Limertinib, also known as ASK-120067, is an orally active, irreversible third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It is designed to inhibit mutant EGFR, including the clinically important EGFR T790M mutation, while showing greater selectivity toward mutant EGFR than wild-type EGFR.
Limertinib has been developed for the treatment of EGFR-mutated non-small cell lung cancer (NSCLC). IUPHAR reports approval in China in January 2025 for T790M-mutated NSCLC, followed by expansion to NSCLC with EGFR exon 19 deletions or exon 21 L858R mutations.
Limertinib is a specialized oncology pharmaceutical API requiring controlled synthesis, purification and comprehensive analytical characterization.
Important quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities and solid-state characteristics.
CAS Number: 1934259-00-3
Molecular Formula: C29H32ClN7O2
Molecular Weight: 546.06 g/mol
Synonym: ASK-120067 / ASK120067
Drug Class: Antineoplastic Agent
Pharmacological Class: EGFR Tyrosine Kinase Inhibitor
Therapeutic Class: Targeted Anticancer Agent
Therapeutic Area: Oncology
Primary Target: EGFR
Molecule Type: Synthetic Small Molecule
Limertinib is an irreversible third-generation EGFR inhibitor. It targets mutant EGFR and forms a covalent interaction with the kinase domain, producing sustained inhibition of EGFR signaling.
Published pharmacological data report an IC50 of approximately 0.3 nM against EGFR T790M and approximately 6.0 nM against EGFR wild-type, demonstrating preferential activity toward the mutant receptor.
Limertinib is associated with targeted treatment of:
Current clinical information should be interpreted according to the applicable regulatory jurisdiction and approved labeling.
Limertinib is designed to selectively inhibit mutant EGFR signaling, including EGFR alterations associated with resistance to earlier-generation EGFR tyrosine kinase inhibitors.
Its activity against EGFR T790M makes it relevant to research and treatment strategies addressing acquired resistance in EGFR-mutated NSCLC.
Limertinib is reported as a solid, with commercial research material described as white to yellow or light-yellow solid. An available analytical CoA reported an observed melting point of 88–90°C for its tested batch.
A controlled Limertinib API manufacturing process may involve:
Typical Limertinib API testing may include:
An available Limertinib CoA reports confirmation by HPLC, MS, NMR and/or microanalysis, with a tested chemical purity of 99.2%.
For pharmaceutical API storage, maintain Limertinib in a tightly closed container under controlled conditions, protected from moisture, heat and direct light. Research-grade supplier information recommends low-temperature storage, including −20°C for powder material. Final commercial API storage conditions should follow validated stability data.
Limertinib is relevant to research involving:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 99.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | ≤ 0.5% |
| Total Impurities | ≤ 1.5% |
| Melting Point | 88°C – 90°C |
| Solubility | Insoluble in water; soluble in DMSO and ethanol |