²¹²Pb: Production Approaches and Targeted Therapy Applications

• Main Authors: Konstantin V. Kokov (Author), Bayirta V. Egorova (Author), Marina N. German (Author), Ilya D. Klabukov (Author), Michael E. Krasheninnikov (Author), Antonius A. Larkin-Kondrov (Author), Kseniya A. Makoveeva (Author), Michael V. Ovchinnikov (Author), Maria V. Sidorova (Author), Dmitry Y. Chuvilin (Author)
• Format: Book
• Published: MDPI AG, 2022-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/pharmaceutics14010189; 1999-4923
• Keywords: lead-212; thorium-228; radionuclide generator; α-radiation sources; targeted alpha therapy; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 14, Iss 1, p 189 (2022)

Over the last decade, targeted alpha therapy has demonstrated its high effectiveness in treating various oncological diseases. Lead-212, with a convenient half-life of 10.64 h, and daughter alpha-emitter short-lived ²¹²Bi (<i>T_1/2</i> = 1 h), provides the possibility for the synthesis and purification of complex radiopharmaceuticals with minimum loss of radioactivity during preparation. As a benefit for clinical implementation, it can be milked from a radionuclide generator in different ways. The main approaches applied for these purposes are considered and described in this review, including chromatographic, solution, and other techniques to isolate ²¹²Pb from its parent radionuclide. Furthermore, molecules used for lead's binding and radiochemical features of preparation and stability of compounds labeled with ²¹²Pb are discussed. The results of preclinical studies with an estimation of therapeutic and tolerant doses as well as recently initiated clinical trials of targeted radiopharmaceuticals are presented.