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Feasibility of the radioastatination of a monoclonal antibody with astatine‐211 purified by wet extraction
Author(s) -
Bourgeois Mickaël,
Guerard François,
Alliot Cyrille,
MouginDegraef Marie,
Rajérison Holisoa,
RemaudLe Saëc Patricia,
Gestin JeanFrançois,
Davodeau François,
Chérel Michel,
Barbet Jacques,
FaivreChauvet Alain
Publication year - 2008
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1543
Subject(s) - chemistry , astatine , labelling , yield (engineering) , extraction (chemistry) , chromatography , monoclonal antibody , distillation , radiochemistry , antibody , biochemistry , physics , materials science , quantum mechanics , voltage , immunology , metallurgy , biology
Astatine‐211, a most promising α ‐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‐ meta ‐trimethylstannylbenzoate 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 µL 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. Copyright © 2008 John Wiley & Sons, Ltd.