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KMID : 1145520150010010053
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Journal of Radiopharmaceuticals and Molecular Probes
2015 Volume.1 No. 1 p.53 ~ p.61
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In vivo comparison of Lu-177-labeled phosphonate compounds as potential agents for bone pain palliation in rodents
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Chang Young-Soo
Lee Yun-Sang
Kim Young-Ju
Jeong Jae-Min
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Abstract
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Lutetium-177 (T1/2=6.71 day) is an adequate radionuclide for therapy, which has both beta emission (Emax=497 keV) for therapeutic effect and gamma emission (113 and 208 keV) for imaging. 177Lu labeled ethylenediamine-N,N,N',N'-tetrakis (methylene phosphonic acid) (EDTMP) and 1,4,7,10-tetraazacyclododecane1,4,7,10-tetraaminomethylenephosphonate
(DOTMP) have been proposed as radiopharmaceuticals for bone pain palliation. In this study, we compared radiochemistry and biodistribution of 177Lu-EDTMP and 177Lu-DOTMP. EDTMP and DOTMP were synthesized, and 1 mg of each was labeled with 177Lu at pH 7~8 with high efficiency (>98%). For comparative biodistribution studies, 177Lu-EDTMP or 177Lu-DOTMP were injected into ICR-mice through tail vein, and then biodistribution data were obtained as percentages of injected dose per gram of tissue (% ID/g). Urine excretions of both agents in mice were checked for 7 days. Rat images were also obtained after injection of 177Lu-EDTMP or 177Lu-DOTMP. 177Lu-DOTMP (100% at 1 min) showed faster labeling than 177Lu-EDTMP (100% at 30 min). Both of them were stable at least for 21 days at room temperature. High bone uptakes were found for both 177Lu-EDTMP and 177Lu-DOTMP: 38.0 and 34.1% ID/g at 3 hr, respectively; and 33.2 and 18.8% ID/g at 7 day, respectively. Rapid excretions to urine were found for both agents (177Lu-EDTMP: 56%, 177Lu-DOTMP: 63% at 1 day). Other organs showed very low uptakes. Rat images of both 177Lu-EDTMP and 177Lu-DOTMP showed high bone uptakes and low soft tissue uptakes. In conclusion, both 177Lu-EDTMP and 177Lu-DOTMP showed high potential as bone pain palliation agents. 177Lu-EDTMP showed higher bone uptake and slower bone clearance in mice than those of 177Lu-DOTMP.
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KEYWORD
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Bone pain palliation, Therapeutic radiopharmaceutical, 177Lu-EDTMP, 177Lu-DOTMP, Biodistribution
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