Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 5, Pages 209-213Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml1000257
Keywords
GS-9350; cobicistat; pharmacoenhancer; PK enhancer; CYP3A inhibitor; ritonavir
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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.
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