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)
1. Suh B-C, Salgaonkar PD, Lee J, Koh JS, Song H-J, Lee IY, Lee J, Jung DS, Kim J-H, Kim S-W. (2016)
Compounds and compositions for modulating EGFR mutant kinase activities.
Patent number: WO2016060443A2. Assignee: Yuhan Corporation. Priority date: 13/10/2014. Publication date: 21/04/2016.