title: Effect of food on the pharmacokinetics of the integrase inhibitor dolutegravir.
abstract: Healthy subjects received dolutegravir at 50 mg in a single-dose crossover study while they were in the fasted state or with low-, moderate-, or high-fat meals. Food increased dolutegravir exposure and reduced the rate of absorption. The area under the concentration-time curve from 0 h to infinity (AUC(0-∞)) increased by 33%, 41%, and 66% when administered with low-, moderate-, or high-fat meals, respectively, compared with fasting. This increase in dolutegravir exposure is not anticipated to impact clinical safety, and therefore dolutegravir can be taken with or without food and without regard to fat content.
authors.affiliation: GlaxoSmithKline, Research Triangle Park, North Carolina, USA.
authors.forename: Ivy
authors.initials: I
authors.lastname: Song
authors.forename: Julie
authors.initials: J
authors.lastname: Borland
authors.forename: Shuguang
authors.initials: S
authors.lastname: Chen
authors.forename: Parul
authors.initials: P
authors.lastname: Patel
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Wajima
authors.forename: Amanda
authors.initials: A
authors.lastname: Peppercorn
authors.forename: Stephen C
authors.initials: SC
authors.lastname: Piscitelli
mesh_terms: D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004041:Dietary Fats / Q000378:metabolism*; D005215:Fasting; D005260:Female; D018565:Food-Drug Interactions; D019428:HIV Integrase Inhibitors / Q000097:blood / Q000493:pharmacokinetics*; D006207:Half-Life; D006575:Heterocyclic Compounds, 3-Ring / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008875:Middle Aged; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D053719:Tandem Mass Spectrometry; D000099226:Dolutegravir
chemical_list: D004041:Dietary Fats; D019428:HIV Integrase Inhibitors; D006575:Heterocyclic Compounds, 3-Ring; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D000099226:Dolutegravir