Citation: Junyi Chen, Mengxin Xu, Yu Liu, Dongban Duan, Yuxiang Han, Zhibo Liu. Isolation of ²¹²Pb from natural thorium for targeted alpha-therapy[J]. Chinese Chemical Letters, ;2022, 33(7): 3474-3477. doi: 10.1016/j.cclet.2022.02.012 shu

Isolation of ²¹²Pb from natural thorium for targeted alpha-therapy

Junyi Chen ^a ,
Mengxin Xu ^a ,
Yu Liu ^b ,
Dongban Duan ^a ,
Yuxiang Han ^a ,
Zhibo Liu ^{a, b, *,}

a.
Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China
b.
Peking-Tsinghua Center for Life Sciences, Peking University, Beijing 100871, China

zbliu@pku.edu.cn

Received Date: 29 November 2021
Revised Date: 5 February 2022
Accepted Date: 7 February 2022
Available Online: 10 February 2022

Figures(4)

Targeted alpha-therapy (TAT) is increasingly attractive due to its extraordinary antitumor efficacy. However, the supply of α-emitters for TAT is insufficient and under control by a limited number of countries. ²¹²Pb is a promising α-emitter with an optimal half-life (10.6 h) and favored decay chain. Of interest, ²¹²Pb 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 ²¹²Pb from natural thorium would be ideal to meet the above challenges, yet is difficult. In theory, the ratio of ²¹²Pb to ^natTh is below 10⁻¹³ in commercially available thorium salts. As a pilot study, 2.2 MBq of ²¹²Pb was successfully extracted from a 5 L solution of thorium nitrate by using a Pb-selective resin. The radiochemical purity of ²¹²Pb is over 99.9% according to gamma-ray analysis. The purified ²¹²Pb was applied to radiolabel a couple of peptides used in clinics (i.e. PSMA, TATE and FAPI-04), and the radiochemical yields are > 85%. Of note, ²¹²Pb can be repeatedly separated from the thorium solution every 2 days. In summary, a practical and scalable method was developed to isolate ²¹²Pb for potentially clinical use, which may be of great importance as it does not require either cyclotron or nuclear reactor.
- ²¹²Pb,
- Targeted alpha-therapy,
- Radiolabeling,
- Radionuclide generator,
- Solid-phase extraction
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Isolation of ²¹²Pb from natural thorium for targeted alpha-therapy