Preferred Label : Polyethyleneglycol-7-ethyl-10-hydroxycamptothecin DFP-13318;
NCIt synonyms : Ultra-Long-Acting-PEG-SN-38; Polyethyleneglycol-7-ethyl-10-hydroxycamptothecin; PEG SN38 DFP-13318; Ultra-long Acting PEG-SN38;
NCIt definition : A long-acting formulation composed of 7-ethyl-10-hydroxycamptothecin (SN38), a camptothecin
derivative and active metabolite of irinotecan conjugated to polyethylene glycol (PEG),
via a proprietary, cleavable linker, with potential antineoplastic activity. Upon
administration, the proprietary linkage system allows for very slow release of SN38
from the formulation. Upon release, SN38 selectively stabilizes covalent topoisomerase
I-DNA complexes, and results in single-stranded and double-stranded DNA breaks, the
inhibition of DNA replication, and the induction of apoptosis. This agent is designed
to deliver the active metabolite to tumor cells without the need for conversion as
is the case with irinotecan. Compared to other PEG-SN38-based formulations, the linker
system in DFP-13318 increases its half-life and the exposure time for tumor cells,
while decreasing both blood plasma concentrations and exposure to off-target organs;
this results in increased efficacy.;
Molecule name : PLX-0264; PL-0264; DFP-13318; PL 0264;
NCI Metathesaurus CUI : CL504040;
Origin ID : C125243;
UMLS CUI : C4085571;
Semantic type(s)
- chemical_or_drug_affects_gene_product
- chemical_or_drug_has_mechanism_of_action
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
