Lazertinib
A third-generation EGFR tyrosine kinase inhibitor used to treat non-small cell lung cancer (NSCLC) with specific EGFR mutations, including those that have developed resistance to earlier EGFR inhibitors. It crosses the blood-brain barrier, making it useful for patients with brain metastases.
Molecular Weight
554.6000 g/mol
LogP
3.40
TPSA
110.00 Ų
Lipinski RO5
Pass
Therapeutic Areas
Mechanism of Action
Selectively inhibits specific receptor tyrosine kinases involved in tumor cell proliferation, angiogenesis, and survival signaling. By blocking ATP binding to the kinase domain, it prevents phosphorylation cascades that drive cancer cell growth.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Selectively inhibits specific receptor tyrosine kinases involved in tumor cell proliferation, angiogenesis, and survival signaling. By blocking ATP binding to the kinase domain, it prevents phosphorylation cascades that drive cancer …
2D Structure
Cite this structure
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SMILES
C=CC(=O)Nc1cc(Nc2nccc(-n3cc(CN(C)C)c(-c4ccccc4)n3)n2)c(OC)cc1N1CCOCC1
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)
Molecular Formula
C30H34N8O3
HBD / HBA
2 / 9
Rotatable Bonds
10
Heavy Atoms
41
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
A third-generation EGFR tyrosine kinase inhibitor used to treat non-small cell lung cancer (NSCLC) with specific EGFR mutations, including those that have developed resistance to earlier EGFR inhibitors. It crosses the blood-brain barrier, making it useful for patients with brain metastases.
Selectively inhibits specific receptor tyrosine kinases involved in tumor cell proliferation, angiogenesis, and survival signaling. By blocking ATP binding to the kinase domain, it prevents phosphorylation cascades that drive cancer cell growth.
Yes, Lazertinib is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL4558324. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 121269225. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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