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Obtaining and evaluating the applicability in the treatment of Prostate Cancer of the PSMA-617 kit for prompt radiolabeling with lutetium-177

Grant number: 18/12965-4
Support type:Scholarships in Brazil - Doctorate
Effective date (Start): September 01, 2018
Effective date (End): November 30, 2020
Field of knowledge:Engineering - Nuclear Engineering - Applications of Radioisotopes
Principal Investigator:Elaine Bortoleti de Araújo
Grantee:Cristian Antonio Wieczorek Villas Boas
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

Abstract

The PSMA is a specific prostatic membrane antigen (glycoprotein type 2) found in the membrane or cytoplasm of the Prostate Cancer cell and has been targeted for treatment of this disease. The discovery of PSMA allowed the creation of novel substances that bind specifically to the antigen and results into more efficient therapies for non-responsive cases, especially of cancer that is not responsive to castration, radiotherapy and chemotherapy, when patient survival is reduced. Currently, there are some antagonists under study, and the most promising results were obtained with PSMA-617.The objective of this project, is to study the radiolabeling parameters of PSMA-617 with lutetium-177 to obtain high specific radiochemical purity and specific activity, evaluate the stability of the radiopharmaceutical and establish the conditions (at therapeutic activity) to transport it without implications on the quality. Chromatographic models (thin layer and High Efficiency Liquid Chromatography) will be tested to evaluate the radiochemical purity of the radiolabelings. Finally, a scale-up study of radiolabeling with activities compatible with radiopharmaceutical production in a manufacturing routine will be conducted. Also the aim of this study is to analyze the therapeutic potential of this radiopharmaceutical with preclinical studies including in vitro tumor cell binding assays and in vivo studies in healthy animals and in animals with a tumor model for Prostate Cancer. The influence of the specific activity of the lutein-177 radionuclide on the efficiency of binding of the radiopharmaceutical to tumor cell receptors will be assessed by in vitro binding studies. (AU)