- Cobicistat
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Systematic (IUPAC) name Thiazol-5-ylmethyl N-[1-benzyl-4-[[2-[[(2-isopropylthiazol-4-yl)methyl-methyl-carbamoyl]amino]-4-morpholino-butanoyl]amino]-5-phenyl-pentyl]carbamate Clinical data Pregnancy cat. ? Legal status ? Identifiers CAS number 1004316-88-4 ATC code ? ChemSpider 25084912 UNII LW2E03M5PG Chemical data Formula C40H53N7O5S2 Mol. mass 776.023 g/mol SMILES eMolecules & PubChem - InChI=1S/C40H53N7O5S2/c1-29(2)38-43-34(27-53-38)25-46(3)39(49)45-36(16-17-47-18-20-51-21-19-47)37(48)42-32(22-30-10-6-4-7-11-30)14-15-33(23-31-12-8-5-9-13-31)44-40(50)52-26-35-24-41-28-54-35/h4-13,24,27-29,32-33,36H,14-23,25-26H2,1-3H3,(H,42,48)(H,44,50)(H,45,49)/t32-,33-,36+/m1/s1
Key:ZCIGNRJZKPOIKD-CQXVEOKZSA-N
(what is this?) (verify) Cobicistat is a drug under experimental investigation for use in the treatment of infection with the human immunodeficiency virus (HIV).
Like ritonovir (Norvir), cobicistat is of interest not for its anti-HIV properties, but rather its ability to inhibit liver enzymes that metabolize other medications used to treat HIV, notably elvitegravir, an HIV integrase inhibitor currently under investigation itself. By combining cobicistat with elvitegravir, higher concentrations of elvitgravir are achieved in the body with lower dosing, theoretically enhancing elvitgravir's viral suppression while diminishing its adverse side-effects. In contrast with ritonavir, the only currently approved booster, cobicistat has no anti-HIV activity of is own.[1]
If approved by the U.S. Food and Drug Administration, cobicistat will be part of the four-drug, fixed-dose combination HIV treatment known as the "Quad Pill".[1][2] The Quad Pill is currently in Phase III clinical trials,[3] and is owned by Gilead Sciences.
References
- ^ a b Highleyman, L. Elvitegravir "Quad" Single-tablet Regimen Shows Continued HIV Suppression at 48 Weeks. HIV and Hepatitis.com
- ^ R Elion, J Gathe, B Rashbaum, and others. The Single-Tablet Regimen of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Disoproxil Fumarate (EVG/COBI/FTC/TDF; Quad) Maintains a High Rate of Virologic Suppression, and Cobicistat (COBI) is an Effective Pharmacoenhancer Through 48 Weeks. 50th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC 2010). Boston, September 12–15, 2010.
- ^ "Quad Pill Phase III Clinical Trials". ClinicalTrials.gov. http://clinicaltrials.gov/ct2/results?term=elvitegravir+GS-9350+OR+cobicistat&phase=2. Retrieved August 2011.
Categories:- Antiretroviral drugs
- Thiazoles
- Morpholines
- Carbamates
- Ureas
- InChI=1S/C40H53N7O5S2/c1-29(2)38-43-34(27-53-38)25-46(3)39(49)45-36(16-17-47-18-20-51-21-19-47)37(48)42-32(22-30-10-6-4-7-11-30)14-15-33(23-31-12-8-5-9-13-31)44-40(50)52-26-35-24-41-28-54-35/h4-13,24,27-29,32-33,36H,14-23,25-26H2,1-3H3,(H,42,48)(H,44,50)(H,45,49)/t32-,33-,36+/m1/s1
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