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213Bi-DOTATOC is an investigational somatostatin receptor-targeted alpha radiopharmaceutical comprising the somatostatin analogue edotreotide labeled with the alpha-emitting radionuclide bismuth-213. It binds primarily to somatostatin receptor subtype 2 on receptor-positive neuroendocrine tumor cells, is internalized, and delivers high-linear-energy-transfer alpha radiation that causes localized cytotoxic DNA damage. Preclinical rat pancreatic carcinoma studies showed dose-related antitumor activity, and first-in-human dose-escalation experience evaluated intra-arterial or systemic administration in patients with advanced neuroendocrine tumors refractory to beta-emitting DOTATOC therapy. ([pmc.ncbi.nlm.nih.gov](https://pmc.ncbi.nlm.nih.gov/articles/PMC4525192/))
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