Lazertinib

Routes of
administrationBy mouthDrug classEGFR inhibitorATC codeLegal statusLegal status IdentifiersCAS NumberPubChem CIDIUPHAR/BPSDrugBankChemSpiderUNIIKEGGChEMBLChemical and physical dataFormulaC₃₀H₃₄N₈O₃Molar mass554.655 g·mol⁻¹3D model (JSmol)

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]

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]

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]

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

Lazertinib is the international nonproprietary name.^[7]

• 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