Overview
Almonertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed for the treatment of non-small cell lung cancer (NSCLC). It specifically targets tumors harboring the EGFR T790M mutation, a common resistance mechanism to first-generation TKIs. Almonertinib's high selectivity and reduced off-target effects make it a promising therapeutic option. Approved in China in 2020, it has shown significant clinical efficacy in patients with advanced NSCLC. Its development represents a breakthrough in overcoming resistance mutations while minimizing adverse effects compared to earlier generations of EGFR inhibitors.
Physical and Chemical Properties
Almonertinib is a small molecule with a molecular weight of 531.04 g/mol, appearing as a white to off-white crystalline powder. It is chemically stable under recommended storage conditions (-20°C, protected from light and moisture) but may degrade when exposed to heat or humidity. The compound exhibits moderate solubility in dimethyl sulfoxide (DMSO) but has limited solubility in aqueous solutions, which influences its pharmaceutical formulation. Its molecular structure includes a chloro-substituted quinazoline core, contributing to its potent binding affinity for mutant EGFR kinases.
Main Applications
The primary application of Almonertinib is the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) in patients with confirmed EGFR T790M mutation who have progressed after first-line EGFR-TKI therapy. Clinical trials demonstrated an objective response rate exceeding 60% in this patient population. Beyond its labeled indication, research is exploring its potential in combination therapies and for other EGFR-mutated cancers. Its targeted action spares wild-type EGFR, reducing side effects like rash and diarrhea commonly associated with earlier-generation inhibitors.
Safety and Storage
As a potent pharmaceutical compound, Almonertinib requires careful handling. Personnel should use appropriate personal protective equipment including gloves, lab coats, and eye protection. Avoid generating dust or aerosols during handling. For long-term stability, store the compound at -20°C in tightly sealed containers with desiccants. Under these conditions, the material typically maintains stability for at least 24 months. Always refer to the certificate of analysis for batch-specific storage recommendations and expiry dates.
B2B Procurement Guide
When sourcing Almonertinib for pharmaceutical manufacturing or research purposes, prioritize suppliers with GMP certification and proven track records in oncology APIs. Key procurement considerations include batch-to-batch consistency, impurity profiles (<2% total impurities), and comprehensive documentation including COA, stability data, and DMF references. Given the compound's high value, consider ordering smaller quantities initially for quality verification. Pricing is typically volume-dependent, with contract manufacturing arrangements offering better economics for large-scale production. Ensure proper cold chain logistics are in place for transport and customs clearance to maintain product integrity.