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European Journal of Nuclear Medicine and Molecular Imaging

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Open Access 01-02-2022 | Positron Emission Tomography | Original Article

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

Authors: Sophie Stotz, Johannes Kinzler, Anne T. Nies, Matthias Schwab, Andreas Maurer

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 3/2022

Abstract

Purpose

Imaging of PARP expression has emerged as valuable strategy for prediction of tumor malignancy. While [¹⁸F]PARPi and [¹⁸F]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 [¹⁸F]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 [¹⁸F]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 [¹⁸F]PARPi, [¹⁸F]FPyPARP, and [¹⁸F]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 [¹⁸F]PARPi, [¹⁸F]FPyPARP, and [¹⁸F]FTT), a partial shift from hepatobiliary to renal clearance of [¹⁸F]FPyPARP was observed, whereas [¹⁸F]PARPi and [¹⁸F]FTT show almost exclusive hepatobiliary clearance.

Conclusion

These findings imply that [¹⁸F]FPyPARP is an alternative to [¹⁸F]PARPi and [¹⁸F]FTT for PET imaging of PARP enzymes.

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Title: Two experts and a newbie: [18F]PARPi vs [18F]FTT vs [18F]FPyPARP—a comparison of PARP imaging agents
Authors: Sophie Stotz
Johannes Kinzler
Anne T. Nies
Matthias Schwab
Andreas Maurer
Publication date: 01-02-2022
Publisher: Springer Berlin Heidelberg
Keyword: Positron Emission Tomography
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue 3/2022
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-021-05436-7

At a glance: The STEP trials

Springer Medicine

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

Abstract

Purpose

Methods

Results

Conclusion

At a glance: The STEP trials

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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