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Updated: May 15, 2026

Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
Published on: February 4, 2017
Bone-targeting radiopharmaceuticals including radium-223.
Darren Brady1, Chris C Parker, Joe M O'Sullivan
1Centre for Cancer Research and Cell Biology, Queen's University Belfast and the Northern Ireland Cancer Centre, BT9 7AB Belfast, Northern Ireland.
Bone-seeking radionuclides offer pain relief for bone metastases. Radium-223 (Ra) shows improved survival in metastatic castration-resistant prostate cancer (CRPC), becoming a key treatment option.
Area of Science:
- Nuclear medicine
- Oncology
- Radiopharmaceutical therapy
Background:
- Bone-seeking radionuclides like samarium-153 and strontium-89 have historically managed bone metastasis pain.
- Radium-223 (Ra), an alpha-emitting radionuclide, shows promise for improved survival in metastatic castration-resistant prostate cancer (CRPC).
Purpose of the Study:
- To review randomized controlled trials of bone-seeking radionuclides for bone metastases.
- To explore optimal use, including dose, radiobiology, and future combination strategies.
Main Methods:
- Literature review of randomized controlled trials.
- Analysis of data from the ALSYMPCA trial comparing radium-223 to placebo.
Main Results:
- Beta-emitting radionuclides provide 60-70% pain response rates in prostate cancer bone metastases.
- Radium-223 demonstrated a significant median overall survival improvement of 3.6 months in symptomatic CRPC patients.
Conclusions:
- Radium-223 is a significant advancement for CRPC treatment, improving survival and offering a favorable safety profile.
- Radium-223 has potential for combination therapies and earlier use in metastatic prostate cancer management.
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