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Vibetocotumab (MRG003) is an antibody-drug conjugate (ADC) targeting the epidermal growth factor receptor (EGFR). It is composed of a humanized anti-EGFR monoclonal antibody conjugated to the potent microtubule-disrupting agent monomethyl auristatin E (MMAE) via a protease-cleavable valine-citrulline (vc) linker. Upon binding to EGFR on the surface of tumor cells, the ADC is internalized through endocytosis and transported to lysosomes, where the linker is cleaved to release MMAE. The released payload then inhibits tubulin polymerization, leading to cell cycle arrest and apoptosis. Vibetocotumab is primarily being developed for the treatment of EGFR-overexpressing solid tumors, including head and neck squamous cell carcinoma (HNSCC), nasopharyngeal carcinoma (NPC), and oral squamous cell carcinoma.
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