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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
Published on: January 29, 2019
Development and clinical application of targeted alpha therapy using astatine (211At)
1Department of Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, 2-2 Yamadaoka, Suita, Osaka, 565-0871, Japan;
Annals of the ICRP
|May 13, 2026
Summary
Targeted alpha therapy using astatine-211 (211At) shows promise for refractory thyroid cancer. This therapy allows patients to leave isolation quickly due to minimal radiation exposure, unlike traditional treatments.
Area of Science:
- Nuclear medicine
- Radiotherapy
- Oncology
Background:
- Targeted alpha therapy (TAT) offers higher efficacy than beta-emitter radionuclide therapy.
- Astatine-211 (211At) is a promising alpha-emitting radionuclide producible with a 30-MeV cyclotron.
- 211At functions as an iodine analogue, suitable for thyroid cancer treatment.
Purpose of the Study:
- To evaluate [211At] NaAt as a targeted alpha therapy for refractory thyroid cancer.
- To assess radiation safety and patient management protocols for 211At-based TAT.
- To explore the potential of 211At for broader oncological applications.
Main Methods:
- Investigator-initiated clinical trial using [211At] NaAt.
- Comparison of radiation dose and exposure with conventional beta-emitters (131I, 177Lu).
- Assessment of radiation exposure to the public and caregivers post-administration.
Main Results:
- 211At requires smaller administration doses compared to beta-emitters.
- 211At emits lower-energy gamma rays, reducing external radiation exposure.
- Radiation exposure levels were demonstrated to be well below public limits, negating the need for isolation wards.
Conclusions:
- [211At] NaAt enables targeted alpha therapy for refractory thyroid cancer without requiring inpatient isolation.
- 211At offers reduced radiation exposure and enhanced safety for patients and caregivers.
- 211At's imaging capabilities and labeling potential position it as a versatile agent for various cancers.
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