Abstract
Lutetium-177 (177Lu) has both beta particle emissions for a therapeutic effect and gamma emissions for imaging. This study was undertaken to synthesize and evaluate 177Lu-EDTMP (ethylenediaminetetramethylene phosphonic acid) as a therapeutic radiopharmaceutical for the palliation of pain from bone metastases. Chelation of 177Lu to EDTMP was obtained by heating for 30 min in boiling water at pH 8.8, resulting in a radiochemical yield of over 99%. The compound was stable for 20 days without any appreciable dissociation. Biodistribution studies in normal rats indicated selective bone accumulation, showing faster blood clearance, higher bone uptake and higher bone-to-soft tissue ratios than 99Tcm-MDP. In conclusion, 177Lu-EDTMP has favourable biological and physical characteristics for the palliative treatment of painful bone metastases.
MeSH terms
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Animals
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Beta Particles
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Bone Neoplasms / physiopathology
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Bone Neoplasms / radiotherapy
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Bone Neoplasms / secondary
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Bone and Bones / metabolism
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Femur / metabolism
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Gamma Rays
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Humans
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Lutetium / pharmacokinetics*
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Lutetium / therapeutic use
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Male
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Organometallic Compounds / pharmacokinetics*
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Organometallic Compounds / therapeutic use
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Organophosphorus Compounds / pharmacokinetics*
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Organophosphorus Compounds / therapeutic use
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Pain
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Palliative Care
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacokinetics*
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Radiopharmaceuticals / therapeutic use
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Rats
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Rats, Wistar
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Technetium Tc 99m Medronate / pharmacokinetics
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Time Factors
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Tissue Distribution
Substances
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Organometallic Compounds
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Organophosphorus Compounds
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Radiopharmaceuticals
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lutetium ethylenediaminetetramethylene phosphonic acid
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Lutetium
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Technetium Tc 99m Medronate