Related Experiment Video
Updated: Oct 6, 2025

09:44
Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
Published on: January 29, 2019
10.2K
212Pb: Production Approaches and Targeted Therapy Applications
Konstantin V Kokov1, Bayirta V Egorova2, Marina N German1
1Physical and Chemical Technology Center, National Research Center Kurchatov Institute, 123182 Moscow, Russia.
Pharmaceutics
|January 21, 2022
Summary
Targeted alpha therapy using Lead-212 shows promise for cancer treatment. This review details methods for preparing Lead-212 radiopharmaceuticals, crucial for effective targeted alpha therapy applications.
Area of Science:
- Nuclear medicine
- Radiopharmaceutical chemistry
- Oncology
Background:
- Targeted alpha therapy (TAT) is a highly effective cancer treatment modality.
- Lead-212 (²¹²Pb) is a promising radionuclide for TAT due to its suitable half-life and alpha-emitting daughters.
- Efficient preparation of ²¹²Pb-based radiopharmaceuticals is critical for clinical success.
Purpose of the Study:
- To review methods for isolating Lead-212 (²¹²Pb) from its parent radionuclide.
- To discuss molecules for lead binding and the radiochemical characteristics of ²¹²Pb-labeled compounds.
- To present preclinical and clinical trial data for ²¹²Pb-based targeted radiopharmaceuticals.
Main Methods:
- Review of chromatographic, solution, and other techniques for ²¹²Pb isolation.
- Analysis of lead-binding molecules and radiolabeling strategies.
- Compilation of data from preclinical studies and initiated clinical trials.
Main Results:
- Various methods exist for milking ²¹²Pb from radionuclide generators.
- Radiochemical features and stability of ²¹²Pb-labeled compounds are crucial for efficacy.
- Preclinical data support therapeutic and tolerant doses, with clinical trials underway.
Conclusions:
- Lead-212 is a viable option for targeted alpha therapy.
- Optimized radiopharmaceutical preparation is key to maximizing therapeutic benefits.
- Ongoing clinical trials will further establish the role of ²¹²Pb in cancer treatment.

