Effect of a High-Fat Meal on the Pharmacokinetics of the HIV Integrase Inhibitor Cabotegravir

Clin Pharmacol Drug Dev. 2019 May;8(4):443-448. doi: 10.1002/cpdd.620. Epub 2018 Sep 19.


Cabotegravir is an integrase inhibitor in clinical development for the treatment and prevention of HIV infection using oral tablets for short-term, lead-in use before subsequent administration of a long-acting injectable formulation. This phase 1, single-center, randomized, 2 × 2 crossover study evaluated the effect of a high-fat meal on the pharmacokinetics (PK) of oral cabotegravir. Healthy adults received oral cabotegravir 30 mg as a single dose on 2 separate occasions, either after fasting or following a high-fat meal (∼53% fat, ∼870 kcal). Safety evaluations and serial PK samples were collected, and a mixed-effects model was used to determine within-participant treatment comparison of noncompartmental PK parameters. Twenty-four patients were enrolled and had a mean body mass index of 25.6 kg/m2 ; 67% were male. Compared with the fasting state, coadministration of cabotegravir with a high-fat meal increased plasma cabotegravir area under the concentration-time curve and maximal drug concentration, each by 14%. The slight 14% to 17% increase in exposure associated with a high-fat, high-calorie meal was not considered clinically significant. No grade 3/4 adverse events (AEs), drug-related AEs, or AEs leading to discontinuation were reported.

Trial registration: ClinicalTrials.gov NCT02799264.

Keywords: absorption; food; high-fat; integrase inhibitor; pharmacokinetics.

Publication types

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

MeSH terms

  • Administration, Oral
  • Adolescent
  • Adult
  • Area Under Curve
  • Body Mass Index
  • Child
  • Cross-Over Studies
  • Diet, High-Fat / adverse effects*
  • Fasting / blood*
  • Female
  • HIV Integrase Inhibitors / administration & dosage
  • HIV Integrase Inhibitors / pharmacokinetics*
  • Healthy Volunteers
  • Humans
  • Male
  • Meals
  • Middle Aged
  • Models, Theoretical
  • Pyridones / administration & dosage
  • Pyridones / pharmacokinetics*
  • Tablets
  • Young Adult


  • HIV Integrase Inhibitors
  • Pyridones
  • Tablets
  • cabotegravir

Associated data

  • ClinicalTrials.gov/NCT02799264