MLchartDataset catalogue

anti-TROP-2 antibody-drug conjugate PF-06664178

Term · Oncology and biomedicine · MLC-T-ONC-011159

An antibody-drug conjugate (ADC) composed of PF-06478924 (RN926), a humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1), site-specifically conjugated via a valine-citrulline cleavable linker with the auristatin-based cytotoxic agent Aur0101 (PF-06380101), with potential antineoplastic activity. Upon administration of anti-TROP-2 ADC PF-06664178, the anti-TROP-2 monoclonal antibody moiety PF-06478924 targets and binds to TROP-2 expressed on tumor cells. Upon binding, internalization and linker cleavage, Aur0101 binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and apoptosis of TROP-2-expressing tumor cells. TROP-2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.

Table 1. Record
IdentifierMLC-T-ONC-011159
FieldOncology and biomedicine
Synonymsanti-TROP-2 ADC PF-06664178; anti-TROP-2/Aur0101 ADC PF-06664178
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-011159",
  "term": "anti-TROP-2 antibody-drug conjugate PF-06664178",
  "field": "Oncology and biomedicine",
  "definition": "An antibody-drug conjugate (ADC) composed of PF-06478924 (RN926), a humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1), site-specifically conjugated via a valine-citrulline cleavable linker with the auristatin-based cytotoxic agent Aur0101 (PF-06380101), with potential antineoplastic activity. Upon administration of anti-TROP-2 ADC PF-06664178, the anti-TROP-2 monoclonal antibody moiety PF-06478924 targets and binds to TROP-2 expressed on tumor cells. Upon binding, internalization and linker cleavage, Aur0101 binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and apoptosis of TROP-2-expressing tumor cells. TROP-2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.",
  "synonyms": [
    "anti-TROP-2 ADC PF-06664178",
    "anti-TROP-2/Aur0101 ADC PF-06664178"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/anti-trop-2-antibody-drug-conjugate-pf-06664178/"
}

Record 2,306 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.