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Version: 17.12d (Release date: 2017-12-26)
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Etirinotecan Pegol (Code C74069)

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Terms & Properties

Preferred Name: Etirinotecan Pegol

Definition: An extended-release (ER) formulation composed of irinotecan, which is a semisynthetic derivative of camptothecin and a topoisomerase I-inhibitor prodrug, that is conjugated, via a proprietary biodegradable ester-based linker, to polyethylene glycol (PEG), with antineoplastic activity. Upon administration of etirinotecan pegol (EP), the agent penetrates into the leaky tumor vasculature and accumulates in the tumor. The linker slowly hydrolyzes and releases irinotecan, which leads to sustained exposure of the tumor to irinotecan. In turn, irinotecan is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN38) by a carboxylesterase. SN38 inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA; this results in DNA breaks that inhibit DNA replication and trigger apoptosis. Pegylation provides improved systemic exposure, increases drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic effects while lowering the toxicity profile.

Display Name: Etirinotecan Pegol

Label: Etirinotecan Pegol

NCI Thesaurus Code: C74069 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3659087  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Etirinotecan Pegol
NKTR 102

External Source Codes: 
CAS Registry Number 848779-32-8 (see NLM ChemIDplus info)
PDQ Closed Trial Search ID 586949
PDQ Open Trial Search ID 586949 (check for NCI PDQ open clinical trial info)
UMLS CUI C3659087

Other Properties:
     Name Value (qualifiers indented underneath)
code C74069
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name Pegylated_Irinotecan_NKTR_102
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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