Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro.

Article Details

Citation

Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS

Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro.

Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30.

PubMed ID
22850510 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drugs
Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
CobicistatATP-binding cassette sub-family G member 2ProteinHumans
Unknown
Inhibitor
Details
CobicistatP-glycoprotein 1ProteinHumans
Unknown
Inhibitor
Details