deulorlatinib

Deulorlatinib (TGRX-326) is a highly brain-penetrant, third-generation dual tyrosine kinase inhibitor (TKI) targeting anaplastic lymphoma kinase (ALK) and ROS proto-oncogene 1 (ROS1). Developed by Shenzhen TargetRx, it is a deuterated derivative of lorlatinib. Deuteration at the key metabolic site of the molecule is intended to achieve higher drug exposure and potentially improved safety and efficacy compared to the parent compound. It demonstrates potent activity against a broad range of ALK-resistant mutations, including the G1202R solvent-front mutation, and is primarily being developed for the treatment of advanced ALK-positive or ROS1-positive non-small cell lung cancer (NSCLC), including patients who have failed prior second-generation ALK inhibitors.

Other names

deulorlatinib