About: Cyclodextrin-Based Polymer-Camptothecin CRLX101     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Cyclodextrin-Based Polymer-Camptothecin CRLX101
rdfs:subClassOf
Semantic_Type
  • Organic Chemical
  • Pharmacologic Substance
Preferred_Name
  • Cyclodextrin-Based Polymer-Camptothecin CRLX101
UMLS_CUI
  • C1831896
PDQ_Open_Trial_Search_ID
  • 489507
PDQ_Closed_Trial_Search_ID
  • 489507
Legacy_Concept_Name
  • Cyclodextrin-Based_Polymer-Camptothecin
FULL_SYN
  • Camptothecin-Polymer Conjugate IT-101SYNCI
  • Cyclodextrin-Based Polymer-Camptothecin CRLX101PTNCI
  • IT-101CNNCI
  • CRLX101CNNCI
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, 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.NCI
code
  • C62600
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