Definition

An antibody-drug conjugate (ADC) consisting of REGN5093, a biparatopic monoclonal antibody that targets two different epitopes of the human tumor-associated antigen (TAA) MET (c-MET; hepatocyte growth factor receptor; HGFR), and conjugated, via a protease cleavable linker, to the cytotoxic maytansine derivative M24, with potential antineoplastic activity. Upon administration of anti-MET x MET ADC REGN5093-M114, the REGN5093 moiety targets and binds to two different, non-overlapping epitopes on MET expressed on the tumor cell surface. After antibody-antigen interaction followed by internalization and protease cleavage, the maytansine M24 moiety binds to tubulin, inhibits microtubule assembly, and induces microtubule disassembly. This leads to a disruption of mitosis and the inhibition of cell proliferation in cancer cells expressing MET. MET, a receptor tyrosine kinase, is overexpressed on the cell surfaces of various solid tumor cell types where it is involved in epithelial-mesenchymal transition; it plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.