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Cobicistat

Synopsis, Chemistry

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Also known as: 1004316-88-4, Cobicistat (gs-9350), Gs-9350, Tybost, Gs 9350, Cobicistat,gs-9350

Molecular Formula

C₄₀H₅₃N₇O₅S₂

Molecular Weight

776.0 g/mol

InChI Key

ZCIGNRJZKPOIKD-CQXVEOKZSA-N

FDA UNII

LW2E03M5PG

A carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with which it is used in combination, for the treatment of HIV INFECTIONS.

Cobicistat is a Cytochrome P450 3A Inhibitor. The mechanism of action of cobicistat is as a Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor, and Cytochrome P450 2D6 Inhibitor, and Organic Anion Transporting Polypeptide 1B1 Inhibitor, and Organic Anion Transporting Polypeptide 1B3 Inhibitor, and Breast Cancer Resistance Protein Inhibitor, and Multidrug and Toxin Extrusion Transporter 1 Inhibitor.

1 2D Structure

Cobicistat

2 Identification

2.1 Computed Descriptors

2.1.1 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

2.1.2 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

2.1.3 InChI Key

ZCIGNRJZKPOIKD-CQXVEOKZSA-N

2.1.4 Canonical SMILES

CC(C)C1=NC(=CS1)CN(C)C(=O)NC(CCN2CCOCC2)C(=O)NC(CCC(CC3=CC=CC=C3)NC(=O)OCC4=CN=CS4)CC5=CC=CC=C5

2.1.5 Isomeric SMILES

CC(C)C1=NC(=CS1)CN(C)C(=O)N[C@@H](CCN2CCOCC2)C(=O)N[C@H](CC[C@H](CC3=CC=CC=C3)NC(=O)OCC4=CN=CS4)CC5=CC=CC=C5

2.2 Other Identifiers

2.2.1 UNII

LW2E03M5PG

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 9350, Gs

2. Gs 9350

3. Gs-9350

4. Gs9350

5. Tybost

2.3.2 Depositor-Supplied Synonyms

1. 1004316-88-4

2. Cobicistat (gs-9350)

3. Gs-9350

4. Tybost

5. Gs 9350

6. Cobicistat,gs-9350

7. Unii-lw2e03m5pg

8. Chebi:72291

9. Lw2e03m5pg

10. 1,3-thiazol-5-ylmethyl [(2r,5r)-5-{[(2s)-2-({[(2-isopropyl-1,3-thiazol-4-yl)methyl](methyl)carbamoyl}amino)-4-(morpholin-4-yl)butanoyl]amino}-1,6-diphenylhexan-2-yl]carbamate

11. 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

12. Thiazol-5-ylmethyl ((2r,5r)-5-((s)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanamido)-1,6-diphenylhexan-2-yl)carbamate

13. 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-yl)butanamido]-1,6-diphenylhexan-2-yl]carbamate

14. 2,7,10,12-tetraazatridecanoic Acid, 12-methyl-13-(2-(1-methylethyl)-4-thiazolyl)-9-(2-(4-morpholinyl)ethyl)-8,11-dioxo-3,6-bis(phenylmethyl)-, 5-thiazolylmethyl Ester, (3r,6r,9s)-

15. Cobicistat [usan]

16. Cobicistat [usan:inn]

17. Cobicistatum

18. 2,7,10,12-tetraazatridecanoic Acid, 12-methyl-13-[2-(1-methylethyl)-4-thiazolyl]-9-[2-(4-morpholinyl)ethyl]-8,11-dioxo-3,6-bis(phenylmethyl)-, 5-thiazolylmethyl Ester, (3r,6r,9s)-

19. Thiazol-5-ylmethyl (2r,5r)-5-((s)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanamido)-1,6-diphenylhexan-2-ylcarbamate

20. Tybost (tn)

21. Cobicistat [mi]

22. Cobicistat [inn]

23. Cobicistat [jan]

24. Cobicistat; Gs-9350

25. Cobicistat [vandf]

26. Cobicistat [who-dd]

27. Cobicistat On Silicon Dioxide

28. Cobicistat (jan/usan/inn)

29. Gtpl7535

30. Schembl2736227

31. Chembl2095208

32. Cobicistat [orange Book]

33. Cobicistat, (r,r,s)-

34. Dtxsid00143269

35. Evotaz Component Cobicistat

36. Genvoya Component Cobicistat

37. Symtuza Component Cobicistat

38. Bcp06630

39. Ex-a2578

40. Rezolsta Component Cobicistat

41. Stribild Component Cobicistat

42. Bdbm50447471

43. Mfcd18251449

44. Prezcobix Component Cobicistat

45. S2900

46. Zinc85537014

47. Cobicistat Component Of Evotaz

48. Akos025404908

49. Cobicistat Component Of Genvoya

50. Cobicistat Component Of Symtuza

51. Ccg-270459

52. Cobicistat Component Of Stribild

53. Cs-0742

54. Db09065

55. Cobicistat Component Of Prezcobix

56. Ncgc00386235-04

57. Ncgc00386235-06

58. Ac-28961

59. As-17061

60. Hy-10493

61. Sw219553-1

62. D09881

63. Ab01566899_01

64. Q5138908

65. (1,3-thiazol-5-yl)methyl (5s,8r,11r)-8,11-dibenzyl-2-methyl-5-(2-(morpholin-4-yl)ethyl)-1-(2-(propan-2-yl)-1,3-thiazol-4-yl)-3,6-dioxo-2,4,7,12-tetraazatridecan-13-oate

66. 1,3-thiazol-5-ylmethyl ((2r,5r)-5-(((2s)-2-((methyl((2-(propan-2-yl)-1,3-thiazol-4-yl)methyl)carbamoyl)amino)-4-(morpholin-4-yl)butanoyl)amino)-1,6-diphenylhexan-2-yl)carbamate

67. Thiazol-5-ylmethyl ((1r,4r)-1-benzyl-4-({(2s)-2-((methyl{(2-(1-methylethyl)thiazol-4-yl)methyl}carbamoyl)amino)-4-(morpholin-4-yl)butanoyl}amino)-5-phenylpentyl)carbamate

68. Thiazol-5-ylmethyl N-[(1r,4r)-1-benzyl-4-[[(2s)-2-[[(2-isopropylthiazol-4-yl)methyl-methyl-carbamoyl]amino]-4-morpholino-butanoyl]amino]-5-phenyl-pentyl]carbamate

2.4 Create Date

2009-02-23

3 Chemical and Physical Properties

Molecular Formula	C₄₀H₅₃N₇O₅S₂
Molecular Weight	776.0 g/mol
XLogP3	5.7
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	10
Rotatable Bond Count	20
Exact Mass	775.35496016 g/mol
Monoisotopic Mass	775.35496016 g/mol
Topological Polar Surface Area	195 Å²
Heavy Atom Count	54
Formal Charge	0
Complexity	1120
Isotope Atom Count	0
Defined Atom Stereocenter Count	3
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

Cobicistat is a CYP3A inhibitor indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. It is not interchangeable with ritonavir to increase systemic exposure of darunavir 600 mg twice daily, fosamprenavir, saquinavir, or tipranavir due to lack of exposure data. The use of cobicistat is not recommended with darunavir 600 mg twice daily, fosamprenavir, saquinavir or tipranavir. Complex or unknown mechanisms of drug interactions preclude extrapolation of ritonavir drug interactions to certain cobicistat interactions. Cobicistat and ritonavir when administered with either atazanavir or darunavir may result in different drug interactions when used with concomitant medications.

FDA Label

Tybost is indicated as a pharmacokinetic enhancer of atazanavir 300 mg once daily or darunavir 800 mg once daily as part of antiretroviral combination therapy in human immunodeficiency virus-1 (HIV-1) infected adults and adolescents aged 12 years and older:

- weighing at least 35 kg coadministered with atazanavir or

- weighing at least 40 kg coadministered with darunavir.

5 Pharmacology and Biochemistry

5.1 MeSH Pharmacological Classification

Anti-HIV Agents

Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. (See all compounds classified as Anti-HIV Agents.)

Cytochrome P-450 CYP3A Inhibitors

Drugs and compounds which inhibit or antagonize the biosynthesis or actions of CYTOCHROME P-450 CYP3A. (See all compounds classified as Cytochrome P-450 CYP3A Inhibitors.)

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

COBICISTAT

5.2.2 FDA UNII

LW2E03M5PG

5.2.3 Pharmacological Classes

Cytochrome P450 2D6 Inhibitors [MoA]; Cytochrome P450 3A Inhibitor [EPC]; Cytochrome P450 3A Inhibitors [MoA]; Organic Anion Transporting Polypeptide 1B1 Inhibitors [MoA]; Organic Anion Transporting Polypeptide 1B3 Inhibitors [MoA]; P-Glycoprotein Inhibitors [MoA]; Breast Cancer Resistance Protein Inhibitors [MoA]

5.3 ATC Code

V03AX03

J05AR14

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

V - Various

V03 - All other therapeutic products

V03A - All other therapeutic products

V03AX - Other therapeutic products

V03AX03 - Cobicistat

5.4 Absorption, Distribution and Excretion

Absorption

Median peak plasma concentrations were observed at 3.5 hours post-dose.

Route of Elimination

With single dose administration of [14C] cobicistat after multiple dosing of cobicistat for six days, the mean percent of the administered dose excreted in feces and urine was 86.2% and 8.2%, respectively.

5.5 Metabolism/Metabolites

Cobicistat is metabolized by CYP3A and to a minor extent by CYP2D6 enzymes and does not undergo glucuronidation.

5.6 Biological Half-Life

The terminal plasma half-life of cobicistat is approximately 3 to 4 hours.

5.7 Mechanism of Action

Cobicistat is a mechanism-based inhibitor of cytochrome P450 3A (CYP3A) isoforms. Inhibition of CYP3A-mediated metabolism by cobicistat increases the systemic exposure of CYP3A substrates atazanavir and darunavir and therefore enables increased anti-viral activity at a lower dosage. Cobicistat does not have any anti-HIV activity on its own.

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