NCIt definition : The adipate form of zeteletinib, an orally bioavailable selective inhibitor of wild-type,
fusion products and mutated forms, including gatekeeper mutations, of the proto-oncogene
receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic
activity. Upon oral administration, zeteletinib selectively binds to and inhibits
the activity of RET. This results in an inhibition of cell growth of tumors cells
that exhibit increased RET activity. RET overexpression, activating mutations, and
fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity
in various cancer cell types; dysregulation of RET activity plays a key role in the
development and progression of these cancers.;
Semantic type(s)