Effects of a Nutritional Protein-Rich Drink on the Pharmacokinetics of Elvitegravir, Cobicistat, Emtricitabine, Tenofovir Alafenamide, and Tenofovir Compared With a Standard Meal in Healthy Japanese Male Subjects

Clin Pharmacol Drug Dev. 2018 Feb;7(2):132-142. doi: 10.1002/cpdd.365. Epub 2017 Jun 5.

Abstract

This study investigated the effects of ingested meal types on the pharmacokinetics of elvitegravir (EVG), cobicistat (COBI), emtricitabine (FTC), tenofovir alafenamide (TAF), and tenofovir (TFV) following a single administration of the single-tablet regimen (STR) of EVG/COBI/FTC/TAF (150/150/200/10 mg) in Japanese HIV-negative healthy subjects (n = 12). In this open-label, randomized, 3-way crossover study, the bioequivalence of the EVG/COBI/FTC/TAF STR following ingestion of a nutritional protein-rich drink with a reference treatment of taking a standard breakfast was evaluated. Administration under fasted conditions, no food intake, resulted in decreases in the mean AUCinf and Cmax of EVG by 50% and 57%, respectively, relative to the administration with a standard breakfast, whereas the systemic exposure of EVG with a nutritional protein-rich drink was comparable to that with a standard breakfast. The mean AUCinf and Cmax of COBI, FTC, TAF, and TFV were comparable regardless of meal intake or meal types. Although the package insert of the EVG/COBI/FTC/TAF STR states that the medication is recommended to be taken with food, this study provides an additional insight into HIV-1-infected patients that a light meal like a nutritional protein-rich drink can be an alternative to a standard meal.

Keywords: Japanese; elvitegravir; food effect; pharmacokinetics; tenofovir alafenamide.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / analogs & derivatives
  • Adenine / pharmacokinetics
  • Administration, Oral
  • Adult
  • Alanine
  • Anti-HIV Agents / pharmacokinetics*
  • Asian People
  • Breakfast
  • Cobicistat / pharmacokinetics
  • Cross-Over Studies
  • Dietary Proteins / pharmacology*
  • Dietary Supplements*
  • Emtricitabine / pharmacokinetics
  • Fasting / metabolism
  • Food-Drug Interactions*
  • Healthy Volunteers
  • Humans
  • Male
  • Quinolones / pharmacokinetics
  • Tenofovir / pharmacokinetics

Substances

  • Anti-HIV Agents
  • Dietary Proteins
  • Quinolones
  • elvitegravir
  • Tenofovir
  • tenofovir alafenamide
  • Emtricitabine
  • Adenine
  • Cobicistat
  • Alanine