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Chemistry

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Also known as: 1903008-80-9, Yh-25448, Gns-1480, Yh25448, Gns1480, Jnj-73841937-aaa
Molecular Formula
C30H34N8O3
Molecular Weight
554.6  g/mol
InChI Key
RRMJMHOQSALEJJ-UHFFFAOYSA-N
FDA UNII
4A2Y23XK11

Lazertinib
Lazertinib is an orally available third-generation, selective inhibitor of certain forms of the epidermal growth factor receptor (EGFR) with activating mutations, including the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation, with potential antineoplastic activity. Upon administration, lazertinib specifically and irreversibly binds to and inhibits selective EGFR mutants, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Lazertinib may inhibit programmed cell death-1 ligand 1 (PD-L1) and inflammatory cytokines in specific cancer cells harboring certain EGFR mutations. Compared to some other EGFR inhibitors, lazertinib may have therapeutic benefits in tumors with T790M- or L858R-mediated drug resistance. In addition, lazertinib penetrates the blood-brain barrier (BBB). This agent shows minimal activity against wild-type EGFR (wtEGFR), and does not cause dose-limiting toxicities, which occur during the use of non-selective EGFR inhibitors and inhibit wtEGFR. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
1 2D Structure

Lazertinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenylpyrazol-1-yl]pyrimidin-2-yl]amino]-4-methoxy-2-morpholin-4-ylphenyl]prop-2-enamide
2.1.2 InChI
InChI=1S/C30H34N8O3/c1-5-28(39)32-23-17-24(26(40-4)18-25(23)37-13-15-41-16-14-37)33-30-31-12-11-27(34-30)38-20-22(19-36(2)3)29(35-38)21-9-7-6-8-10-21/h5-12,17-18,20H,1,13-16,19H2,2-4H3,(H,32,39)(H,31,33,34)
2.1.3 InChI Key
RRMJMHOQSALEJJ-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CN(C)CC1=CN(N=C1C2=CC=CC=C2)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N5CCOCC5)OC
2.2 Other Identifiers
2.2.1 UNII
4A2Y23XK11
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 2-propenamide, N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)-

2. Leclaza

3. N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)acrylamide

2.3.2 Depositor-Supplied Synonyms

1. 1903008-80-9

2. Yh-25448

3. Gns-1480

4. Yh25448

5. Gns1480

6. Jnj-73841937-aaa

7. Lazertinib [usan]

8. C-18112003-g

9. N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenylpyrazol-1-yl]pyrimidin-2-yl]amino]-4-methoxy-2-morpholin-4-ylphenyl]prop-2-enamide

10. 4a2y23xk11

11. N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamide

12. 2-propenamide, N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)-

13. Leclaza

14. Lazertinib [inn]

15. Lazertinib [inn]

16. Lazertinib (yh25448)

17. Lazertinib [who-dd]

18. Unii-4a2y23xk11

19. Chembl4558324

20. Schembl17670400

21. Gtpl10136

22. Bcp30440

23. Ex-a1912

24. Bdbm50555575

25. S8724

26. Who 10587

27. Akos037515597

28. Ccg-270023

29. Lazertinib (yh25448,gns-1480)

30. Yh-25448;gns-1480

31. Ac-36243

32. Bs-15742

33. Compound 73 [wo2016060443a2]

34. Hy-109061

35. Cs-0032992

36. A16827

37. A903188

38. Yh-25448; Yh 25448; Yh25448; Gns-1480; Gns 1480; Gns1480

39. N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)acrylamide

40. N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1h-pyrazol-1-yl)pyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide

2.4 Create Date
2016-08-06
3 Chemical and Physical Properties
Molecular Weight 554.6 g/mol
Molecular Formula C30H34N8O3
XLogP33.4
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count9
Rotatable Bond Count10
Exact Mass554.27538698 g/mol
Monoisotopic Mass554.27538698 g/mol
Topological Polar Surface Area110 Ų
Heavy Atom Count41
Formal Charge0
Complexity837
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.)


KDMF

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Yuhan Corporation

South Korea
SupplySide West 2024
Not Confirmed
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Yuhan Corporation

South Korea
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SupplySide West 2024
Not Confirmed

Lasertinib

Registrant Name : Yuhan Chemical Co., Ltd.

Registration Date : 2021-01-18

Registration Number : 1791-9-ND

Manufacturer Name : Yuhan Chemical Co., Ltd.

Manufacturer Address : 402, 5-ba, Sihwa Industrial Complex, 45 Jiwon-ro, Danwon-gu, Ansan-si, Gyeonggi-do (S...

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API Reference Price

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15-Jan-2021
26-Jun-2021
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Drugs in Development

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Details:

Rybrevant (amivantamab) in combination with Lazcluze (lazertinib) and dexamethasone reduces infusion-related reactions in patients with EGFR-mutated non-small cell lung cancer.


Lead Product(s): Amivantamab,Lazertinib,Dexamethasone

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 10, 2024

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01

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Details : Rybrevant (amivantamab) in combination with Lazcluze (lazertinib) and dexamethasone reduces infusion-related reactions in patients with EGFR-mutated non-small cell lung cancer.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

September 10, 2024

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Details:

Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is indicated in combination with Lazertinib for the treatment of Advanced or Metastatic Non-small Cell Lung Cancer.


Lead Product(s): Amivantamab,Lazertinib,Dexamethasone

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: ApprovedProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable August 20, 2024

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02

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Details : Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is indicated in combination with Lazertinib for the treatment of Advanced or Metastatic Non-small Cell Lung Cancer.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

August 20, 2024

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Details:

Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of Advanced or Metastatic Non-small Cell Lung Cancer.


Lead Product(s): Amivantamab,Lazertinib

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 17, 2024

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03

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Lead Product(s) : Amivantamab,Lazertinib

Therapeutic Area : Oncology

Highest Development Status : Phase III

Partner/Sponsor/Collaborator : Not Applicable

Deal Size : Not Applicable

Deal Type : Not Applicable

Details : Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of Advanced or Metastatic Non-small Cell Lung Cancer.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

June 17, 2024

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Details:

Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of exon 19 deletions or L858R mutated NSCLC.


Lead Product(s): Amivantamab,Lazertinib,Carboplatin

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 03, 2024

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04

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Details : Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of exon 19 deletions or L858R mutated NSCLC.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

June 03, 2024

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Details:

Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of Advanced or Metastatic Non-small Cell Lung Cancer.


Lead Product(s): Amivantamab,Lazertinib

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 31, 2024

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05

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Lead Product(s) : Amivantamab,Lazertinib

Therapeutic Area : Oncology

Highest Development Status : Phase III

Partner/Sponsor/Collaborator : Not Applicable

Deal Size : Not Applicable

Deal Type : Not Applicable

Details : Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of Advanced or Metastatic Non-small Cell Lung Cancer.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

May 31, 2024

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Details:

Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of EGFR-mutated NSCLC after failure of prior therapy.


Lead Product(s): Amivantamab,Lazertinib,Carboplatin

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 31, 2024

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06

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Details : Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib for the treatment of EGFR-mutated NSCLC after failure of prior therapy.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

May 31, 2024

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Details:

Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody evaluated with lazertinib for first-line treatment of patients with EGFR-mutated non-small cell lung cancer.


Lead Product(s): Amivantamab,Lazertinib

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable February 08, 2024

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07

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Lead Product(s) : Amivantamab,Lazertinib

Therapeutic Area : Oncology

Highest Development Status : Phase III

Partner/Sponsor/Collaborator : Not Applicable

Deal Size : Not Applicable

Deal Type : Not Applicable

Details : Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody evaluated with lazertinib for first-line treatment of patients with EGFR-mutated non-small cell lung cancer.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

February 08, 2024

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Details:

JNJ-73841937 (lazertinib) is an oral, third-generation, brain-penetrant EGFR TKI that targets both the T790M mutation. It is under phase 3 clinical development in combination with Rybrevant (amivantamab) for the treatment of EGFR-mutated non-small cell lung cancer.


Lead Product(s): Lazertinib,Amivantamab-vmjw

Therapeutic Area: Oncology Brand Name: JNJ-73841937

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 21, 2023

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08

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Lead Product(s) : Lazertinib,Amivantamab-vmjw

Therapeutic Area : Oncology

Highest Development Status : Phase III

Partner/Sponsor/Collaborator : Not Applicable

Deal Size : Not Applicable

Deal Type : Not Applicable

Details : JNJ-73841937 (lazertinib) is an oral, third-generation, brain-penetrant EGFR TKI that targets both the T790M mutation. It is under phase 3 clinical development in combination with Rybrevant (amivantamab) for the treatment of EGFR-mutated non-small cell l...

Brand Name : JNJ-73841937

Molecule Type : Small molecule

Upfront Cash : Not Applicable

December 21, 2023

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Details:

Rybrevant (amivantamab) is a fully-human bispecific antibody targeting EGFR and MET with immune cell-directing activity. It is being evaluated in combination with lazertinib for the treatment of patients with EGFR-mutated non-small cell lung cancer.


Lead Product(s): Amivantamab,Lazertinib,Carboplatin

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 21, 2023

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09

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Details : Rybrevant (amivantamab) is a fully-human bispecific antibody targeting EGFR and MET with immune cell-directing activity. It is being evaluated in combination with lazertinib for the treatment of patients with EGFR-mutated non-small cell lung cancer.

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

December 21, 2023

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Details:

Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib & chemotherapy for the treatment of adult patients with advanced egfr-mutated non-small cell lung cancer after failure of prior therapy.


Lead Product(s): Amivantamab,Lazertinib,Pemetrexed

Therapeutic Area: Oncology Brand Name: Rybrevant

Study Phase: Phase IIIProduct Type: Large molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 23, 2023

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10

SupplySide West 2024
Not Confirmed
SupplySide West 2024
Not Confirmed

Details : Rybrevant (amivantamab) is a fully-human EGFR-MET bispecific antibody. It is being evaluated in combination with Lazertinib & chemotherapy for the treatment of adult patients with advanced egfr-mutated non-small cell lung cancer after failure of prior th...

Brand Name : Rybrevant

Molecule Type : Large molecule

Upfront Cash : Not Applicable

October 23, 2023

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