Lazertinib

Lazertinib

Clinical data
Trade names	Lazcluze, others
AHFS/Drugs.com	Monograph
MedlinePlus	a624058
License data	US DailyMed: Lazertinib
Routes of administration	By mouth
Drug class	EGFR inhibitor
ATC code	L01EB09 (WHO)
Legal status
Legal status	US: ℞-only[1] EU: Rx-only[2][3] In general: ℞ (Prescription only)
Identifiers
IUPAC name N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenylpyrazol-1-yl]pyrimidin-2-yl]amino]-4-methoxy-2-morpholin-4-ylphenyl]prop-2-enamide
CAS Number	1903008-80-9
PubChem CID	121269225
IUPHAR/BPS	10136
DrugBank	DB16216
ChemSpider	64835231
UNII	4A2Y23XK11
KEGG	D11980 D12245
ChEMBL	ChEMBL4558324
Chemical and physical data
Formula	C30H34N8O3
Molar mass	554.655 g·mol−1
3D model (JSmol)	Interactive image
SMILES 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) Key:RRMJMHOQSALEJJ-UHFFFAOYSA-N

Lazertinib, sold under the brand name Lazcluze among others, is an anti-cancer medication used for the treatment of non-small cell lung cancer.^[1][4][5] It is a kinase inhibitor of epidermal growth factor receptor.^[1]

The most common adverse reactions include rash, nail toxicity, infusion-related reactions (amivantamab), musculoskeletal pain, edema, stomatitis, venous thromboembolism, paresthesia, fatigue, diarrhea, constipation, COVID-19 infection, hemorrhage, dry skin, decreased appetite, pruritus, nausea, and ocular toxicity.^[4]

Lazertinib was approved for medical use in South Korea in January 2021,^[6][7] in the United States in August 2024,^{[4][8][9][10]} and in the European Union in January 2025.^[2][3]

Lazertinib is indicated in combination with amivantamab for the first-line treatment of adults with locally advanced or metastatic non-small cell lung cancer with epidermal growth factor receptor exon 19 deletions or exon 21 L858R substitution mutations.^[1][4][2][3]

Efficacy was evaluated in MARIPOSA (NCT04487080), a randomized, active-controlled, multicenter trial of 1074 participants with exon 19 deletion or exon 21 L858R substitution mutation-positive locally advanced or metastatic non-small cell lung cancer and no prior systemic therapy for advanced disease.^[4] Participants were randomized (2:2:1) to receive lazertinib in combination with amivantamab, osimertinib monotherapy, or lazertinib monotherapy (an unapproved regimen for non-small cell lung cancer) until disease progression or unacceptable toxicity.^[4]

Lazertinib was approved for medical use in the United States in August 2024.^[4]

In November 2024, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Lazcluze, intended in combination with amivantamab, for the treatment of non-small cell lung cancer (NSCLC) with activating epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations.^[2] The applicant for this medicinal product is Janssen-Cilag International NV.^[2][11] Lazertinib was approved for medical use in the European Union in January 2025.^[2][3]

Lazertinib is the international nonproprietary name.^[12]

Lazertinib is sold under the brand name Lazcluze.^[1][2]

• Clinical trial number NCT04487080 for "A Study of Amivantamab and Lazertinib Combination Therapy Versus Osimertinib in Locally Advanced or Metastatic Non-Small Cell Lung Cancer (MARIPOSA)" at ClinicalTrials.gov

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

• v
• t
• e