MLchartDataset catalogue

davamotecan pegadexamer

Term · Oncology and biomedicine · MLC-T-ONC-012934

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.

Table 1. Record
IdentifierMLC-T-ONC-012934
FieldOncology and biomedicine
Synonymscamptothecin-polymer conjugate IT-101; cyclodextrin-based polymer-camptothecin CRLX101; linear cyclodextrin-cysteine-PEG based polymer conjugate of camptothecin
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-012934",
  "term": "davamotecan pegadexamer",
  "field": "Oncology and biomedicine",
  "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.",
  "synonyms": [
    "camptothecin-polymer conjugate IT-101",
    "cyclodextrin-based polymer-camptothecin CRLX101",
    "linear cyclodextrin-cysteine-PEG based polymer conjugate of camptothecin"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/davamotecan-pegadexamer/"
}

Record 5,720 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.