title: Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro.
abstract: The experimental pharmacoenhancer cobicistat (COBI), a potent mechanism-based inhibitor of cytochrome P450 3A enzymes, was found to inhibit the intestinal efflux transporters P-glycoprotein and breast cancer resistance protein. Consistent with its transporter inhibition, COBI significantly increased the absorptive flux of potential candidates for clinical coadministration, including the HIV protease inhibitors atazanavir and darunavir and the lymphoid cell- and tissue-targeted prodrug of the nucleotide analog tenofovir, GS-7340, through monolayers of Caco-2 cells in vitro.
authors: Gilead Sciences, Inc., Foster City, California, USA.
authors: Eve-Irene
authors: EI
authors: Lepist
authors: Truc K
authors: TK
authors: Phan
authors: Anupma
authors: A
authors: Roy
authors: Leah
authors: L
authors: Tong
authors: Kelly
authors: K
authors: Maclennan
authors: Bernard
authors: B
authors: Murray
authors: Adrian S
authors: AS
authors: Ray
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000378:metabolism; D000409:Alanine; D018938:Caco-2 Cells; D002219:Carbamates / Q000494:pharmacology*; D000069547:Cobicistat; D017320:HIV Protease Inhibitors / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D000068698:Tenofovir / Q000031:analogs & derivatives; D013844:Thiazoles / Q000494:pharmacology*
chemical_list: D002219:Carbamates; D017320:HIV Protease Inhibitors; D013844:Thiazoles; D000068698:Tenofovir; C442442:tenofovir alafenamide; D000225:Adenine; D000069547:Cobicistat; D000409:Alanine