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Olmutinib

Olmutinib

Synopsis, Chemistry

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Also known as: 1353550-13-6, Hm61713, Bi 1482694, 1802181-20-9, Olmutinib [inn], Hm-61713

Molecular Formula

C₂₆H₂₆N₆O₂S

Molecular Weight

486.6 g/mol

InChI Key

FDMQDKQUTRLUBU-UHFFFAOYSA-N

FDA UNII

CHL9B67L95

Olmutinib is an orally available small molecule, mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild type form.

1 2D Structure

Olmutinib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]thieno[3,2-d]pyrimidin-4-yl]oxyphenyl]prop-2-enamide

2.1.2 InChI

InChI=1S/C26H26N6O2S/c1-3-23(33)27-19-5-4-6-21(17-19)34-25-24-22(11-16-35-24)29-26(30-25)28-18-7-9-20(10-8-18)32-14-12-31(2)13-15-32/h3-11,16-17H,1,12-15H2,2H3,(H,27,33)(H,28,29,30)

2.1.3 InChI Key

FDMQDKQUTRLUBU-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4

2.2 Other Identifiers

2.2.1 UNII

CHL9B67L95

2.3 Synonyms

2.3.1 Depositor-Supplied Synonyms

1. 1353550-13-6

2. Hm61713

3. Bi 1482694

4. 1802181-20-9

5. Olmutinib [inn]

6. Hm-61713

7. Olmutinib [who-dd]

8. Bi-1482694

9. N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]thieno[3,2-d]pyrimidin-4-yl]oxyphenyl]prop-2-enamide

10. Chl9b67l95

11. N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)thieno[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide

12. N-{3-[(2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}thieno[3,2-d]pyrimidin-4-yl)oxy]phenyl}prop-2-enamide

13. 2-propenamide, N-(3-((2-((4-(4-methyl-1-piperazinyl)phenyl)amino)thieno(3,2-d)pyrimidin-4-yl)oxy)phenyl)-

14. N-(3-((2-(4-(4-methylpiperazin-1-yl)anilino)thieno(3,2-d)pyrimidin-4-yl)oxy)phenyl)prop-2-enamide

15. 1938072-69-5

16. 2-propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]-

17. Hm-61713 (bi-1482694)

18. Hm 61713

19. Hm71224;olmutinib

20. Olmutinib (usan/inn)

21. Olmutinib [usan:inn]

22. Olmutinib [usan]

23. Olmutinib(hm-71224)

24. Unii-chl9b67l95

25. Gtpl9196

26. Chembl3786343

27. Schembl14914931

28. Ex-a879

29. Dtxsid001319119

30. Bcp16733

31. Bdbm50160871

32. Mfcd29918158

33. Nsc792848

34. Nsc800980

35. S8294

36. Akos030632791

37. Zinc198970879

38. Ccg-269594

39. Cs-5413

40. Db13164

41. Nsc-792848

42. Nsc-800980

43. Sb19797

44. Example 1 [us20130116213]

45. Ac-30225

46. Ac-35418

47. As-74850

48. Hm 71224

49. Hy-19730

50. Bi1482694

51. Ds-015877

52. Ft-0700176

53. Olmutinib (hm61713, Bi 1482694)

54. J3.435.413h

55. D10859

56. W12116

57. Hm61713, Bi 1482694

58. A900418

59. J-690142

60. Q27088175

61. 4-{[4-({[(1r,2s)-2-phenylcyclopropyl]amino}methyl)-1-piperidinyl]methyl}benzoic Acid

62. Bi1482694;bi 1482694;bi-1482694;hm 61713;hm-61713;hm61713

63. N-(3-(2-(4-(4 Methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidine-4-yloxy)phenyl)acrylamide

64. N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidine-4-yloxy)phenyl)acrylamide

65. N-(3-{2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-thieno[3,2-d]pyrimidin-4-yloxy}-phenyl)-acrylamide

2.4 Create Date

2012-01-09

3 Chemical and Physical Properties

Molecular Formula	C₂₆H₂₆N₆O₂S
Molecular Weight	486.6 g/mol
XLogP3	4.7
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	7
Exact Mass	486.18379527 g/mol
Monoisotopic Mass	486.18379527 g/mol
Topological Polar Surface Area	111 Å²
Heavy Atom Count	35
Formal Charge	0
Complexity	712
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

For use in treatment of metastatic T790M mutation positive non-small cell lung cancer.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Olmutinib selectively and irreversibly binds and inhibits epidermal growth factor receptors (EGFR) with the T790M activating mutation. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen activated protein kinase pathways which both promote cell survival and proliferation. By inhibiting EGFR activation, olmutinib attenuates the activation of these tumor promoting pathways.

5.2 ATC Code

L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EB - Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors

L01EB06 - Olmutinib

5.3 Absorption, Distribution and Excretion

Absorption

tmax of 3-4h with oral administration.

Route of Elimination

Data not yet available.

Volume of Distribution

Data not yet available.

Clearance

Data not yet available.

5.4 Metabolism/Metabolites

Data not yet available.

5.5 Biological Half-Life

8-11h.

5.6 Mechanism of Action

Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor. This inhibits receptor signalling as phosphorylation is necessary for recruitment of signalling cascade proteins.