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Purpose Imaging of PARP expression has emerged as valuable strategy for prediction of tumor malignancy. While [ 18 F]PARPi and [ 18 F]FTT are already in clinical translation, both suffer from mainly hepatobiliary clearance hampering their use for detection of abdominal lesions, e.g., liver metastases. Our novel radiotracer [ 18 F]FPyPARP aims to bridge this gap with a higher renal clearance and an easily translatable synthesis route for potential clinical application. Methods We developed a less lipophilic variant of [ 18 F]PARPi by exchange of the fluorobenzoyl residue with a fluoronicotinoyl group and automated the radiosyntheses of the three radiotracers. We then conducted a comparative side-by-side study of [ 18 F]PARPi, [ 18 F]FPyPARP, and [ 18 F]FTT in NOD.CB17-Prkdc scid /J mice bearing HCC1937 xenografts to assess xenograft uptake and pharmacokinetics focusing on excretion pathways. Results Together with decent uptake of all three radiotracers in the xenografts (tumor-to-blood ratios 3.41 ± 0.83, 3.99 ± 0.99, and 2.46 ± 0.35, respectively, for [ 18 F]PARPi, [ 18 F]FPyPARP, and [ 18 F]FTT), a partial shift from hepatobiliary to renal clearance of [ 18 F]FPyPARP was observed, whereas [ 18 F]PARPi and [ 18 F]FTT show almost exclusive hepatobiliary clearance. Conclusion These findings imply that [ 18 F]FPyPARP is an alternative to [ 18 F]PARPi and [ 18 F]FTT for PET imaging of PARP enzymes.

Two experts and a newbie: [18F]PARPi vs [18F]FTT vs [18F]FPyPARP—a comparison of PARP imaging agents