Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2020 Jun 8:12:49-52.
doi: 10.2147/CPAA.S250751. eCollection 2020.

The Effect of Moderate- and High-Fat Meals on the Bioavailability of Dolutegravir/Rilpivirine Fixed-Dose Combination Tablet

Rashmi Mehta  1 , Joseph Piscitelli  2 , Allen Wolstenholme  3 , Caifeng Fu  4 , Herta Crauwels  5 , Brian Wynne  6 , Kimberly Adkison  7
Affiliations

The Effect of Moderate- and High-Fat Meals on the Bioavailability of Dolutegravir/Rilpivirine Fixed-Dose Combination Tablet

Rashmi Mehta et al. Clin Pharmacol. .

Abstract

Dolutegravir 50 mg (DTG) and rilpivirine 25 mg (RPV) are a newly approved 2-drug regimen for the treatment of HIV in virally suppressed patients. A 2-part study evaluated the relative bioavailability and food effect of five experimental fixed-dose combination (FDC) tablet formulations of DTG/RPV. When given with a moderate- or high-fat meal, the absorption of both DTG and RPV was increased, resulting in higher exposures. As per product labelling, DTG/RPV FDC should be taken with a meal.

Keywords: dolutegravir; food effect; pharmacokinetics; rilpivirine.

PubMed Disclaimer

Conflict of interest statement

Rashmi Mehta and Allen Wolstenholme are employees of GlaxoSmithKline. Caifeng Fu is an employee of PAREXEL International. Herta Crauwels is a full-time employee of Janssen Pharmaceutical Companies, which is owned by Johnson and Johnson, and stockholder of Johnson and Johnson, market authorisation holder of rilpivirine. Brian Wynne and Kimberly Adkison are employees of ViiV Healthcare. The authors report no other conflicts of interest in this work.

Figures

Figure 1
Figure 1
Mean plasma concentration–time profile of dolutegravir (left) and rilpivirine (right) following a single oral dose of dolutegravir/rilpivirine fixed-dose combination tablet (Formulation AM) in healthy subjects.
See this image and copyright information in PMC

References

    1. Llibre JM, Hung C-C, Brinson C, et al. Efficacy, safety, and tolerability of dolutegravir-rilpivirine for the maintenance of virological suppression in adults with HIV-1: phase 3, randomised, non-inferiority SWORD-1 and SWORD-2 studies. Lancet. 2018;391(10123):839–849. doi:10.1016/S0140-6736(17)33095-7 - DOI - PubMed
    1. Mehta R, Wolstenholme A, Di Lullo KD, et al. Bioequivalence of a fixed-dose combination tablet of the complete two-drug regimen of dolutegravir and rilpivirine for treatment of HIV-1 infection. Antimicrob Agents Chemother. 2018;62(9). doi:10.1128/aac.00748-18 - DOI - PMC - PubMed
    1. Adkison KK, Wolstenholme A, Choukour M, et al. Relative bioavailability and food effect of fixed-dose combination tablets of dolutegravir and rilpivirine in healthy subjects. 17th International Workshop on Clinical Pharmacology of HIV & Hepatitis Therapy; June 8–10, 2016; Washington, DC.
    1. U.S. Department of Health and Human Services Food and Drug Administration. Center for Drug Evaluation and Research. Guidance for Industry: Food-Effect Bioavailability and Fed Bioequivalence Studies; 2002.
    1. Song IH, Borland J, Savina PM, et al. Pharmacokinetics of single-dose dolutegravir in HIV-seronegative subjects with moderate hepatic impairment compared to healthy matched controls. Clin Pharmacol Drug Dev. 2013;2(4):342–348. doi:10.1002/cpdd.55 - DOI - PMC - PubMed