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Filgotinib

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2 NDC API
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$ API Reference Price

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Chemistry

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Also known as: 1206101-20-3, Glpg0634, 1206161-97-8, Glpg-0634, N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide, Filgotinib (glpg0634)

Molecular Formula

C₂₁H₂₃N₅O₃S

Molecular Weight

425.5 g/mol

InChI Key

RIJLVEAXPNLDTC-UHFFFAOYSA-N

FDA UNII

3XVL385Q0M

Filgotinib is an orally bioavailable inhibitor of the tyrosine kinase Janus kinase 1 (JAK1), with potential anti-inflammatory and immunomodulating activities. Upon oral administration, filgotinib specifically targets, binds to, and inhibits the phosphorylation of JAK1, which interferes with JAK/STAT (signal transducer and activator of transcription)-dependent signaling. As JAK1 mediates signaling of many pro-inflammatory cytokines, JAK1 inhibition prevents cytokine signaling and activity in many inflammatory and immune-mediated processes and leads to a decrease in inflammation and activation of certain immune cells. JAK1 plays a key role in the signaling and activity of many cytokines and growth factors and is often dysregulated in a variety of autoimmune and inflammatory diseases, as well as some malignancies.

1 2D Structure

Filgotinib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

2.1.2 InChI

InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27)

2.1.3 InChI Key

RIJLVEAXPNLDTC-UHFFFAOYSA-N

2.1.4 Canonical SMILES

C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5

2.2 Other Identifiers

2.2.1 UNII

3XVL385Q0M

2.3 Synonyms

2.3.1 Depositor-Supplied Synonyms

1. 1206101-20-3

2. Glpg0634

3. 1206161-97-8

4. Glpg-0634

5. N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide

6. Filgotinib (glpg0634)

7. Filgotinib(glpg0634)

8. Gs-6034 Free Base

9. 3xvl385q0m

10. Gplg0634

11. N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

12. G146034

13. G-146034

14. N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

15. Jyseleca

16. Filgotinib [inn]

17. N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide.

18. Filgotinib [usan:inn]

19. Unii-3xvl385q0m

20. Glpg 0634

21. N-(5-{4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide

22. Glpg0634-analogue

23. Filgotinib (usan/inn)

24. Filgotinib [usan]

25. Filgotinib; Gplg0634

26. Filgotinib [who-dd]

27. Schembl253559

28. Filgotinib Pound Glpg0643)

29. Gtpl7913

30. Chembl3301607

31. Amy3802

32. Dtxsid80152935

33. Ex-a741

34. Bdbm103727

35. Hms3653p15

36. Hms3673e07

37. Bcp08496

38. Mfcd20527867

39. Nsc800100

40. S7605

41. Zinc96174616

42. Akos025291103

43. Ccg-268951

44. Db14845

45. Nsc-800100

46. Sb16799

47. Ncgc00345855-01

48. Ncgc00345855-07

49. As-16295

50. Bf159062

51. Da-33603

52. Da-33604

53. Hy-18300

54. Ft-0700114

55. Ft-0761510

56. Sw220020-1

57. A14232

58. D10871

59. P12798

60. Us8563545, 1

61. A892158

62. J-690063

63. Syn1158;glpg 0634; Glpg-0634; Filgotinib

64. Q19904163

65. Cyclopropanecarboxamide, N-(5-(4-((1,1-dioxido-4-thiomorpholinyl)methyl)phenyl)(1,2,4)triazolo(1,5-a)pyridin-2-yl)-

66. Glpg0634;n-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

67. N-(5-(4-((1,1-oxo-.lambda.6-thiomorpholin-4-yl)methyl)phenyl((1,2,4)triazolo(1,5-a)pyridin-2-yl)cyclopropanecarboxamide

2.4 Create Date

2011-01-10

3 Chemical and Physical Properties

Molecular Formula	C₂₁H₂₃N₅O₃S
Molecular Weight	425.5 g/mol
XLogP3	1.4
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	5
Exact Mass	425.15216079 g/mol
Monoisotopic Mass	425.15216079 g/mol
Topological Polar Surface Area	105 Å²
Heavy Atom Count	30
Formal Charge	0
Complexity	715
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
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

Filgotinib is indicated for the treatment of active moderate to severe rheumatoid arthritis alone or in combination with methotrexate. Filgotinib is currently reserved for patients who are unable to tolerate or who have not responded adequately to one or more disease-modifying anti-rheumatic drugs (DMARDS). Filgotinib is also indicated for treatment of moderately to severely active ulcerative colitis in adult patients who had an inadequate response with, lost response to, or were intolerant to either conventional therapy or a biologic agent.

Treatment of chronic idiopathic arthritis (including rheumatoid arthritis , ankylosing spondylarthritis , psoriatic arthritis , and juvenile idiopathic arthritis )

Rheumatoid arthritis

Jyseleca is indicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease modifying anti rheumatic drugs (DMARDs). Jyseleca may be used as monotherapy or in combination with methotrexate (MTX).

Ulcerative colitis

Jyseleca is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis who have had an inadequate response with, lost response to, or were intolerant to either conventional therapy or a biologic agent.

Treatment of Crohn's disease, Treatment of ulcerative colitis

5 Pharmacology and Biochemistry

5.1 Pharmacology

In addition to targeted Janus kinase (JAK) 1 inhibition, filgotinib targets pro-inflammatory cytokine signalling by inhibiting IL-6 induced STAT1 phosphorylation. Serum C-reactive protein levels are also reduced in response to filgotinib administration.

5.2 ATC Code

L04AA

L - Antineoplastic and immunomodulating agents

L04 - Immunosuppressants

L04A - Immunosuppressants

L04AA - Selective immunosuppressants

L04AA45 - Filgotinib

5.3 Absorption, Distribution and Excretion

Absorption

Filgotinib is rapidly absorbed after oral administration. Median peak plasma concentrations occurred 2-3 hours post-dose for filgotinib and 5 hours post-dose for GS-829845. Steady-state concentrations can be observed in 2-3 days for filgotinib and in 4 days for GS-829845. Food does not appear to have a significant effect on the absorption of filgotinib; therefore, the medication can be administered without regard to food. After repeated oral dosing of filgotinib 200 mg, the reported Cmax and AUC values of filgotinib were 2.15 ug/mL and 6.77 ugxh/mL, respectively. For GS-829845 (the major metabolite) the reported Cmax was 4.43 ug/mL and the reported AUC was 83.2 ugxh/mL.

Route of Elimination

Of the total administered dose of filgotinib, approximately 87% undergoes renal elimination while 15% undergoes faecal elimination.

5.4 Metabolism/Metabolites

Carboxylesterase enzymes are involved in the metabolism of filgotinib. The carboxylesterase 2 (CES2) isoform is chiefly responsible for metabolizing filgotinib to its major metabolite, GS-829845. Although carboxylesterase 1 (CES1) plays a less prominent role in the biotransformation of filgotinib, in vitro studies have demonstrated that CES1 will partially compensate in the event of CES2 saturation. GS-829845 is thus far the only major circulating metabolite to have been identified.

5.5 Biological Half-Life

The half-life of filgotinib is estimated to be 7 hours, while the half-life of its active metabolite GS-829845 is estimated to be 19 hours.

5.6 Mechanism of Action

There are four Janus kinase (JAK) enzymes including JAK1, JAK2, JAK3, and tyrosine kinase 2. JAK1 mediates inflammatory cytokine signaling, while JAK2 and JAK3 are important components of hematologic and immune functions. Filgotinib selectively inhibits JAK1 and is for example nearly 30-fold more selective for JAK1 compared to JAK2. The Janus kinase (JAK)-signal transducer and activator of transcription (STAT) pathway is implicated in several inflammatory pathologies and has been found to be continuously active in patients who have RA. Sustained activation of this pathway contributes to aberrant processes which lead to disease progression including elevated levels of matrix metalloproteinases (MMPs) and reduced cell apoptosis in RA affected synovial tissues. Filgotinib acts on the JAK-STAT pathway by selectively inhibiting JAK1 phosphorylation and preventing STAT activation, which ultimately results in reduced proinflammatory cytokine signaling.

API SUPPLIERS

01

Metrochem API Private Limited

India

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

AES 2024

Not Confirmed

Metrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

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India

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USDMF CEP/COS JDMF EU-WC NDC KDMF VMF Others AUDIT

02

Shanghai Hope Chem

China

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

AES 2024

Not Confirmed

03

Beijing Sjar Technology Developmen...

China

USDMF, CEP/COS, JDMF, EU-WC, NDC, KDMF, VMF, Others

AES 2024

Not Confirmed

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Listed Suppliers

01

Metrochem API Private Limited

India

Medlab Asia & Asia Health

Not Confirmed

Metrochem has been delivering customized volume & quality products to customers across the world, taking utmost care of their needs.

Contact Supplier

India

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Filgotinib

About the Company :

Established in 2004, Metrochem API is one of the fastest-growing APIs, pellets & intermediates manufacturers. It has 6 dedicated manufacturing facilities for its 3 core product ...

Established in 2004, Metrochem API is one of the fastest-growing APIs, pellets & intermediates manufacturers. It has 6 dedicated manufacturing facilities for its 3 core product groups and has been approved by ISO 9001-2015, USFDA, WHO GMP, Cofepris & Japanese authorities. Metrochem’s in-depth industry knowledge, & hi-tech & advanced infrastructure, helps it provide quality products to its customers. Note: None of the products will be supplied to the countries where this could conflict with existing patents. Further, any products under patent will be offered for R&D purposes only. However, the final responsibility lies with the buyer