Citation: Feize Li, Yuanyou Yang, Jiali Liao, Ning Liu. Recent progress of astatine-211 in endoradiotherapy: Great advances from fundamental properties to targeted radiopharmaceuticals[J]. Chinese Chemical Letters, ;2022, 33(7): 3325-3338. doi: 10.1016/j.cclet.2022.03.025 shu

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

Key Laboratory of Radiation Physics and Technology of the Ministry of Education, Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064, China

nliu720@scu.edu.cn

Received Date: 26 December 2021
Revised Date: 1 March 2022
Accepted Date: 6 March 2022
Available Online: 9 March 2022

Figures(3)

Astatine-211 (²¹¹At, t_1/2 = 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.
- Radionuclides,
- Astatine-211,
- Target-alpha therapy,
- Radiopharmaceuticals
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