title: Comparative studies of 177Lu-EDTMP and 177Lu-DOTMP as potential agents for palliative radiotherapy of bone metastasis.
abstract: (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.
authors: Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India.
authors: Sudipta
authors: S
authors: Chakraborty
authors: Tapas
authors: T
authors: Das
authors: Haladhar Dev
authors: HD
authors: Sarma
authors: Meera
authors: M
authors: Venkatesh
authors: Sharmila
authors: S
authors: Banerjee
mesh_terms: D000818:Animals; D001859:Bone Neoplasms; D004355:Drug Stability; D008187:Lutetium / Q000493:pharmacokinetics / Q000627:therapeutic use*; D009942:Organometallic Compounds / Q000493:pharmacokinetics / Q000627:therapeutic use*; D009943:Organophosphorus Compounds / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010146:Pain; D010166:Palliative Care; D011817:Rabbits; D011868:Radioisotopes / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: C531954:177Lu-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylenephosphonic acid); D009942:Organometallic Compounds; D009943:Organophosphorus Compounds; D011868:Radioisotopes; C119503:lutetium ethylenediaminetetramethylene phosphonic acid; D008187:Lutetium