lazertinib   Click here for help

GtoPdb Ligand ID: 10136

Synonyms: Compound 73 [WO2016060443A2] | GNS-1480 | GNS1480 | Leclaza® | YH-25448 | YH25448
Approved drug
lazertinib is an approved drug (S. Korea (2021))
Compound class: Synthetic organic
Comment: Lazertinib (YH-25448, GNS-1480) is an oral, third-generation inhibitor of the aberrant activity of mutant EGFR kinases (EGFR T790M and the activating EGFR mutations Ex19del and L858R), that was originally developed by Yuhan Corporation for antineoplastic potential in cancers with (acquired) resistance to existing EGFR tyrosine kinase inhibitors [1], in particular for EGFR mutation positive, advanced non-small cell lung cancer (NSCLC). It is claimed in Yuhan's patent WO2016060443A2 as compound 73 [1].
In addition to predicted efficacy for the treatment of primary lung and extracranial lesions, lazertinib is expected to be beneficial for NSCLC brain metastases as it is able to cross the blood brain barrier.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 9
Hydrogen bond donors 2
Rotatable bonds 11
Topological polar surface area 109.15
Molecular weight 554.28
XLogP 3.49
No. Lipinski's rules broken 0
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Canonical SMILES C=CC(=O)Nc1cc(Nc2nccc(n2)n2cc(c(n2)c2ccccc2)CN(C)C)c(cc1N1CCOCC1)OC
Isomeric SMILES C=CC(=O)Nc1cc(Nc2nccc(n2)n2cc(c(n2)c2ccccc2)CN(C)C)c(cc1N1CCOCC1)OC
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)
Classification Click here for help
Compound class Synthetic organic
Approved drug? Yes (S. Korea (2021))
IUPAC Name Click here for help
International Nonproprietary Names Click here for help
INN number INN
10587 lazertinib
Synonyms Click here for help
Compound 73 [WO2016060443A2] | GNS-1480 | GNS1480 | Leclaza® | YH-25448 | YH25448
Database Links Click here for help
CAS Registry No. 1903008-80-9 (source: WHO INN record)
GtoPdb PubChem SID 381118846
PubChem CID 121269225
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