tcsc0742 Cobicistat

Cobicistat is a potent, and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC₅₀ of 30-285 nM.

IC50 & Target: IC50: 30-285 nM (Cytochrome P450)^[1]

In Vitro: Cobicistat (GS-9350) is a potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes as a pharmacoenhancer. GS-9350 inhibits CYP3A with IC₅₀ spectrum from 30 nM to 285 nM. In contrast to ritonavir, GS-9350 is devoid of anti-HIV activity, with IC₅₀ of > 30 μM against HIV-1 protease and EC₅₀ of > 30μM in MT-2 HIV infection assay, and is thus more suitable for use in boosting anti-HIV drugs without risking selection of potential drug-resistant HIV variants. GS-9350 shows reduced liability for drug interactions and may have potential improvements in tolerability over ritonavir^[1]. Cobicistat is a novel cytochrome P450 3A4 inhibitor in advanced clinical evaluation for use as a pharmacoenhancer of antiretroviral drugs. It lacks significant anti-HIV activity and is more selective than ritonavir in its enzyme inhibition^[2].