Preferred Label : RET Inhibitor EP0031;
NCIt synonyms : SRI EP0031; Selective RET Inhibitor EP0031;
NCIt definition : An orally bioavailable selective inhibitor of the proto-oncogene receptor tyrosine
kinase rearranged during transfection (RET), with potential antineoplastic activity.
Upon oral administration, RET inhibitor EP0031 selectively binds to various RET fusions
and mutations, including solvent front resistance mutations, and inhibits 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. EP0031 is able to penetrate
the blood-brain barrier (BBB) and may also be able to overcome resistance mechanisms
to first generation selective RET inhibitors (SRIs).;
Molecule name : A-400; EP 0031; EP-0031; A 400;
NCI Metathesaurus CUI : CL1794262;
Origin ID : C189067;
UMLS CUI : C5706535;
Semantic type(s)
- concept_is_in_subset
- has_target
