Lazertinib
{{Short description|Anti-cancer medication}}
{{Use American English|date=August 2024}}
{{Use dmy dates|date=June 2025}}
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{{Infobox drug
| image = Lazertinib.svg
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| tradename = Lazcluze, others
| Drugs.com = {{drugs.com|monograph|lazertinib-mesylate}}
| MedlinePlus = a624058
| DailyMedID = Lazertinib
| pregnancy_AU =
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| routes_of_administration = By mouth
| class = EGFR inhibitor
| ATC_prefix = L01
| ATC_suffix = EB09
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| legal_CA = Rx-only
| legal_CA_comment = {{cite web | title=Summary Basis of Decision for Lazcluze | website=Drug and Health Products Portal | date=28 May 2025 | url=https://dhpp.hpfb-dgpsa.ca/review-documents/resource/SBD1748529563500 | access-date=22 June 2025}}{{cite web | title=Register of Innovative Drugs | website=Health Canada | date=3 November 2006 | url=https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/applications-submissions/register-innovative-drugs.html | access-date=17 April 2025}}
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| legal_US = Rx-only
| legal_EU = Rx-only
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| legal_status = Rx-only
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| CAS_number = 1903008-80-9
| PubChem = 121269225
| IUPHAR_ligand = 10136
| DrugBank = DB16216
| ChemSpiderID = 64835231
| UNII = 4A2Y23XK11
| KEGG = D11980
| KEGG2 = D12245
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| ChEMBL = 4558324
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| IUPAC_name = N-[5-[
| 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
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Lazertinib, sold under the brand name Lazcluze among others, is an anti-cancer medication used for the treatment of non-small cell lung cancer.{{cite journal | vauthors = Dhillon S | title = Lazertinib: First Approval | journal = Drugs | volume = 81 | issue = 9 | pages = 1107–1113 | date = June 2021 | pmid = 34028784 | pmc = 8217052 | doi = 10.1007/s40265-021-01533-x }} 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.{{cite web | title=FDA approves lazertinib with amivantamab-vmjw for non-small lung cancer | website=U.S. Food and Drug Administration (FDA) | date=19 August 2024 | url=https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-lazertinib-amivantamab-vmjw-non-small-lung-cancer | access-date=21 August 2024}} {{PD-notice}}
Lazertinib was approved for medical use in South Korea in January 2021,{{Cite web |title=Yuhan wins approval as MFDS clear T790M EGFR TKI drug 'Lazertinib' |url=http://biospectator.com/view/news_view.php?varAtcId=12319 |access-date=23 August 2024 |website=바이오스펙테이터}}{{Cite journal |last=Dhillon |first=Sohita |date=2021 |title=Lazertinib: First Approval |journal=Drugs |volume=81 |issue=9 |pages=1107–1113 |doi=10.1007/s40265-021-01533-x |issn=0012-6667 |pmc=8217052 |pmid=34028784}} in the United States in August 2024,{{cite web | title=Drug Trials Snapshots: Lazcluze | website=U.S. Food and Drug Administration | date=19 August 2024 | url=https://www.fda.gov/drugs/drug-approvals-and-databases/drug-trials-snapshots-lazcluze | access-date=24 June 2025}} {{PD-notice}} and in the European Union in January 2025.
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.
History
Efficacy was evaluated in MARIPOSA (NCT04487080), a randomized, active-controlled, multi-center 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. The US Food and Drug Administration (FDA) approved lazertinib in combination with amivantamab based on evidence from one clinical trial (MARIPOSA, NCT04487080) using data from 858 adult participants with locally advanced or metastatic non-small cell lung cancer with EGFR exon 19 deletions or exon 21 L858R substitution mutations. The trial was conducted at 204 sites in 26 countries including China, South Korea, Brazil, Japan, Malaysia, Spain, Taiwan, Russian Federation, Turkey, Thailand, Mexico, France, Italy, Ukraine, Argentina, Poland, the United States, India, Australia, Portugal, Israel, the United Kingdom, Germany, Belgium, Hungary, and Netherlands. Of the 858 participants, 12 were enrolled at sites in the United States. Among the 858 participants, all were evaluated for efficacy and 849 were evaluated for safety.
Society and culture
= Legal status =
Lazertinib was approved for medical use in the United States in August 2024.{{cite web | title=Novel Drug Approvals for 2024 | website=U.S. Food and Drug Administration (FDA) | date=1 October 2024 | url=https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2024 | archive-url=https://web.archive.org/web/20240419180642/https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2024 | url-status=live | archive-date=19 April 2024 | access-date=8 November 2024}}{{cite report | title=New Drug Therapy Approvals 2024 | website=U.S. Food and Drug Administration (FDA) | date=January 2025 | url=https://www.fda.gov/media/184967/download | format=PDF | access-date=21 January 2025 | archive-url=https://web.archive.org/web/20250121045744/https://www.fda.gov/media/184967/download | archive-date=21 January 2025 | url-status=live }}{{cite press release | title=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 | website=Johnson & Johnson | date=20 August 2024 | url=https://www.jnj.com/media-center/press-releases/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 | access-date=21 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.{{cite web | title=Lazcluze EPAR | website=European Medicines Agency (EMA) | date=14 November 2024 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/lazcluze | access-date=16 November 2024}} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.{{cite web | title=Meeting highlights from the Committee for Medicinal Products for Human Use (CHMP) 11-14 November 2024 | website=European Medicines Agency (EMA) | date=15 November 2024 | url=https://www.ema.europa.eu/en/news/meeting-highlights-committee-medicinal-products-human-use-chmp-11-14-november-2024 | access-date=16 November 2024}} Lazertinib was authorized for medical use in the European Union in January 2025.{{cite web | title=Lazcluze PI | website=Union Register of medicinal products | date=21 January 2025 | url=https://ec.europa.eu/health/documents/community-register/html/h1886.htm | access-date=25 January 2025}}
= Names =
Lazertinib is the international nonproprietary name.{{cite journal | vauthors = ((World Health Organization)) | year = 2018 | title = International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 79 | journal = WHO Drug Information | volume = 32 | issue = 1 | hdl = 10665/330941 | hdl-access = free | author-link = World Health Organization }}
Lazertinib is sold under the brand name Lazcluze and in South Korea as Leclaza.
References
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External links
- {{ClinicalTrialsGov|NCT04487080|A Study of Amivantamab and Lazertinib Combination Therapy Versus Osimertinib in Locally Advanced or Metastatic Non-Small Cell Lung Cancer (MARIPOSA)}}
{{Targeted cancer therapeutic agents}}
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Category:Tyrosine kinase inhibitors