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Version: 17.06d (Release date: 2017-06-26)
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Gimatecan (Code C65804)

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Terms & Properties

Preferred Name: Gimatecan

Definition: An orally bioavailable, semi-synthetic lipophilic analogue of camptothecin, a quinoline alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic and antiangiogenic activities. Gimatecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Although the mechanism of its antiangiogenic activity has yet to be full elucidated, this agent may inhibit endothelial cell migration, tumor neovascularization, and the expression of proangiogenic basic fibroblast growth factor (bFGF).

NCI-GLOSS Definition: A substance that is being studied in the treatment of cancer. It belongs to the family of drugs called topoisomerase inhibitors.

Display Name: Gimatecan

Label: Gimatecan

NCI Thesaurus Code: C65804 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C0969276  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
7-t-Butoxyiminomethylcamptothecin
Gimatecan
gimatecan
GIMATECAN
LBQ707
ST1481
STI481

External Source Codes: 
CAS Registry Number 292618-32-7 (see NLM ChemIDplus info)
FDA UNII Code 7KKS9R192F
PDQ Closed Trial Search ID 537638
PDQ Open Trial Search ID 537638 (check for NCI PDQ open clinical trial info)
UMLS CUI C0969276

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C25H25N3O5
code C65804
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name Gimatecan
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C65804

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