dosimertinib

Dosimertinib is a clinical-stage, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) developed by Bio Genuine (Henan Genuine Biotech Co.) for the treatment of non-small cell lung cancer (NSCLC). As a deuterated derivative of the approved covalent inhibitor osimertinib, dosimertinib is designed to improve the metabolic profile of the parent drug. Preclinical data suggests that deuteration reduces the formation of toxic metabolites by approximately 80% while maintaining high potency and selectivity against EGFR mutations, including the T790M resistance mutation. It is currently undergoing Phase I/II clinical evaluation in China, where it has completed the dose-escalation stage.

Other names

deuterated osimertinib