Development and application of new 18F-labeled glycoconjugates for PET

• Applicant: Dr. Simone Maschauer
• Subject Area: Pharmacy ; Nuclear Medicine, Radiotherapy, Radiobiology
• Term: from 2018 to 2022
• Project identifier: Deutsche Forschungsgemeinschaft (DFG) - Project number 405583239

Positron emission tomography (PET) is established as highly sensitive method in clinical and experimental molecular imaging. With the aim to use this method more efficiently, there is a need for the development of new 18F-labeled radiopharmaceuticals, which can be used in PET studies in patients. A particular difficulty of 18F-chemistry is the complex and time-consuming radiosynthesis taking into account the short half-life of 2 hours. The optimization and efficient application of fast and reliable labeling strategies are the basic requirements for the development of new PET radiopharmaceuticals. Therefore, the aim of this project is to use the well-established method of 18F-fluoroglycosylation to develop new 18F-fluoroglycosylated radioligands and to characterize these radioligands preclinically. These ligands are intended to address the integrin avb6, the prostate-specific antigen PSMA, as well as the estradiol receptor, so that new diagnostic PET radiopharmaceuticals for the imaging of prostate, breast and pancreatic tumors and their metastases arise. Furthermore, animal models will be used to test whether these PET radiopharmaceuticals, as well as an already established 18F-fluoroglycosyl tracer for the neurotensin receptor, are suitable for the therapy monitoring of endoradiotherapy of neurotensin receptor-positive tumors with [177Lu]Lu-FAUC 469. The automated and GMP-compliant production of selected 18F-labeled glycoconjugates will be validated in the clean room laboratory, with the long-term goal of ensuring the translation of the selected 18F-fluoroglycoconjugates into the clinic for patient application.

• DFG Programme: Research Grants