1363TiP A phase I/II study of TPX-0131, a novel oral ALK tyrosine kinase inhibitor, in patients with ALK+ advanced/metastatic NSCLC

TPX-0131 is a next-generation ALK tyrosine kinase inhibitor (TKI) designed to overcome a broad array of mutations that can limit the effectiveness of previous generation ALK TKIs. In cellular assays, TPX-0131 potently inhibits wild-type ALK (IC50 = 0.4 nM) and many clinically observed resistance mutations, including the G1202R solvent front mutation (IC50 = 0.2 nM), L1196M gatekeeper mutation (IC50 = 0.5 nM) and multiple compound mutations (IC50 < 1 nM). In vivo studies show brain tissue penetration.