Preferred Label : Anti-5T4/D-2102 Antibody-Drug Conjugate ACR246;
NCIt synonyms : Anti-5T4/D-2102 ADC ACR246; Anti-5T4 ADC ACR246; ADC ACR246;
NCIt definition : An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed
against the oncofetal antigen 5T4 and site-specifically conjugated, via a cleavable
linker, to the cell penetrating cytotoxic agent and DNA topoisomerase I inhibitor
D-2102, with potential antineoplastic activity. Upon administration of anti-5T4/D-2102
ADC ACR246, the anti-5T4 antibody moiety of ACR246 selectively binds to cells expressing
5T4. After internalization and cleavage within the tumor cell cytosol, the topoisomerase
I inhibitor D-2102 is released and inhibits DNA topoisomerase I activity, thereby
inhibiting DNA replication and resulting in DNA damage, cell cycle arrest and apoptosis
in tumor cells overexpressing 5T4. In addition, ACR246 induces a bystander effect,
thereby killing neighboring tumor cells in the tumor environment (TME). 5T4, a transmembrane
glycoprotein, is overexpressed by a variety of cancer cell types while its expression
is limited in normal adult tissues; its expression is correlated with increased invasiveness.;
Molecule name : ACR 246; ACR-246;
Origin ID : C207270;
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