Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A As a Novel Pharmacoenhancer

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2014 Jun 6

PMID 24900196

Citations 58

Authors

Lianhong Xu

Hongtao Liu

Bernard P Murray

Christian Callebaut

Melody S Lee

Allen Hong

Robert G Strickley

Luong K Tsai

Kirsten M Stray

Yujin Wang

Gerry R Rhodes

Manoj C Desai

Affiliations

Soon will be listed here.

Abstract

Cobicistat (3, GS-9350) is a newly discovered, potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes. In contrast to ritonavir, 3 is devoid of anti-HIV activity and is thus more suitable for use in boosting anti-HIV drugs without risking selection of potential drug-resistant HIV variants. Compound 3 shows reduced liability for drug interactions and may have potential improvements in tolerability over ritonavir. In addition, 3 has high aqueous solubility and can be readily coformulated with other agents.

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