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Becotatug vedotin (MRG003) is a novel epidermal growth factor receptor (EGFR)-targeted antibody-drug conjugate (ADC). It consists of a humanized monoclonal antibody conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE) via a protease-cleavable valine-citrulline linker. Developed by Lepu Biopharma, the drug is designed to selectively deliver its cytotoxic payload to tumor cells that overexpress EGFR, leading to cell cycle arrest and apoptosis. It is the world's first approved EGFR-targeted ADC for the treatment of recurrent or metastatic nasopharyngeal carcinoma (R/M NPC). The US FDA has also granted it Breakthrough Therapy designation for this indication. Clinical evaluations are ongoing for its use in combination with other agents, such as sintilimab and chemoradiotherapy, for locally advanced nasopharyngeal carcinoma.
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