MLchartDataset catalogue

anti-5T4/D-2102 antibody-drug conjugate ACR246

Term · Oncology and biomedicine · MLC-T-ONC-010108

An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed against the oncofetal antigen 5T4 and site-specifically conjugated, via a cleavable linker, to the cell penetrating cytotoxic agent and DNA topoisomerase I inhibitor D-2102, with potential antineoplastic activity. Upon administration of anti-5T4/D-2102 ADC ACR246, the anti-5T4 antibody moiety of ACR246 selectively binds to cells expressing 5T4. After internalization and cleavage within the tumor cell cytosol, the topoisomerase I inhibitor D-2102 is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in DNA damage, cell cycle arrest and apoptosis in tumor cells overexpressing 5T4. In addition, ACR246 induces a bystander effect, thereby killing neighboring tumor cells in the tumor environment (TME). 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types while its expression is limited in normal adult tissues; its expression is correlated with increased invasiveness.

Table 1. Record
IdentifierMLC-T-ONC-010108
FieldOncology and biomedicine
Synonymsanti-5T4 ADC ACR246; ADC ACR246; anti-5T4/D-2102 ADC ACR246
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-010108",
  "term": "anti-5T4/D-2102 antibody-drug conjugate ACR246",
  "field": "Oncology and biomedicine",
  "definition": "An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed against the oncofetal antigen 5T4 and site-specifically conjugated, via a cleavable linker, to the cell penetrating cytotoxic agent and DNA topoisomerase I inhibitor D-2102, with potential antineoplastic activity. Upon administration of anti-5T4/D-2102 ADC ACR246, the anti-5T4 antibody moiety of ACR246 selectively binds to cells expressing 5T4. After internalization and cleavage within the tumor cell cytosol, the topoisomerase I inhibitor D-2102 is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in DNA damage, cell cycle arrest and apoptosis in tumor cells overexpressing 5T4. In addition, ACR246 induces a bystander effect, thereby killing neighboring tumor cells in the tumor environment (TME). 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types while its expression is limited in normal adult tissues; its expression is correlated with increased invasiveness.",
  "synonyms": [
    "anti-5T4 ADC ACR246",
    "ADC ACR246",
    "anti-5T4/D-2102 ADC ACR246"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/anti-5t4-d-2102-antibody-drug-conjugate-acr246/"
}

Record 1,174 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.