Lazertinib is an oral, third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed for the treatment of selected patients with EGFR-mutated non-small cell lung cancer (NSCLC).
It selectively targets activating EGFR mutations and the T790M resistance mutation, while showing greater selectivity for mutant EGFR compared with wild-type EGFR.
Lazertinib is a specialized oncology pharmaceutical API manufactured through controlled chemical synthesis, purification and crystallization.
Important quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities, polymorphic form and stability.
CAS Number: 1357476-66-4
Molecular Formula: C30H34N6O3
Molecular Weight: 526.64 g/mol
Drug Class: Antineoplastic Agent
Pharmacological Class: Third-Generation EGFR Tyrosine Kinase Inhibitor
Therapeutic Class: Targeted Anticancer Agent
Therapeutic Area: Oncology
Lazertinib is an irreversible EGFR tyrosine kinase inhibitor that preferentially inhibits mutant forms of EGFR.
It targets:
By inhibiting EGFR signaling, lazertinib interferes with pathways responsible for cancer-cell proliferation and survival.
Lazertinib is used in approved settings for patients with EGFR-mutated locally advanced or metastatic NSCLC.
It may be used as a targeted therapy in combination with other anticancer treatment depending on the applicable regulatory approval and treatment setting.
Lazertinib was designed to address acquired resistance to earlier-generation EGFR inhibitors, particularly resistance associated with the EGFR T790M mutation.
Its mutant-selective profile is intended to provide effective EGFR inhibition while reducing inhibition of wild-type EGFR relative to earlier EGFR TKIs.
Typical API manufacturing may involve:
Lazertinib API quality evaluation may include:
Lazertinib should be stored in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive heat, moisture and direct light. Final storage conditions should be established through validated stability studies.
Lazertinib is relevant to research involving:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 1.0% |