Development and clinical potential of ¹⁸F-PSiMA for prostate cancer PET imaging.

ABSTRACT: Prostate-specific membrane antigen (PSMA) is a key target for diagnosing prostate cancer through positron emission tomography (PET). While ⁶⁸Ga-labeled PSMA compounds are widely used, ¹⁸F-labeled PSMA inhibitors have gained traction for clinical tumor imaging. We previously investigated PSMA-targeting compounds based on the Lys-urea-Glu motif, incorporating a silicon fluoride-acceptor (SiFA) and chemical auxiliaries to enhance in vivo biodistribution. This led to the development of ¹⁸F-PSiMA, a SiFA-based radiotracer with an optimized linker exhibiting favorable PSMA potency (IC₅₀ = 154 ± 47 nM in LNCaP cells). ¹⁸F-PSiMA radiosynthesis with low to high concentrations of ¹⁸F and precursor achieved molar activities (

SUBMITTER: Gower-Fry L 

PROVIDER: S-EPMC12127850 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature