AP26113 is an investigational oral inhibitor of anaplastic lymphoma kinase (ALK). AP26113 was internally discovered by ARIAD scientists, and targets unique genetic features of cancer cells.
ALK was first identified as a chromosomal rearrangement in anaplastic large-cell lymphoma (ALCL). Genetic studies indicate that abnormal expression of ALK is a key driver of certain types of non-small cell lung cancer (NSCLC) and neuroblastomas, as well as ALCL. Since ALK is generally not expressed in normal adult tissues, it represents a highly promising molecular target for cancer therapy.
AP26113 was designed to overcome mutation-based resistance, including the L1196M “gatekeeper” mutation and other resistance mutations which have been observed clinically in patients who initially responded to crizotinib and then relapsed.