Evaluation of complexing properties of chelating agents for the bismuth-213

The bismuth-213 is an alpha- and beta-emitting radioelement of very short physical half-life (45 min) obtained by means of a (225Ac-213Bi) generator. Given its radiotoxicity, this element presents an interest in radioimmunotherapy (RIT). At present, the DTPA derivatives alone are used in radiolabelling of antibodies for RIT. This study presents the complexing properties of other chelates potentially usable to this goal. Four original chelating agents were synthesized in order to choose the families giving the best results in complexing the 213Bi: the tri-ethylene-tetra-amino-hexa-carboxylic acid (HETA), the 1, 4, 7, 10-tetra-aza-cyclo-dodecane-1, 4, 7, 10-tetraacetic- 1- Gly-L-p-nitro Phe-amide (DOTA-pept), the 1, 4, 8, 11-tetrakis [(S)-2 hydroxy-propyl]-1, 4, 8, 11-tetra-aza-cyclo-tetra-decane (THEOH), and the ethylenediamine di-acetate di-acetamide-bis-thiophenol (EDTA-TH). Given the physical characteristics of 213Bi and the goal of our research, the studies of complexation were conducted by C.C.M. on silica, in highly diluted solution, with fixed chelates-213Bi incubation time (15 min), and variable temperature and concentrations. Analysis of the results have been done by means of a phosphor-imager by measuring the number of pixels associated to every chromatographic spot. The obtained results show that the poly-aza poly-carboxylic derivatives and poly-aza di-thio dicarboxylic derivatives are the only able ones to complex rapidly and quantitatively the 213Bi