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Vibekotutamab (MRG003) is an antibody-drug conjugate (ADC) targeting the epidermal growth factor receptor (EGFR). It consists of a humanized anti-EGFR monoclonal antibody conjugated to the potent microtubule-disrupting agent monomethyl auristatin E (MMAE) through a protease-cleavable valine-citrulline (vc) linker. By binding to EGFR, which is frequently overexpressed in various solid tumors, the ADC is internalized via endocytosis, leading to the intracellular release of MMAE. The released payload then binds to tubulin, inhibiting its polymerization and causing cell cycle arrest and apoptosis. Developed by Mabwell and Lepu Biopharma, vibekotutamab is being investigated for the treatment of EGFR-positive malignancies, including nasopharyngeal carcinoma, head and neck squamous cell carcinoma, and urogenital squamous cell carcinoma.
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