PDF(Pubmed)
Abstract：
Astatine-211 (211At) 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 211At-labeled radiopharmaceuticals remains a major challenge. This review provides a comprehensive overview of the current strategies for 211At 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 211At-labeled compounds. The preclinical and clinical applications of 211At-labeled radiopharmaceuticals, including small molecules, peptides, and antibodies, are also discussed. Looking forward, the identification of new molecular targets, the optimization of 211At production and quality control methods, and the continued evaluation of 211At-labeled radiopharmaceuticals in preclinical and clinical settings will be the key to realizing the full potential of 211At-based targeted alpha therapy. With the growing interest and investment in this field, 211At-labeled radiopharmaceuticals are poised to play an increasingly important role in future cancer treatment.
摘要：
Astatine-211（211At）由于其有利的核性质，已成为有前途的放射性核素用于癌症的靶向α治疗。然而,211At标记的放射性药物的有限的体内稳定性仍然是一个主要挑战。这篇综述全面概述了211At放射性标记的当前策略，包括亲核和亲电取代反应，以及新型双功能偶联剂和标记方法的最新进展，以增强211At标记化合物的稳定性。211At标记放射性药物的临床前和临床应用，包括小分子，肽，和抗体，也讨论了。展望未来,识别新的分子靶标，211At生产和质量控制方法的优化，在临床前和临床环境中对211At标记的放射性药物的持续评估将是实现基于211At的靶向α治疗的全部潜力的关键。随着人们对这一领域的兴趣和投资的增长，211At标记的放射性药物有望在未来的癌症治疗中发挥越来越重要的作用。
