title: Single vial kit formulation of DOTATATE for preparation of (177) Lu-labeled therapeutic radiopharmaceutical at hospital radiopharmacy.
abstract: The clinical applications of radiolabeled somatostatin analogue (177) Lu-DOTA-Tyr(3) -Thr(8) -Octreotide ((177) Lu-DOTATATE) constitute a promising treatment option for patients with disseminated and inoperable neuroendocrine (NET) tumors. Formulation of (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. (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 (177) Lu-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 (177) Lu-DOTATATE carried out in normal Swiss mice. Deployment of in-house produced (177) LuCl3 , cold kits and easy adaptability of synthesis setup at hospital radiopharmacy for preparation is likely to expand applications of peptide receptor radionuclide therapy.
authors.affiliation: Isotope Production & Applications Division, Bhabha Atomic Research Centre, Mumbai, 400085, India.
authors.forename: Archana
authors.initials: A
authors.lastname: Mukherjee
authors.forename: Sharad
authors.initials: S
authors.lastname: Lohar
authors.forename: Ashutosh
authors.initials: A
authors.lastname: Dash
authors.forename: Haladhar Dev
authors.initials: HD
authors.lastname: Sarma
authors.forename: Grace
authors.initials: G
authors.lastname: Samuel
authors.forename: Aruna
authors.initials: A
authors.lastname: Korde
mesh_terms: D003287:Contrast Media / Q000138:chemical synthesis*; D007553:Isotope Labeling / Q000295:instrumentation / Q000379:methods*; D008187:Lutetium / Q000737:chemistry*; D008422:Materials Testing; D015282:Octreotide / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D009942:Organometallic Compounds / Q000138:chemical synthesis*; D011868:Radioisotopes / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D011933:Reagent Kits, Diagnostic
chemical_list: D003287:Contrast Media; D009942:Organometallic Compounds; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D011933:Reagent Kits, Diagnostic; D008187:Lutetium; C447941:lutetium Lu 177 dotatate; D015282:Octreotide
keywords: 177Lu-DOTATATE; cold kits for radiopharmaceuticals; radiolabeled peptides; radiopharmaceuticals; somatostatin analogues