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**213Bi-trastuzumab** is a radiopharmaceutical composed of the monoclonal antibody trastuzumab conjugated to the alpha particle–emitting radionuclide bismuth-213. Trastuzumab is a humanized IgG1 monoclonal antibody that binds with high affinity to the extracellular domain of the human epidermal growth factor receptor 2 (HER2), which is overexpressed in certain cancers, notably HER2-positive breast and gastric cancers[1][3][4]. The addition of bismuth-213 enables **targeted alpha therapy (TAT)**, delivering highly cytotoxic alpha radiation specifically to HER2-positive tumor cells. The alpha particles cause double-stranded breaks in DNA, leading to potent, localized cell death[2]. This approach minimizes damage to surrounding healthy tissues compared to non-targeted radiotherapy. 213Bi-trastuzumab is under investigation primarily for HER2-positive malignancies and operates by both immunotherapy and radiopharmaceutical mechanisms.
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