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Molecular imaging of PARP in cancer: state-of-the-art
Luca Filippi1, Luca Urso2, Viviana Frantellizzi3
1Nuclear Medicine Unit, Department of Oncohaematology, Fondazione PTV Policlinico Tor Vergata University Hospital, Rome, Italy.
Introduction:
Poly-ADP-ribose-polymerase inhibitors (PARPi), which exploit the processes of so-called 'synthetic lethality,' have been successfully implemented in oncological practice. However, not all patients respond to PARPi, and there is an unmet need for noninvasive biomarkers suitable for patient selection and monitoring during PARPi therapy.
Areas Covered:
The first clinical applications of molecular imaging with positron emission tomography/computed tomography (PET/CT) with [18F]-FluorThanatrace ([18F]-FTT) and [18F]-PARPi, highly effective PARP-ligands, in patients with several malignancies (head and neck, ovarian, prostate, and breast cancer) are covered, with a particular focus on its potential for pre-treatment selection and follow-up.
Expert Opinion:
By a search made on the most common database, such as PubMed and Google Scholar in a period from January 2010 and 2023, first clinical evidence suggests that PET/CT with [18F]-FTT and [18F]-PARPi might represent a reliable tool for in vivo imaging and quantification of PARP-1 expression in ovarian, prostate, breast, head, and neck cancer, supporting their potential usefulness for patient selection before PARPi-therapies. In addition, a reduction in [18F]-FTT uptake has been registered after therapy initiation and seems to be correlated with patient outcome after PARPi-based regimens. Further studies are needed to better address the value of PARPI-radiolabeled PET imaging in these clinical settings, especially as it concerns technical features such as optimal scan modality (dynamic vs. static) and timing.
Insights
Positron emission tomography/computed tomography (PET/CT) with novel radioligands shows promise for selecting cancer patients for poly-ADP-ribose-polymerase inhibitor (PARPi) therapy and monitoring treatment response.
Area of Science:
- Oncology
- Molecular Imaging
- Radiochemistry
Background:
- Poly-ADP-ribose-polymerase inhibitors (PARPi) are effective cancer treatments utilizing synthetic lethality.
- Not all patients respond to PARPi, highlighting the need for predictive biomarkers.
- Noninvasive methods for patient selection and monitoring are crucial for PARPi therapy.
Purpose of the Study:
- To review the clinical applications of PET/CT with [18F]-FluorThanatrace ([18F]-FTT) and [18F]-PARPi.
- To evaluate the potential of these imaging agents for patient selection and treatment monitoring in various cancers.
Main Methods:
- Literature search of PubMed and Google Scholar (January 2010-2023).
- Focus on clinical evidence of PET/CT with [18F]-FTT and [18F]-PARPi in head and neck, ovarian, prostate, and breast cancers.
Main Results:
- PET/CT with [18F]-FTT and [18F]-PARPi shows potential for in vivo imaging and quantification of PARP-1 expression.
- These imaging agents may aid in selecting patients for PARPi therapy.
- Reduced [18F]-FTT uptake post-therapy correlates with patient outcomes.
Conclusions:
- PET/CT with [18F]-FTT and [18F]-PARPi may serve as a reliable tool for PARP-1 imaging in specific malignancies.
- Further research is needed to optimize technical aspects of PARPi-radiolabeled PET imaging.

