Cobicistat (GS-9350)


CAS No. : 1004316-88-4

Cobicistat (GS-9350),1004316-88-4
Product Details
Cat No:A001226
Synonyms:Cobicistat; GS-9350
Molecular Formula:C40H53N7O5S2
Molecular Weight:776.02
Target:CYP3A/CYP450
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Appearance:white solid powder
Purity: > 98%
Cat No:A001226
Cas No:1004316-88-4
Product-Name:Cobicistat (GS-9350)
IUPAC Name:1,3-thiazol-5-ylmethyl N-[(2R,5R)-5-[[(2S)-2-[[methyl-[(2-propan-2-yl-1,3-thiazol-4-yl)methyl]carbamoyl]amino]-4-morpholin-4-ylbutanoyl]amino]-1,6-diphenylhexan-2-yl]carbamate
InChI: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
InChIKey:ZCIGNRJZKPOIKD-CQXVEOKZSA-N
SMILES:O=C(OCC1=CN=CS1)N[C@H](CC[C@@H](NC([C@@H](NC(N(CC2=CSC(C(C)C)=N2)C)=O)CCN3CCOCC3)=O)CC4=CC=CC=C4)CC5=CC=CC=C5
Cobicistat(cas ), also known as GS9350, is an approved drug for use in the treatment of infection with the human immunodeficiency virus (HIV). Like ritonavir (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 its own. Cobicistat is a component of the four-drug, fixed-dose combination HIV treatment elvitegravir/cobicistat/emtricitabine/tenofovir (known as the /Quad Pill/). The Quad Pill was approved by the FDA in August 2012 for use in the United States and is owned by Gilead Sciences.

1: Andreatta K, Miller MD, White KL. HIV-2 Antiviral Potency and Selection of Drug Resistance Mutations by the Integrase Strand Transfer Inhibitor Elvitegravir and NRTIs Emtricitabine and Tenofovir In Vitro. J Acquir Immune Defic Syndr. 2012 Nov 26. [Epub ahead of print] PubMed PMID: 23187937.
2: FDA approves new 4-drug once-a-day HIV treatment. AIDS Policy Law. 2012 Oct;27(11):1. PubMed PMID: 23155506.
3: Olin JL, Spooner LM, Klibanov OM. Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Disoproxil Fumarate Single Tablet for HIV-1 Infection Treatment (December). Ann Pharmacother. 2012 Nov 7. [Epub ahead of print] PubMed PMID: 23136357.
4: von Hentig N, Haberl A. Safety of pharmacoenhancers for HIV therapy. Expert Rev Clin Pharmacol. 2012 Sep;5(5):557-68. doi: 10.1586/ecp.12.45. PubMed PMID: 23121278.
5: Permpalung N, Putcharoen O, Avihingsanon A, Ruxrungtham K. Treatment of HIV infection with once-daily regimens. Expert Opin Pharmacother. 2012 Nov;13(16):2301-17. doi: 10.1517/14656566.2012.729040. Epub 2012 Oct 8. PubMed PMID: 23043453.
6: Pommer P. [A single tablet against HIV: new combination preparation improves therapy]. Dtsch Med Wochenschr. 2012 Aug;137(34-35):1673. doi: 10.1055/s-0032-131866. Epub 2012 Aug 14. German. PubMed PMID: 22893044.
7: Lee FJ, Carr A. Tolerability of HIV integrase inhibitors. Curr Opin HIV AIDS. 2012 Sep;7(5):422-8. doi: 10.1097/COH.0b013e328356682a. Review. PubMed PMID: 22886031.
8: Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS. Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30. PubMed PMID: 22850510; PubMed Central PMCID: PMC3457391.
9: Schrijvers R, Debyser Z. Combinational therapies for HIV: a focus on EVG/COBI/FTC/TDF. Expert Opin Pharmacother. 2012 Sep;13(13):1969-83. doi: 10.1517/14656566.2012.712514. Epub 2012 Jul 31. PubMed PMID: 22849516.
10: Llibre JM, Clotet B. Once-daily single-tablet regimens: a long and winding road to excellence in antiretroviral treatment. AIDS Rev. 2012 Jul;14(3):168-78. Review. PubMed PMID: 22833060.
  
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