Current medicine and the field of cancer management increasingly profits from radionuclide imaging methods. In our research, we introduce a conceptually novel series of radioiodinated ligands, which are applicable in diagnostics and potentially also in therapy (theranostics) of diseases related to pathological expression or function of choline transport proteins (ChTs). Compared to 11C and 18F-labeled choline derivatives already used in clinical practice for imaging mainly in prostate cancer patients, the herein described iodinated compounds are applicable for both positron emission tomography (PET) and single-photon emission tomography (SPECT) as well as for therapy depending on the iodine isotope selection. Some of the 50 compounds presented in this work possess considerably higher binding affinities towards ChTs (nanomolar ligands) than fluorocholine or the natural ligand - choline. Biodistribution data acquired for eighteen 125I-labeled ligands in murine human prostate cancer xenograft model (PC-3 cells) revealed two compounds which exhibit significantly improved biodistribution profile in comparison with clinically used [18F]fluorocholine. Interestingly, all tested radioiodinated ligands displayed tumor-to-bone uptake ratios superior to [18F]fluorocholine. Furthermore, unlike 11C and 18F-labeled choline derivatives, the presented iodinated ligands can be prepared in their radiolabeled form by a facile palladium-catalyzed isotopic exchange in aqueous environment under mild conditions.

Radioiodinated aromatic choline analog tracers

2019 Spring National Meeting

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