Development of 225Ac Radiopharmaceuticals: TRIUMF Perspectives and Experiences
Open accessAbstract
BACKGROUND: The development of radiopharmaceuticals containing 225Ac for targeted alpha therapy is an active area of academic and commercial research worldwide. OBJECTIVES: Despite promising results from recent clinical trials, 225Ac-radiopharmaceutical development still faces significant challenges that must be overcome to realize the widespread clinical use of 225Ac. Some of these challenges include the limited availability of the isotope, the challenging chemistry required to isolate 225Ac from any co-produced isotopes, and the need for stable targeting systems with high radiolabeling yields. RESULTS: Here we provide a review of available literature pertaining to these challenges in the 225Acradiopharmaceutical field and also provide insight into how performed and planned efforts at TRIUMF - Canada's particle accelerator centre - aim to address these issues.
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Radiolabelled compounds allow doctors and researchers to see, measure, and adjust molecular-level processes in the body.
“These radiolabelled compounds, now armed with radioactive ability, allow doctors and researchers to see, measure, and adjust what is happening in the body at the molecular level [10].”
From Radiopharmaceuticals: navigating the frontier of precision medicine and therapeutic innovation (2024) · cites this paper as [10]
The Introduction describes radiolabelled targeting agents delivering radiation to diseased cells, and “Assessing the Biodistribution of the 225Ac Decay Chain” describes imaging and quantifying where radionuclides go in the body (page unavailable). The paper does not establish that these methods let users see or measure processes at the molecular level; it explicitly notes that current in vivo imaging lacks even sub-organ detail. (LLM, conf=0.86)
Experimental — accuracy not yet measuredThe 225Ac-DOTA complex outperformed other chelators in in vitro serum stability testing, with >90% of complexes still intact after 10 days.
“Further in vitro serum stability testing showed that the 225Ac-DOTA complex outperformed the rest with >90% of complexes still intact after 10 days (104).”
From Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists (2022) · cites this paper as [104]
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- Authors
- Robertson, A. K. H., Ramogida, C. F., Schaffer, P., & Radchenko, V.
- Affiliations
- TRIUMF (CA)
- Corresponding author
- Radchenko, Valery
- Venue
- Current Radiopharmaceuticals
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2018-10-22
- Volume
- 11
- Issue
- 3
- Pages
- 156-172
- ISSN
- 1874-4710 (ISSN-L)
- PMC
- PMC6249690
- OpenAlex
- W2801430183
- Cited by
- 202
- References
- 59
- Citations by year
- 2026: 23 · 2025: 35 · 2024: 34 · 2023: 24 · 2022: 22 · 2021: 29 · 2020: 26 · 2019: 8 · 2018: 1
- FWCI
- 11.05
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- cc-by-nc
- Locations
- Current Radiopharmaceuticals (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion, cc-by-nc)
- PubMed Central (publishedVersion, cc-by-nc)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Chemical Reactions and Isotopes
- Health Sciences › Health Professions › Radiological and Ultrasound Technology › Radioactivity and Radon Measurements
- Keywords
- actinium-225, radiopharmaceuticals, targeted alpha therapy, TRIUMF, isotope separation, radiolabeling yield, alpha-emitting radionuclides
- MeSH terms
- Actinium, Alpha Particles, Humans, Neoplasms, Radiochemistry, Radionuclide Generators, Radiopharmaceuticals
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