NCIt definition : The hydrochloride salt form of ensartinib, 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.;