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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
Published on: January 29, 2019
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[Clinical Application of Targeted Alpha Therapy Using Astatine]
1Graduate School of Medicine, The University of Osaka.
Summary
Targeted alpha therapy using astatine-211 shows promise for treating advanced thyroid cancer. A first-in-human trial demonstrated clinical efficacy, with ongoing research exploring its potential for other cancers.
Area of Science:
- Nuclear medicine
- Oncology
- Radiochemistry
Background:
- Targeted alpha therapy (TAT) offers superior efficacy over beta-emitter therapies.
- Astatine-211 (211At) is a promising alpha emitter for TAT, producible via cyclotron.
- Astatine's chemical similarity to iodine facilitates its uptake in thyroid cancer cells.
Purpose of the Study:
- To evaluate the clinical efficacy and safety of 211At-labeled sodium astatide (NaAt) in patients with metastatic thyroid cancer.
- To explore the development of novel 211At-based radiopharmaceuticals for various cancers.
Main Methods:
- Conducted a first-in-human clinical trial using [211At]NaAt in radioiodine-refractory metastatic thyroid cancer patients.
- Developed and preclinically evaluated 211At-labeled compounds targeting prostate-specific membrane antigen (PSMA).
- Actively developing pan-tumor targeting probes, including LAT1 and EphA2 targeting agents.
Main Results:
- Observed disappearance of iodine-avid lesions in treated patients.
- Reported a significant reduction in serum thyroglobulin levels, indicating tumor response.
- Preclinical studies show promise for 211At-PSMA and other novel agents.
Conclusions:
- 211At-based targeted alpha therapy demonstrates significant potential for treating metastatic thyroid cancer.
- Ongoing development of diverse 211At radiopharmaceuticals may broaden applications in oncology.
- Astatine-211 holds promise for revolutionizing future cancer treatment strategies.
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