Effect of P-glycoprotein and Cotreatment with Sofosbuvir on the Intestinal Permeation of Tenofovir Disoproxil Fumarate and Tenofovir Alafenamide Fumarate.
P-glycoprotein
intestinal permeability
sofosbuvir
tenofovir alafenamide fumarate
tenofovir disoproxil fumarate
Journal
Pharmaceutical research
ISSN: 1573-904X
Titre abrégé: Pharm Res
Pays: United States
ID NLM: 8406521
Informations de publication
Date de publication:
Sep 2023
Sep 2023
Historique:
received:
02
06
2023
accepted:
26
07
2023
medline:
5
10
2023
pubmed:
18
8
2023
entrez:
18
8
2023
Statut:
ppublish
Résumé
We aimed to compare the effects of P-glycoprotein (ABCB1) on the intestinal uptake of tenofovir disoproxil fumarate (TDF), tenofovir alafenamide fumarate (TAF), and metabolites, tenofovir isoproxil monoester (TEM) and tenofovir (TFV), and to study the molecular mechanism of drug-drug interaction (DDI) between sofosbuvir (SOF) and TDF/TAF. Bidirectional transport experiments in Caco-2 cells and accumulation studies in precision-cut intestinal slices prepared from the ileal segment of rodent (rPCIS) and human (hPCIS) intestines were performed. TDF and TAF were extensively metabolised but TAF exhibited greater stability. ABCB1 significantly reduced the intestinal transepithelial transfer and uptake of the TFV TDF and TAF likely produce comparable concentrations of TFV-equivalents in the portal vein and the extent of permeation is reduced by the activity of ABCB1. DDI on ABCB1 can thus potentially affect TDF and TAF absorption. SOF does not inhibit ABCB1-mediated transport of TDF and TAF but does stabilise TDF, albeit without affecting the quantity of TFV
Identifiants
pubmed: 37594591
doi: 10.1007/s11095-023-03581-2
pii: 10.1007/s11095-023-03581-2
doi:
Substances chimiques
Tenofovir
99YXE507IL
Sofosbuvir
WJ6CA3ZU8B
Anti-HIV Agents
0
ATP Binding Cassette Transporter, Subfamily B, Member 1
0
Adenine
JAC85A2161
ATP Binding Cassette Transporter, Subfamily B
0
Fumarates
0
Alanine
OF5P57N2ZX
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2109-2120Subventions
Organisme : Grantová Agentura, Univerzita Karlova
ID : GAUK 364521
Organisme : Grantová Agentura České Republiky
ID : GACR 18-07281Y
Organisme : Ministerstvo Školství, Mládeže a Tělovýchovy
ID : SVV No. 260 663
Organisme : Ministerstvo Školství, Mládeže a Tělovýchovy
ID : EFSA-CDN (reg. no.: CZ.02.1.01/0.0/0.0/16_019/0000841) co-funded by ERDF
Informations de copyright
© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.
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