Preparation and evaluation of 177Lu-DOTA-Tyr3-Octreotate for use as atherapeutic radiopharmaceutical

摘要

The present paper describes the radiolabeling of DOTA-tyrosine-3-octreotate (DOTATATE)rnwith 177Lu and the in-vitro and in-vivo biological evaluation of the radiolabeled peptide.rnTyrosine-3-octreotate, a disulphide-linked cyclic octapeptide and a somatostatin analogue, is reportedrnto bind with a wide variety of tumours over-expressing somatostatin receptors. 177Lu is presentlyrnbeing considered as a promising radionuclide for the development of peptide receptor radionucliderntherapy (PRRT) agents. The production of 177Lu with adequately high specific activity and excellentrnradionuclidic purity was optimized using moderate flux reactor. The radiolabeling of DOTA-TATErnwith 177Lu was achieved with excellent radiochemical purity and the radiolabeled agent showed highrnstability. The receptor specificity of the developed radiochemical agent was determined by carryingrnout in-vitro cell binding studies with three different cell-lines as well as by imaging studies in nudernmice bearing tumours over-expressing somatostatin receptors.