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anti-HER2 antibody-drug conjugate FDA022-BB05

Term · Oncology and biomedicine · MLC-T-ONC-010740

An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated, via a valine-alanine (Val-Ala)-based cathepsin B-cleavable linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration, anti-HER2 ADC FDA022-BB05 targets and binds to HER2 expressed on tumor cells. Upon binding, internalization, and linker cleavage, DXd is released. DXd inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of HER2-expressing tumor cells. FDA022-BB05 is also able to induce a bystander effect on neighboring cells in the tumor environment. This further inhibits the proliferation of tumor cells. HER2, a receptor tyrosine kinase that is mutated or overexpressed in many tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization.

Table 1. Record
IdentifierMLC-T-ONC-010740
FieldOncology and biomedicine
SynonymsADC FDA022-BB05; anti-HER2 ADC FDA022-BB05; trastuzumab/DXd ADC FDA022-BB05
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-010740",
  "term": "anti-HER2 antibody-drug conjugate FDA022-BB05",
  "field": "Oncology and biomedicine",
  "definition": "An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated, via a valine-alanine (Val-Ala)-based cathepsin B-cleavable linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration, anti-HER2 ADC FDA022-BB05 targets and binds to HER2 expressed on tumor cells. Upon binding, internalization, and linker cleavage, DXd is released. DXd inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of HER2-expressing tumor cells. FDA022-BB05 is also able to induce a bystander effect on neighboring cells in the tumor environment. This further inhibits the proliferation of tumor cells. HER2, a receptor tyrosine kinase that is mutated or overexpressed in many tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization.",
  "synonyms": [
    "ADC FDA022-BB05",
    "anti-HER2 ADC FDA022-BB05",
    "trastuzumab/DXd ADC FDA022-BB05"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/anti-her2-antibody-drug-conjugate-fda022-bb05/"
}

Record 1,848 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.