Brief Description

Cobicistat (GS-9350) is a potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes (Ki=939 nM).
IC50 value: 939 nM (Ki) [1]
Target: CYP3A
Cobicistat is a novel cytochrome P450 3A4 (CYP3A4) 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. In addition, its water solubility may lend itself to coformulation with other drugs. Renal adverse effects and a considerable drug interaction potential limit its clinical utility and caution is required when using it. A fixed-dose combination product containing cobicistat in addition to elvitegravir, tenofovir and emtricitabine, and providing a one-pill, once-a-day, antiretroviral regimen was recently approved.
References on Cobicistat:
[1]. Lianhong Xu, et al. Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer. ACS Med. Chem. Lett., 2010, 1 (5), pp 209–213
[2]. Temesgen Z. Cobicistat, a pharmacoenhancer for HIV treatments.Drugs Today (Barc). 2013 Apr;49(4):233-7.

Solubility

10 mM in DMSO

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid