A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate Cancer
Recently, prostate-specific membrane antigen (PSMA) has gained momentum in tumor nuclear molecular imaging as an excellent target for both the diagnosis and therapy of prostate cancer. Since 2008, after years of preclinical research efforts, a plentitude of radiolabeled compounds mainly based on low...
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| Format: | Article |
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MDPI AG
2022-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/9/2617 |
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| author | Sara Brunello Nicola Salvarese Debora Carpanese Carolina Gobbi Laura Melendez-Alafort Cristina Bolzati |
| author_facet | Sara Brunello Nicola Salvarese Debora Carpanese Carolina Gobbi Laura Melendez-Alafort Cristina Bolzati |
| author_sort | Sara Brunello |
| collection | DOAJ |
| description | Recently, prostate-specific membrane antigen (PSMA) has gained momentum in tumor nuclear molecular imaging as an excellent target for both the diagnosis and therapy of prostate cancer. Since 2008, after years of preclinical research efforts, a plentitude of radiolabeled compounds mainly based on low molecular weight PSMA inhibitors (PSMA-i) have been described for imaging and theranostic applications, and some of them have been transferred to the clinic. Most of these compounds include radiometals (e.g., <sup>68</sup>Ga, <sup>64</sup>Cu, <sup>177</sup>Lu) for positron emission tomography (PET) imaging or endoradiotherapy. Nowadays, although the development of new PET tracers has caused a significant drop in single-photon emission tomography (SPECT) research programs and the development of new technetium-99m (<sup>99m</sup>Tc) tracers is rare, this radionuclide remains the best atom for SPECT imaging owing to its ideal physical decay properties, convenient availability, and rich and versatile coordination chemistry. Indeed, <sup>99m</sup>Tc still plays a relevant role in diagnostic nuclear medicine, as the number of clinical examinations based on <sup>99m</sup>Tc outscores that of PET agents and <sup>99m</sup>Tc-PSMA SPECT/CT may be a cost-effective alternative for <sup>68</sup>Ga-PSMA PET/CT. This review aims to give an overview of the specific features of the developed [<sup>99m</sup>Tc]Tc-tagged PSMA agents with particular attention to [<sup>99m</sup>Tc]Tc-PSMA-i. The chemical and pharmacological properties of the latter will be compared and discussed, highlighting the pros and cons with respect to [<sup>68</sup>Ga]Ga-PSMA11. |
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| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T03:56:06Z |
| publishDate | 2022-04-01 |
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| record_format | Article |
| series | Molecules |
| spelling | doaj.art-f336efa2ba0042f4a15569a5cc37cbba2023-11-23T08:47:09ZengMDPI AGMolecules1420-30492022-04-01279261710.3390/molecules27092617A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate CancerSara Brunello0Nicola Salvarese1Debora Carpanese2Carolina Gobbi3Laura Melendez-Alafort4Cristina Bolzati5Institute of Condensed Matter Chemistry and Technologies for Energy ICMATE-CNR, Corso Stati Uniti 4, 35127 Padova, ItalyInstitute of Condensed Matter Chemistry and Technologies for Energy ICMATE-CNR, Corso Stati Uniti 4, 35127 Padova, ItalyImmunology and Molecular Oncology Unit, Veneto Institute of Oncology IOV-IRCCS, Via Gattamelata 64, 35124 Padova, ItalyDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Marzolo 5, 35131 Padova, ItalyImmunology and Molecular Oncology Unit, Veneto Institute of Oncology IOV-IRCCS, Via Gattamelata 64, 35124 Padova, ItalyInstitute of Condensed Matter Chemistry and Technologies for Energy ICMATE-CNR, Corso Stati Uniti 4, 35127 Padova, ItalyRecently, prostate-specific membrane antigen (PSMA) has gained momentum in tumor nuclear molecular imaging as an excellent target for both the diagnosis and therapy of prostate cancer. Since 2008, after years of preclinical research efforts, a plentitude of radiolabeled compounds mainly based on low molecular weight PSMA inhibitors (PSMA-i) have been described for imaging and theranostic applications, and some of them have been transferred to the clinic. Most of these compounds include radiometals (e.g., <sup>68</sup>Ga, <sup>64</sup>Cu, <sup>177</sup>Lu) for positron emission tomography (PET) imaging or endoradiotherapy. Nowadays, although the development of new PET tracers has caused a significant drop in single-photon emission tomography (SPECT) research programs and the development of new technetium-99m (<sup>99m</sup>Tc) tracers is rare, this radionuclide remains the best atom for SPECT imaging owing to its ideal physical decay properties, convenient availability, and rich and versatile coordination chemistry. Indeed, <sup>99m</sup>Tc still plays a relevant role in diagnostic nuclear medicine, as the number of clinical examinations based on <sup>99m</sup>Tc outscores that of PET agents and <sup>99m</sup>Tc-PSMA SPECT/CT may be a cost-effective alternative for <sup>68</sup>Ga-PSMA PET/CT. This review aims to give an overview of the specific features of the developed [<sup>99m</sup>Tc]Tc-tagged PSMA agents with particular attention to [<sup>99m</sup>Tc]Tc-PSMA-i. The chemical and pharmacological properties of the latter will be compared and discussed, highlighting the pros and cons with respect to [<sup>68</sup>Ga]Ga-PSMA11.https://www.mdpi.com/1420-3049/27/9/2617technetium-99mgallium-68SPECTPSMAprostate cancertarget-specific |
| spellingShingle | Sara Brunello Nicola Salvarese Debora Carpanese Carolina Gobbi Laura Melendez-Alafort Cristina Bolzati A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate Cancer Molecules technetium-99m gallium-68 SPECT PSMA prostate cancer target-specific |
| title | A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate Cancer |
| title_full | A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate Cancer |
| title_fullStr | A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate Cancer |
| title_full_unstemmed | A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate Cancer |
| title_short | A Review on the Current State and Future Perspectives of [<sup>99m</sup>Tc]Tc-Housed PSMA-i in Prostate Cancer |
| title_sort | review on the current state and future perspectives of sup 99m sup tc tc housed psma i in prostate cancer |
| topic | technetium-99m gallium-68 SPECT PSMA prostate cancer target-specific |
| url | https://www.mdpi.com/1420-3049/27/9/2617 |
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