NCIt definition : An orally available, small molecule inhibitor of the receptor tyrosine kinase anaplastic
lymphoma kinase (ALK), with potential antineoplastic activity. Upon oral administration,
ASP3026 binds to and inhibits ALK tyrosine kinase, ALK fusion proteins and ALK point
mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling
and the inhibition of cell growth in ALK-expressing tumor cells. ALK belongs to the
insulin receptor superfamily and plays an important role in nervous system development.
ALK is not expressed in healthy adult human tissue but ALK dysregulation and gene
rearrangements are associated with a series of tumors. Additionally, ALK mutations
are associated with acquired resistance to small molecule tyrosine kinase inhibitors.;