212Bi-DOTMP: an alpha particle emitting bone-seeking agent for targeted radiotherapy.
The synthesis and in vivo stability of the bone-seeking alpha-particle emitting compounds 212Bi-DOTMP and 212Pb/212Bi-DOTMP are described. 212Bi-DOTMP, injected i.v. into Balb/c mice, showed prominent bone localization and a rapid clearance from blood and other organs. Femur/blood ratios increased from 13 at 15 min up to 490 at 2.0 h postinjection. Enhanced uptake of 212Bi-DOTMP was demonstrated in regions with high bone turnover. A comparison between 212Bi-DOTMP and [153Sm]Sm-EDTMP showed essentially no differences in biodistribution. 212Pb/212Bi-DOTMP followed a similar biodistribution, except for slightly elevated levels of 212Bi in the kidneys. The present study has shown 212Bi-DOTMP to be an in vivo stable bone-seeking radiopharmaceutical with promising biological properties for the treatment of sclerotic metastases and osteoblastic osteosarcoma.
Hassfjell
S P
SP
Department of Chemistry, University of Oslo, Norway.
Bruland
O S
OS
Hoff
P
P
D000512:Alpha Particles; D000818:Animals; D001729:Bismuth / Q000737:chemistry*; D001842:Bone and Bones / Q000378:metabolism*; D004355:Drug Stability; D005260:Female; D005269:Femur / Q000378:metabolism; D007856:Lead Radioisotopes; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008807:Mice, Inbred BALB C; D009943:Organophosphorus Compounds / Q000737:chemistry* / Q000493:pharmacokinetics; D011868:Radioisotopes; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution
D007856:Lead Radioisotopes; D009943:Organophosphorus Compounds; D011868:Radioisotopes; D019275:Radiopharmaceuticals; C082084:1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylenephosphonic acid); D001729:Bismuth