MLchartDataset catalogue

nendratareotide uzatansine

Term · Oncology and biomedicine · MLC-T-ONC-015468

A miniaturized drug conjugate composed of a peptide analog of somatostatin that targets the somatostatin receptor 2 (SSTR2) and is conjugated, through a cleavable linker, to the microtubule-binding cytotoxic maytansinoid DM1 (mertansine), with potential anti-tumor activity. Upon administration, the peptide ligand moiety of nendratareotide uzatansine targets and binds to SSTR2, which is overexpressed on certain tumor cell types. Binding stimulates SSTR2-mediated endocytosis of the agent; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics. This inhibits both cell division and the proliferation of SSTR2-expressing cancer cells. Compared to antibody-drug conjugates (ADCs), miniaturized drug conjugates are much smaller and can more easily penetrate and distribute in dense tumor tissue.

Table 1. Record
IdentifierMLC-T-ONC-015468
FieldOncology and biomedicine
SynonymsSSTR2-targeting protein/DM1 conjugate PEN-221
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-015468",
  "term": "nendratareotide uzatansine",
  "field": "Oncology and biomedicine",
  "definition": "A miniaturized drug conjugate composed of a peptide analog of somatostatin that targets the somatostatin receptor 2 (SSTR2) and is conjugated, through a cleavable linker, to the microtubule-binding cytotoxic maytansinoid DM1 (mertansine), with potential anti-tumor activity. Upon administration, the peptide ligand moiety of nendratareotide uzatansine targets and binds to SSTR2, which is overexpressed on certain tumor cell types. Binding stimulates SSTR2-mediated endocytosis of the agent; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics. This inhibits both cell division and the proliferation of SSTR2-expressing cancer cells. Compared to antibody-drug conjugates (ADCs), miniaturized drug conjugates are much smaller and can more easily penetrate and distribute in dense tumor tissue.",
  "synonyms": [
    "SSTR2-targeting protein/DM1 conjugate PEN-221"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/nendratareotide-uzatansine/"
}

Record 11,684 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.