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Version: 17.06d (Release date: 2017-06-26)
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Silatecan AR-67 (Code C64618)

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Terms & Properties

Preferred Name: Silatecan AR-67

Definition: A synthetic, highly lipophilic derivative of camptothecin, with potential antineoplastic and radiosensitizing activities. 7-tert-butyldimethylsilyl-10-hydroxycamptothecin binds to and stabilizes the topoisomerase I-DNA covalent complex. This inhibits the religation of topoisomerase I-mediated single-stranded DNA breaks and produces lethal double-stranded DNA breaks when encountered by the DNA replication machinery, thereby inhibiting DNA replication and inducing apoptosis. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active lactone structure to an inactive carboxylate form. Modifications on the E ring of camptothecin prevent binding of human serum albumin, which prefers the inactive carboxylate form, thereby enhancing the stability of the active lactone structure and resulting in prolonged agent activity. In addition, this agent sensitizes tumor cells toward radiation treatment.

Display Name: Silatecan AR-67

Label: Silatecan AR-67

NCI Thesaurus Code: C64618 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1955483  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Silatecan AR-67

External Source Codes: 
PDQ Closed Trial Search ID 522726
PDQ Open Trial Search ID 522726 (check for NCI PDQ open clinical trial info)
UMLS CUI C1955483

Other Properties:
     Name Value (qualifiers indented underneath)
code C64618
Contributing_Source CTRP
Legacy_Concept_Name _7-Tert-butyldimethylsilyl-10-hydroxycamptothecin
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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