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Feasibility of the radioastatination of a monoclonal antibody with astatine-211 purified by wet extraction

Abstract : Astatine-211, a most promising a-particle emitter for targeted radiotherapy, is generally obtained by high-temperature distillation. However, a liquid-liquid extraction procedure (wet extraction) has also been described. The purpose of this study was to develop and optimize the labelling of the stannylated-activated ester N-hydroxysuccinimidyl-metatrimethylstannylbenzoate ester (MeSTB) with astatine-211 extracted in di-isopropylether (DIPE) in the presence of the oxidant N-chlorosuccinimide (NCS). The effect of final volume, incubation duration and NCS amounts on radiolabelling yield was studied. The best yields (85-90%) of N-hydroxysuccinimidyl-meta-[ 211 At]astatobenzoate ester (SAB) were obtained with 20 nmol of MeSTB, 100 nmol of NCS in 120 mL of DIPE after 15 min. The astatine-211-labelled-activated ester was then used to radiolabel a monoclonal antibody (mAb). The labelling yield was 20-25% and the radiochemical purity was 97-99%. These results show that mAbs may be efficiently labelled with astatine-211 obtained by wet extraction, a fully automatable technique that may prove to be a useful alternative to dry distillation for high activity labelling of radiopharmaceuticals.
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https://www.hal.inserm.fr/inserm-03290253
Contributor : François Guérard Connect in order to contact the contributor
Submitted on : Monday, July 19, 2021 - 11:38:32 AM
Last modification on : Friday, July 30, 2021 - 4:03:08 AM

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Mickaël Bourgeois, François Guérard, Cyrille Alliot, Marie Mougin-Degraef, Holisoa Rajerison, et al.. Feasibility of the radioastatination of a monoclonal antibody with astatine-211 purified by wet extraction. Journal of Labelled Compounds and Radiopharmaceuticals, Wiley-Blackwell, 2008, 51 (11), pp.379 - 383. ⟨10.1002/jlcr.1543⟩. ⟨inserm-03290253⟩

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