NCIt definition : An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody (AGS-16C)
directed to the ectonucleotide pyrophosphatase/phosphodiesterase family member 3 (ENPP3),
conjugated via a non-cleavable linker to monomethyl auristatin F (MMAF), an auristatin
derivative and a potent microtubule inhibitor, that has potential antineoplastic activity.
Upon intravenous administration of ADC AGS-16C3F, the monoclonal antibody moiety of
this conjugate selectively binds to ENPP3 then is internalized and undergoes proteolytic
cleavage to release MMAF. MMAF binds to and inhibits tubulin polymerization, resulting
in G2/M phase arrest and tumor cell apoptosis. While normally expressed at low levels
in the proximal tubules of the kidney, the type II transmembrane glycoprotein ENPP3
has been found to be overexpressed in renal neoplasms.;
Semantic type(s)