Lazertinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Lazertinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2024. Its mechanism of action is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A4 Inhibitors and Kinase Inhibitors. DrugCentral lists 3 molecular targets, including EGFR, SYK and ERBB2. Recorded indications include Non-small cell lung cancer.

• Approval status: onp (first approved 2024 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 3A4 Inhibitors; Kinase Inhibitors.
• Molecular targets: EGFR, SYK and ERBB2 (3 listed in DrugCentral).
• Indications: Non-small cell lung cancer.
• ATC code: L01EB09 (Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors).
• Molecular formula: C30H34N8O3; molecular weight 554.65 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Non-small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 3A4 Inhibitors; Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (3)

Target	Gene	Action	Activity
Epidermal growth factor receptor	EGFR	inhibitor	IC50 7.53
Tyrosine-protein kinase SYK	SYK	inhibitor	IC50 6.70
Receptor tyrosine-protein kinase erbB-2	ERBB2	unknown	Ki 6.36

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2025-01-20	EMA	—	Janssen Cilag International NV
2024-08-19	FDA	—	: Janssen Biotech, Inc

ATC classification

ATC code	Therapeutic hierarchy
L01EB09	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: EGFR · Testing Required
• EMA label: GSTM1 · No Clinical PGx
• FDA label: GSTM1 · No Clinical PGx
• FDA label: EGFR · Testing Required
• HCSC label: EGFR · Testing Required
• HCSC label: GSTM1 · No Clinical PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Paronychia	158.8
Rash	131.8
Infusion related reaction	100.1
Neuropathy peripheral	60.5
Skin toxicity	55.7
Dermatitis acneiform	51.2

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Lazertinib is on its molecule page.

• Molecular formula: C₃₀H₃₄N₈O₃
• Molecular weight: 554.65 g/mol
• CAS number: —
• InChIKey: RRMJMHOQSALEJJ-UHFFFAOYSA-N
• PubChem CID: 121269225

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

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Lazertinib used for?

DrugCentral lists the following indications for Lazertinib: Non-small cell lung cancer.

How does Lazertinib work?

Lazertinib is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A4 Inhibitors and Kinase Inhibitors; its molecular targets in DrugCentral include EGFR (inhibitor), SYK (inhibitor) and ERBB2.

When was Lazertinib first approved?

Lazertinib was first approved by the FDA in 2024.

What drug class does Lazertinib belong to?

Lazertinib is in the Kinase Inhibitor class.

What is the chemical formula of Lazertinib?

Lazertinib has the molecular formula C30H34N8O3 and a molecular weight of 554.65 g/mol.

Sources

• DrugCentral drug card 5832 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4558324 — compound record and bioactivity
• PubChem CID 121269225 — chemical identifiers
• DrugBank DB16216 — drug record
• FDA UNII 4A2Y23XK11 — substance identity
• DailyMed: FDA labels for Lazertinib — current prescribing information (label search)
• UniProt P00533 (EGFR) — target protein
• UniProt P43405 (SYK) — target protein
• UniProt P04626 (ERBB2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.