NCIt definition : A Bicycle toxin conjugate (BTC) composed of 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.;