Title Isolation of Pb-212 from natural thorium for targeted alpha-therapy
Authors Chen, Junyi
Xu, Mengxin
Liu, Yu
Duan, Dongban
Han, Yuxiang
Liu, Zhibo
Affiliation Peking Univ, Radiochem & Radiat Chem Key Lab Fundamental Sci, Coll Chem & Mol Engn, Beijing Natl Lab Mol Sci, Beijing 100871, Peoples R China
Peking Univ, Peking Tsinghua Ctr Life Sci, Beijing 100871, Peoples R China
Keywords RADIATION
GENERATOR
CANCER
AC-225
BI-212
Issue Date Jul-2022
Publisher CHINESE CHEMICAL LETTERS
Abstract Targeted alpha-therapy (TAT) is increasingly attractive due to its extraordinary antitumor efficacy. However, the supply of alpha-emitters for TAT is insufficient and under control by a limited number of countries. Pb-212 is a promising alpha-emitter with an optimal half-life (10.6h) and favored decay chain. Of interest, Pb-212 can be extracted directly from natural thorium, which may be abundant in the mining waste of rare-earth, uranium, etc. Indeed, radioactive thorium waste has been a longstanding environmental challenge that needs immediate action. Developing an on-demand and facile process to isolate Pb-212 from natural thorium would be ideal to meet the above challenges, yet is difficult. In theory, the ratio of Pb-212 to Th-nat is below 10(-13) in commercially available thorium salts. As a pilot study, 2.2 MBq of Pb-212 was successfully extracted from a 5 L solution of thorium nitrate by using a Pb-selective resin. The radiochemical purity of Pb-212 is over 99.9% according to gamma-ray analysis. The purified Pb-212 was applied to radiolabel a couple of peptides used in clinics (Le. PSMA, TATE and FAPI-04), and the radiochemical yields are >85%. Of note, Pb-212 can be repeatedly separated from the thorium solution every 2 days. In summary, a practical and scalable method was developed to isolate Pb-212 for potentially clinical use, which may be of great importance as it does not require either cyclotron or nuclear reactor. (C) 2022 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.
URI http://hdl.handle.net/20.500.11897/647536
ISSN 1001-8417
DOI 10.1016/j.cclet.2022.02.012
Indexed SCI(E)
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生命科学学院

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