Cited by 203Radiopharmaceutical Chemistry and ApplicationsChemical Reactions and IsotopesRadioactivity and Radon Measurements

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Development of 225Ac Radiopharmaceuticals: TRIUMF Perspectives and Experiences

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Robertson, Andrew Kyle Henderson, Ramogida, Caterina Fortunata, Schaffer, Paul, Radchenko, Valery·2018·Current Radiopharmaceuticals

DOI 10.2174/1874471011666180416161908PMC PMC6249690

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Abstract

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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Fig. (1) Decay schematic showing the decay and production pathways for 225Ac. Gamma emissions useful for quantification of 225Ac are shown in red. (The color version of the figure is available in the electronic copy of the article).CC BY-NC · PubMed Central

Fig. (2) Depiction of the recoil effect associated with α-decay of 225Ac. Daughter isotope 221Fr is released from the chelating agent due to the 100 keV recoil energy associated with the alpha emission of 225Ac. 221Fr and its decay daughters are consequently free to migrate within in the body.CC BY-NC · PubMed Central

Fig. (3) DOTA-urea conjugate PSMA-617 used for targeting of prostate-specific membrane antigen.CC BY-NC · PubMed Central

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Authors: Robertson, A. K. H., Ramogida, C. F., Schaffer, P., & Radchenko, V.
Affiliations: TRIUMF (CA)
Corresponding author: Radchenko, Valery
ORCID: Robertson, Andrew Kyle Henderson
Ramogida, Caterina Fortunata
Schaffer, Paul
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)
DOI: 10.2174/1874471011666180416161908
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
Physical Sciences › Physics and Astronomy › Radiation › 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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Development of 225Ac Radiopharmaceuticals: TRIUMF Perspectives and Experiences

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