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213Bi-matuzumab is an experimental radiopharmaceutical and antibody-drug conjugate (ADC) consisting of the humanized monoclonal antibody matuzumab conjugated to the alpha-emitting radionuclide Bismuth-213 (^213Bi). Developed through a collaboration between the Technical University of Munich and the European Commission's Joint Research Centre, it specifically targets the epidermal growth factor receptor (EGFR), which is frequently overexpressed in various malignancies. Upon binding to EGFR on tumor cells, the conjugate delivers high-energy, short-range alpha radiation that induces lethal DNA double-strand breaks. This mechanism is particularly effective in treating hypoxic tumor cells and minimizing damage to surrounding healthy tissue. It has been primarily investigated for the intravesical treatment of BCG-refractory carcinoma in situ of the bladder, as well as for glioblastoma and squamous cell carcinoma.
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