Drug Information

Drug (ID: DG01656) and It's Reported Resistant Information

• Name: Lazertinib
• Synonyms: Lazertinib; 1903008-80-9; GNS-1480; YH25448; YH-25448; GNS1480; JNJ-73841937-AAA; UNII-4A2Y23XK11; N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenylpyrazol-1-yl]pyrimidin-2-yl]amino]-4-methoxy-2-morpholin-4-ylphenyl]prop-2-enamide; C-18112003-G; 4A2Y23XK11; N-(5-((4-(4-((Dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamide; Leclaza; Lazertinib [USAN]; Lazertinib [INN]; Lazertinib (YH25448); CHEMBL4558324; SCHEMBL17670400; GTPL10136; BCP30440; EX-A1912; BDBM50555575; s8724; WHO 10587; AKOS037515597; CCG-270023; Lazertinib (YH25448,GNS-1480); YH-25448;GNS-1480; BS-15742; Compound 73 [WO2016060443A2]; HY-109061; CS-0032992; A16827; A903188; YH-25448; YH 25448; YH25448; GNS-1480; GNS 1480; GNS1480; 2-Propenamide, N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)-; N-(5-((4-(4-((Dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)-2-pyrimidinyl)amino)-4-methoxy-2-(4-morpholinyl)phenyl)acrylamide; N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide
• Indication:
  In total 1 Indication(s)
  Non-small-cell lung cancer [ICD-11: 2C25]; Phase 2; [1]
• Target: .; NOUNIPROTAC; [1]
• Formula: 10
• IsoSMILES: 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
• 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)
• InChIKey: RRMJMHOQSALEJJ-UHFFFAOYSA-N
• PubChem CID: 121269225
• DrugBank ID: DB16216

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Missense mutation; p.L858R (c.2573T>G)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: PC9 cells; Lung; Homo sapiens (Human); CVCL_B260
• In Vitro Model: PC9GR cells; Lung; Homo sapiens (Human); CVCL_V337
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• In Vitro Model: H2291 cells; Lung; Homo sapiens (Human); CVCL_1546
• In Vivo Model: Female BALB/c nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Sanger sequencing assay
• Experiment for Drug Resistance: Cell-free kinase assay; IC50 assay

Lung cancer [ICD-11: 2C25]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Missense mutation; p.L858R (c.2573T>G)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: PC9 cells; Lung; Homo sapiens (Human); CVCL_B260
• In Vitro Model: PC9GR cells; Lung; Homo sapiens (Human); CVCL_V337
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• In Vitro Model: H2291 cells; Lung; Homo sapiens (Human); CVCL_1546
• In Vivo Model: Female BALB/c nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Sanger sequencing assay
• Experiment for Drug Resistance: Cell-free kinase assay; IC50 assay

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Missense mutation; p.L861Q (c.2582T>A)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: PC9 cells; Lung; Homo sapiens (Human); CVCL_B260
• In Vitro Model: PC9GR cells; Lung; Homo sapiens (Human); CVCL_V337
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• In Vitro Model: H2291 cells; Lung; Homo sapiens (Human); CVCL_1546
• In Vivo Model: Female BALB/c nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Sanger sequencing assay
• Experiment for Drug Resistance: Cell-free kinase assay; IC50 assay

References

• Ref 1: YH25448, an Irreversible EGFR-TKI with Potent Intracranial Activity in EGFR Mutant Non-Small Cell Lung CancerClin Cancer Res. 2019 Apr 15;25(8):2575-2587. doi: 10.1158/1078-0432.CCR-18-2906. Epub 2019 Jan 22.