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

作者：Lianhong Xu, Hongtao Liu, Bernard P. Murray, Christian Callebaut, Melody S. Lee, Allen Y. Hong, Robert G. Strickley, Luong Tsai, Kirsten M. Stray, Yujin Wang, Gerry Rhodes, Manoj C. Desai · 发表于：ACS Medicinal Chemistry Letters · 年份：2010 · DOI：10.1021/ml1000257 · 被引用次数：201 · 研究领域：HIV/AIDS drug development and treatment、HIV-related health complications and treatments、Adenosine and Purinergic Signaling

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.