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Rene Raave, Gerwin Sandker, Sandra Heskamp, Otto Boerman, Mark Rijpkema, Floriane Mangin, Michel Meyer, Jean-Claude Chambron, Mathieu Moreau, Claire Bernhard, Victor Goncalves, Franck Denat

ESRR 18, 19th European Symposium on Radiopharmacy and Radiopharmaceuticals, 05-08 April 2018, Groningen, Netherlands

Abstract

The current “gold standard” chelator to label antibodies with ⁸⁹Zr for immunoPET is desferrioxamine (DFO). Preclinical studies have shown that the ⁸⁹Zr-DFO complex is partly unstable in vivo, resulting in release of ⁸⁹Zr and subsequent accumulation of ⁸⁹Zr in mineral bone tissue. This bone uptake may prevent the detection of bone metastases, and hampers accurate estimation of the radiation dose to the bone marrow in dose planning for radioimmunotherapy. Therefore, there is a need for a more stable ⁸⁹Zr chelator. Here we report DFO-cyclo*, a preorganized extended DFO derivative introducing an octacoordination, and investigate the stability of its ⁸⁹Zr complex over the unsaturated hexacoordinated ⁸⁹Zr-DFO complex in vitro and in vivo.