Preparation and Evaluation of 177Lu-TDTMP: A Potential Theranostic Agent for Bone Metastases

Document Type : Original Article

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Ass.professor -labelled compounds-Hot Labs center

Abstract

177Lu was produced in high-specific activity and excellent radionuclidic purity by thermal neutron bombardment of 176Yb target.Tetramethylene diamine tetramethylenephosphonic acid (TDTMP) was radiolabeled with 177Lu and complexation parameters were studied and optimized: 8.4 µg TDTMP, ~243 Ci of 177Lu activity, pH= 8 and the reaction mixture was kept at room temperature for 30 min.The complex, formed with high yield (>99%) and retained its stability for more than 14 days. The complex structure was predicted and its binding to target enzyme was assessed in-silico..Biodistribution study carried out in normal and tumorized Wister rats showed significant skeletal uptake, the 177Lu-TDTMP, results clearly indicated that it has high affinity for bone mineral. Femur and tibia uptakes of the labelled complex were ~ 6.4 % and ~7.1 % at 3 hours post injection compared to ~ 4 % and ~ 4.3 % in case of 177LuCl3. Thereafter, the uptakes increased continuously to a maximum of ~ 7.9 % and ~ 8.3 % at 48 hours after injection were noticed.

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