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Synopsis

Synopsis

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Chemistry

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Also known as: 946128-88-7, Ro5126766, Ro-5126766, Ch5126766, Ro-5126766 free base, Avutometinib
Molecular Formula
C21H18FN5O5S
Molecular Weight
471.5  g/mol
InChI Key
LMMJFBMMJUMSJS-UHFFFAOYSA-N
FDA UNII
D0D4252V97

Avutometinib
Avutometinib is an orally bioavailable inhibitor of the serine/threonine protein kinases Raf and mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK), with potential antineoplastic activity. Upon oral administration, avutometinib specifically targets, binds to and inhibits the kinase activities of Raf and MEK, resulting in the inhibition of Raf/MEK-mediated signal transduction pathways. This results in the inhibition of Raf/MEK-dependent tumor cell proliferation and survival. The RAS/RAF/MEK/extracellular signal-regulated kinase (ERK) signaling pathway is often dysregulated in human cancers and plays a key role in tumor cell proliferation, differentiation and survival.
1 2D Structure

Avutometinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
3-[[3-fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one
2.1.2 InChI
InChI=1S/C21H18FN5O5S/c1-12-15-5-4-14(31-21-25-7-3-8-26-21)11-17(15)32-20(28)16(12)10-13-6-9-24-19(18(13)22)27-33(29,30)23-2/h3-9,11,23H,10H2,1-2H3,(H,24,27)
2.1.3 InChI Key
LMMJFBMMJUMSJS-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)NS(=O)(=O)NC)F
2.2 Other Identifiers
2.2.1 UNII
D0D4252V97
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Ch5126766

2. Ro5126766

2.3.2 Depositor-Supplied Synonyms

1. 946128-88-7

2. Ro5126766

3. Ro-5126766

4. Ch5126766

5. Ro-5126766 Free Base

6. Avutometinib

7. Ro 5126766

8. Ch-5126766

9. Rg-7304

10. Cki-27

11. Ro5126766(ch5126766)

12. Chebi:78825

13. Ro 5126766 - Bio-x

14. Vs-6766

15. Chembl3264002

16. Ro5126766 (ch5126766)

17. D0d4252v97

18. R-7304

19. N-(3-fluoro-4-{[4-methyl-2-oxo-7-(pyrimidin-2-yloxy)-2h-chromen-3-yl]methyl}pyridin-2-yl)-n'-methylsulfuric Diamide

20. Sulfamide, N-(3-fluoro-4-((4-methyl-2-oxo-7-(2-pyrimidinyloxy)-2h-1-benzopyran-3-yl)methyl)-2-pyridinyl)-n'-methyl-

21. 3wig

22. Chu

23. Avutometinib [inn]

24. Schembl960093

25. Unii-d0d4252v97

26. Gtpl11867

27. Bcp21067

28. Ex-a2151

29. Bdbm50010462

30. Nsc758248

31. Nsc800871

32. S7170

33. Zinc68247388

34. Akos030527032

35. Ccg-269457

36. Compound 1 [pmid: 24900832]

37. Cs-5254

38. Db15254

39. Nsc-758248

40. Nsc-800871

41. Sb16628

42. Ro 5126766 [who-dd]

43. Ac-35949

44. Da-40233

45. Hy-18652

46. Ch 5126766

47. Ft-0737411

48. A916428

49. Ro5126766; Ch5126766

50. Q27147976

51. Ro 5126766; Ro5126766; Ch5126766; Ch5126766; Ch 5126766

52. 3-[(2-((n-methylsulfamoyl)amino)-3-fluoropyridin-4-yl)methyl]-4-methyl-7-(pyrimidin-2-yloxy)-chromen-2-one

53. 3-[[3-fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one

54. N-(3-fluoro-4-((4-methyl-2-oxo-7-(pyrimidin-2-yloxy)-2h-chromen-3-yl)methyl)pyridin-2-yl)-n'-methylsulfamide

2.4 Create Date
2007-08-27
3 Chemical and Physical Properties
Molecular Weight 471.5 g/mol
Molecular Formula C21H18FN5O5S
XLogP32
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count11
Rotatable Bond Count7
Exact Mass471.10126803 g/mol
Monoisotopic Mass471.10126803 g/mol
Topological Polar Surface Area141 Ų
Heavy Atom Count33
Formal Charge0
Complexity845
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

Drugs in Development

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Details:

Avutometinib is a Miscellaneous drug candidate, which is currently being evaluated in Phase I clinical studies for the treatment of Endometrial Neoplasms.


Lead Product(s): Verastem Oncology,Avutometinib,Defactinib,16719221,Everolimus,Approved API

Therapeutic Area: Oncology Brand Name: Undisclosed

Study Phase: Phase IProduct Type: Miscellaneous

Sponsor: Verastem Oncology

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable January 06, 2026

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01

BePharma
Not Confirmed
BePharma
Not Confirmed

Details : Avutometinib is a Miscellaneous drug candidate, which is currently being evaluated in Phase I clinical studies for the treatment of Endometrial Neoplasms.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Inapplicable

January 06, 2026

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Details:

The proceeds from the offering will be used to fund the clinical development of Avutometinib for KRAS-mutated recurrent Low-Grade Serous Ovarian Cancer.


Lead Product(s): Avutometinib,Defactinib

Therapeutic Area: Oncology Brand Name: Avmapkitm Fakzynjatm Co-Pack

Study Phase: Approved FDFProduct Type: Miscellaneous

Sponsor: Jefferies | Guggenheim Securities | Cantor

Deal Size: $90.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering November 14, 2025

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BePharma
Not Confirmed
BePharma
Not Confirmed

Lead Product(s) : Avutometinib,Defactinib

Therapeutic Area : Oncology

Highest Development Status : Approved FDF

Partner/Sponsor/Collaborator : Jefferies | Guggenheim Securities | Cantor

Deal Size : $90.0 million

Deal Type : Public Offering

Details : The proceeds from the offering will be used to fund the clinical development of Avutometinib for KRAS-mutated recurrent Low-Grade Serous Ovarian Cancer.

Product Name : Avmapkitm Fakzynjatm Co-Pack

Product Type : Miscellaneous

Upfront Cash : Undisclosed

November 14, 2025

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Details:

The proceeds from the offering will be used to fund the clinical development of Avutometinib for KRAS-mutated recurrent Low-Grade Serous Ovarian Cancer.


Lead Product(s): Avutometinib,Defactinib

Therapeutic Area: Oncology Brand Name: Avmapkitm Fakzynjatm Co-Pack

Study Phase: Approved FDFProduct Type: Miscellaneous

Sponsor: Jefferies | Guggenheim Securities | Cantor

Deal Size: Undisclosed Upfront Cash: Undisclosed

Deal Type: Public Offering November 13, 2025

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03

BePharma
Not Confirmed
BePharma
Not Confirmed

Lead Product(s) : Avutometinib,Defactinib

Therapeutic Area : Oncology

Highest Development Status : Approved FDF

Partner/Sponsor/Collaborator : Jefferies | Guggenheim Securities | Cantor

Deal Size : Undisclosed

Deal Type : Public Offering

Details : The proceeds from the offering will be used to fund the clinical development of Avutometinib for KRAS-mutated recurrent Low-Grade Serous Ovarian Cancer.

Product Name : Avmapkitm Fakzynjatm Co-Pack

Product Type : Miscellaneous

Upfront Cash : Undisclosed

November 13, 2025

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Details:

Defactinib is a Other Small Molecule drug candidate, which is currently being evaluated in Phase II clinical studies for the treatment of Pancreatic Neoplasms.


Lead Product(s): Defactinib,Avutometinib

Therapeutic Area: Oncology Brand Name: Undisclosed

Study Phase: Phase IIProduct Type: Miscellaneous

Sponsor: Verastem Oncology | Foundation for Barnes-Jewish Hospital

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable August 17, 2025

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BePharma
Not Confirmed
BePharma
Not Confirmed

Lead Product(s) : Defactinib,Avutometinib

Therapeutic Area : Oncology

Highest Development Status : Phase II

Partner/Sponsor/Collaborator : Verastem Oncology | Foundation for Barnes-Jewish Hospital

Deal Size : Inapplicable

Deal Type : Inapplicable

Details : Defactinib is a Other Small Molecule drug candidate, which is currently being evaluated in Phase II clinical studies for the treatment of Pancreatic Neoplasms.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Inapplicable

August 17, 2025

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Details:

Through the collaboration, Tempus completed testing in Verastem’s trial, which evaluated the combination of VS-6766 (avutometinib) and defactinib to treat recurrent low-grade serous ovarian cancer.


Lead Product(s): Avutometinib,Defactinib

Therapeutic Area: Oncology Brand Name: Undisclosed

Study Phase: Phase IIProduct Type: Miscellaneous

Sponsor: Verastem Oncology

Deal Size: Undisclosed Upfront Cash: Undisclosed

Deal Type: Collaboration May 20, 2025

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Tempus

U.S.A
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BePharma
Not Confirmed

Tempus

U.S.A
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BePharma
Not Confirmed

Details : Through the collaboration, Tempus completed testing in Verastem’s trial, which evaluated the combination of VS-6766 (avutometinib) and defactinib to treat recurrent low-grade serous ovarian cancer.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Undisclosed

May 20, 2025

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Details:

Avmapki Fakzynja Co-Pack, a combination of avutometinib and defactinib, each kinase inhibitors, is indicated for the treatment of adult patients with KRAS-mutated recurrent LGSOC.


Lead Product(s): Avutometinib,Defactinib

Therapeutic Area: Oncology Brand Name: Avmapki Fakzynja Co-Pack

Study Phase: Approved FDFProduct Type: Miscellaneous

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable May 08, 2025

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06

BePharma
Not Confirmed
BePharma
Not Confirmed

Details : Avmapki Fakzynja Co-Pack, a combination of avutometinib and defactinib, each kinase inhibitors, is indicated for the treatment of adult patients with KRAS-mutated recurrent LGSOC.

Product Name : Avmapki Fakzynja Co-Pack

Product Type : Miscellaneous

Upfront Cash : Inapplicable

May 08, 2025

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Details:

The proceeds from the financing are expected to fund the potential launch of VS-6766 (avutometinib) and defactinib in recurrent low-grade serous ovarian cancer.


Lead Product(s): Avutometinib,Defactinib

Therapeutic Area: Oncology Brand Name: Undisclosed

Study Phase: Phase IIIProduct Type: Miscellaneous

Sponsor: RTW Investments

Deal Size: $75.0 million Upfront Cash: Undisclosed

Deal Type: Private Placement April 25, 2025

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BePharma
Not Confirmed
BePharma
Not Confirmed

Details : The proceeds from the financing are expected to fund the potential launch of VS-6766 (avutometinib) and defactinib in recurrent low-grade serous ovarian cancer.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Undisclosed

April 25, 2025

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Details:

The financing aims to advance the clinical development of company's lead product, VS-6766 (Avutometinib) plus defactinib. It is being evaluated for the KRAS mutant low-grade serous ovarian cancer.


Lead Product(s): Avutometinib,Defactinib

Therapeutic Area: Oncology Brand Name: Undisclosed

Study Phase: Phase IIIProduct Type: Miscellaneous

Sponsor: Oberland Capital Management

Deal Size: $157.5 million Upfront Cash: Undisclosed

Deal Type: Financing January 13, 2025

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BePharma
Not Confirmed
BePharma
Not Confirmed

Details : The financing aims to advance the clinical development of company's lead product, VS-6766 (Avutometinib) plus defactinib. It is being evaluated for the KRAS mutant low-grade serous ovarian cancer.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Undisclosed

January 13, 2025

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Details:

Combination of avutometinib, a RAF/MEK clamp, and defactinib, a selective FAK inhibitor, being development for adults with recurrent KRAS mutant low-grade serous ovarian cancer.


Lead Product(s): Avutometinib,Defactinib

Therapeutic Area: Oncology Brand Name: Undisclosed

Study Phase: Phase IIIProduct Type: Miscellaneous

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable December 30, 2024

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09

BePharma
Not Confirmed
BePharma
Not Confirmed

Details : Combination of avutometinib, a RAF/MEK clamp, and defactinib, a selective FAK inhibitor, being development for adults with recurrent KRAS mutant low-grade serous ovarian cancer.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Inapplicable

December 30, 2024

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Details:

Combination of avutometinib, a RAF/MEK clamp with sotorasib & defactinib, , being developed for the treatment of KRAS G12C mutant non-small cell lung cancer.


Lead Product(s): Avutometinib,Defactinib,Sotorasib

Therapeutic Area: Oncology Brand Name: Undisclosed

Study Phase: Phase IIIProduct Type: Miscellaneous

Sponsor: Undisclosed

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable December 18, 2024

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BePharma
Not Confirmed
BePharma
Not Confirmed

Details : Combination of avutometinib, a RAF/MEK clamp with sotorasib & defactinib, , being developed for the treatment of KRAS G12C mutant non-small cell lung cancer.

Product Name : Undisclosed

Product Type : Miscellaneous

Upfront Cash : Inapplicable

December 18, 2024

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FDF Dossiers

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BePharma
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AVUTOMETINIB POTASSIUM; DEFACTINIB HYDROCHLORIDE

Brand Name : AVMAPKI FAKZYNJA CO-PACK (COPACKAGED)

Dosage Form : CAPSULE, TABLET;ORAL

Dosage Strength : EQ 0.8MG BASE;EQ 200MG BASE

Packaging :

Approval Date : 2025-05-08

Application Number : 219616

Regulatory Info : RX

Registration Country : USA

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FDA Orange Book

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VERASTEM INC

U.S.A
BePharma
Not Confirmed
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VERASTEM INC

U.S.A
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BePharma
Not Confirmed

AVUTOMETINIB POTASSIUM; DEFACTINIB HYDROCHLORIDE

Brand Name : AVMAPKI FAKZYNJA CO-PACK (COPACKAGED)

Dosage Form : CAPSULE, TABLET;ORAL

Dosage Strength : EQ 0.8MG BASE;EQ 200MG BASE

Approval Date : 2025-05-08

Application Number : 219616

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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ABOUT THIS PAGE

Looking for 946128-88-7 / Avutometinib API manufacturers, exporters & distributors?

Avutometinib manufacturers, exporters & distributors 1

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PharmaCompass offers a list of Avutometinib 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 Avutometinib manufacturer or Avutometinib supplier for your needs.

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

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

API | Excipient name

Avutometinib

Synonyms

946128-88-7, Ro5126766, Ro-5126766, Ch5126766, Ro-5126766 free base, Ro 5126766

Cas Number

946128-88-7

Unique Ingredient Identifier (UNII)

D0D4252V97

About Avutometinib

Avutometinib is an orally bioavailable inhibitor of the serine/threonine protein kinases Raf and mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK), with potential antineoplastic activity. Upon oral administration, avutometinib specifically targets, binds to and inhibits the kinase activities of Raf and MEK, resulting in the inhibition of Raf/MEK-mediated signal transduction pathways. This results in the inhibition of Raf/MEK-dependent tumor cell proliferation and survival. The RAS/RAF/MEK/extracellular signal-regulated kinase (ERK) signaling pathway is often dysregulated in human cancers and plays a key role in tumor cell proliferation, differentiation and survival.

Avutometinib Manufacturers

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

Avutometinib Suppliers

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

Avutometinib GMP

Avutometinib 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 Avutometinib 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 Avutometinib GMP manufacturer or Avutometinib GMP API supplier for your needs.

Avutometinib CoA

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

Avutometinib CoA mostly includes findings from lab analyses of a specific batch. For each Avutometinib 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.

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