Lazertinib is a tyrosine kinase inhibitor used in combiantion with amivantamab to treat non-small cell lung cancer with EGFR mutations. Lazertinib is an oral, third-generation, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI).
- Mechanism
- Curator reviewed · 7 references
Lazertinib is a kinase inhibitor of mutant epidermal growth factor receptor (EGFR). It targets EGFR single (Ex19del, L858R, T790M) and double (Ex19del/T790M and L858R/T790M) mutations. The inhibition of wild-type EGFR by lazertinib is less selective and potent. Lazertinib irreversibly inhibits EGFR by forming a covalent bond to the Cys797 residue in the ATP-binding site of the EGFR kinase domain. It blocks the EGFR downstream signalling cascades - including the phosphorylation of EGFR, AKT and ERK - and promotes apoptosis of EGFR-mutant lung cancer cells.
- Primary indication
- Lazertinib, in combination with amivantamab, is indicated for the first-line treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 19 deletions or exon...Curator reviewed · 6 structured indications
- Formula / weight
- C30H34N8O3 · 554.655 g/mol (avg)
- First approval
- Canada, 2025 · United States, 2024 · European Union, 2025
- Also known as
- 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
- Code names
- C-18112003-G · GNS-1480 · JNJ-73841937 · JNJ-73841937-AAA · YH-25448
- Brand names
Resolves to
RRMJMHOQSALEJJ-UHFFFAOYSA-NSMILESCOC1=C(NC2=NC=CC(=N2)N2C=C(CN(C)C)C(=N2)C2=CC=CC=C2)C=C(NC(=O)C=C)C(=C1)N1CCOCC1What you can answer from here — as of September 13, 2026
Which drugs share a target with Lazertinib, and which of those have an active Phase 3 trial?
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