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Brief Report: Pharmacokinetics of Bictegravir and Tenofovir in Combination With Darunavir/Cobicistat in Treatment-Experienced Persons With HIV.
- Source :
-
Journal of acquired immune deficiency syndromes (1999) [J Acquir Immune Defic Syndr] 2021 Dec 01; Vol. 88 (4), pp. 389-392. - Publication Year :
- 2021
-
Abstract
- Background: Bictegravir coformulated with emtricitabine and tenofovir alafenamide as a fixed-dose combination (BIC/FTC/TAF 50/200/25 mg) is recommended as an initial regimen in patients who are antiretroviral (ARV)-naïve or virologically suppressed on a stable ARV regimen. However, no real-world pharmacokinetic (PK) data are available in treatment-experienced patients with antiretroviral resistance receiving BIC/FTC/TAF plus a boosted protease inhibitor.<br />Setting/methods: This prospective, single-center, nonrandomized pharmacokinetic study enrolled adult treatment-experienced persons with HIV and creatinine clearance >30 mL/min receiving BIC/FTC/TAF + DRV/c as part of routine clinical care. Steady-state PK profiles of BIC, TAF, tenofovir (TFV), and DRV after daily dosing of BIC/FTC/TAF + darunavir/cobicistat (DRV/c) were obtained with samples at predose and 0.5, 1, 2, and 4 hours postdose. The AUC0-24 at steady state was extrapolated by imputing C0 for C24 for each participant (AUC0-tau,exp).<br />Results: Nine participants were enrolled with a median age of 59 years (range 54-67) and median number of years on ART of 19 (range 5.8-30). The median (interquartile range [IQR]) BIC AUC0-tau,exp and Cmax values were 128.9 µg*h/mL (78.1-159.5) and 6.9 µg/mL (5.1-9.8), respectively. The median (IQR) TAF AUC0-tau,exp and Cmax values were 0.376 µg*h/mL (0.199-0.430) and 0.276 µg/mL (0.149-0.543), respectively. Predose concentrations of TFV and DRV were comparable with historical data.<br />Conclusion: Treatment-experienced persons with HIV receiving BIC/FTC/TAF + darunavir/cobicistat (DRV/c) had BIC exposures (AUC0-tau) that were increased by approximately 26% compared with historical PK data. Although TAF exposures were substantially increased, plasma TFV was only modestly higher. These results suggest that BIC/TAF/FTC + DRV/c is a viable antiviral regimen option for treatment-experienced persons.<br />Competing Interests: The authors have no conflicts of interest to disclose.<br /> (Copyright © 2021 Wolters Kluwer Health, Inc. All rights reserved.)
- Subjects :
- Aged
Amides blood
Anti-HIV Agents blood
Antiretroviral Therapy, Highly Active methods
Chromatography, Liquid
Cobicistat blood
Darunavir blood
Female
Heterocyclic Compounds, 3-Ring blood
Humans
Male
Middle Aged
Piperazines blood
Prospective Studies
Pyridones blood
Tandem Mass Spectrometry
Tenofovir blood
Amides pharmacokinetics
Anti-HIV Agents pharmacokinetics
Cobicistat pharmacokinetics
Darunavir pharmacokinetics
HIV Infections drug therapy
Heterocyclic Compounds, 3-Ring pharmacokinetics
Piperazines pharmacokinetics
Pyridones pharmacokinetics
Tenofovir pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1944-7884
- Volume :
- 88
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Journal of acquired immune deficiency syndromes (1999)
- Publication Type :
- Academic Journal
- Accession number :
- 34285156
- Full Text :
- https://doi.org/10.1097/QAI.0000000000002765