Single vial kit formulation of DOTATATE for preparation of 177Lu‐labeled therapeutic radiopharmaceutical at hospital radiopharmacy

The clinical applications of radiolabeled somatostatin analogue ¹⁷⁷Lu‐DOTA‐Tyr³‐Thr⁸‐Octreotide (¹⁷⁷Lu‐DOTATATE) constitute a promising treatment option for patients with disseminated and inoperable neuroendocrine (NET) tumors. Formulation of ¹⁷⁷Lu‐DOTATATE in hospital radiopharmacy under aseptic conditions in a safe and reliable manner is a major constraint for its extensive use. The present work was intended to develop a kit for the safe preparation of the therapeutic radiopharmaceutical, viz. ¹⁷⁷Lu‐DOTATATE of high quality that can be easily adapted at conventional hospital radiopharmacies. Single vial kits of DOTATATE were formulated and evaluated for suitability for radiolabeling as well as stability on its storage. Patient dose of ¹⁷⁷Lu‐DOTATATE (7.4 GBq) could be successfully prepared using semi‐automated in‐house setup that assures safe handling and high yields of product of pharmaceutical purity suitable for clinical use. Fast clearance of activity via renal route was observed in preclinical biodistribution studies of ¹⁷⁷Lu‐DOTATATE carried out in normal Swiss mice. Deployment of in‐house produced ¹⁷⁷LuCl₃, cold kits and easy adaptability of synthesis setup at hospital radiopharmacy for preparation is likely to expand applications of peptide receptor radionuclide therapy.