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REGN5093-M114 is an investigational antibody-drug conjugate (ADC) developed for the treatment of cancers characterized by overexpression of the mesenchymal epithelial transition factor (MET), also known as hepatocyte growth factor receptor (HGFR). The ADC consists of a biparatopic human IgG4p monoclonal antibody (REGN5093) that targets two distinct epitopes on the MET protein. This antibody is covalently linked via a protease-cleavable linker to M24, a potent maytansine derivative that inhibits microtubule assembly. The design allows selective delivery of cytotoxic payload to tumor cells with high surface expression of MET, leading to cell death. Preclinical studies demonstrated significant antitumor activity in models with high MET expression and resistance to EGFR tyrosine kinase inhibitors. Clinical development focused on advanced non-small cell lung cancer (NSCLC) with high levels of MET overexpression[1][3][6][7]. As of early 2025, clinical development has been discontinued due to insufficient efficacy signals in early-stage trials[8].
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