| Tradename: | Lazcluze, others |
| Dailymedid: | Lazertinib |
| Routes Of Administration: | By mouth |
| Class: | EGFR inhibitor |
| Atc Prefix: | L01 |
| Atc Suffix: | EB09 |
| Legal Us: | Rx-only |
| Legal Us Comment: | [1] |
| Legal Status: | Rx-only |
| Cas Number: | 1903008-80-9 |
| Pubchem: | 121269225 |
| Iuphar Ligand: | 10136 |
| Drugbank: | DB16216 |
| Chemspiderid: | 64835231 |
| Unii: | 4A2Y23XK11 |
| Kegg: | D11980 |
| Kegg2: | D12245 |
| Chembl: | 4558324 |
| Iupac Name: | N-[5-[<nowiki/>[4-[4-[(dimethylamino)methyl]-3-phenylpyrazol-1-yl]pyrimidin-2-yl]amino]-4-methoxy-2-morpholin-4-ylphenyl]prop-2-enamide |
| C: | 30 |
| H: | 34 |
| N: | 8 |
| O: | 3 |
| 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 |
| Stdinchi: | 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) |
| Stdinchikey: | 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.[2] It is a kinase inhibitor of epidermal growth factor receptor.
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.
Lazertinib was approved for medical use in South Korea in January 2021,[3] [4] and in the United States in August 2024 to treat non-small cell lung cancer.[5] [6] [7]
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.
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. 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.
Lazertinib was approved for medical use in the United States in August 2024.
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. The applicant for this medicinal product is Janssen-Cilag International NV.[8] [9]
Lazertinib is the international nonproprietary name.[10]