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Chemistry

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Also known as: 1869057-83-9, Furmonertinib, Ast2818, Ast-2818, A49a7a5yn4, Ivesa
Molecular Formula
C28H31F3N8O2
Molecular Weight
568.6  g/mol
InChI Key
GHKOONMJXNWOIW-UHFFFAOYSA-N
FDA UNII
A49A7A5YN4

Furmonertinib
Alflutinib is an orally available selective inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. Upon administration, alflutinib specifically binds to and inhibits the tyrosine kinase activity of EGFR T790M, a secondarily acquired resistance mutation. This prevents EGFR T790M-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells. EGFR, a receptor tyrosine kinase that is mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. Compared to some other EGFR inhibitors, alflutinib may have therapeutic benefits in tumors with T790M-mediated drug resistance.
1 2D Structure

Furmonertinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[2-[2-(dimethylamino)ethyl-methylamino]-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-6-(2,2,2-trifluoroethoxy)pyridin-3-yl]prop-2-enamide
2.1.2 InChI
InChI=1S/C28H31F3N8O2/c1-6-24(40)33-21-15-22(26(41-17-28(29,30)31)36-25(21)38(4)14-13-37(2)3)35-27-32-12-11-20(34-27)19-16-39(5)23-10-8-7-9-18(19)23/h6-12,15-16H,1,13-14,17H2,2-5H3,(H,33,40)(H,32,34,35)
2.1.3 InChI Key
GHKOONMJXNWOIW-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(N=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OCC(F)(F)F
2.2 Other Identifiers
2.2.1 UNII
A49A7A5YN4
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Aflutinib

2. Ast2818

3. Furmonertinib

4. Furmonertinib Mesylate

5. Ivesa

6. N-(2-(2-(dimethylamino)ethyl-methylamino)-5-((4-(1-methylindol-3-yl)pyrimidin-2-yl)amino)-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)prop-2-enamide

2.3.2 Depositor-Supplied Synonyms

1. 1869057-83-9

2. Furmonertinib

3. Ast2818

4. Ast-2818

5. A49a7a5yn4

6. Ivesa

7. N-[2-[2-(dimethylamino)ethyl-methylamino]-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-6-(2,2,2-trifluoroethoxy)pyridin-3-yl]prop-2-enamide

8. N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)acrylamide

9. 2-propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-5-((4-(1-methyl-1h-indol-3-yl)-2-pyrimidinyl)amino)-6-(2,2,2-trifluoroethoxy)-3-pyridinyl)-

10. Aflutinib

11. N-(2-(2-(dimethylamino)ethyl-methylamino)-5-((4-(1-methylindol-3-yl)pyrimidin-2-yl)amino)-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)prop-2-enamide

12. Alflutinib (pseudo Inn)

13. Unii-a49a7a5yn4

14. Furmonertinib [who-dd]

15. Chembl4297258

16. Schembl17490447

17. Gtpl10477

18. Bcp30339

19. Example 3 [us10072002b2]

20. Ex-a2868-1

21. Ac-36862

22. Hy-112870

23. Alflutinib;ast-2818;ast 2818;ask120067;ask 120067;ask-120067

2.4 Create Date
2016-04-09
3 Chemical and Physical Properties
Molecular Weight 568.6 g/mol
Molecular Formula C28H31F3N8O2
XLogP34.4
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count11
Rotatable Bond Count11
Exact Mass g/mol
Monoisotopic Mass g/mol
Topological Polar Surface Area100
Heavy Atom Count41
Formal Charge0
Complexity865
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Pharmacology and Biochemistry
4.1 MeSH Pharmacological Classification

Protein Kinase Inhibitors

Agents that inhibit PROTEIN KINASES. (See all compounds classified as Protein Kinase Inhibitors.)


Drugs in Development

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Details:

ICP-189 is a potent and selective oral allosteric inhibitor of SHP2, which is being evaluated in combiation with furmonertinib for the treatment of advanced or metastatic non-small cell lung cancer.


Lead Product(s): ICP-189,Furmonertinib

Therapeutic Area: Oncology Brand Name: ICP-189

Study Phase: Phase IProduct Type: Other Small Molecule

Sponsor: Inapplicable

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable March 28, 2024

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01

AACR Annual meeting
Not Confirmed
AACR Annual meeting
Not Confirmed

Details : ICP-189 is a potent and selective oral allosteric inhibitor of SHP2, which is being evaluated in combiation with furmonertinib for the treatment of advanced or metastatic non-small cell lung cancer.

Product Name : ICP-189

Product Type : Other Small Molecule

Upfront Cash : Inapplicable

March 28, 2024

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Details:

Proceeds will support NDA approval for furmonertinib, a novel oral EGFR kinase inhibitor with broad activity across EGFR mutations.


Lead Product(s): Furmonertinib

Therapeutic Area: Oncology Brand Name: AST2818

Study Phase: Phase IIIProduct Type: Other Small Molecule

Sponsor: Goldman Sachs & Co

Deal Size: $175.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering January 25, 2024

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02

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Details : Proceeds will support NDA approval for furmonertinib, a novel oral EGFR kinase inhibitor with broad activity across EGFR mutations.

Product Name : AST2818

Product Type : Other Small Molecule

Upfront Cash : Undisclosed

January 25, 2024

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Details:

The net proceeds will be used for the clinical development of (furmonertinib), which focuses on EGFR mutant-selective tyrosine kinase inhibitors that are developed for NSCLC patients.


Lead Product(s): Furmonertinib

Therapeutic Area: Oncology Brand Name: AST2818

Study Phase: Phase IIIProduct Type: Other Small Molecule

Sponsor: Goldman Sachs & Co

Deal Size: $135.7 million Upfront Cash: Undisclosed

Deal Type: Public Offering January 22, 2024

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03

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Details : The net proceeds will be used for the clinical development of (furmonertinib), which focuses on EGFR mutant-selective tyrosine kinase inhibitors that are developed for NSCLC patients.

Product Name : AST2818

Product Type : Other Small Molecule

Upfront Cash : Undisclosed

January 22, 2024

blank

Details:

AST2818 (furmonertinib) is an oral, small molecule, highly brain-penetrant, pan-EGFR mutant inhibitor that targets both classical (exon 19 deletion and L858R) and atypical EGFR mutations, including exon 20 insertion mutations as well as HER2 exon 20 insertion mutations.


Lead Product(s): Furmonertinib

Therapeutic Area: Oncology Brand Name: AST2818

Study Phase: Phase IIIProduct Type: Other Small Molecule

Sponsor: Inapplicable

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable October 30, 2023

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04

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Details : AST2818 (furmonertinib) is an oral, small molecule, highly brain-penetrant, pan-EGFR mutant inhibitor that targets both classical (exon 19 deletion and L858R) and atypical EGFR mutations, including exon 20 insertion mutations as well as HER2 exon 20 inse...

Product Name : AST2818

Product Type : Other Small Molecule

Upfront Cash : Inapplicable

October 30, 2023

blank

Details:

ICP-189 is a potent and selective oral allosteric inhibitor of SHP2, developed by InnoCare for the treatment of solid tumors as a single agent and/or in combination in combination with furmonertinib, a highly brain-penetrant, broadly active mutation-selective EGFR inhibitor.


Lead Product(s): ICP-189,Furmonertinib

Therapeutic Area: Oncology Brand Name: ICP-189

Study Phase: IND EnablingProduct Type: Other Small Molecule

Sponsor: Inapplicable

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable September 13, 2023

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05

AACR Annual meeting
Not Confirmed
AACR Annual meeting
Not Confirmed

Details : ICP-189 is a potent and selective oral allosteric inhibitor of SHP2, developed by InnoCare for the treatment of solid tumors as a single agent and/or in combination in combination with furmonertinib, a highly brain-penetrant, broadly active mutation-sele...

Product Name : ICP-189

Product Type : Other Small Molecule

Upfront Cash : Inapplicable

September 13, 2023

blank

Details:

Under the agreement, InnoCare and ArriVent will jointly evaluate the anti-tumor activity and safety of ICP-189, a novel SHP2 allosteric inhibitor, combined with furmonertinib, a highly brain-penetrant, broadly active mutation-selective EGFR inhibitor, in advanced NSCLC.


Lead Product(s): ICP-189,Furmonertinib

Therapeutic Area: Oncology Brand Name: ICP-189

Study Phase: IND EnablingProduct Type: Other Small Molecule

Sponsor: Arrivent

Deal Size: Undisclosed Upfront Cash: Undisclosed

Deal Type: Collaboration July 13, 2023

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06

AACR Annual meeting
Not Confirmed
AACR Annual meeting
Not Confirmed

Details : Under the agreement, InnoCare and ArriVent will jointly evaluate the anti-tumor activity and safety of ICP-189, a novel SHP2 allosteric inhibitor, combined with furmonertinib, a highly brain-penetrant, broadly active mutation-selective EGFR inhibitor, in...

Product Name : ICP-189

Product Type : Other Small Molecule

Upfront Cash : Undisclosed

July 13, 2023

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Details:

The net proceedings will be used to support pivotal Phase 3 and additional studies with the Company’s lead product candidate AST2818 (furmonertinib), a highly brain penetrant, mutant-specific EGFR kinase inhibitor.


Lead Product(s): Furmonertinib

Therapeutic Area: Oncology Brand Name: AST2818

Study Phase: Phase IIIProduct Type: Other Small Molecule

Sponsor: Sofinnova Investments

Deal Size: $155.0 million Upfront Cash: Undisclosed

Deal Type: Series B Financing March 27, 2023

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07

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Lead Product(s) : Furmonertinib

Therapeutic Area : Oncology

Highest Development Status : Phase III

Partner/Sponsor/Collaborator : Sofinnova Investments

Deal Size : $155.0 million

Deal Type : Series B Financing

Details : The net proceedings will be used to support pivotal Phase 3 and additional studies with the Company’s lead product candidate AST2818 (furmonertinib), a highly brain penetrant, mutant-specific EGFR kinase inhibitor.

Product Name : AST2818

Product Type : Other Small Molecule

Upfront Cash : Undisclosed

March 27, 2023

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Details:

The licensed small-molecule antagonist of EGFR ABK3376 is a pre-clinical candidate developed by Abbisko Therapeutics' proprietary drug discovery platform, which is a novel, highly potent, selective, and brain-penetrating new-generation EGFR inhibitor.


Lead Product(s): ABK3376,Furmonertinib

Therapeutic Area: Oncology Brand Name: ABK3376

Study Phase: PreclinicalProduct Type: Other Small Molecule

Sponsor: Shanghai Allist Pharmaceuticals

Deal Size: $187.9 million Upfront Cash: Undisclosed

Deal Type: Licensing Agreement January 03, 2023

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08

AACR Annual meeting
Not Confirmed
AACR Annual meeting
Not Confirmed

Lead Product(s) : ABK3376,Furmonertinib

Therapeutic Area : Oncology

Highest Development Status : Preclinical

Partner/Sponsor/Collaborator : Shanghai Allist Pharmaceuticals

Deal Size : $187.9 million

Deal Type : Licensing Agreement

Details : The licensed small-molecule antagonist of EGFR ABK3376 is a pre-clinical candidate developed by Abbisko Therapeutics' proprietary drug discovery platform, which is a novel, highly potent, selective, and brain-penetrating new-generation EGFR inhibitor.

Product Name : ABK3376

Product Type : Other Small Molecule

Upfront Cash : Undisclosed

January 03, 2023

blank

Details:

AST2818 (furmonertinib) is an oral, small molecule, highly brain-penetrant, pan-EGFR mutant inhibitor that targets both classical (exon 19 deletion and L858R) and atypical EGFR mutations, including exon 20 insertion mutations as well as HER2 exon 20 insertion mutations.


Lead Product(s): Furmonertinib

Therapeutic Area: Oncology Brand Name: AST2818

Study Phase: Phase IIIProduct Type: Other Small Molecule

Sponsor: Inapplicable

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable May 07, 2022

blank

09

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Details : AST2818 (furmonertinib) is an oral, small molecule, highly brain-penetrant, pan-EGFR mutant inhibitor that targets both classical (exon 19 deletion and L858R) and atypical EGFR mutations, including exon 20 insertion mutations as well as HER2 exon 20 inse...

Product Name : AST2818

Product Type : Other Small Molecule

Upfront Cash : Inapplicable

May 07, 2022

blank

Details:

Allist Pharma received approval for furmonertinib in EGFR T790M mutation-positive locally advanced or metastatic non-small-cell lung cancer (NSCLC) indications in China in March 2021.


Lead Product(s): Furmonertinib

Therapeutic Area: Oncology Brand Name: AST2818

Study Phase: Approved FDFProduct Type: Other Small Molecule

Sponsor: Hillhouse Capital Group

Deal Size: $150.0 million Upfront Cash: Undisclosed

Deal Type: Series A Financing June 30, 2021

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10

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Arrivent

U.S.A
arrow
AACR Annual meeting
Not Confirmed

Lead Product(s) : Furmonertinib

Therapeutic Area : Oncology

Highest Development Status : Approved FDF

Partner/Sponsor/Collaborator : Hillhouse Capital Group

Deal Size : $150.0 million

Deal Type : Series A Financing

Details : Allist Pharma received approval for furmonertinib in EGFR T790M mutation-positive locally advanced or metastatic non-small-cell lung cancer (NSCLC) indications in China in March 2021.

Product Name : AST2818

Product Type : Other Small Molecule

Upfront Cash : Undisclosed

June 30, 2021

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Looking for 1869057-83-9 / Furmonertinib API manufacturers, exporters & distributors?

Furmonertinib manufacturers, exporters & distributors 1

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

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

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

API | Excipient name

Furmonertinib

Synonyms

1869057-83-9, Ast2818, Ast-2818, A49a7a5yn4, Ivesa, N-[2-[2-(dimethylamino)ethyl-methylamino]-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]-6-(2,2,2-trifluoroethoxy)pyridin-3-yl]prop-2-enamide

Cas Number

1869057-83-9

Unique Ingredient Identifier (UNII)

A49A7A5YN4

About Furmonertinib

Alflutinib is an orally available selective inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. Upon administration, alflutinib specifically binds to and inhibits the tyrosine kinase activity of EGFR T790M, a secondarily acquired resistance mutation. This prevents EGFR T790M-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells. EGFR, a receptor tyrosine kinase that is mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. Compared to some other EGFR inhibitors, alflutinib may have therapeutic benefits in tumors with T790M-mediated drug resistance.

Furmonertinib Manufacturers

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

Furmonertinib Suppliers

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

Furmonertinib GMP

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

Furmonertinib CoA

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

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

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