177Lu-EDTMP: a potential therapeutic bone agent.
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.
Ando
A
A
School of Health Sciences, Faculty of Medicine, Kanazawa University, Japan.
Ando
I
I
Tonami
N
N
Kinuya
S
S
Kazuma
K
K
Kataiwa
A
A
Nakagawa
M
M
Fujita
N
N
D000818:Animals; D001610:Beta Particles; D001859:Bone Neoplasms / Q000503:physiopathology / Q000532:radiotherapy / Q000556:secondary; D001842:Bone and Bones / Q000378:metabolism; D005269:Femur / Q000378:metabolism; D005720:Gamma Rays; D006801:Humans; D008187:Lutetium / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008297:Male; D009942:Organometallic Compounds / Q000493:pharmacokinetics* / Q000627:therapeutic use; D009943:Organophosphorus Compounds / Q000493:pharmacokinetics* / Q000627:therapeutic use; D010146:Pain; D010166:Palliative Care; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D013669:Technetium Tc 99m Medronate / Q000493:pharmacokinetics; D013997:Time Factors; D014018:Tissue Distribution
D009942:Organometallic Compounds; D009943:Organophosphorus Compounds; D019275:Radiopharmaceuticals; C119503:lutetium ethylenediaminetetramethylene phosphonic acid; D008187:Lutetium; D013669:Technetium Tc 99m Medronate