A third ARIAD-discovered compound.
The latest candidate to enter ARIAD’s early-stage pipeline, AP26113, is a small-molecule anaplastic lymphoma kinase (ALK) inhibitor. Discovered by ARIAD scientists, this ALK inhibitor targets a unique genetic feature of cancer cells similar to AP24534.
ALK was first identified as a chromosomal rearrangement in anaplastic large cell lymphoma (ALCL). Genetic studies now indicate that abnormal expression of ALK is a key driver of certain types of non-small cell lung cancer and neuroblastomas, as well as ALCL. Since ALK is generally not expressed in normal adult tissues, it represents a highly promising target for molecularly targeted cancer therapy.
ARIAD scientists have identified multiple potent compounds that inhibit ALK both in vitro and in vivo while maintaining significant selectivity over the highly similar insulin-like growth factor-1 receptor and insulin receptor tyrosine kinase. ARIAD’s candidate is the lead compound in this class, potently inhibiting tumor cells that express ALK while having no effects on cells that do not express ALK. In addition, this compound is active when administered orally in in vivo animal models of lymphoma and lung cancer, with minimal effects on insulin or glucose levels.
Our candidate is based on proprietary ARIAD chemistry—with once-daily oral dosing and best-in-class promise, and the potential for patient identification to maximize clinical benefit.