²¹²Pb in targeted radionuclide therapy: a review

Area of Science:

• Nuclear medicine
• Radiochemistry
• Oncology

Background:

• Alpha-particle emitting radionuclides offer targeted cancer therapy due to their high cytotoxicity and short range.
• Lead-212 (212Pb), as the parent of bismuth-212 (212Bi), is increasingly used in therapy due to favorable decay properties and chemistry.
• This review details the clinical progression of 212Pb, focusing on its production, chelation, and therapeutic application.

Purpose of the Study:

• To comprehensively review the recent clinical development of Lead-212 (212Pb) in cancer therapy.
• To highlight advancements in 212Pb production, chelation chemistry, and its therapeutic integration.

Main Methods:

• Improved generator technology has increased the availability of 212Pb, facilitating research.
• Development of bifunctional chelators allows conjugation of 212Pb to tumor-targeting agents.
• Advancements in nuclear imaging, including the use of 203Pb, enable accurate biodistribution and dosimetry studies.

Main Results:

• Increased availability and improved targeting strategies have accelerated 212Pb research and clinical translation.
• 212Pb is being investigated in clinical trials for treating a variety of cancers.
• Significant commercial interest is driving the rapid adoption of 212Pb in clinical settings.

Conclusions:

• 212Pb radiotherapy demonstrates substantial promise in both preclinical and clinical cancer studies.
• While challenges persist, considerable progress has been made in overcoming them for wider 212Pb adoption.
• The full therapeutic potential of 212Pb is beginning to be realized in cancer treatment.