Cobicistat Boosts the Intestinal Absorption of Transport Substrates, Including HIV Protease Inhibitors and GS-7340, In Vitro | Zendy

EveIrene Lepist | Zendy; Truc K. Phan | Zendy; Anupma Roy | Zendy; L. Tong | Zendy; Kelly MacLennan | Zendy; Bernard P. Murray | Zendy; Adrian S. Ray | Zendy

Open Access

Cobicistat Boosts the Intestinal Absorption of Transport Substrates, Including HIV Protease Inhibitors and GS-7340, In Vitro

Author(s) -

EveIrene Lepist,

Truc K. Phan,

Anupma Roy,

L. Tong,

Kelly MacLennan,

Bernard P. Murray,

Adrian S. Ray

Publication year - 2012

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.01089-12

Subject(s) - cobicistat , atazanavir , darunavir , abcg2 , prodrug , pharmacology , chemistry , ritonavir , in vitro , efflux , transporter , biochemistry , atp binding cassette transporter , biology , virology , virus , viral load , antiretroviral therapy , gene

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 cellsin vitro .

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