anti-CD20 antibody-drug conjugate MRG001

An antibody-drug conjugate (ADC) composed of a chimeric anti-CD20 monoclonal antibody conjugated via a valine citrulline linker to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of anti-CD20 ADC MRG001, the monoclonal antibody moiety of MRG001 targets and binds to CD20 on the surfaces of tumor B cells and is rapidly internalized, thereby delivering MMAE intracellularly. Upon proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M checkpoint arrest and apoptosis in CD20-expressing tumor cells. CD20 is a non-glycosylated cell surface phosphoprotein which is exclusively expressed on B-cells during most stages of B-cell development. It is often overexpressed in B-cell malignancies.