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- NCIT_C189067 IAO_0000115 "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)." @default.
- NCIT_C189067 NCIT_A7 NCIT_C18539 @default.
- NCIT_C189067 NCIT_NHC0 "C189067" @default.
- NCIT_C189067 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C189067 NCIT_P107 "RET Inhibitor EP0031" @default.
- NCIT_C189067 NCIT_P108 "RET Inhibitor EP0031" @default.
- NCIT_C189067 NCIT_P208 "CL1794262" @default.
- NCIT_C189067 NCIT_P322 "CTRP" @default.
- NCIT_C189067 NCIT_P322 "GDC" @default.
- NCIT_C189067 NCIT_P399 "810266" @default.
- NCIT_C189067 normalizedInformationContent "100" @default.
- NCIT_C189067 referenceCount "1" @default.
- NCIT_C189067 hasExactSynonym "A 400" @default.
- NCIT_C189067 hasExactSynonym "A-400" @default.
- NCIT_C189067 hasExactSynonym "A400" @default.
- NCIT_C189067 hasExactSynonym "EP 0031" @default.
- NCIT_C189067 hasExactSynonym "EP-0031" @default.
- NCIT_C189067 hasExactSynonym "EP0031" @default.
- NCIT_C189067 hasExactSynonym "RET Inhibitor EP0031" @default.
- NCIT_C189067 hasExactSynonym "SRI EP0031" @default.
- NCIT_C189067 hasExactSynonym "Selective RET Inhibitor EP0031" @default.
- NCIT_C189067 inSubset NCIT_C116977 @default.
- NCIT_C189067 inSubset NCIT_C116978 @default.
- NCIT_C189067 inSubset NCIT_C128784 @default.
- NCIT_C189067 inSubset NCIT_C157711 @default.
- NCIT_C189067 inSubset NCIT_C157712 @default.
- NCIT_C189067 inSubset NCIT_C176424 @default.
- NCIT_C189067 type Class @default.
- NCIT_C189067 isDefinedBy ncit.owl @default.
- NCIT_C189067 label "RET Inhibitor EP0031" @default.
- NCIT_C189067 subClassOf NCIT_C129824 @default.
- NCIT_C189067 subClassOf NCIT_C129825 @default.
- NCIT_C189067 subClassOf NCIT_C1404 @default.
- NCIT_C189067 subClassOf NCIT_C159438 @default.
- NCIT_C189067 subClassOf NCIT_C163758 @default.
- NCIT_C189067 subClassOf NCIT_C189067 @default.
- NCIT_C189067 subClassOf NCIT_C1908 @default.
- NCIT_C189067 subClassOf NCIT_C1909 @default.
- NCIT_C189067 subClassOf NCIT_C1967 @default.
- NCIT_C189067 subClassOf NCIT_C2189 @default.
- NCIT_C189067 subClassOf NCIT_C274 @default.
- NCIT_C189067 subClassOf NCIT_C471 @default.