ingested food types on the pharmacokinetics of elvitegravir, cobicistat, emtricitabine, and tenofovir as a single-tablet regimen (STR) in Japanese HIV-negative healthy subjects. In this open-label, randomized, three-way crossover study, the pharmacokinetic profiles of elvitegravir, cobicistat, emtricitabine, and tenofovir were evaluated when administered with a standard breakfast, under fasting conditions, or with a nutritional protein-rich drink. All subjects (N = 11) received a single morning dose of elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate (150/150/200/300 mg). Administration under fasting conditions resulted in decreases in the mean AUCinf of elvitegravir and tenofovir by 50% and 28%, respectively, relative to administration with a standard breakfast, whereas the bioavailabilities of elvitegravir and tenofovir were comparable when administered with a standard breakfast or a nutritional protein-rich drink. Under fasting conditions, it appears that the bioavailabilities of elvitegravir and tenofovir were not equivalent to those when they were administered with either type of food, although they were bioequivalent to each other under fed conditions. Cobicistat and emtricitabine were bioequivalent under all conditions. These findings suggest that elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate should be administered with food, and that the bioavailability of elvitegravir and tenofovir is not affected by the type of meal ingested.
authors.affiliation: Clinical Development Department, Pharmaceutical Division, Japan Tobacco Inc., Tokyo, Japan.
authors.forename: Mari
authors.initials: M
authors.lastname: Shiomi
authors.forename: Shunji
authors.initials: S
authors.lastname: Matsuki
authors.forename: Atsushi
authors.initials: A
authors.lastname: Ikeda
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Ishikawa
authors.forename: Noriaki
authors.initials: N
authors.lastname: Nishino
authors.forename: Miyuki
authors.initials: M
authors.lastname: Kimura
authors.forename: Shin
authors.initials: S
authors.lastname: Irie
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D000328:Adult; D019380:Anti-HIV Agents / Q000097:blood / Q000493:pharmacokinetics; D044466:Asian People; D001628:Beverages; D002219:Carbamates / Q000097:blood / Q000493:pharmacokinetics*; D000069547:Cobicistat; D018592:Cross-Over Studies; D003841:Deoxycytidine / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D004044:Dietary Proteins / Q000494:pharmacology*; D004338:Drug Combinations; D000068679:Emtricitabine; D018565:Food-Drug Interactions; D006801:Humans; D008297:Male; D008875:Middle Aged; D063065:Organophosphonates / Q000097:blood / Q000493:pharmacokinetics*; D015363:Quinolones / Q000097:blood / Q000493:pharmacokinetics*; D000068698:Tenofovir; D013844:Thiazoles / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D019380:Anti-HIV Agents; D002219:Carbamates; D004044:Dietary Proteins; D004338:Drug Combinations; D063065:Organophosphonates; D015363:Quinolones; D013844:Thiazoles; D003841:Deoxycytidine; C509700:elvitegravir; D000068698:Tenofovir; D000068679:Emtricitabine; D000225:Adenine; D000069547:Cobicistat
keywords: Japanese; elvitegravir; food effect; pharmacokinetics; stribild