Implementation of the Cu-mediated radiofluorination methods to the production of PET radiotracers for preclinical and clinical applications

• Applicant: Professor Dr. Boris Zlatopolskiy
• Subject Area: Pharmacy
• Term: from 2016 to 2022
• Project identifier: Deutsche Forschungsgemeinschaft (DFG) - Project number 317671364

The great diagnostic potential of many 18F-labeled PET-probes remains incompletely exploited in current clinical practice mainly owing to the lack of simple and efficient procedures for their preparation. Implementation of emerging methods for transition metal-mediated radiofluorination using [18F]fluoride should facilitate the accessibility of known PET tracers and, furthermore, enable an accelerated development of novel molecular probes for clinical applications. This in turn will improve the efficacy of clinical diagnostics and, ultimately, patient care. The main focus of this project is to develop simple and time-saving procedures for the efficient preparation of known and novel PET-tracers using Cu-mediated radiofluorination. The main emphasis of this project lies on the development of radiolabeling protocols which enable efficient and time-saving production of probes which are impossible or difficult to synthesize using conventional radiofluorination procedures. Our efforts will be concentrated on the preparation of already known and novel 18F-labeled amino acids and TSPO ligands suitable for visualization of tumors and neurological disorders. Radiolabeled amino acids enable to assess the high protein synthesis rate in cancer as well as the integritiy of monoaminergic systems, dysregulated in various neurodegenerative diseases. TSPO ligands are in turn suitable for imaging of inflammatory processes closely related to dysfunctions of the brain like Parkinsons disease, stroke and Huntingtons disease. Importantly, cGMP-compliant procedures for the automated preparation of the tracers are to be developed. Radiotracers will be evaluated in vitro and in vivo in a chorioallantoic membrane model as well as in suitable rodent models. This project will be carried out in cooperation with Prof. R. Krasikova (IHB RAS; Russian Federation) who has many years of experience in the development of procedures for the preparation of radiolabeled amino acids and other PET-tracers as well as in automation of radiosyntheses.

• DFG Programme: Research Grants
• International Connection: Russia
• Partner Organisation: Russian Foundation for Basic Research
• Co-Investigator: Professorin Dr. Heike Endepols