MLchartDataset catalogue

Zelenectide pevedotin

Term · Oncology and biomedicine · MLC-T-ONC-017658

A Bicycle toxin conjugate (BTC) composed of a zelenectide, a synthetic, bicyclic peptide targeting the cell adhesion molecule nectin-4 (PVRL4) and conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), via an inert sarcosine spacer chain and a valine-citrulline cleavable linker, with potential antineoplastic activity. Upon administration, the bicyclic peptide moiety of zelenectide pevedotin selectively binds to nectin-4. After internalization and proteolytic cleavage by peptidases that are upregulated in the tumor microenvironment (TME), MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in nectin-4 overexpressing tumor cells. Nectin-4, a tumor associated antigen (TAA) belonging to the nectin family, is overexpressed in a variety of cancers, but has a restricted distribution in normal tissue. It is associated with poor disease prognosis.

Table 1. Record
IdentifierMLC-T-ONC-017658
FieldOncology and biomedicine
SynonymsPVRL4-targeting bicyclic peptide toxin conjugate BT8009; bicycle-MMAE BT8009; bicycle toxin conjugate BT8009; BTC BT8009; Nectin-4-binding bicycle-MMAE BT8009; nectin-4-targeting bicyclic peptide toxin conjugate BT8009; nectin-4-targeting bicyclic peptide/MMAE BT8009
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-017658",
  "term": "Zelenectide pevedotin",
  "field": "Oncology and biomedicine",
  "definition": "A Bicycle toxin conjugate (BTC) composed of a zelenectide, a synthetic, bicyclic peptide targeting the cell adhesion molecule nectin-4 (PVRL4) and conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), via an inert sarcosine spacer chain and a valine-citrulline cleavable linker, with potential antineoplastic activity. Upon administration, the bicyclic peptide moiety of zelenectide pevedotin selectively binds to nectin-4. After internalization and proteolytic cleavage by peptidases that are upregulated in the tumor microenvironment (TME), MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in nectin-4 overexpressing tumor cells. Nectin-4, a tumor associated antigen (TAA) belonging to the nectin family, is overexpressed in a variety of cancers, but has a restricted distribution in normal tissue. It is associated with poor disease prognosis.",
  "synonyms": [
    "PVRL4-targeting bicyclic peptide toxin conjugate BT8009",
    "bicycle-MMAE BT8009",
    "bicycle toxin conjugate BT8009",
    "BTC BT8009",
    "Nectin-4-binding bicycle-MMAE BT8009",
    "nectin-4-targeting bicyclic peptide toxin conjugate BT8009",
    "nectin-4-targeting bicyclic peptide/MMAE BT8009"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/zelenectide-pevedotin/"
}

Record 17,614 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.