Astatine-211 ( 211 At, t 1/2 = 7.21 h) 发射两个α粒子，能量分别为 5.87 和 7.45 MeV，可导致高线性能量转移 (LET = 98.84 keV/µm) 和短组织范围 (50∼ 90 微米）。自 1950 年代以来，211 At 已进入放射内治疗，并一直被认为是各种恶性肿瘤靶向 α 治疗 (TAT) 中最有前途的α发射体之一。在过去的二十年里，211在相关的放射性药物对砹的基本理化性质的研究方面取得了很大进展，211在标签策略、临床前和临床研究中，对核医学产生了深远的影响。这项工作将概述近 20 年来211 At 相关研究，涵盖211 At 放射化学和应用标记化合物的基本见解。可为TAT等放射性药物在肿瘤放射治疗中的研究提供一些重要的启示。

"点击查看英文标题和摘要"

Recent progress of astatine-211 in endoradiotherapy: Great advances from fundamental properties to targeted radiopharmaceuticals

Astatine-211 (211At, t1/2 = 7.21 h) emitting two α particles with energies of 5.87 and 7.45 MeV, can lead to a high linear energy transfer (LET = 98.84 keV/µm) and short tissue range (50∼90 µm). Since the 1950s, 211At had stepped into endoradiotherapy and has always been regarded as one of the most promising α-emitters for targeted-alpha therapy (TAT) in various malignancies. In the past two decades, 211At related radiopharmaceuticals have achieved great progress in the studies of basic physicochemical properties of astatine, 211At labeling strategies, preclinical and clinical studies, producing profound effects in nuclear medicine. This work will give a panorama of 211At-related researches in the recent 20 years, which will cover both the fundamental insights of 211At radiochemistry and applied labeling compounds. It can provide some important hints for the studies of TAT and other radiopharmaceuticals applied in tumor radiotherapy.