TPX-0131

TPX-0131 is a next-generation ALK inhibitor drug candidate currently being evaluated in our Phase 1/2 FORGE-1 clinical trial of patients with ALK+ advanced non-small lung cancer (NSCLC). It has been designed with a novel compact macrocyclic structure and has shown preclinical potent inhibition of wildtype and numerous ALK mutations, including the clinically observed G1202R solvent-front mutation and the G1202R/L1196M compound mutation.

What are the latest updates on TPX-0131?

TPX-0131, a Potent Inhibitor of Wild Type ALK and a Broad Spectrum of Both Single and Compound ALK Resistance Mutations. AACR 2021

Designed to be Different.

TPX-0131 inhibits Anaplastic Lymphoma Kinase (ALK). Rearrangements of ALK can lead to cancer growth and proliferation. Multiple FDA-approved ALK inhibitors are available to patients for the treatment of ALK+ NSCLC, yet none are active against a broad spectrum of resistant mutations (i.e., solvent front, gatekeeper and compound).

ALK-driven tumors are estimated to represent 3-5% percent of driver oncogenes in NSCLC, and of patients who develop a resistance mutation, G1202R has been reported in approximately 42 percent of NSCLC patients.