lazertinib

CAS 1903008-80-9

 554.655, C₃₀H₃₄N₈O₃

FDA APPROVED, 8/19/2024, Lazcluze, To treat non-small cell lung cancer
Drug Trials Snapshot

2-PROPENAMIDE, N-(5-((4-(4-((DIMETHYLAMINO)METHYL)-3-PHENYL-1H-PYRAZOL-1-YL)-2-PYRIMIDINYL)AMINO)-4-METHOXY-2-(4-MORPHOLINYL)PHENYL)-

• N-(5-((4-(4-((DIMETHYLAMINO)METHYL)-3-PHENYL-1H-PYRAZOL-1-YL)PYRIMIDIN-2-YL)AMINO)-4-METHOXY-2-MORPHOLINOPHENYL)ACRYLAMIDE
• C-18112003-G
• GNS 1480
• GNS-1480
• GNS1480
• JNJ-73841937-AAA
• YH 25448
• YH-25448
• YH25448

FDA APPROVED 

8/19/2024

To treat non-small cell lung cancer, Lazcluze

Ingredient	UNII	CAS	InChI Key
Lazertinib mesylate monohydrate	WUT449BEG5	2411549-88-5	ZJPNGZUERUYZEG-UHFFFAOYSA-N

Lazertinib is an oral, third-generation, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI).^2,3 Lazertinib was first approved in South Korea on January 18, 2021, for the treatment of EGFR T790M mutation-positive non-small cell lung cancer (NSCLC) with EGFR mutations.¹ It was approved by the FDA on August 19, 2024.⁵ Lazertinib is used alone or in combination with other chemotherapeutic agents.⁴

Lazertinib, sold under the brand name Lazcluze and Leclaza, 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.^[2][6]

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.^[7]

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References

1. ^ Jump up to:^a b c “Lazcluze- lazertinib tablet, film coated”. DailyMed. 20 August 2024. Retrieved 5 September 2024.
2. ^ Jump up to:^{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.
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. ^ 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

Clinical data
Trade names	Lazcluze, Leclaza
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]
Identifiers
showIUPAC name
CAS Number	1903008-80-9
PubChem CID	121269225
IUPHAR/BPS	10136
DrugBank	DB16216
ChemSpider	64835231
UNII	4A2Y23XK11
KEGG	D11980D12245
ChEMBL	ChEMBL4558324
Chemical and physical data
Formula	C30H34N8O3
Molar mass	554.655 g·mol−1
3D model (JSmol)	Interactive image
showSMILES
showInChI

/////////lazertinib, C-18112003-G, GNS 1480, GNS-1480, GNS1480, JNJ-73841937-AAA, YH 25448, YH-25448, YH25448, Lazcluze, FDA 2024, APPROVALS 2024

COC1=C(NC2=NC=CC(=N2)N2C=C(CN(C)C)C(=N2)C2=CC=CC=C2)C=C(NC(=O)C=C)C(=C1)N1CCOCC1