Preferred Label : Polymeric Nanoparticle-conjugated Camptothecin DAN-222;
NCIt synonyms : Polymeric Nanoparticles DAN-222; Polymeric Nanoparticle-containing Camptothecin DAN-222;
NCIt definition : A polymeric nanoparticle formulation of the topoisomerase I inhibitor camptothecin
(CPT), an alkaloid isolated from the Chinese tree Camptotheca acuminata, covalently
conjugated, via a linker, to a biocompatible polymer scaffold, with potential antineoplastic
activity. Upon intravenous administration of polymeric nanoparticle-conjugated CPT
DAN-222, the nanoparticles accumulate in tumor tissue and CPT is released from the
formulation at the tumor site and taken up by tumor cells. During the S phase of the
cell cycle, CPT selectively stabilizes topoisomerase I-DNA covalent complexes, thereby
inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing
potentially lethal double-strand DNA breaks when encountered by the DNA replication
machinery. Compared to CPT alone, the nanoparticle formulation has a prolonged half-life
and greatly improves the biodistribution of CPT resulting in an accumulation of CPT
at the tumor site, which enhances tumor exposure while greatly reducing toxic side
effects.;
Molecule name : DAN-222; DAN 222;
NCI Metathesaurus CUI : CL1792032;
Origin ID : C187116;
UMLS CUI : C5706363;
Semantic type(s)
- concept_is_in_subset
- has_target
