177Lu-labeled cyclic polyaminophosphonates as potential agents for bone pain palliation.
177Lu (T 1/2 = 6.71 d, Ebeta(max) = 497 keV) has radionuclidic properties suitable for use in palliative therapy of bone pain due to metastasis. 177Lu was produced in high-specific activity (3-4TBq/g) and excellent radionuclidic purity (100%) by thermal neutron bombardment of natural Lu target. Two cyclic tetraaminomethylene phosphonate ligands, namely DOTMP and CTMP were synthesized and radiolabeled with 177Lu. The 177Lu-DOTMP complex was formed with very high yield (> 99%) and showed excellent stability (up to 40 d at room temperature). Biodistribution of 177Lu-DOTMP was carried out in Wistar rats and the complex showed significant bone uptake (4.23%/g in femur and 5.23% in tibia at 3 h p. i.), rapid clearance from blood (no activity at 3 h p. i.) and minimum uptake in soft tissues.
Das
Tapas
T
Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India.
Chakraborty
Sudipta
S
Unni
P R
PR
Banerjee
Sharmila
S
Samuel
Grace
G
Sarma
H D
HD
Venkatesh
Meera
M
Pillai
M R A
MR
D000818:Animals; D001859:Bone Neoplasms / Q000503:physiopathology / Q000532:radiotherapy / Q000556:secondary; D006573:Heterocyclic Compounds, 1-Ring / Q000493:pharmacokinetics / Q000627:therapeutic use; D008187:Lutetium / Q000493:pharmacokinetics / Q000627:therapeutic use*; D063065:Organophosphonates / Q000493:pharmacokinetics / Q000627:therapeutic use; D009943:Organophosphorus Compounds / Q000493:pharmacokinetics / Q000627:therapeutic use; D010146:Pain / Q000532:radiotherapy*; D010166:Palliative Care; D011868:Radioisotopes / Q000493:pharmacokinetics / Q000627:therapeutic use*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
C440011:1,4,8,11-tetraazacyclotetradecyl-1,4,8,11-tetramethylenephosphonic acid; D006573:Heterocyclic Compounds, 1-Ring; D063065:Organophosphonates; D009943:Organophosphorus Compounds; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D008187:Lutetium; C082084:1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylenephosphonic acid)