Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer.
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ABSTRACT:
SUBMITTER: Xu L
PROVIDER: S-EPMC4007915 | biostudies-literature | 2010 Aug
REPOSITORIES: biostudies-literature
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Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer.
Xu Lianhong L Liu Hongtao H Murray Bernard P BP Callebaut Christian C Lee Melody S MS Hong Allen A Strickley Robert G RG Tsai Luong K LK Stray Kirsten M KM Wang Yujin Y Rhodes Gerry R GR Desai Manoj C MC
ACS medicinal chemistry letters 20100517 5
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 c ...[more]
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