Comparative studies of 177Lu-EDTMP and 177Lu-DOTMP as potential agents for palliative radiotherapy of bone metastasis.
(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.
Chakraborty
Sudipta
S
Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India.
Das
Tapas
T
Sarma
Haladhar Dev
HD
Venkatesh
Meera
M
Banerjee
Sharmila
S
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
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