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- NCIT_C187037 IAO_0000115 "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." @default.
- NCIT_C187037 NCIT_A7 NCIT_C18539 @default.
- NCIT_C187037 NCIT_NHC0 "C187037" @default.
- NCIT_C187037 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C187037 NCIT_P107 "RET Inhibitor LOXO-260" @default.
- NCIT_C187037 NCIT_P108 "RET Inhibitor LOXO-260" @default.
- NCIT_C187037 NCIT_P208 "CL1779247" @default.
- NCIT_C187037 NCIT_P322 "CTRP" @default.
- NCIT_C187037 NCIT_P322 "GDC" @default.
- NCIT_C187037 NCIT_P399 "809262" @default.
- NCIT_C187037 normalizedInformationContent "100" @default.
- NCIT_C187037 referenceCount "1" @default.
- NCIT_C187037 hasExactSynonym "LOX-19260" @default.
- NCIT_C187037 hasExactSynonym "LOXO 260" @default.
- NCIT_C187037 hasExactSynonym "LOXO-260" @default.
- NCIT_C187037 hasExactSynonym "LOXO260" @default.
- NCIT_C187037 hasExactSynonym "LY3838915" @default.
- NCIT_C187037 hasExactSynonym "RET Inhibitor LOXO-260" @default.
- NCIT_C187037 inSubset NCIT_C116977 @default.
- NCIT_C187037 inSubset NCIT_C116978 @default.
- NCIT_C187037 inSubset NCIT_C128784 @default.
- NCIT_C187037 inSubset NCIT_C157711 @default.
- NCIT_C187037 inSubset NCIT_C157712 @default.
- NCIT_C187037 inSubset NCIT_C176424 @default.
- NCIT_C187037 type Class @default.
- NCIT_C187037 isDefinedBy ncit.owl @default.
- NCIT_C187037 label "RET Inhibitor LOXO-260" @default.
- NCIT_C187037 subClassOf NCIT_C129824 @default.
- NCIT_C187037 subClassOf NCIT_C129825 @default.
- NCIT_C187037 subClassOf NCIT_C1404 @default.
- NCIT_C187037 subClassOf NCIT_C159438 @default.
- NCIT_C187037 subClassOf NCIT_C163758 @default.
- NCIT_C187037 subClassOf NCIT_C187037 @default.
- NCIT_C187037 subClassOf NCIT_C1908 @default.
- NCIT_C187037 subClassOf NCIT_C1909 @default.
- NCIT_C187037 subClassOf NCIT_C1967 @default.
- NCIT_C187037 subClassOf NCIT_C2189 @default.
- NCIT_C187037 subClassOf NCIT_C274 @default.
- NCIT_C187037 subClassOf NCIT_C471 @default.