Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging
Abstract Background Poly (ADP-ribose) polymerase (PARP) inhibitors have emerged as a promising class of therapeutics, particularly in the treatment of cancers with defective DNA repair mechanisms, such as those with breast cancer genes (BRCA) mutations. Their effectiveness in cancer therapy is now w...
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SpringerOpen
2025-07-01
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| Series: | EJNMMI Radiopharmacy and Chemistry |
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| Online Access: | https://doi.org/10.1186/s41181-025-00364-5 |
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| author | Gianluca Destro Rebecca Rizzo Chiara Rua Raha Rouhbakhsh Azimi Silvia Morbelli |
| author_facet | Gianluca Destro Rebecca Rizzo Chiara Rua Raha Rouhbakhsh Azimi Silvia Morbelli |
| author_sort | Gianluca Destro |
| collection | DOAJ |
| description | Abstract Background Poly (ADP-ribose) polymerase (PARP) inhibitors have emerged as a promising class of therapeutics, particularly in the treatment of cancers with defective DNA repair mechanisms, such as those with breast cancer genes (BRCA) mutations. Their effectiveness in cancer therapy is now well-established, but the ongoing advancements in radiochemistry are expanding their potential to combine both therapeutic and imaging capabilities. Radiolabelled PARP inhibitors, used in conjunction with positron emission tomography (PET) or single-photon emission computed tomography (SPECT), might enable precise imaging of PARP expression in tumours, potentially providing invaluable insights into treatment response, tumor heterogeneity, and molecular profiling. Main body The radiochemistry of PARP inhibitors involves incorporating radioisotopes (most of all Fluorine-18) into the molecular structure of these molecules. The first strategy used to achieve this goal was the use of prosthetic groups bearing the fluorine-18. Then, the development of radioisotopologue have gained ground, followed later by the replacement with other halogens such as bromine, iodine, or astatine has taken place. Another frontier is represented by the metal radiolabelling of these inhibitors through the introduction of a chelator moiety to these molecules, thus further expanding both imaging and therapy applications. Conclusion Finally, emerging evidence suggest the possibility to involve PARP-related radiopharmaceuticals in theranostics approaches. Despite challenges such as the complexity of radiolabelling, regulatory hurdles, and the need for more robust clinical validation, the continued exploration of the radiochemistry of PARP inhibitors promises to revolutionize both the diagnosis and treatment of cancer, offering hope for more effective and personalized cancer care. |
| format | Article |
| id | doaj-art-8f38b37b62ce4f978d47feb06803c7f2 |
| institution | DOAJ |
| issn | 2365-421X |
| language | English |
| publishDate | 2025-07-01 |
| publisher | SpringerOpen |
| record_format | Article |
| series | EJNMMI Radiopharmacy and Chemistry |
| spelling | doaj-art-8f38b37b62ce4f978d47feb06803c7f22025-08-20T03:04:17ZengSpringerOpenEJNMMI Radiopharmacy and Chemistry2365-421X2025-07-0110113310.1186/s41181-025-00364-5Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imagingGianluca Destro0Rebecca Rizzo1Chiara Rua2Raha Rouhbakhsh Azimi3Silvia Morbelli4Department of Molecular Biotechnology and Health Sciences, University of TurinDepartment of Molecular Biotechnology and Health Sciences, University of TurinDepartment of Molecular Biotechnology and Health Sciences, University of TurinDepartment of Molecular Biotechnology and Health Sciences, University of TurinDepartment of Nuclear Medicine, University of TurinAbstract Background Poly (ADP-ribose) polymerase (PARP) inhibitors have emerged as a promising class of therapeutics, particularly in the treatment of cancers with defective DNA repair mechanisms, such as those with breast cancer genes (BRCA) mutations. Their effectiveness in cancer therapy is now well-established, but the ongoing advancements in radiochemistry are expanding their potential to combine both therapeutic and imaging capabilities. Radiolabelled PARP inhibitors, used in conjunction with positron emission tomography (PET) or single-photon emission computed tomography (SPECT), might enable precise imaging of PARP expression in tumours, potentially providing invaluable insights into treatment response, tumor heterogeneity, and molecular profiling. Main body The radiochemistry of PARP inhibitors involves incorporating radioisotopes (most of all Fluorine-18) into the molecular structure of these molecules. The first strategy used to achieve this goal was the use of prosthetic groups bearing the fluorine-18. Then, the development of radioisotopologue have gained ground, followed later by the replacement with other halogens such as bromine, iodine, or astatine has taken place. Another frontier is represented by the metal radiolabelling of these inhibitors through the introduction of a chelator moiety to these molecules, thus further expanding both imaging and therapy applications. Conclusion Finally, emerging evidence suggest the possibility to involve PARP-related radiopharmaceuticals in theranostics approaches. Despite challenges such as the complexity of radiolabelling, regulatory hurdles, and the need for more robust clinical validation, the continued exploration of the radiochemistry of PARP inhibitors promises to revolutionize both the diagnosis and treatment of cancer, offering hope for more effective and personalized cancer care.https://doi.org/10.1186/s41181-025-00364-5PARPPARP1PARP inhibitorRadiolabellingPARP imagingPARP therapy |
| spellingShingle | Gianluca Destro Rebecca Rizzo Chiara Rua Raha Rouhbakhsh Azimi Silvia Morbelli Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging EJNMMI Radiopharmacy and Chemistry PARP PARP1 PARP inhibitor Radiolabelling PARP imaging PARP therapy |
| title | Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging |
| title_full | Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging |
| title_fullStr | Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging |
| title_full_unstemmed | Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging |
| title_short | Exploring the radiochemistry of PARP inhibitors: a new era in therapy and imaging |
| title_sort | exploring the radiochemistry of parp inhibitors a new era in therapy and imaging |
| topic | PARP PARP1 PARP inhibitor Radiolabelling PARP imaging PARP therapy |
| url | https://doi.org/10.1186/s41181-025-00364-5 |
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