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The novel bis(methylphosphonate) 2,2′-[4,10-bis(phosphonomethyl)-1,4,7,10-tetraazacyclododecane-1,7-diyl] diacetic acid,  trans -H 6 DO2A2P, has been synthesized and characterized by multinuclear NMR spectroscopy ( 1 H,  13 C and  31 P).  153 Sm and  166 Ho complexes with  trans -H 6 DO2A2P have been prepared in high yield using a 1:2 metal to ligand molar ratio at 70 °C, pH 8−9. These complexes are hydrophilic, negatively charged and stable  in vitro  under physiological solutions, up to 48 h. They present a low plasmatic protein binding and some  in vitro  hydroxyapatite adsorption, mainly for  166 Ho- trans -DO2A2P. Both complexes are stable  in vivo , have a fast tissue clearance from most organs and a rapid total excretion from whole animal body. Moderate bone uptake was also observed but the accumulated radioactivity rapidly decreases with time.

Radiochemical and biological behaviour of 153 Sm and 166 Ho complexes anchored by a novel bis(methylphosphonate) tetraazamacrocycle