zotizalkib

Zotizalkib (TPX-0131) is a next-generation, orally available, compact macrocyclic small molecule inhibitor of anaplastic lymphoma kinase (ALK). It was designed to be brain-penetrant and to inhibit both wild-type ALK and a broad spectrum of clinically relevant ALK resistance mutations, including the G1202R solvent front mutation and L1196M gatekeeper mutation. Preclinical studies demonstrated superior potency compared to all five approved ALK inhibitors against wild-type and mutant forms of ALK. The drug was developed for use in patients with advanced or metastatic non-small cell lung cancer (NSCLC) who have previously been treated with other ALK tyrosine kinase inhibitors[1][3][6]. Developed by Turning Point Therapeutics (now part of Bristol-Myers Squibb), clinical development included Phase 1/2 trials but was terminated due to an adverse change in the risk/benefit ratio[3].

Other names

zotizalkibTPX-0131TPX0131TPX 0131