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

ACS Med Chem Lett. 2010 May 17;1(5):209-13. doi: 10.1021/ml1000257. eCollection 2010 Aug 12.


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.

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