Population Pharmacokinetics of Cabotegravir Following Oral Administration and Long-Acting Intramuscular Injection in Real-World People with HIV.

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State: Public
Version: Final published version
License: CC BY-NC 4.0
Serval ID
serval:BIB_A008171B295E
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Population Pharmacokinetics of Cabotegravir Following Oral Administration and Long-Acting Intramuscular Injection in Real-World People with HIV.
Journal
Clinical pharmacology and therapeutics
Author(s)
Thoueille P., Saldanha S.A., Schaller F., Choong E., Veuve F., Munting A., Cavassini M., Braun D., Günthard H.F., Duran Ramirez J.J., Surial B., Furrer H., Rauch A., Ustero P., Calmy A., Stöckle M., Di Benedetto C., Bernasconi E., Schmid P., Marzolini C., Girardin F.R., Buclin T., Decosterd L.A., Guidi M.
Working group(s)
Swiss HIV Cohort Study
Contributor(s)
Abela I., Aebi-Popp K., Anagnostopoulos A., Battegay M., Bernasconi E., Braun D.L., Bucher H.C., Calmy A., Cavassini M., Ciuffi A., Dollenmaier G., Egger M., Elzi L., Fehr J., Fellay J., Furrer H., Fux C.A., Günthard H.F., Hachfeld A., Haerry D., Hasse B., Hirsch H.H., Hoffmann M., Hösli I., Huber M., Jackson-Perry D., Kahlert C.R., Kaiser L., Keiser O., Klimkait T., Kouyos R.D., Kovari H., Kusejko K., Labhardt N., Leuzinger K., Martinez de Tejada B., Marzolini C., Metzner K.J., Müller N., Nemeth J., Nicca D., Notter J., Paioni P., Pantaleo G., Perreau M., Rauch A., Salazar-Vizcaya L., Schmid P., Speck R., Stöckle M., Tarr P., Trkola A., Wandeler G., Weisser M., Yerly S.
ISSN
1532-6535 (Electronic)
ISSN-L
0009-9236
Publication state
Published
Issued date
06/2024
Peer-reviewed
Oui
Volume
115
Number
6
Pages
1450-1459
Language
english
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't
Publication Status: ppublish
Abstract
Long-acting cabotegravir has been studied mainly in the stringent framework of clinical trials, which does not necessarily reflect the situation of people with HIV (PWH) in routine clinical settings. The present population pharmacokinetic analysis aims to build real-world reference percentile curves of cabotegravir concentrations, accounting for patient-related factors that may affect cabotegravir exposure. The second objective is to simulate whether dosing interval adjustments of cabotegravir could be considered in specific subpopulations. Overall, 238 PWH contributed to 1,038 cabotegravir levels (186 during the initial oral administration phase and 852 after intramuscular injection). Cabotegravir pharmacokinetics was best described using a one-compartment model with distinct first order-absorption for oral and intramuscular administrations, and identical volume and clearance. Our model showed almost 40% faster absorption and 30% higher clearance than previously reported, resulting in a time to steady-state of 8 months and an elimination half-life of 4.6 weeks for long-acting cabotegravir. Sex and body mass index significantly influenced absorption, and bodyweight affected clearance. Model-based simulations showed that cabotegravir trough concentrations in females were 25% lower 4 weeks after the intramuscular loading dose, but 42% higher during the late maintenance phase. Finally, simulations indicated that in females, despite significantly higher cabotegravir concentrations, longer intervals between injections may not consistently ensure levels above the 4-fold protein-adjusted 90% inhibitory target concentration.
Keywords
Humans, Injections, Intramuscular, Female, Male, HIV Infections/drug therapy, Pyridones/pharmacokinetics, Pyridones/administration & dosage, Adult, Administration, Oral, Middle Aged, Models, Biological, Anti-HIV Agents/pharmacokinetics, Anti-HIV Agents/administration & dosage, Half-Life, Delayed-Action Preparations/pharmacokinetics, Young Adult, Aged, Diketopiperazines
Pubmed
Web of science
Open Access
Yes
Create date
25/03/2024 14:32
Last modification date
06/08/2024 6:02
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