MLchartDataset catalogue

anti-FRalpha/exatecan ADC LY4170156

Term · Oncology and biomedicine · MLC-T-ONC-010673

An antibody-drug conjugate (ADC) composed of a Fc-silenced, humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting folate receptor alpha (FRa; FolRa; FOLR1) linked, via a dipeptide cleavable linker and a polysarcosine hydrophobicity masking agent, to the camptothecin analog and topoisomerase 1 inhibitor exatecan, with potential antineoplastic activity. Upon administration of anti-FRalpha/exatecan ADC LY4170156, the antibody moiety targets and binds to FRa expressed on tumor cells. Upon binding, cellular uptake and linker cleavage, exatecan is released. Exatecan inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and generating DNA single- and double-strand breaks. This leads to cell cycle arrest and tumor cell apoptosis. In addition, exatecan is able to induce a bystander effect on neighboring cells in the tumor environment. This inhibits the proliferation of FRa-expressing tumor cells. FRa is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its expression is limited in normal tissues.

Table 1. Record
IdentifierMLC-T-ONC-010673
FieldOncology and biomedicine
SynonymsADC LY4170156; anti-FRa ADC LY4170156; antibody-drug conjugate LY4170156
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-010673",
  "term": "anti-FRalpha/exatecan ADC LY4170156",
  "field": "Oncology and biomedicine",
  "definition": "An antibody-drug conjugate (ADC) composed of a Fc-silenced, humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting folate receptor alpha (FRa; FolRa; FOLR1) linked, via a dipeptide cleavable linker and a polysarcosine hydrophobicity masking agent, to the camptothecin analog and topoisomerase 1 inhibitor exatecan, with potential antineoplastic activity. Upon administration of anti-FRalpha/exatecan ADC LY4170156, the antibody moiety targets and binds to FRa expressed on tumor cells. Upon binding, cellular uptake and linker cleavage, exatecan is released. Exatecan inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and generating DNA single- and double-strand breaks. This leads to cell cycle arrest and tumor cell apoptosis. In addition, exatecan is able to induce a bystander effect on neighboring cells in the tumor environment. This inhibits the proliferation of FRa-expressing tumor cells. FRa is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its expression is limited in normal tissues.",
  "synonyms": [
    "ADC LY4170156",
    "anti-FRa ADC LY4170156",
    "antibody-drug conjugate LY4170156"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/anti-fralpha-exatecan-adc-ly4170156/"
}

Record 1,775 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.