anti-c-Kit/MMAE antibody-drug conjugate NN3201

An antibody-drug conjugate (ADC) composed of 2G4, a human monoclonal antibody directed against the stem cell factor receptor c-Kit (SCFR; KIT; CD117), conjugated to the auristatin derivative and microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of anti-c-Kit/MMAE ADC NN3201, the 2G4 antibody targets and binds to the cell surface antigen c-Kit. Upon binding and internalization, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in c-Kit-expressing tumor cells. c-Kit, a transmembrane protein and receptor tyrosine kinase (RTK) overexpressed in various solid tumors and hematological malignancies, plays a key role in the regulation of cell differentiation and proliferation.