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Conference Abstract: Novel 89Zr chelator
Evaluation of the in vitro and in vivo characteristics of the novel89Zr-octacoordinated chelator DFO-cyclo* compared to the hexacoordinated DFO (Conference Abstract)
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
31st Annual Congress of the European Association of Nuclear Medicine, 13-17 October 2018, Duesseldorf
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 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 89Zrr complex over the unsaturated hexacoordinated 89Zr-DFO complex in vitro and in vivo.