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Binimetinib

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1 US Medicaid Prescriptions, 2 Finished Drug Prices, 8 Annual Reports

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9 US Patents
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Synopsis

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Health Canada Patents

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Chemistry

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Also known as: 606143-89-9, Mek162, Arry-162, Mektovi, Arry-438162, Mek-162

Molecular Formula

C₁₇H₁₅BrF₂N₄O₃

Molecular Weight

441.2 g/mol

InChI Key

ACWZRVQXLIRSDF-UHFFFAOYSA-N

FDA UNII

181R97MR71

Binimetinib is an orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2 dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.

1 2D Structure

Binimetinib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

6-(4-bromo-2-fluoroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

2.1.2 InChI

InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

2.1.3 InChI Key

ACWZRVQXLIRSDF-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO

2.2 Other Identifiers

2.2.1 UNII

181R97MR71

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Mek162

2. Mektovi

2.3.2 Depositor-Supplied Synonyms

1. 606143-89-9

2. Mek162

3. Arry-162

4. Mektovi

5. Arry-438162

6. Mek-162

7. 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzimidazole-6-carboxamide

8. Arry 438162

9. Arry 162

10. Binimetinib (mek-162)

11. Nvp-mek162

12. Mek162 (arry-162, Arry-438162)

13. Mfcd22124525

14. Binimetinib (mek162, Arry-162, Arry-438162)

15. 181r97mr71

16. 6-(4-bromo-2-fluoroanilino)-7-fluoro-n-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

17. 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo[d]imidazole-6-carboxamide

18. 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo[d]imidazole-6-carboxamide.

19. 5-(4-bromo-2-fluoroanilino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzimidazole-6-carboxamide

20. Binimetinib [usan:inn]

21. Binimetinibum

22. Unii-181r97mr71

23. 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzimidazole-6-carboxamide

24. 5-(4-bromo-2-fluorophenylamino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo(d)imidazole-6-carboxamide

25. 5-(4-bromo-2-fluorophenylamino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo[d]imidazole-6-carboxamide

26. Mektovi (tn)

27. Arry-162; Arry-438162; Mek 162; Arry 162; Arry 438162

28. Binimetinib; Mek162

29. Mek162(binimetinib)

30. Binimetinib [mi]

31. Binimetinib (mek162)

32. Binimetinib [inn]

33. Binimetinib [jan]

34. Binimetinib (jan/usan)

35. Binimetinib [usan]

36. Binimetinib [who-dd]

37. Mls006011180

38. Schembl570088

39. Gtpl7921

40. Chembl3187723

41. Amy9056

42. Binimetinib [orange Book]

43. Dtxsid70209422

44. Arry-162,mek-162

45. Chebi:145371

46. Bdbm520649

47. Hms3652j14

48. Hms3747g09

49. Bcp06780

50. Ex-a1024

51. Nsc764042

52. Nsc788187

53. Nsc799361

54. S7007

55. Zinc38460704

56. Akos026750517

57. Ccg-269133

58. Cs-0627

59. Db11967

60. Nsc-764042

61. Nsc-788187

62. Nsc-799361

63. Sb16501

64. Ncgc00345804-01

65. Ncgc00345804-10

66. 1073666-70-2

67. 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methylbenzimidazole-6-carboxamide

68. 6-(4-bromo-2-fluorophenylamino)-7-fluoro-n-(2-hydroxyethoxy)-3-methyl-3h-benzo[d]imidazole-5-carboxamide

69. Ac-29023

70. As-16706

71. Da-35030

72. Hy-15202

73. Smr004702949

74. Sy284756

75. Cas:606143-89-9;mek162

76. Ft-0697088

77. Sw219910-1

78. D10604

79. Binimetinib;mek-162; Arry-162;arry-438162

80. J-516581

81. Q19903515

82. Us11147816, Binimetinib (arry-162, Arry-438162)

83. 1h-benzimidazole-6-carboxamide, 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-

84. 5-((4-bromo-2-fluorophenylamino)-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzo (d) Imidazole-6-carboxamide

85. 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-1,3-benzodiazole-6-carboxamide

86. 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-n-(2-hydroxyethoxy)-1-methyl-1h-benzimidazole-6-carboxami

87. 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3h-benzoimidazole-5-carboxylic Acid (2-hydroxyethyoxy)-amide

88. 6-[(4-bromo-2-fluorophenyl)amino]-7-fluoro-n-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

89. N-(2-hydroxyethoxy)-4-fluoro-5-(2-fluoro-4-bromophenylamino)-1-methyl-1h-benzoimidazole-6-carboxamide

90. Qo7

2.4 Create Date

2006-10-25

3 Chemical and Physical Properties

Molecular Formula	C₁₇H₁₅BrF₂N₄O₃
Molecular Weight	441.2 g/mol
XLogP3	3.1
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	6
Exact Mass	440.02956 g/mol
Monoisotopic Mass	440.02956 g/mol
Topological Polar Surface Area	88.4 Å²
Heavy Atom Count	27
Formal Charge	0
Complexity	521
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

On June 27, 2018, the Food and Drug Administration approved encorafenib and binimetinib in combination patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test.

Binimetinib in combination with encorafenib is indicated for the treatment of adult patients with unresectable or metastatic melanoma with a BRAF V600 mutation.

Treatment of colorectal carcinoma

Treatment of melanoma

5 Pharmacology and Biochemistry

5.1 Pharmacology

Binimetinib is a MEK inhibitor. MEK is an enzyme that regulates the biosynthesis of the inflammatory cytokines TNF, IL-6 and IL-1. MEK inhibitors interfere with these biosynthetic processes. It is a chemotherapeutic agent that has anti-tumor activity,.

5.2 ATC Code

L01EE03

L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EE - Mitogen-activated protein kinase (mek) inhibitors

L01EE03 - Binimetinib

5.3 Absorption, Distribution and Excretion

Absorption

Following oral administration in a pharmacokinetic study, at least 50% of the binimetinib dose was absorbed with a median time to maximum concentration (Tmax) of 1.6 hours. The administration of a single dose of MEKTOVI 45 mg with a high-fat, high-calorie meal (consisting of approximately 150 calories from protein, 350 calories from carbohydrate, and 500 calories from fat) in healthy subjects had no effect on binimetinib exposure.

Route of Elimination

Following a single oral dose of 45 mg radiolabeled binimetinib in healthy subjects, 62% (32% unchanged) of the administered dose was recovered in the feces while 31% (6.5% unchanged) was recovered in the urine.

Volume of Distribution

The geometric mean (CV%) of apparent volume of distribution of binimetinib is 92 L (45%)

Clearance

20.2 L/h (24%)

5.4 Metabolism/Metabolites

The primary metabolic pathway is glucuronidation with UGT1A1 contributing up to 61% of the binimetinib metabolism. Other pathways of binimetinib metabolism include N-dealkylation, amide hydrolysis, and loss of ethane-diol from the side chain. The active metabolite M3 produced by CYP1A2 and CYP2C19 represents 8.6% of the binimetinib exposure. Following a single oral dose of 45 mg radiolabeled binimetinib, approximately 60% of the circulating radioactivity AUC in plasma was attributable to binimetinib.

5.5 Biological Half-Life

The mean (CV%) terminal half-life (t1/2) of binimetinib is 3.5 hours (28.5%).

5.6 Mechanism of Action

Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. The inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors. This process can result in the inhibition of growth factor-mediated cell signaling. This may lead to the inhibition of tumor cell proliferation and an inhibition in the production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are themselves threonine and tyrosine kinases that possess a dual specificity. They subsequently contribute critically to the activation of the RAS/RAF/MEK/ERK pathway and are typically upregulated in a number of different tumor cell types.

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