Preferred Label : Conditionally-activated Anti-EpCAM Antibody-drug Conjugate CX-2051;
NCIt synonyms : Protease-activated Anti-EpCAM ADC CX-2051; Conditionally-activated Anti-EpCAM ADC CX-2051; Masked Anti-EpCAM ADC CX-2051; Anti-EpCAM/TOP1i ADC CX-2051; Anti-EpCAM ADC CX-2051;
NCIt definition : An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against
the tumor-associated antigen (TAA) human epithelial cell adhesion molecule (Ep-CAM;
EpCAM; CD326), linked to a proprietary masking peptide through a protease-cleavable
linker, and conjugated to a derivative of camptothecin, with potential antineoplastic
activity. Upon administration of conditionally-activated anti-EpCAM ADC CX-2051, the
linkage system is stable in the circulation and, upon extravasation into the tumor
microenvironment (TME), the peptide mask is cleaved by tumor-associated proteases.
These proteases are present in high concentrations and aberrantly activated in the
TME, while expressed as inactive forms, at much lower concentrations, in normal, healthy
tissue. Protease cleavage of the linker enables the binding of the unmasked, fully
active anti-EpCAM antibody moiety of CX-2051 to EpCAM-expressing tumor cells. Upon
binding and internalization, the camptothecin derivative is released. The camptothecin
derivative inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication
and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation
of EpCAM-expressing tumor cells. EpCAM, a cell surface protein upregulated on many
tumor cell types, promotes the proliferation, migration and invasiveness of tumor
cells.;
Molecule name : CX 2051; CX-2051;
NCI Metathesaurus CUI : CL1928832;
Origin ID : C206677;
concept_is_in_subset
- has_target
