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Ixazomib

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Also known as: 1072833-77-2, Mln2238, Mln-2238, Mln 2238, Ixazomib [inn], (r)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic acid

Molecular Formula

C₁₄H₁₉BCl₂N₂O₄

Molecular Weight

361.0 g/mol

InChI Key

MXAYKZJJDUDWDS-LBPRGKRZSA-N

FDA UNII

71050168A2

Ixazomib is an active metabolite of MLN9708, a second generation, boron containing peptide proteasome inhibitor (PI) with potential antineoplastic activity. Ixazomib binds to and inhibits the 20S catalytic core of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome, which results in an accumulation of unwanted or misfolded proteins; disruption of various cell signaling pathways may follow, resulting in the induction of apoptosis. Compared to first generation PIs, second generation PIs may have an improved pharmacokinetic profile with increased potency and less toxicity. Proteasomes are large protease complexes that degrade unneeded or damaged proteins that have been ubiquinated.

Ixazomib is a Proteasome Inhibitor. The mechanism of action of ixazomib is as a Proteasome Inhibitor.

1 2D Structure

Ixazomib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic acid

2.1.2 InChI

InChI=1S/C14H19BCl2N2O4/c1-8(2)5-12(15(22)23)19-13(20)7-18-14(21)10-6-9(16)3-4-11(10)17/h3-4,6,8,12,22-23H,5,7H2,1-2H3,(H,18,21)(H,19,20)/t12-/m0/s1

2.1.3 InChI Key

MXAYKZJJDUDWDS-LBPRGKRZSA-N

2.1.4 Canonical SMILES

B(C(CC(C)C)NC(=O)CNC(=O)C1=C(C=CC(=C1)Cl)Cl)(O)O

2.1.5 Isomeric SMILES

B([C@H](CC(C)C)NC(=O)CNC(=O)C1=C(C=CC(=C1)Cl)Cl)(O)O

2.2 Other Identifiers

2.2.1 UNII

71050168A2

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Mln 9708

2. Mln-9708

3. Mln9708

4. Ninlaro

2.3.2 Depositor-Supplied Synonyms

1. 1072833-77-2

2. Mln2238

3. Mln-2238

4. Mln 2238

5. Ixazomib [inn]

6. (r)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic Acid

7. (r)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic Acid

8. Ixazomib (mln2238)

9. Mln-9708 Free Base

10. Chembl2141296

11. Ixazomib (usan)

12. Ixazomib [usan]

13. [(1r)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic Acid

14. [(1r)-1-{2-[(2,5-dichlorophenyl)formamido]acetamido}-3-methylbutyl]boronic Acid

15. Boronic Acid, B-((1r)-1-((2-((2,5-dichlorobenzoyl)amino)acetyl)amino)-3-methylbutyl)-

16. 71050168a2

17. Ixazomib [usan:inn]

18. Ixozamib

19. Ixazomib Impurity

20. Unii-71050168a2

21. Ixazomib(mln2238)

22. Mln2238(ixazomib)

23. Ixazomib [mi]

24. Ixazomib [who-dd]

25. Ixazomib (mln-2238)

26. Gtpl8450

27. Schembl3742758

28. Chebi:90942

29. Ex-a547

30. Dtxsid701025662

31. Amy19380

32. Bcp02410

33. Bcp24078

34. Bdbm50398609

35. Mfcd18251438

36. Nsc766907

37. S2180

38. Akos015995120

39. Zinc169946773

40. Bcp9000953

41. Ccg-264938

42. Cs-1657

43. Db09570

44. Nsc-766907

45. 1072833-77-2 (free)

46. Ncgc00249611-01

47. Ncgc00249611-03

48. Ncgc00249611-04

49. Ac-28456

50. As-55976

51. Hy-10453

52. Sw219743-1

53. J3.602.191h

54. A25328

55. D10130

56. J-001749

57. Brd-k78659596-001-01-3

58. Q20948663

59. N-[(1r)-1-borono-3-methylbutyl]-n(2)-(2,5-dichlorobenzoyl)glycinamide

60. ((1r)-1-((2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic Acid

61. (r)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic Acid;ixazomib

62. [(1r)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methyl-butyl]boronic Acid

2.4 Create Date

2009-03-16

3 Chemical and Physical Properties

Molecular Formula	C₁₄H₁₉BCl₂N₂O₄
Molecular Weight	361.0 g/mol
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	7
Exact Mass	360.0814926 g/mol
Monoisotopic Mass	360.0814926 g/mol
Topological Polar Surface Area	98.7 Å²
Heavy Atom Count	23
Formal Charge	0
Complexity	412
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
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

Ixazomib is indicated in combination with lenalidomide and dexamethasone for the treatment of patients with multiple myeloma who have received at least one prior therapy.

FDA Label

Treatment of lymphoid malignancies (excluding multiple myeloma)

5 Pharmacology and Biochemistry

5.1 Pharmacology

In vitro studies have shown ixazomib to induce apoptosis in multiple myeloma cells sensitive or resistant to other conventional therapies. In mouse xenograft models, ixazomib induced tumor growth inhibition.

5.2 MeSH Pharmacological Classification

Antineoplastic Agents

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)

Protease Inhibitors

Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES). (See all compounds classified as Protease Inhibitors.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

IXAZOMIB

5.3.2 FDA UNII

71050168A2

5.3.3 Pharmacological Classes

Proteasome Inhibitors [MoA]; Proteasome Inhibitor [EPC]

5.4 ATC Code

L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01X - Other antineoplastic agents

L01XG - Proteasome inhibitors

L01XG03 - Ixazomib

5.5 Absorption, Distribution and Excretion

Absorption

After oral administration, the time to reach maximum concentration in plasma was 1 hour. The mean absolute oral bioavailability is 58%.

Route of Elimination

62% in urine and 22% in feces.

Volume of Distribution

The steady-state volume of distribution is 543 L.

5.6 Metabolism/Metabolites

Metabolism of ixazomib is expected to be by CYP and non-CYP pathways, with no predominant CYP isozyme contribution. At higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms with estimated relative contributions of 3A4 (42%), 1A2 (26%), 2B6 (16%), 2C8 (6%), 2D6 (5%), 2C19 (5%) and 2C9 (<1%).

5.7 Biological Half-Life

Terminal half-life is 9.5 days.

5.8 Mechanism of Action

Ixazomib is an N-capped dipeptidyl leucine boronic acid which reversibly inhibits the CT-L proteolytic (5) site of the 20S proteasome. At higher concentrations, ixazomib also seems to inhibit the proteolytic 1 and 2 subunits and to induce accumulation of ubiquitinated proteins.