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Literature DB >> 24900196

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

Lianhong Xu¹, Hongtao Liu¹, Bernard P Murray², Christian Callebaut³, Melody S Lee², Allen Hong¹, Robert G Strickley⁴, Luong K Tsai³, Kirsten M Stray³, Yujin Wang², Gerry R Rhodes², Manoj C Desai¹.

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.

Entities: Chemical Disease Gene Species

Keywords: CYP3A inhibitor; GS-9350; PK enhancer; cobicistat; pharmacoenhancer; ritonavir

Year: 2010 PMID： 24900196 PMCID： PMC4007915 DOI： 10.1021/ml1000257

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

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