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.
| Identifier | MLC-T-ONC-017658 |
|---|---|
| Field | Oncology and biomedicine |
| 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 (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.