Cobicistat

Base Information

• Chemical Name: Cobicistat
• CAS No.: 1004316-88-4
• Molecular Formula: C40H53N7O5S2
• Molecular Weight: 776.02
• Mol file: 1004316-88-4.mol

Synonyms:GS 9350;

Chemical Property of Cobicistat

Chemical Property:

• Boiling Point: 974.526 °C at 760 mmHg
• PKA: 11.86±0.46(Predicted)
• Flash Point: 543.174 °C
• PSA: 194.50000
• Density: 1.229 g/cm³
• LogP: 7.11130
• Storage Temp.: Hygroscopic, Refrigerator, under inert atmosphere
• Solubility.: Chloroform (Slightly), DMSO (Slightly), Ethyl Acetate (Slightly), Methanol (Slig

Purity/Quality:

97% ^*data from raw suppliers

Cobicistat-d8 ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• Description: Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM. Cobicistat, a selective, mechanism-based CYP3A inhibitor, was discovered and developed by Gilead Sciences, Inc. In 2013, European Medicines Agency (EMA) approved cobicistat (Tybost) for the treatment of HIV-1 infection in combination with protease inhibitors (PIs) atazanavir or darunavir. Interestingly, cobicistat does not interact with HIV directly, but instead serves as a pharmacokinetic enhancer to boost the anti-HIV effect of atazanavir or darunavir through blockade of CYP3A. Cobicistat slows CYP-mediated metabolism of atazanavir and darunavir, resulting in prolonged systemic exposure of the drug(s). Cobicistat is also available as part of a fixed-dose combination tablet (Stribild) of four additional drugs with CYP3A liabilities (elvitegravir, cobicistat, emtricitabine and tenofovir disoproxil fumarate), which was approved in U.S. in 2012, and subsequently approved in Europe and Japan in 2013.
• Uses: Cobicistat is a HIV protease inhibitor and have been coadministered with low-dose ritonavir (R535000) as a pharmacoenhancer, significantly increasing their plasma concentrations. Isotope labelled analogue of Cobicistat (C633150), a HIV protease inhibitor and have been coadministered with low-dose ritonavir (R535000) as a pharmacoenhancer, significantly increasing their plasma concentrations. Antiretroviral;Labeled Cobicistat, intended for use as an internal standard for the quantification of Cobicistat by GC- or LC-mass spectrometry.
• Clinical Use: Pharmacokinetic enhancer used to increase the effect of atazanavir and darunavir
• Drug interactions: Potentially hazardous interactions with other drugsAlpha-blockers: concentration of alfuzosin possibly increased - avoid. Anti-arrhythmics: concentration of amiodarone possibly increased - avoid. Antibacterials: concentration reduced by rifabutin and rifampicin - adjust cobicistat dose, avoid with rifampicin. Anticoagulants: avoid with apixaban; anticoagulant effect of rivaroxaban possibly enhanced - avoid. Antidepressants: concentration possibly reduced by St John’s wort - avoid. Antiepileptics: concentration of cobicistat possibly reduced by carbamazepine, fosphenytoin phenobarbital, phenytoin and primidone - avoid. Antifungals: concentration of itraconazole and ketoconazole possibly increased - reduce antifungal dose. Antipsychotics: concentration of lurasidone and pimozide possibly increased - avoid. Antivirals: concentration of daclatasvir and maraviroc possibly increased - reduce daclatasvir and maraviroc dose; avoid with dasabuvir, nevirapine, ombitasvir, paritaprevir, ritonavir and simeprevir; concentration of elbasvir and grazoprevir increased - avoid; concentration of olaparib possibly increased - avoid or reduce olaparib dose; concentration of both drugs reduced with tipranavir - avoid. Anxiolytics: avoid with oral midazolam. Avanafil: concentration of avanafil possibly increased - avoid. Bosentan: avoid concomitant use. Cardiac glycosides: concentration of digoxin possibly increased - reduce initial dose of digoxin. Corticosteroids: concentration of corticosteroids possibly increased avoid or use with caution. Cytotoxics: concentration of ibrutinib possibly increased - reduce ibrutinib dose; concentration of olaparib possibly increased - avoid or reduce dose of olaparib. Domperidone: possible increased risk of ventricular arrhythmias - avoid. Ergot alkaloids: concentration of ergot alkaloids possibly increased - avoid. Immunosuppression: concentration of ciclosporin, sirolimus and tacrolimus possibly increased. Lipid-lowering drugs: concentration of atorvastatin possibly increased - reduce atorvastatin dose; avoid with simvastatin. Oestrogens: metabolism of oestrogens accelerated, reduced contraceptive effect - avoid or use with caution. Salmeterol: avoid concomitant use. Sildenafil: concentration of sildenafil possibly increased - avoid sildenafil for pulmonary arterial hypertension, reduce dose for erectile dysfunction. Tadalafil: concentration of tadalafil possibly increased - reduce dose of tadalafil. Vardenafil: concentration of vardenafil possibly increased - reduce dose of vardenafil.