NCIt definition : An orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic
lymphoma kinase (ALK), with potential antineoplastic activity. Upon oral administration,
ensartinib binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation
variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and
eventually inhibits tumor cell growth in ALK-expressing tumor cells. In addition,
ensartinib inhibits various other kinases, including the receptor tyrosine kinase
c-Met (hepatocyte growth factor receptor; HGFR; MET) and the receptor tyrosine kinase
C-ros oncogene 1 (ROS1). 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; ALK mutations are associated with acquired resistance to small molecule
tyrosine kinase inhibitors.;