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Also known as: 1029712-80-8, Incb28060, Inc280, Inc-280, Nvp-inc280-nx, Incb-28060
Molecular Formula
C23H17FN6O
Molecular Weight
412.4  g/mol
InChI Key
LIOLIMKSCNQPLV-UHFFFAOYSA-N
FDA UNII
TY34L4F9OZ

Capmatinib
Capmatinib is an orally bioavailable inhibitor of the proto-oncogene c-Met (also known as hepatocyte growth factor receptor (HGFR)) with potential antineoplastic activity. Capmatinib selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.
Capmatinib is a Kinase Inhibitor. The mechanism of action of capmatinib is as a Mesenchymal Epithelial Transition Inhibitor, and Cytochrome P450 1A2 Inhibitor, and P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor, and Multidrug and Toxin Extrusion Transporter 1 Inhibitor, and Multidrug and Toxin Extrusion Transporter 2 K Inhibitor.
1 2D Structure

Capmatinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
2.1.2 InChI
InChI=1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)
2.1.3 InChI Key
LIOLIMKSCNQPLV-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F
2.2 Other Identifiers
2.2.1 UNII
TY34L4F9OZ
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 2-fluoro-4-(7-((quinolin-6-yl)methyl)imidazo(1,2-b)(1,2,4)triazin-2-yl)benzoic Acid

2. 2-fluoro-4-(7-((quinolin-6-yl)methyl)imidazo(1,2-b)-(1,2,4)triazin-2-yl)benzamide

3. 2-fluoro-n-methyl-4-(7-((quinolin-6-yl)methyl)imidazo(1,2- B)(1,2,4)triazin-2-yl)benzamide Dihydrochloride Monohydrate

4. 2-fluoro-n-methyl-4-(7-(quinolin-6-yl-methyl)imidazo(1,2-b)(1,2,4)triazin-2-yl)benzamide

5. 2-fluoro-n-methyl-4-(7-(quinolin-6-ylmethyl)imidazo(1,2-b)(1,2,4)triazin-2-yl)benzamide

6. 2-fluoro-n-methyl-4-(7-(quinolin-6-ylmethyl)imidazo(1,2-b)(1,2,4)triazin-2-yl)benzamide Dihydrochloride

7. Capmatinib Dihydrochloride

8. Capmatinib Dihydrochloride Monohydrate

9. Capmatinib Hydrochloride

10. Capmatinib Hydrochloride Anhydrous

11. Capmatinib Metabolite M13

12. Capmatinib Metabolite M18

13. Cmc-583

14. Cmc583

15. Cnj-294

16. Cnj294

17. Inc-280

18. Inc280

19. Incb-28060

20. Incb-28060 Free Base

21. Incb28060

22. Nvp-inc280

23. Nvp-inc280-nx

24. Tabrecta

2.3.2 Depositor-Supplied Synonyms

1. 1029712-80-8

2. Incb28060

3. Inc280

4. Inc-280

5. Nvp-inc280-nx

6. Incb-28060

7. Nvp-inc280

8. 2-fluoro-n-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide

9. Tabrecta

10. Capmatinib (incb28060)

11. Capmatinib [usan]

12. Incb-28060 Free Base

13. Inc28060

14. 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide

15. Ty34l4f9oz

16. Incb 28060

17. Benzamide, 2-fluoro-n-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]-

18. 2-fluoro-n-methyl-4-(7-(quinolin-6-ylmethyl)imidazo(1,2-b)(1,2,4)triazin-2-yl)benzamide

19. Benzamide, 2-fluoro-n-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]-;benzamide, 2-fluoro-n-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]-

20. Capmatinib [inn]

21. Unii-ty34l4f9oz

22. Benzamide Hcl

23. Benzamide, 2-fluoro-n-methyl-4-(7-(6-quinolinylmethyl)imidazo(1,2-b)(1,2,4)triazin-2-yl)-

24. Capmatinib [mi]

25. Capmatinib (usan/inn)

26. Capmatinib [usan:inn]

27. Capmatinib(incb28060)

28. Incb28060(capmatinib)

29. Nyp-inc280-nx

30. Capmatinib [who-dd]

31. Mls006010965

32. Gtpl7904

33. Schembl1426819

34. Chembl3188267

35. Dtxsid90145595

36. Ex-a446

37. Amy18553

38. Bcp23444

39. Bdbm50146167

40. Mfcd18633285

41. Nsc777878

42. Nsc800067

43. S2788

44. Zinc43195321

45. Akos025396439

46. Bcp9000785

47. Ccg-268791

48. Cs-1541

49. Db11791

50. Nsc-777878

51. Nsc-800067

52. Sb16608

53. Ncgc00346702-01

54. Ncgc00346702-02

55. Ncgc00346702-05

56. Ac-25890

57. As-74142

58. Da-33530

59. Hy-13404

60. Smr004702769

61. Ft-0746310

62. D10696

63. J-509516

64. Q27075685

65. 2-fluoro-n-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2- Yl)benzamide

66. 2-fluoro-n-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide

67. 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazolo[1,2-b][1,2,4]triazin-2-yl]benzamide

68. 2-fluoro-n-methyl-4-{7-[(quinolin-6-yl)methyl]imidazo[1,2-b][1,2,4]triazin-2-yl}benzamide

2.4 Create Date
2009-02-09
3 Chemical and Physical Properties
Molecular Weight 412.4 g/mol
Molecular Formula C23H17FN6O
XLogP32.9
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count6
Rotatable Bond Count4
Exact Mass412.14478735 g/mol
Monoisotopic Mass412.14478735 g/mol
Topological Polar Surface Area85.1 Ų
Heavy Atom Count31
Formal Charge0
Complexity637
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Capmatinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping as detected by an FDA-approved test.


FDA Label


Tabrecta as monotherapy is indicated for the treatment of adult patients with advanced non small cell lung cancer (NSCLC) harbouring alterations leading to mesenchymal epithelial transition factor gene exon 14 (METex14) skipping, who require systemic therapy following prior treatment with immunotherapy and/or platinum based chemotherapy.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Capmatinib inhibits the overactivity of c-Met, a receptor tyrosine kinase encoded by the _MET_ proto-oncogene. Mutations in _MET_ are involved in the proliferation of many cancers, including non-small cell lung cancer (NSCLC). Capmatinib may cause photosensitivity reactions in patients following ultraviolet (UV) exposure - patients undergoing therapy with capmatinib should be advised to use sunscreen and protective clothing to limit exposure to UV radiation. Instances of interstitial lung disease/pneumonitis, which can be fatal, occurred in patients being treated with capmatinib. Patients presenting with signs or symptoms of lung disease (e.g. cough, dyspnea, fever) should have capmatinib immediately withheld, and capmatinib should be permanently discontinued if no other feasible causes of the lung-related symptoms are identified.


5.2 FDA Pharmacological Classification
5.2.1 Active Moiety
CAPMATINIB
5.2.2 FDA UNII
TY34L4F9OZ
5.2.3 Pharmacological Classes
Cytochrome P450 1A2 Inhibitors [MoA]; Kinase Inhibitor [EPC]; Mesenchymal Epithelial Transition Inhibitors [MoA]; Multidrug and Toxin Extrusion Transporter 1 Inhibitors [MoA]; Multidrug and Toxin Extrusion Transporter 2 K Inhibitors [MoA]; P-Glycoprotein Inhibitors [MoA]; Breast Cancer Resistance Protein Inhibitors [MoA]
5.3 ATC Code

L01EX17


L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EX - Other protein kinase inhibitors

L01EX17 - Capmatinib


5.4 Absorption, Distribution and Excretion

Absorption

The oral bioavailability of capmatinib is estimated to be >70%. Following oral administration, maximum plasma concentrations are achieved within 1 to 2 hours (Tmax). Co-administration with a high-fat meal increased capmatinib AUC by 46% with no change in Cmax (as compared to fasted conditions), and co-administration with a low-fat meal had no clinically meaningful effects on exposure.


Route of Elimination

Following oral administration of radiolabeled capmatinib, approximately 78% of the radioactivity is recovered in feces, of which ~42% is unchanged parent drug, and 22% is recovered in the urine, of which a negligible amount remains unchanged parent drug.


Volume of Distribution

The apparent volume of distribution at steady-state is 164 L.


Clearance

The mean apparent clearance of capmatinib at steady-state is 24 L/h.


5.5 Metabolism/Metabolites

Capmatinib undergoes metabolism primarily via CYP3A4 and aldehyde oxidase. Specific biotransformation pathways and metabolic products have yet to be elucidated.


5.6 Biological Half-Life

The elimination half-life is 6.5 hours.


5.7 Mechanism of Action

Aberrant activation of c-Met has been documented in many cancers, including non-small cell lung cancer (NSCLC). Mutations that result in the skipping of _MET_ exon 14 lead to the formation of a mutant c-Met with a missing regulatory domain - these mutant proteins have a reduced ability to negatively regulate, leading to a pathological increase in their downstream activity. Capmatinib inhibits the phosphorylation of both wild-type and mutant variants of c-Met triggered by the binding of its endogenous ligand, hepatocyte growth factor - in doing so, it prevents c-Met-mediated phosphorylation of downstream signaling proteins, as well as the proliferation and survival of c-Met-dependent tumor cells.


API Reference Price

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11-Feb-2023
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Looking for 1029712-80-8 / Capmatinib API manufacturers, exporters & distributors?

Capmatinib manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Capmatinib API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Capmatinib manufacturer or Capmatinib supplier for your needs.

Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Capmatinib manufacturer or Capmatinib supplier.

PharmaCompass also assists you with knowing the Capmatinib API Price utilized in the formulation of products. Capmatinib API Price is not always fixed or binding as the Capmatinib Price is obtained through a variety of data sources. The Capmatinib Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

API | Excipient name

Capmatinib

Synonyms

1029712-80-8, Incb28060, Inc280, Inc-280, Nvp-inc280-nx, Incb-28060

Cas Number

1029712-80-8

Unique Ingredient Identifier (UNII)

TY34L4F9OZ

About Capmatinib

Capmatinib is an orally bioavailable inhibitor of the proto-oncogene c-Met (also known as hepatocyte growth factor receptor (HGFR)) with potential antineoplastic activity. Capmatinib selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.

Capmatinib Manufacturers

A Capmatinib manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Capmatinib, including repackagers and relabelers. The FDA regulates Capmatinib manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Capmatinib API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of Capmatinib manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

Capmatinib Suppliers

A Capmatinib supplier is an individual or a company that provides Capmatinib active pharmaceutical ingredient (API) or Capmatinib finished formulations upon request. The Capmatinib suppliers may include Capmatinib API manufacturers, exporters, distributors and traders.

click here to find a list of Capmatinib suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Capmatinib GMP

Capmatinib Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Capmatinib GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Capmatinib GMP manufacturer or Capmatinib GMP API supplier for your needs.

Capmatinib CoA

A Capmatinib CoA (Certificate of Analysis) is a formal document that attests to Capmatinib's compliance with Capmatinib specifications and serves as a tool for batch-level quality control.

Capmatinib CoA mostly includes findings from lab analyses of a specific batch. For each Capmatinib CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Capmatinib may be tested according to a variety of international standards, such as European Pharmacopoeia (Capmatinib EP), Capmatinib JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Capmatinib USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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