Realizing the potential of the Actinium-225 radionuclide generator in targeted alpha particle therapy applications
Open accessAbstract
Alpha particle-emitting isotopes have been proposed as novel cytotoxic agents for augmenting targeted therapy. Properties of alpha particle radiation such as their limited range in tissue of a few cell diameters and their high linear energy transfer leading to dense radiation damage along each alpha track are promising in the treatment of cancer, especially when single cells or clusters of tumor cells are targeted. Actinium-225 (225 Ac) is an alpha particle-emitting radionuclide that generates 4 net alpha particle isotopes in a short decay chain to stable 209 Bi, and as such can be described as an alpha particle nanogenerator. This article reviews the literature pertaining to the research, development, and utilization of targeted 225 Ac to potently and specifically affect cancer.
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Alpha-emitting radionuclides like 223Ra selectively irradiate bone metastases while minimizing damage to surrounding tissues.
“The dynamic landscape of bone-targeted radiopharmaceuticals is further emphasized through cases involving alpha-emitting radionuclides, like ^223Ra, which leverage the unique properties of these particles to selectively irradiate bone metastases while minimizing damage to surrounding tissues [111].”
From Radiopharmaceuticals: navigating the frontier of precision medicine and therapeutic innovation (2024) · cites this paper as [111]
The Introduction (section 1; page unavailable) says alpha particles have a short range that confines their toxic effect near the site of decay, supporting the claim about limiting damage to surrounding tissue. The passages on targeted therapy do not establish that 223Ra selectively irradiates bone metastases; searches for “223Ra bone metastases” and “radium-223 bone metastases” found no such passage. (LLM, conf=0.86)
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“The dynamic landscape of bone-targeted radiopharmaceuticals is further emphasized through cases involving alpha-emitting radionuclides, like ^223Ra, which leverage the unique properties of these particles to selectively irradiate bone metastases while minimizing damage to surrounding tissues [111].”
BackgroundHooijman, E. L., Chalashkan, Y., Ling, S. W., Kahyargil, F. F., Segbers, M., Bruchertseifer, F., Morgenstern, A., Seimbille, Y., Koolen, S. L. W., Brabander, T., et al. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13050715 · Cited by 59 · see citing works
- Authors
- Miederer, M., Scheinberg, D. A., & McDevitt, M. R.
- Affiliations
- TUM Klinikum (DE)
- Memorial Sloan Kettering Cancer Center (US)
- Corresponding author
- McDevitt, Michael R.
- Venue
- Advanced Drug Delivery Reviews
- Publisher
- Elsevier BV
- Published
- 2008-09
- Volume
- 60
- Issue
- 12
- Pages
- 1371-1382
- ISSN
- 0169-409X (ISSN-L)
- PMC
- PMC3630456
- OpenAlex
- W2034149747
- Cited by
- 210
- References
- 57
- Citations by year
- 2026: 11 · 2025: 15 · 2024: 12 · 2023: 12 · 2022: 19 · 2021: 18 · 2020: 18 · 2019: 16 · 2018: 13 · 2017: 10 · 2016: 12 · 2015: 2 · 2014: 14 · 2013: 8 · 2012: 11
- FWCI
- 0.85
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Advanced Drug Delivery Reviews (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- mediaTUM – the media and publications repository of the Technical University Munich (Technical University Munich) (submittedVersion)
- Funders
- National Cancer Institute (R21CA128406, R01CA166078, P30CA008748)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Physical Sciences › Energy › Nuclear Energy and Engineering › Advanced Energy Technologies and Civil Engineering Innovations
- Health Sciences › Health Professions › Radiological and Ultrasound Technology › Radioactivity and Radon Measurements
- Keywords
- actinium-225, radionuclide generator, targeted alpha therapy, decay chains, linear energy transfer, cancer therapy
- MeSH terms
- Actinium, Alpha Particles, Animals, Clinical Trials as Topic, Humans, Radiometry, Radionuclide Generators, Tissue Distribution
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