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Issue 3, 2017
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Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development

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Abstract

We report our initial investigations into the use of tetraazamacrocycles as zirconium-89 chelators. We describe the synthesis and complete characterization of several Zr tetraazamacrocycle complexes, and definitively describe the first crystal structure of zirconium 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (Zr–DOTA) using single crystal X-ray diffraction analysis. After evaluating several radioactive analogs, we found that 89Zr–DOTA is superior to 89Zr–DFO, the only 89Zr-complex to be used clinically in 89Zr-radiopharmaceutical applications. Finally, we provide a rationale for the unanticipated and extraordinary stability of these complexes in vitro and in vivo. These results may inform the development of safer and more robust immuno-PET agents for precision medicine applications.

Graphical abstract: Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development

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Publication details

The article was received on 14 Sep 2016, accepted on 12 Dec 2016 and first published on 13 Dec 2016


Article type: Edge Article
DOI: 10.1039/C6SC04128K
Chem. Sci., 2017,8, 2309-2314
  • Open access: Creative Commons BY license
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    Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development

    D. N. Pandya, N. Bhatt, H. Yuan, C. S. Day, B. M. Ehrmann, M. Wright, U. Bierbach and T. J. Wadas, Chem. Sci., 2017, 8, 2309
    DOI: 10.1039/C6SC04128K

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