Lazertinib

Lazertinib
Clinical data
Trade names	Lazcluze, others
AHFS/Drugs.com	Lazcluze
License data	US DailyMed: Lazertinib;
Routes of; administration	By mouth
Drug class	EGFR inhibitor
ATC code	L01EB09 (WHO) ;
Legal status
Legal status	US: ℞-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]^[2]^[3] 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.^[2]

Lazertinib was approved for medical use in South Korea in January 2021,^[4]^[5] and in the United States in August 2024 to treat non-small cell lung cancer.^[2]^[6]^[7]

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]

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.^[2] 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.^[2]

Society and culture

Legal status

Lazertinib was approved for medical use in the United States in August 2024.^[2]

Names

Lazertinib is the international nonproprietary name.^[8]

References

^ ^a ^b ^c "Lazcluze- lazertinib tablet, film coated". DailyMed. 20 August 2024. Retrieved 5 September 2024.
^ ^a ^b ^c ^d ^e ^f ^g "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. This article incorporates text from this source, which is in the public domain.
^ Dhillon S (June 2021). "Lazertinib: First Approval". Drugs. 81 (9): 1107–1113. doi:10.1007/s40265-021-01533-x. PMC 8217052. PMID 34028784.
^ "Yuhan wins approval as MFDS clear T790M EGFR TKI drug 'Lazertinib'". 바이오스펙테이터. Retrieved 23 August 2024.
^ 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.
^ "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.
^ "Novel Drug Approvals for 2024". U.S. Food and Drug Administration (FDA). 1 October 2024. Retrieved 8 November 2024.
^ World Health Organization (2018). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 79". WHO Drug Information. 32 (1). hdl:10665/330941.

External links

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

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[Lazcluze_FDA_label-1] "Lazcluze- lazertinib tablet, film coated". DailyMed. 20 August 2024. Retrieved 5 September 2024.

[FDA_20240819-2] ^ ^a ^b ^c ^d ^e ^f ^g "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. This article incorporates text from this source, which is in the public domain.

[Dhillon_2021-3] Dhillon S (June 2021). "Lazertinib: First Approval". Drugs. 81 (9): 1107–1113. doi:10.1007/s40265-021-01533-x. PMC 8217052. PMID 34028784.

[4] "Yuhan wins approval as MFDS clear T790M EGFR TKI drug 'Lazertinib'". 바이오스펙테이터. Retrieved 23 August 2024.

[5] 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.

[6] "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.

[7] "Novel Drug Approvals for 2024". U.S. Food and Drug Administration (FDA). 1 October 2024. Retrieved 8 November 2024.

[8] 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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