Comparative studies of 177Lu-EDTMP and 177Lu-DOTMP as potential agents for palliative radiotherapy of bone metastasis

Appl Radiat Isot. 2008 Sep;66(9):1196-205. doi: 10.1016/j.apradiso.2008.02.061. Epub 2008 Feb 17.


(177)Lu is presently considered as an excellent radionuclide for developing bone pain palliation agents owing to its suitable nuclear decay characteristics [T(1/2)=6.73d, E(beta)((max))=497keV, E(gamma)=113keV (6.4%) and 208keV (11%)] and large-scale production feasibility with adequate specific activity using moderate flux research reactors. Multidentate polyaminophosphonic acids have already been proven as the carrier molecule of choice for radiolanthanides and similar +3 metal ions in designing agents for palliative radiotherapy of bone pain due to skeletal metastases. The present paper describes a comparison between (177)Lu complexes of two potential polyaminophosphonic acid ligands, namely Ethylenediaminetetramethylene phosphonic acid (EDTMP) and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene phosphonic acid (DOTMP) with respect to their radiochemical and in-vivo biological characteristics. Although both the agents have exhibited promising features, the study reveals that (177)Lu-EDTMP has marginally higher skeletal accumulation in comparison to that of (177)Lu-DOTMP, while the latter has slightly faster blood clearance along with lower retention in liver and kidneys in animal models.

MeSH terms

  • Animals
  • Bone Neoplasms
  • Drug Stability
  • Lutetium / pharmacokinetics
  • Lutetium / therapeutic use*
  • Organometallic Compounds / pharmacokinetics
  • Organometallic Compounds / therapeutic use*
  • Organophosphorus Compounds / pharmacokinetics
  • Organophosphorus Compounds / therapeutic use*
  • Pain
  • Palliative Care
  • Rabbits
  • Radioisotopes / pharmacokinetics
  • Radioisotopes / therapeutic use*
  • Rats
  • Rats, Wistar
  • Tissue Distribution


  • 177Lu-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylenephosphonic acid)
  • Organometallic Compounds
  • Organophosphorus Compounds
  • Radioisotopes
  • lutetium ethylenediaminetetramethylene phosphonic acid
  • Lutetium