Preferred Label : RET Inhibitor LOXO-260;
NCIt definition : An orally bioavailable selective inhibitor of fusion products and mutated forms of
the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET),
with potential antineoplastic activity. Upon oral administration, the RET inhibitor
LOXO-260 selectively binds to and inhibits the activity of RET, including the RET
V804 gatekeeper and the G810 solvent-front mutations. This results in an inhibition
of cell growth of susceptible 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.
Solvent front and gatekeeper resistance mutations, both individually and when co-expressed,
play a key role in acquired tumor resistance to RET inhibitors.;
Molecule name : LY3838915; LOXO-260; LOX-19260; LOXO 260;
NCI Metathesaurus CUI : CL1779247;
Origin ID : C187037;
UMLS CUI : C5667097;
Semantic type(s)
- concept_is_in_subset
- has_target
