Preferred Label : Davamotecan Pegadexamer;
NCIt synonyms : Camptothecin-Polymer Conjugate IT-101; Cyclodextrin-Based Polymer-Camptothecin; Cyclodextrin-Based Polymer-Camptothecin CRLX101; Linear Cyclodextrin-cysteine-PEG Based Polymer Conjugate of Camptothecin;
NCIt definition : A formulation of camptothecin, an alkaloid isolated from the Chinese tree Camptotheca
acuminata, conjugated with to a hydrophilic, cyclodextrin-based linear polymer with
potential antineoplastic activity. Upon intravenous administration of davamotecan
pegadexamer, camptothecin is slowly released from the formulation at the tumor site
and taken up by tumor cells. During the S phase of the cell cycle, camptothecin 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 camptothecin alone, the cyclodextrin-based polymer formulation has a prolonged
half life and greatly improves the biodistribution of camptothecin resulting in an
accumulation of camptothecin at the tumor site, which enhances tumor exposure while
greatly reducing toxic side effects. In addition, cyclodextrin-based polymer-camptothecin
may be able to overcome certain kinds of multidrug resistance.;
UNII : NFH8D7ZGF5;
CAS number : 1883668-61-8; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1883668-61-8
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G-SRS /a ;
Molecule name : IT-101; CRLX101; EP0057;
Origin ID : C62600;
UMLS CUI : C5557434;
Semantic type(s)
- concept_is_in_subset
- has_target
