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)
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Summary of Clinical Use Click here for help
Lazertinib was advanced to late stage clinical trial in patients with EGFR mutation positive advanced NSCLC. It was evaluated as a first-line treatment and for advanced disease that is resistant to other chemotherapies. It is also being evaluated in combination with the EGFR/MET bispecific mAb amivantamab (NCT04487080, NCT04077463). Click here to link to's full list of lazertinib trials. First clinical approval was granted by South Korea's regulatory agency in 2021.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT04075396 A Study of Lazertinib in Participants With Epidermal Growth Factor Receptor (EGFR) Mutation Positive Advanced Non-Small Cell Lung Cancer (NSCLC) Phase 1/Phase 2 Interventional Janssen Research & Development, LLC
NCT04248829 Clinical Trial of YH25448(Lazertinib) as the First-line Treatment in Patients With EGFR Mutation Positive Locally Advanced or Metastatic NSCLC (LASER301) Phase 3 Interventional Yuhan Corporation
NCT04487080 A Study of Amivantamab and Lazertinib Combination Therapy Versus Osimertinib in Locally Advanced or Metastatic Non-Small Cell Lung Cancer Phase 3 Interventional Janssen Research & Development, LLC
NCT02609776 Study of JNJ-61186372, a Human Bispecific EGFR and cMet Antibody, in Participants With Advanced Non-Small Cell Lung Cancer Phase 1 Interventional Janssen Research & Development, LLC