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- NCIT_C151953 IAO_0000115 "A miniature drug conjugate composed of the irinotecan metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) conjugated, through a cleavable linker, to a ligand of chaperone protein heat shock protein 90 (Hsp90), with potential antineoplastic activity. Upon administration of locnartecan, the HSP90 ligand moiety targets HSP90, which allows the conjugate to penetrate, accumulate and be retained in the tumor cell. Once the linker is cleaved, the SN-38 moiety is released in a sustained manner. SN-38 then binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, which results in DNA breaks, inhibition of DNA replication and apoptosis. Compared to SN-38 alone, locnartecan preferentially targets, accumulates and is retained in the tumor cells due to its binding to Hsp90, which results in increased concentrations of SN-38 at the tumor site. This allows sustained release of SN-38 and leads to increased and prolonged efficacy while reducing toxicity to normal, healthy tissues. Hsp90, a chaperone protein upregulated and activated in a variety of tumor cells compared to normal healthy tissue, regulates the folding, stability and degradation of many oncogenic signaling proteins." @default.
- NCIT_C151953 NCIT_A32 NCIT_C1909 @default.
- NCIT_C151953 NCIT_A7 NCIT_C17766 @default.
- NCIT_C151953 NCIT_NHC0 "C151953" @default.
- NCIT_C151953 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C151953 NCIT_P107 "Locnartecan" @default.
- NCIT_C151953 NCIT_P108 "Locnartecan" @default.
- NCIT_C151953 NCIT_P208 "CL601355" @default.
- NCIT_C151953 NCIT_P210 "1472614-83-7" @default.
- NCIT_C151953 NCIT_P319 "56DL1J49LR" @default.
- NCIT_C151953 NCIT_P322 "CTRP" @default.
- NCIT_C151953 NCIT_P322 "FDA" @default.
- NCIT_C151953 NCIT_P322 "GDC" @default.
- NCIT_C151953 NCIT_P329 "793183" @default.
- NCIT_C151953 NCIT_P330 "793183" @default.
- NCIT_C151953 NCIT_P375 "HSP90-targeted SN-38 Conjugate PEN-866" @default.
- NCIT_C151953 NCIT_P399 "793183" @default.
- NCIT_C151953 normalizedInformationContent "100" @default.
- NCIT_C151953 referenceCount "1" @default.
- NCIT_C151953 hasExactSynonym "HDC SN-38" @default.
- NCIT_C151953 hasExactSynonym "HSP90-targeted SN-38 Conjugate PEN-866" @default.
- NCIT_C151953 hasExactSynonym "LOCNARTECAN" @default.
- NCIT_C151953 hasExactSynonym "Locnartecan" @default.
- NCIT_C151953 hasExactSynonym "PEN 866" @default.
- NCIT_C151953 hasExactSynonym "PEN-866" @default.
- NCIT_C151953 hasExactSynonym "PEN866" @default.
- NCIT_C151953 hasExactSynonym "STA-12-8666" @default.
- NCIT_C151953 hasExactSynonym "STA-8666" @default.
- NCIT_C151953 inSubset NCIT_C116977 @default.
- NCIT_C151953 inSubset NCIT_C116978 @default.
- NCIT_C151953 inSubset NCIT_C128784 @default.
- NCIT_C151953 inSubset NCIT_C157711 @default.
- NCIT_C151953 inSubset NCIT_C157712 @default.
- NCIT_C151953 inSubset NCIT_C176424 @default.
- NCIT_C151953 inSubset NCIT_C177537 @default.
- NCIT_C151953 inSubset NCIT_C63923 @default.
- NCIT_C151953 type Class @default.
- NCIT_C151953 isDefinedBy ncit.owl @default.
- NCIT_C151953 label "Locnartecan" @default.
- NCIT_C151953 subClassOf NCIT_C129824 @default.
- NCIT_C151953 subClassOf NCIT_C129825 @default.
- NCIT_C151953 subClassOf NCIT_C151953 @default.
- NCIT_C151953 subClassOf NCIT_C1748 @default.
- NCIT_C151953 subClassOf NCIT_C1904 @default.
- NCIT_C151953 subClassOf NCIT_C1908 @default.
- NCIT_C151953 subClassOf NCIT_C1909 @default.
- NCIT_C151953 subClassOf NCIT_C2189 @default.
- NCIT_C151953 subClassOf NCIT_C274 @default.
- NCIT_C151953 subClassOf NCIT_C471 @default.