Pegylated Liposomal Irinotecan

Preferred Label : Pegylated Liposomal Irinotecan;

NCIt synonyms : Liposomal Irinotecan;

NCIt definition : A formulation of polyethylene glycol (PEG)-modified liposomes encapsulating the semisynthetic derivative of camptothecin irinotecan, with antineoplastic activity. As a prodrug, irinotecan is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. In turn, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA, resulting in DNA breaks. This results in an inhibition of DNA replication and an induction of apoptosis. Pegylated liposomal delivery of irinotecan improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of exposure while lowering systemic toxicity.;

Molecule name : IHL-305;

Details

Origin ID

C62789;

UMLS CUI

C1881411;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
Validated automatic mappings to NTBT
- Irinotecan liposome (substance) [SNOMED CT concept]
chemical_or_drug_affects_gene_product
- DNA Topoisomerase 1 [NCIt concept]
chemical_or_drug_has_mechanism_of_action
- Enzyme Inhibition [NCIt concept]
chemical_or_drug_has_physiologic_effect
- Apoptosis [NCIt concept]
- DNA Replication Inhibition [NCIt concept]
- DNA Strand Break [NCIt concept]
- RNA Transcription Inhibition [NCIt concept]
chemical_or_drug_is_metabolized_by_enzyme
- Cytochrome P450 3A4 [NCIt concept]
- Cytochrome P450 3A5 [NCIt concept]
- Cytochrome P450 3A7 [NCIt concept]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP Terminology [NCIt concept]
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- GDC Value Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- DNA Topoisomerase 1 [NCIt concept]

Keyword's position in hierarchy(ies) :

Main resources

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