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Clinical Trial
. 2019 May;8(4):443-448.
doi: 10.1002/cpdd.620. Epub 2018 Sep 19.

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

Parul Patel  1 , Susan L Ford  2 , Yu Lou  3 , Kalpana Bakshi  4 , Allan R Tenorio  1 , Zhiping Zhang  3 , Rennan Pan  4 , William Spreen  1
Affiliations
Clinical Trial

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

Parul Patel et al. Clin Pharmacol Drug Dev. 2019 May.

Abstract

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.

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Figures

Figure 1
Figure 1
Mean (SD) concentration‐time profiles of cabotegravir after administration in a fasted state or with a high‐fat meal.
See this image and copyright information in PMC

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