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M. Paula Campello, Fernanda Marques, Lurdes Gano, Sara Lacerda, Isabel Santos

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

Keywords: Radiolanthanides, Mixed-tetraazamacrocycles, Radiopharmaceuticals, Biodistribution

The novel bis(methylphosphonate) 2,2′-[4,10-bis(phosphonomethyl)-1,4,7,10-tetraazacyclododecane-1,7-diyl] diacetic acid, trans-H₆DO2A2P, has been synthesized and characterized by multinuclear NMR spectroscopy (¹H, ¹³C and ³¹P). ¹⁵³Sm and ¹⁶⁶Ho complexes with trans-H₆DO2A2P 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 ¹⁶⁶Ho-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.

Radiochimica Acta, Oldenbourg Wissenschaftsverlag

Print ISSN: 0033-8230
Volume: 95, 06/2007
Pages: 329 - 334

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