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Preparation and evaluation of a radiogallium complex-conjugated bisphosphonate as a bone scintigraphy agent

Kazuma Ogawa; Kenichiro Takai; Hiroya Kanbara; Tatsuto Kiwada; Yoji Kitamura; Kazuhiro Shiba; Akira Odani (Profiled Authors: AKIRA ODANI; KAZUMA OGAWA; TATSUTO KIWADA; KAZUHIRO SHIBA; YOJI KITAMURA)

Nuclear Medicine and Biology. 2011;38(5):631-636.

Introduction: ⁶⁸Ga is a radionuclide of great interest as a positron emitter for positron emission tomography (PET). To develop a new bone-imaging agent with radiogallium, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) was chosen as a chelating site and Ga-DOTA complex-conjugated bisphosphonate, which has a high affinity for bone, was prepared and evaluated. Although we are interested in developing ⁶⁸Ga-labeled bone imaging agents for PET, in these initial studies ⁶⁷Ga was used because of its longer half-life. Methods: DOTA-conjugated bisphosphonate (DOTA-Bn-SCN-HBP) was synthesized by conjugation of 2-(4-isothiocyanatebenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid to 4-amino-1-hydroxybutylidene-1,1-bisphosphonate (alendronate). ⁶⁷Ga-DOTA-Bn-SCN-HBP was prepared by coordination with ⁶⁷Ga, and its in vitro and in vivo evaluations were performed. Results: ⁶⁷Ga-DOTA-Bn-SCN-HBP was prepared with a radiochemical purity of over 95% without purification. ⁶⁷Ga-DOTA-Bn-SCN-HBP had great affinity for hydroxyapatite in binding assay. In biodistribution experiments, ⁶⁷Ga-DOTA-Bn-SCN-HBP accumulated in bone rapidly but was hardly observed in tissues other than bone. Pretreatment of an excess amount of alendronate inhibited the bone accumulation of ⁶⁷Ga-DOTA-Bn-SCN-HBP. Conclusions: ⁶⁷Ga-DOTA-Bn-SCN-HBP showed ideal biodistribution characteristics as a bone-imaging agent. These findings should provide useful information on the drug design of bone imaging agents for PET with ⁶⁸Ga. © 2011 Elsevier Inc.

PMID: 21718937    

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