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

Astatine-211 (At-211, t(1/2) =7.21 h) emitting two a particles with energies of 5.87 and 7.45 MeV, can lead to a high linear energy transfer (LET= 98.84 keV/pm) and short tissue range (50-90pm). Since the 1950s, At-211 had stepped into endoradiotherapy and has always been regarded as one of the most promising alpha-emitters for targeted-alpha therapy (TAT) in various malignancies. In the past two decades, At-211 related radiopharmaceuticals have achieved great progress in the studies of basic physicochemical properties of astatine, At-211 labeling strategies, preclinical and clinical studies, producing profound effects in nuclear medicine. This work will give a panorama of At-211-related researches in the recent 20 years, which will cover both the fundamental insights of At-211 radiochemistry and applied labeling compounds. It can provide some important hints for the studies of TAT and other radiopharmaceuticals applied in tumor radiotherapy. (C) 2022 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.

Automated summary

Astatine-211 (At-211) is a promising alpha-emitter for targeted-alpha therapy (TAT) in various malignancies, due to its high linear energy transfer and short tissue range. In the past two decades, significant progress has been made in At-211-related radiopharmaceutical research, providing important insights for tumor radiotherapy and other radiopharmaceutical studies.