MLchartDataset catalogue

PSMA-targeted tubulysin B-containing conjugate EC1169

Term · Oncology and biomedicine · MLC-T-ONC-016284

An injectable, water soluble, small molecule drug conjugate (SMDC) containing a ligand specific for prostate-specific membrane antigen (PSMA), conjugated via a stable, enzyme-cleavable linker to the cytotoxic agent tubulysin B hydrazide (TubBH), with potential antineoplastic activity. Upon administration of PSMA-targeted tubulysin B-containing conjugate EC1169, the PSMA ligand specifically targets and binds to PSMA, a protein which is abundantly expressed on the surface of metastatic and hormone-refractory prostate cancer cells as well as on the neovasculature of many solid tumors. This allows for the specific delivery of TubBH to PSMA-expressing cancer cells. Upon internalization and cleavage, tubulysin B binds to tubulin and inhibits microtubule polymerization, which blocks cell division and results in G2/M phase arrest, tumor cell apoptosis and a decrease in PSMA-expressing tumor cells.

Table 1. Record
IdentifierMLC-T-ONC-016284
FieldOncology and biomedicine
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-016284",
  "term": "PSMA-targeted tubulysin B-containing conjugate EC1169",
  "field": "Oncology and biomedicine",
  "definition": "An injectable, water soluble, small molecule drug conjugate (SMDC) containing a ligand specific for prostate-specific membrane antigen (PSMA), conjugated via a stable, enzyme-cleavable linker to the cytotoxic agent tubulysin B hydrazide (TubBH), with potential antineoplastic activity. Upon administration of PSMA-targeted tubulysin B-containing conjugate EC1169, the PSMA ligand specifically targets and binds to PSMA, a protein which is abundantly expressed on the surface of metastatic and hormone-refractory prostate cancer cells as well as on the neovasculature of many solid tumors. This allows for the specific delivery of TubBH to PSMA-expressing cancer cells. Upon internalization and cleavage, tubulysin B binds to tubulin and inhibits microtubule polymerization, which blocks cell division and results in G2/M phase arrest, tumor cell apoptosis and a decrease in PSMA-expressing tumor cells.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/psma-targeted-tubulysin-b-containing-conjugate-ec1169/"
}

Record 13,822 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.