| 總結: | Astatine-211 (<sup>211</sup>At) has emerged as a promising radionuclide for targeted alpha therapy of cancer by virtue of its favorable nuclear properties. However, the limited in vivo stability of <sup>211</sup>At-labeled radiopharmaceuticals remains a major challenge. This review provides a comprehensive overview of the current strategies for <sup>211</sup>At radiolabeling, including nucleophilic and electrophilic substitution reactions, as well as the recent advances in the development of novel bifunctional coupling agents and labeling approaches to enhance the stability of <sup>211</sup>At-labeled compounds. The preclinical and clinical applications of <sup>211</sup>At-labeled radiopharmaceuticals, including small molecules, peptides, and antibodies, are also discussed. Looking forward, the identification of new molecular targets, the optimization of <sup>211</sup>At production and quality control methods, and the continued evaluation of <sup>211</sup>At-labeled radiopharmaceuticals in preclinical and clinical settings will be the key to realizing the full potential of <sup>211</sup>At-based targeted alpha therapy. With the growing interest and investment in this field, <sup>211</sup>At-labeled radiopharmaceuticals are poised to play an increasingly important role in future cancer treatment.
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