TPX-0131 is a next-generation ALK inhibitor entering IND-enabling studies. 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.
Multiple FDA-approved ALK inhibitors are available to patients for the treatment of ALK+ non-small cell lung cancer (NSCLC), yet none are approved to treat solvent-front mutations that lead to drug resistance.
Targeting Known Mechanisms of Resistance
ALK-driven tumors are estimated to represent up to 7 percent of driver oncogenes in NSCLC and of patients who develop a resistance mutation, G1202R has been reported in approximately 42 percent.