Lazertinib

Last updated

Lazertinib
Lazertinib.svg
Clinical data
Trade names Lazcluze, others
AHFS/Drugs.com Monograph
MedlinePlus a624058
License data
Routes of
administration 		By mouth
Drug class EGFR inhibitor
ATC code
Legal status
Legal status
Identifiers
  • 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
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C30H34N8O3
Molar mass 554.655 g·mol−1
3D model (JSmol)
  • 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=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. [2] [5] [6] It is a kinase inhibitor of epidermal growth factor receptor. [2]

Contents

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. [5]

Lazertinib was approved for medical use in South Korea in January 2021, [7] [8] in the United States in August 2024, [5] [9] [10] [11] and in the European Union in January 2025. [3] [4]

Medical uses

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. [2] [5] [3] [4]

History

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. [5] 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. [5]

Society and culture

Lazertinib was approved for medical use in the United States in August 2024. [5]

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. [3] The applicant for this medicinal product is Janssen-Cilag International NV. [3] [12] Lazertinib was authorized for medical use in the European Union in January 2025. [3] [4]

Names

Lazertinib is the international nonproprietary name. [13]

Lazertinib is sold under the brand name Lazcluze [2] [3] and in South Korea as Leclaza. [7]

References

  1. ↑ "Register of Innovative Drugs". Health Canada . 3 November 2006. Retrieved 17 April 2025.
  2. 1 2 3 4 5 "Lazcluze- lazertinib tablet, film coated". DailyMed. 20 August 2024. Retrieved 5 September 2024.
  3. 1 2 3 4 5 6 7 "Lazcluze EPAR". European Medicines Agency (EMA). 14 November 2024. Retrieved 16 November 2024. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  4. 1 2 3 4 "Lazcluze PI". Union Register of medicinal products. 21 January 2025. Retrieved 25 January 2025.
  5. 1 2 3 4 5 6 7 "FDA approves lazertinib with amivantamab-vmjw for non-small lung cancer". U.S. Food and Drug Administration (FDA). 19 August 2024. Retrieved 21 August 2024.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  6. ↑ Dhillon S (June 2021). "Lazertinib: First Approval". Drugs. 81 (9): 1107–1113. doi:10.1007/s40265-021-01533-x. PMC   8217052 . PMID   34028784.
  7. 1 2 "Yuhan wins approval as MFDS clear T790M EGFR TKI drug 'Lazertinib'". 바이오스펙테이터. Retrieved 23 August 2024.
  8. ↑ Dhillon S (2021). "Lazertinib: First Approval". Drugs. 81 (9): 1107–1113. doi:10.1007/s40265-021-01533-x. ISSN   0012-6667. PMC   8217052 . PMID   34028784.
  9. ↑ "Rybrevant (amivantamab-vmjw) plus Lazcluze (lazertinib) approved in the U.S. as a first-line chemotherapy-free treatment for patients with EGFR-mutated advanced lung cancer". Johnson & Johnson (Press release). 20 August 2024. Retrieved 21 August 2024.
  10. ↑ "Novel Drug Approvals for 2024". U.S. Food and Drug Administration (FDA). 1 October 2024. Archived from the original on 19 April 2024. Retrieved 8 November 2024.
  11. ↑ New Drug Therapy Approvals 2024 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2025. Archived from the original on 21 January 2025. Retrieved 21 January 2025.
  12. ↑ "Meeting highlights from the Committee for Medicinal Products for Human Use (CHMP) 11-14 November 2024". European Medicines Agency (EMA). 15 November 2024. Retrieved 16 November 2024.
  13. ↑ World Health Organization (2018). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 79". WHO Drug Information. 32 (1). hdl: 10665/330941 .
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