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.
Publication types
-
Randomized Controlled Trial
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Administration, Oral
-
Adult
-
Area Under Curve
-
Biological Availability
-
Chromatography, High Pressure Liquid
-
Cross-Over Studies
-
Dietary Fats / metabolism*
-
Fasting
-
Female
-
Food-Drug Interactions*
-
HIV Integrase Inhibitors / blood
-
HIV Integrase Inhibitors / pharmacokinetics*
-
Half-Life
-
Heterocyclic Compounds, 3-Ring / blood
-
Heterocyclic Compounds, 3-Ring / pharmacokinetics*
-
Humans
-
Intestinal Absorption
-
Male
-
Middle Aged
-
Oxazines
-
Piperazines
-
Pyridones
-
Tandem Mass Spectrometry
Substances
-
Dietary Fats
-
HIV Integrase Inhibitors
-
Heterocyclic Compounds, 3-Ring
-
Oxazines
-
Piperazines
-
Pyridones
-
dolutegravir