Single vial kit formulation of DOTATATE for preparation of super(177)Lu-labeled therapeutic radiopharmaceutical at hospital radiopharmacy

• Published in: Journal of labelled compounds & radiopharmaceuticals Vol. 58; no. 4; pp. 166 - 172
• Main Authors: Mukherjee, Archana, Lohar, Sharad, Dash, Ashutosh, Sarma, Haladhar Dev, Samuel, Grace, Korde, Aruna
• Format: Journal Article
• Language: English
• Published: 01.04.2015
• ISSN: 0362-4803; 1099-1344
• DOI: 10.1002/jlcr.3267

The clinical applications of radiolabeled somatostatin analogue super(177)Lu-DOTA-Tyr super(3)-Thr super(8)-Octreotide ( super(177)Lu-DOTATATE) constitute a promising treatment option for patients with disseminated and inoperable neuroendocrine (NET) tumors. Formulation of super(177)Lu-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. super(177)Lu-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 super(177)Lu-DOTATATE (7.4GBq) 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 super(177)Lu-DOTATATE carried out in normal Swiss mice. Deployment of in-house produced super(177)LuCl sub(3), cold kits and easy adaptability of synthesis setup at hospital radiopharmacy for preparation is likely to expand applications of peptide receptor radionuclide therapy. Schematics of semi-automated module for super(177)Lu-DOTATATE preparation.