Preferred Label : RET Inhibitor TY-1091;
NCIt definition : An orally bioavailable, selective, second-generation inhibitor of the proto-oncogene
receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic
activity. Upon oral administration, RET inhibitor TY-1091 selectively targets and
binds to wild-type RET and various RET fusions and mutations, including, but not limited
to solvent front and gatekeeper mutations RET G810S, RET V804M/L/E, RET V804M/G810S
and M918T/G810S, thereby inhibiting the activity of RET. This results in an inhibition
of cell growth of tumors that exhibit increased RET activity due to these fusions
and mutations. RET overexpression, activating mutations, and fusions result in the
upregulation and/or overactivation of RET tyrosine kinase activity in various cancer
cell types. Dysregulated RET activity plays a key role in the development and progression
of certain cancers. Solvent front and gatekeeper resistance mutations play a key role
in acquired tumor resistance to RET inhibitors.;
Molecule name : TY-1091; TY 1091;
NCI Metathesaurus CUI : CL1906242;
Origin ID : C199307;
concept_is_in_subset
- has_target
