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Pharmacotechnical development of DOTATATO lyophilized kit for 68Ga labeling and preclinical evaluation

Grant number: 19/04172-7
Support type:Scholarships in Brazil - Doctorate
Effective date (Start): April 01, 2019
Effective date (End): March 31, 2021
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Elaine Bortoleti de Araújo
Grantee:Maria Renata Valente Brandão Freire
Home Institution: Instituto de Pesquisas Energéticas e Nucleares (IPEN). Secretaria de Desenvolvimento Econômico (São Paulo - Estado). São Paulo , SP, Brazil
Associated research grant:17/50332-0 - Scientific, technological and infrastructure qualification in radiopharmaceuticals, radiation and entrepreneurship for health purposes, AP.PDIP


Neuroendocrine tumors represent a heterogeneous group of carcinomas, which originate in neural and endocrine cells and whose incidence and prevalence has increased over the last decades. Currently, gallium-68-labeled somatostatin analogues, such as 68Ga-DOTATOC [DOTA-D-Phe1-Tyr3-ocreotide] 68Ga-DOTANOC [1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid]-1-Na13-ocreotide], 68Ga-DOTATATE (DOTA-Tyr3-Octreotate) are considered gold standard in the diagnosis of neuroendocrine tumors, since they overexpress various types of receptors, such as somatostatin. The development of DOTA-peptide lyophilized kits for 68Ga labeling will enable wide distribution and the easy adaptation of the marking method in hospital radiopharmacies at more accessible costs, will expand the diagnostic applications of neuroendocrine tumors by PET in the country.The present work aims the pharmacotechnical development, quality control and biological evaluation of a DOTATATE lyophilized kit for 68Ga labeling obtained from different 68Ge/68Ga generators, as a strategy that will promote its widespread use in the radiopharmacies of the hospital's nuclear medicine centers in the country. The performance of the kit will be evaluated for expected biodistribution, lesion detection and dose optimization, and compared to the performance of 68Ga-DOTATATE produced in an automated synthesis module. The freeze-dried kit for obtaining 68Ga-DOTATATE to be developed at the IPEN Radiopharmacy Center, represents a real possibility of expansion of the diagnosis and management of the treatment of patients with recurrent neuroendocrine tumor, as well as a sensitive tool to support clinical trials. (AU)