Cobicistat
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MedKoo CAT#: 300151

CAS#: 1004316-88-4

Description: Cobicistat, 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.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 650 Same day
200mg USD 1050 Same day
500mg USD 1950 Same day
1g USD 3250 2 Weeks
2g USD 5450 2 Weeks
5g USD 8750 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-02-28. Prices are subject to change without notice.

Cobicistat purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 300151
Name: Cobicistat
CAS#: 1004316-88-4
Chemical Formula: C40H53N7O5S2
Exact Mass: 775.35496
Molecular Weight: 776.02
Elemental Analysis: C, 61.91; H, 6.88; N, 12.63; O, 10.31; S, 8.26


Synonym: GS9350; GS-9350; GS 9350; Cobicistat, brand name: Tybost; Genvoya.

IUPAC/Chemical Name: thiazol-5-ylmethyl ((2R,5R)-5-((S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanamido)-1,6-diphenylhexan-2-yl)carbamate

InChi Key: ZCIGNRJZKPOIKD-CQXVEOKZSA-N

InChi Code: 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

SMILES Code: 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


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Cattaneo D, Cossu MV, Rizzardini G. Pharmacokinetic drug evaluation of ritonavir (versus cobicistat) as adjunctive therapy in the treatment of HIV. Expert Opin Drug Metab Toxicol. 2019 Nov;15(11):927-935. doi: 10.1080/17425255.2019.1685495. Epub 2019 Nov 3. Review. PubMed PMID: 31668105.

2: Common Drug Review New Combination Product Submission: Darunavir/Cobicistat/Emtricitabine/Tenofovir alafenamide (Symtuza): (Janssen Canada Inc.): Indication: A complete regimen for the treatment of HIV type 1 infection in adults and adolescents (aged 12 years and older with body weight at least 40 kg) with no known mutations associated with resistance to the individual components of Symtuza [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Aug. Available from http://www.ncbi.nlm.nih.gov/books/NBK540525/ PubMed PMID: 31034191.

3: CADTH Canadian Drug Expert Committee Recommendation: Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (Symtuza — Janssen Inc.): Indication: Treatment of HIV type 1 (HIV-1) infection [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Jul. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK540287/ PubMed PMID: 31013021.

4: Giacomet V, Cossu MV, Capetti AF, Zuccotti G, Rizzardini G. An evaluation of elvitegravir plus cobicistat plus tenofovir alafenamide plus emtricitabine as a single-tablet regimen for the treatment of HIV in children and adolescents. Expert Opin Pharmacother. 2019 Feb;20(3):269-276. doi: 10.1080/14656566.2018.1559299. Epub 2018 Dec 26. Review. PubMed PMID: 30586314.

5: Squillace N, Bozzi G, Colella E, Gori A, Bandera A. Darunavir-cobicistat-emtricitabine-tenofovir alafenamide: safety and efficacy of a protease inhibitor in the modern era. Drug Des Devel Ther. 2018 Oct 29;12:3635-3643. doi: 10.2147/DDDT.S147493. eCollection 2018. Review. PubMed PMID: 30464395; PubMed Central PMCID: PMC6211373.

6: Deeks ED. Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Jul;78(10):1013-1024. doi: 10.1007/s40265-018-0934-2. Review. PubMed PMID: 29915897.

7: Cevik M, Orkin C. Fixed dose darunavir boosted with cobicistat combined with emtricitabine and tenofovir alafenamide fumarate. Curr Opin HIV AIDS. 2018 Jul;13(4):315-319. doi: 10.1097/COH.0000000000000465. Review. PubMed PMID: 29528852.

8: Institute for Quality and Efficiency in Health Care. Elvitegravir / Cobicistat / Emtricitabine / Tenofovir Alafenamide -- Addendum to Commission A15-61 [Internet]. Cologne, Germany: Institute for Quality and Efficiency in Health Care (IQWiG); 2016 May 27. Available from http://www.ncbi.nlm.nih.gov/books/NBK458451/ PubMed PMID: 29144710.

9: Institute for Quality and Efficiency in Health Care. Elvitegravir / Cobicistat / Emtricitabine / Tenofovir Alafenamide -- Benefit Assessment According to §35a Social Code Book V [Internet]. Cologne, Germany: Institute for Quality and Efficiency in Health Care (IQWiG); 2016 Mar 30. Available from http://www.ncbi.nlm.nih.gov/books/NBK458440/ PubMed PMID: 29144685.

10: Tseng A, Hughes CA, Wu J, Seet J, Phillips EJ. Cobicistat Versus Ritonavir: Similar Pharmacokinetic Enhancers But Some Important Differences. Ann Pharmacother. 2017 Nov;51(11):1008-1022. doi: 10.1177/1060028017717018. Epub 2017 Jun 19. Review. PubMed PMID: 28627229; PubMed Central PMCID: PMC5702580.

11: Angione SA, Cherian SM, Özdener AE. A Review of the Efficacy and Safety of Genvoya® (Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide) in the Management of HIV-1 Infection. J Pharm Pract. 2018 Apr;31(2):216-221. doi: 10.1177/0897190017710519. Epub 2017 May 30. Review. PubMed PMID: 28558493.

12: Antunes F. Atazanavir sulfate + cobicistat for the treatment of HIV infection. Expert Rev Anti Infect Ther. 2017 Jun;15(6):569-576. doi: 10.1080/14787210.2017.1323634. Epub 2017 May 9. Review. PubMed PMID: 28443391.

13: Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (EVG/COBI/FTC/TAF) (Genvoya) Fixed-Dose Combination, Oral Tablet) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016 Nov. Available from http://www.ncbi.nlm.nih.gov/books/NBK409851/ PubMed PMID: 28121099.

14: González-Domenech CM, Palacios R, Santos J. [Pharmacological aspects of darunavir/cobicistat]. Enferm Infecc Microbiol Clin. 2016 May;34 Suppl 1:30-33. doi: 10.1016/S0213-005X(17)30006-X. Review. Spanish. PubMed PMID: 28081761.

15: Navarro J, Curran A. Profile of once-daily darunavir/cobicistat fixed-dose combination for the treatment of HIV/AIDS. HIV AIDS (Auckl). 2016 Oct 31;8:175-182. eCollection 2016. Review. PubMed PMID: 27843352; PubMed Central PMCID: PMC5098528.

16: Darunavir/Cobicistat (Prezcobix) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2015 Jul. Available from http://www.ncbi.nlm.nih.gov/books/NBK362499/ PubMed PMID: 27227212.

17: Nguyen T, McNicholl I, Custodio JM, Szwarcberg J, Piontkowsky D. Drug Interactions with Cobicistat- or Ritonavir-Boosted Elvitegravir. AIDS Rev. 2016 Apr-Jun;18(2):101-11. Review. PubMed PMID: 27196356.

18: Greig SL, Deeks ED. Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2016 Jun;76(9):957-68. doi: 10.1007/s40265-016-0586-z. Review. PubMed PMID: 27189707.

19: Crutchley RD, Guduru RC, Cheng AM. Evaluating the role of atazanavir/cobicistat and darunavir/cobicistat fixed-dose combinations for the treatment of HIV-1 infection. HIV AIDS (Auckl). 2016 Mar 9;8:47-65. doi: 10.2147/HIV.S99063. eCollection 2016. Review. PubMed PMID: 27022304; PubMed Central PMCID: PMC4790521.

20: von Hentig N. Clinical use of cobicistat as a pharmacoenhancer of human immunodeficiency virus therapy. HIV AIDS (Auckl). 2015 Dec 22;8:1-16. doi: 10.2147/HIV.S70836. eCollection 2016. Review. PubMed PMID: 26730211; PubMed Central PMCID: PMC4694690.