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Radiolabeled macrocyclic bisphosphonate ligands have recently been demonstrated to be highly efficacious in treatment of patients with painful bone metastases. Herein, we report a robust protocol for formulation of therapeutically relevant doses of  177 Lu-labeled bisphosphonate amide of DOTA (BPAMD) using moderate specific activity  177 Lu produced by direct (n,γ) route and its preliminary investigation in human patients. Doses (2.8 ± 0.2 GBq) were formulated with high radiochemical purity (98.3 ± 0.4 %) using a protocol optimized after extensive radiochemical studies.  In vitro  binding studies with mineralized osteosarcoma cells demonstrated specific binding of the radiotracer. Biodistribution studies in healthy Wistar rats demonstrated rapid skeletal accumulation with fast clearance from the non-target organs. In a patient administered with 555 MBq dose of  177 Lu-BPAMD, intense radiotracer uptake was observed in the metastatic skeletal lesions with insignificant uptake in any other major non-targeted organs. Preliminary clinical investigations carried out after administration of 2.6 GBq of  177 Lu-BPAMD revealed significant reduction in pain after 1 week without any adverse effects. The developed protocol for formulation of  177 Lu-BPAMD doses using moderate specific activity carrier added  177 Lu has been found to be effective and warrants wider investigations in patients with painful skeletal metastases.

radiochimica acta

Formulation of ‘ready-to-use’ human clinical doses of  177 Lu-labeled bisphosphonate amide of DOTA using moderate specific activity  177 Lu and its preliminary evaluation in human patient