Abstract
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.
MeSH terms
-
Animals
-
Bone Neoplasms / physiopathology
-
Bone Neoplasms / radiotherapy
-
Bone Neoplasms / secondary
-
Heterocyclic Compounds, 1-Ring / pharmacokinetics
-
Heterocyclic Compounds, 1-Ring / therapeutic use
-
Lutetium / pharmacokinetics
-
Lutetium / therapeutic use*
-
Organophosphonates / pharmacokinetics
-
Organophosphonates / therapeutic use
-
Organophosphorus Compounds / pharmacokinetics
-
Organophosphorus Compounds / therapeutic use
-
Pain / radiotherapy*
-
Palliative Care
-
Radioisotopes / pharmacokinetics
-
Radioisotopes / therapeutic use*
-
Radiopharmaceuticals / pharmacokinetics
-
Radiopharmaceuticals / therapeutic use*
-
Rats
-
Rats, Wistar
-
Tissue Distribution
Substances
-
1,4,8,11-tetraazacyclotetradecyl-1,4,8,11-tetramethylenephosphonic acid
-
Heterocyclic Compounds, 1-Ring
-
Organophosphonates
-
Organophosphorus Compounds
-
Radioisotopes
-
Radiopharmaceuticals
-
Lutetium
-
1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis(methylenephosphonic acid)