unecritinib

Unecritinib (TQ-B3101) is an orally administered, small molecule inhibitor of receptor tyrosine kinases including anaplastic lymphoma kinase (ALK), ROS1 protein, and proto-oncogene protein c-Met. It is a novel derivative of crizotinib designed to overcome resistance and improve efficacy in cancers driven by these targets. Unecritinib inhibits AKT phosphorylation and downstream signaling molecules such as ERK1/2, demonstrating potent antitumor activity in preclinical models with ALK rearrangements or c-MET overexpression. In clinical trials, it has shown high objective response rates and intracranial activity in patients with advanced or metastatic non-small cell lung cancer (NSCLC) harboring ROS1 rearrangements who are naive to prior ROS1 inhibitors. The drug is primarily metabolized by carboxylesterase 2 (CES2). Development has been led by Chia Tai Tianqing Pharmaceutical Group under Sino Biopharmaceutical[1][2][3][5][6].

Other names

TQ-B3101TQ-B-3101TQ-B 3101unecritinib fumarate