Investigation into the metabolic stability of 18F-labeled PSMA inhibitor derivatives bearing aryl-fluorosulfates for PET tracer development applications

This poster highlights the use of the sulfur [18F]fluoride exchange approach to radiolabel a PSMA inhibitor ([18F]2) and test its radiolabeling, in vitro and in vivo properties.

• [18F]2 shows good binding kinetics compared to known radiotracers (1 nM) but ~20%

defluorination occurs in human serum after 120 min.

• [18F]2 binds to LNCaP xenograft sections in a similar pattern as [68Ga]Ga-PSMA-11.
• PET imaging experiments show defluorination but also accumulation in LNCaP tumor

xenografts (SUVmax = 4.4).

• Further work: Radiosynthesis of [18F]4 starting from precursor 3 (in poster)