Definition

An antibody-drug conjugate (ADC) consisting of a human immunoglobulin G1 (IgG1) monoclonal antibody directed against the epidermal growth factor receptor (EGFR) conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of anti-EGFR ADC MRG003, the monoclonal antibody moiety binds to EGFR on tumor cell surfaces. Following receptor internalization, the MMAE moiety is released and binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and apoptosis. This inhibits the proliferation of EGFR-expressing tumor cells. EGFR, overexpressed by a variety of cancers, plays a key role in tumor cell proliferation and survival.