title: Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer.
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.
authors.affiliation: Department of Medicinal Chemistry.
authors.forename: Lianhong
authors.initials: L
authors.lastname: Xu
authors.affiliation: Department of Medicinal Chemistry.
authors.forename: Hongtao
authors.initials: H
authors.lastname: Liu
authors.affiliation: Drug Metabolism.
authors.forename: Bernard P
authors.initials: BP
authors.lastname: Murray
authors.affiliation: Biology.
authors.forename: Christian
authors.initials: C
authors.lastname: Callebaut
authors.affiliation: Drug Metabolism.
authors.forename: Melody S
authors.initials: MS
authors.lastname: Lee
authors.affiliation: Department of Medicinal Chemistry.
authors.forename: Allen
authors.initials: A
authors.lastname: Hong
authors.affiliation: Formulation.
authors.forename: Robert G
authors.initials: RG
authors.lastname: Strickley
authors.affiliation: Biology.
authors.forename: Luong K
authors.initials: LK
authors.lastname: Tsai
authors.affiliation: Biology.
authors.forename: Kirsten M
authors.initials: KM
authors.lastname: Stray
authors.affiliation: Drug Metabolism.
authors.forename: Yujin
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Drug Metabolism.
authors.forename: Gerry R
authors.initials: GR
authors.lastname: Rhodes
authors.affiliation: Department of Medicinal Chemistry.
authors.forename: Manoj C
authors.initials: MC
authors.lastname: Desai
keywords: CYP3A inhibitor; GS-9350; PK enhancer; cobicistat; pharmacoenhancer; ritonavir