212Bi-DOTMP: an alpha particle emitting bone-seeking agent for targeted radiotherapy

Nucl Med Biol. 1997 Apr;24(3):231-7. doi: 10.1016/s0969-8051(97)00059-0.


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.

MeSH terms

  • Alpha Particles
  • Animals
  • Bismuth / chemistry*
  • Bone and Bones / metabolism*
  • Drug Stability
  • Female
  • Femur / metabolism
  • Lead Radioisotopes
  • Magnetic Resonance Spectroscopy
  • Mice
  • Mice, Inbred BALB C
  • Organophosphorus Compounds / chemistry*
  • Organophosphorus Compounds / pharmacokinetics
  • Radioisotopes
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / pharmacokinetics
  • Tissue Distribution


  • Lead Radioisotopes
  • Organophosphorus Compounds
  • Radioisotopes
  • Radiopharmaceuticals
  • 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylenephosphonic acid)
  • Bismuth