lazertinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5832 1903008-80-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lazertinib
  • lazertinib mesilate
  • lazcluze
  • leclaza
  • YH25448
  • GNS-1480
  • JNJ-73841937
Lazertinib is a kinase inhibitor of epidermal growth factor receptor (EGFR) that inhibits EGFR exon 19 deletions and exon 21 L858R substitution mutations at lower concentrations than wild-type EGFR. In human NSCLC cells and mouse xenograft models of EGFR exon 19 deletions or EGFR L858R substitution mutations, lazertinib demonstrated anti-tumor activity. Treatment with lazertinib in combination with amivantamab increased in vivo anti-tumor activity compared to either agent alone in a mouse xenograft model of human NSCLC with an EGFR L858R mutation.
  • Molecular weight: 554.66
  • Formula: C30H34N8O3
  • CLOGP: 4.10
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 2
  • TPSA: 109.67
  • ALOGS:
  • ROTB: 10
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Aug. 19, 2024 FDA : Janssen Biotech, Inc
Jan. 20, 2025 EMA Janssen Cilag International NV

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Paronychia 75.22 44.13 14 264 7992 90620177
Neuropathy peripheral 46.83 44.13 17 261 136953 90491216

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Paronychia 83.07 49.00 17 464 11064 110577754
Neuropathy peripheral 70.21 49.00 27 454 179250 110409568
Infusion related reaction 65.37 49.00 32 449 381130 110207688
Dermatitis acneiform 52.78 49.00 12 469 12683 110576135

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EB09 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA MoA N0000175082 Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L01EB Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors 8 drugs
afatinibdacomitiniberlotinibgefitinibicotinibmobocertinibolmutinibosimertinib

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 80MG BASE LAZCLUZE JANSSEN BIOTECH N219008 Aug. 19, 2024 RX TABLET ORAL 9593098 Oct. 13, 2035 FIRST-LINE TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 L858R SUBSTITUTION MUTATIONS, IN COMBINATION WITH AMIVANTAMAB
EQ 80MG BASE LAZCLUZE JANSSEN BIOTECH N219008 Aug. 19, 2024 RX TABLET ORAL 11981659 April 18, 2038 FIRST-LINE TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 L858R SUBSTITUTION MUTATIONS, IN COMBINATION WITH AMIVANTAMAB
EQ 80MG BASE LAZCLUZE JANSSEN BIOTECH N219008 Aug. 19, 2024 RX TABLET ORAL 12599606 May 14, 2040 FIRST-LINE TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 L858R SUBSTITUTION MUTATIONS, BY ADMINISTRATION OF EQ 80 MG BASE LAZERTINIB IN COMBINATION WITH AMIVANTAMAB
EQ 80MG BASE LAZCLUZE JANSSEN BIOTECH N219008 Aug. 19, 2024 RX TABLET ORAL 11879013 May 21, 2040 FIRST-LINE TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 L858R SUBSTITUTION MUTATIONS, IN COMBINATION WITH AMIVANTAMAB
EQ 80MG BASE LAZCLUZE JANSSEN BIOTECH N219008 Aug. 19, 2024 RX TABLET ORAL 11850248 Aug. 1, 2041 FIRST-LINE TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EGFR EXON 19 DELETIONS OR EXON 21 L858R SUBSTITUTION MUTATIONS, IN COMBINATION WITH AMIVANTAMAB

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 80MG BASE LAZCLUZE JANSSEN BIOTECH N219008 Aug. 19, 2024 RX TABLET ORAL Aug. 19, 2029 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Epidermal growth factor receptor Kinase INHIBITOR IC50 7.53 DRUG LABEL DRUG LABEL
Receptor tyrosine-protein kinase erbB-2 Kinase Ki 6.36 CHEMBL
Tyrosine-protein kinase SYK Kinase INHIBITOR IC50 6.70 IUPHAR
Tyrosine-protein kinase SYK Kinase INHIBITOR IC50 6.70 IUPHAR

External reference:

IDSource
CHEMBL4558324 ChEMBL_ID
C000707992 MESH_SUPPLEMENTAL_RECORD_UI
DB16216 DRUGBANK_ID
4043347 VANDF
C4724849 UMLSCUI
CHEBI:757712 CHEBI
CHEMBL6068478 ChEMBL_ID
10587 INN_ID
121269225 PUBCHEM_CID
388578 MMSL
43083 MMSL
d10215 MMSL
10136 IUPHAR_LIGAND_ID
4A2Y23XK11 UNII
2691150 RXNORM
1373927003 SNOMEDCT_US
933451401000036107 SNOMEDCT_US
D11980 KEGG_DRUG
019839 NDDF
019840 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LAZCLUZE HUMAN PRESCRIPTION DRUG LABEL 1 57894-080 TABLET, FILM COATED 80 mg ORAL NDA 32 sections
LAZCLUZE HUMAN PRESCRIPTION DRUG LABEL 1 57894-080 TABLET, FILM COATED 80 mg ORAL NDA 32 sections
LAZCLUZE HUMAN PRESCRIPTION DRUG LABEL 1 57894-240 TABLET, FILM COATED 240 mg ORAL NDA 32 sections
LAZCLUZE HUMAN PRESCRIPTION DRUG LABEL 1 57894-240 TABLET, FILM COATED 240 mg ORAL NDA 32 sections