MLchartDataset catalogue

Ruzaltatug rezetecan

Term · Oncology and biomedicine · MLC-T-ONC-016608

An antibody-drug conjugate (ADC) composed of ruzaltatug, an immunoglobulin G1 (IgG1) human monoclonal antibody directed against human epidermal growth factor receptor 3 (HER3; ErbB3), conjugated, via a cleavable peptide linker, to rezetecan, an exatecan derivative and cytotoxic DNA topoisomerase I inhibitor, with potential antineoplastic activity. Upon administration of ruzaltatug rezetecan, the anti-HER3 antibody moiety targets and binds to HER3 expressed on tumor cells. Upon binding, internalization and linker cleavage, rezetecan targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA and resulting in DNA breaks, inhibition of DNA replication and apoptosis in HER3-expressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors.

Table 1. Record
IdentifierMLC-T-ONC-016608
FieldOncology and biomedicine
Synonymsanti-HER3 ADC SHR-A2009; anti-HER3 antibody-drug conjugate SHR-A2009
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-016608",
  "term": "Ruzaltatug rezetecan",
  "field": "Oncology and biomedicine",
  "definition": "An antibody-drug conjugate (ADC) composed of ruzaltatug, an immunoglobulin G1 (IgG1) human monoclonal antibody directed against human epidermal growth factor receptor 3 (HER3; ErbB3), conjugated, via a cleavable peptide linker, to rezetecan, an exatecan derivative and cytotoxic DNA topoisomerase I inhibitor, with potential antineoplastic activity. Upon administration of ruzaltatug rezetecan, the anti-HER3 antibody moiety targets and binds to HER3 expressed on tumor cells. Upon binding, internalization and linker cleavage, rezetecan targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA and resulting in DNA breaks, inhibition of DNA replication and apoptosis in HER3-expressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors.",
  "synonyms": [
    "anti-HER3 ADC SHR-A2009",
    "anti-HER3 antibody-drug conjugate SHR-A2009"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/ruzaltatug-rezetecan/"
}

Record 14,616 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.