Bone-targeting radiopharmaceuticals for the treatment of prostate cancer with bone metastases
Open accessAbstract
Patients with castration-resistant prostate cancer (CRPC) frequently have metastases to the bone, which may cause pain and lead to a deterioration in quality-of-life. Bone-seeking radiopharmaceuticals are agents which, when administered systemically, localize to the site of bone metastases and deliver focal radiation there. In this review, we will summarize the current literature on bone-targeting radiopharmaceuticals for CRPC, focusing on strontium-89, samarium-153, rhenium-186 and radium-223. We will discuss their indications, clinical efficacy, and toxicities and highlight some of the challenges in optimizing treatment with these agents. Historically, clinical trials with these drugs have failed to demonstrate survival improvements, restricting their use for palliative purposes only. Radium-223 is the first agent in this class to show an overall survival advantage in CRPC patients with bone metastases. This landmark finding will likely have a considerable impact on the treatment paradigm of bone-metastatic CRPC, and will pave the way for further developments in the future.
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Targeted radiopharmaceutical therapies such as strontium-89 chloride or samarium-153 lexidronam deliver focused radiation to osteoblastic or osteolytic lesions, offering pain relief and promoting skeletal stability.
“Striking examples emerge where targeted radiopharmaceutical therapies, such as strontium-89 chloride or samarium-153 lexidronam, deliver focused radiation to osteoblastic or osteolytic lesions, offering relief from pain and promoting skeletal stability [107].”
From Radiopharmaceuticals: navigating the frontier of precision medicine and therapeutic innovation (2024) · cites this paper as [107]
Sections 4.1 and 4.2 describe preferential uptake of strontium-89 and samarium-153 in bone metastases and report pain relief. But Section 3 advises that patients with osteolytic lesions generally should not receive these agents, and the cited passages do not show that they promote skeletal stability. (LLM, conf=0.90)
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Jani, C., & Sharma, J. N. (2026) · Springer eBooks · doi:10.1007/978-3-032-09498-8_26
From β-Blasts to α-Bombs: Bone-Targeting Radiopharmaceutical Therapies
Chong, N. E., Wienhoff, B., & Kuo, N. P. (2026) · Journal of Nuclear Medicine Technology · doi:10.2967/jnmt.126.273620
- Authors
- Goyal, J., & Antonarakis, E. S.
- Affiliations
- University of Alabama at Birmingham (US)
- Johns Hopkins University (US)
- Corresponding author
- Antonarakis, Emmanuel S.
- Venue
- Cancer Letters
- Publisher
- Elsevier BV
- Published
- 2012-10
- Volume
- 323
- Issue
- 2
- Pages
- 135-146
- ISSN
- 0304-3835 (ISSN-L)
- PMC
- PMC4124611
- OpenAlex
- W2004538226
- Cited by
- 94
- References
- 117
- Citations by year
- 2026: 2 · 2025: 3 · 2024: 3 · 2023: 3 · 2022: 8 · 2021: 5 · 2020: 12 · 2019: 5 · 2018: 6 · 2017: 7 · 2016: 11 · 2015: 7 · 2014: 9 · 2013: 12 · 2012: 1
- FWCI
- 1.57
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Cancer Letters (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Cancer Institute (P30CA006973)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Health Sciences › Medicine › Oncology › Bone health and treatments
- Keywords
- castration-resistant prostate cancer, bone metastasis, strontium-89, samarium-153, rhenium-186, radium-223, palliative radiotherapy, overall survival, treatment toxicity, pain management
- MeSH terms
- Bone Neoplasms, Humans, Male, Prostatic Neoplasms, Quality of Life, Drug Delivery Systems, Radiopharmaceuticals
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