MLchartDataset catalogue

Nuzefatide pevedotin

Term · Oncology and biomedicine · MLC-T-ONC-015560

A bicyclic peptide targeting Ephrin receptor A2 (EphA2) and conjugated, through an inert sarcosine spacer chain and a valine-citrulline cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE), an auristatin derivative and a potent inhibitor of microtubule polymerization, with potential antineoplastic activity. Upon administration, nuzefatide pevedotin targets and binds to EphA2-expressing tumor cells. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAE binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) involved in mammalian development, is overexpressed by a variety of different cancer cell types. EphA2 expression is associated with poor prognosis.

Table 1. Record
IdentifierMLC-T-ONC-015560
FieldOncology and biomedicine
Synonymsbicycle BT5528; bicycle toxin conjugate-targeting EphA2 BT5528; bicyclic peptide conjugate BT5528; BTC BT5528; EphA2-targeting Bicycle Toxin Conjugate BT5528; EphA2-targeting BTC BT5528; EphA2-targeting-MMAE bicycle toxin BT5528
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-015560",
  "term": "Nuzefatide pevedotin",
  "field": "Oncology and biomedicine",
  "definition": "A bicyclic peptide targeting Ephrin receptor A2 (EphA2) and conjugated, through an inert sarcosine spacer chain and a valine-citrulline cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE), an auristatin derivative and a potent inhibitor of microtubule polymerization, with potential antineoplastic activity. Upon administration, nuzefatide pevedotin targets and binds to EphA2-expressing tumor cells. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAE binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) involved in mammalian development, is overexpressed by a variety of different cancer cell types. EphA2 expression is associated with poor prognosis.",
  "synonyms": [
    "bicycle BT5528",
    "bicycle toxin conjugate-targeting EphA2 BT5528",
    "bicyclic peptide conjugate BT5528",
    "BTC BT5528",
    "EphA2-targeting Bicycle Toxin Conjugate BT5528",
    "EphA2-targeting BTC BT5528",
    "EphA2-targeting-MMAE bicycle toxin BT5528"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/nuzefatide-pevedotin/"
}

Record 12,032 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.