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Review
. 2018;11(3):156-172.
doi: 10.2174/1874471011666180416161908.

Development of 225Ac Radiopharmaceuticals: TRIUMF Perspectives and Experiences

Andrew Kyle Henderson Robertson  1   2 , Caterina Fortunata Ramogida  1 , Paul Schaffer  1   3 , Valery Radchenko  1
Affiliations
Review

Development of 225Ac Radiopharmaceuticals: TRIUMF Perspectives and Experiences

Andrew Kyle Henderson Robertson et al. Curr Radiopharm. 2018.

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.

Keywords: Actinium-225; TRIUMF; isotope production; radiochemistry; radiolabeling; targeted alpha therapy..

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Figures

Fig. (1)
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).
Fig. (2)
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.
Fig. (3)
Fig. (3)
DOTA-urea conjugate PSMA-617 used for targeting of prostate-specific membrane antigen.
See this image and copyright information in PMC

References

    1. McDevitt M.R., Sgouros G., Finn R.D., Humm L.J., Jurcic J.G., Larson S.M., Scheinberg D.A. Radioimmunotherapy with alpha-emitting nuclides. Eur. J. Nucl. Med. Mol. Imaging. 1998;25(9):1341–1351. - PubMed
    1. Couturier O., Supiot S., Degraef-Mougin M., Faivre-Chauvet A., Car-lier T., Chatal J.F., Davodeau F., Cherel M. Cancer radioimmunotherapy with alpha-emitting nuclides. Eur. J. Nucl. Med. Mol. Imaging. 2005;32(5):601–614. - PubMed
    1. Mulford D.A., Scheinberg D.A., Jurcic J.G. The promise of targeted {alpha}-particle therapy. J. Nucl. Med. 2005;46(1):S199–S204. - PubMed
    1. Brechbiel M.W. Targeted alpha-therapy: Past, present, future? Dalton Trans. 2007;43:4918–4928. - PMC - PubMed
    1. Wilbur S.D. Chemical and radiochemical considerations in radiolabeling with α-emitting radionuclides. Curr. Radiopharm. 2011;4:214–217. - PubMed

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