The Theranostic Optimization of PSMA-GCK01 Does Not Compromise the Imaging Characteristics of 99mTcTc-PSMA-GCK01 Compared to Dedicated Diagnostic 99mTcTc-EDDA/HYNIC-iPSMA in Prostate Cancer
Radiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which...
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| creator | Mamlins, Eduards Scharbert, Lara Cardinale, Jens Krotov, Maria Winter, Erik Rathke, Hendrik Strodel, Birgit Ankrah, Alfred O Sathekge, Mike Haberkorn, Uwe Kratochwil, Clemens Giesel, Frederik L |
| description | Radiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.PURPOSERadiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.Two cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. The imaging data were retrospective analyzed for salivary gland, kidney, liver, soft tissue, and tumor uptake on a semi-automated ROI-analysis using HERMES Medical Solutions AB (HMS, Sweden).PROCEDURESTwo cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. |
| doi_str_mv | 10.1007/s11307-023-01881-y |
| format | Article |
| fullrecord | <record><control><sourceid>proquest</sourceid><recordid>TN_cdi_proquest_miscellaneous_2902959878</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2902959878</sourcerecordid><originalsourceid>FETCH-proquest_miscellaneous_29029598783</originalsourceid><addsrcrecordid>eNqVjk1LAzEQhoMoWD_-gKc5eomdZNHdPZZstUWsBffiqYQ03UY2SU3Sg_43_5tZqNCrh2Fm4H1eHkJuGN4xxHIcGSuwpMgLiqyqGP06ISNWPSDliPz06D4nFzF-ILKS8WJEftqthjxBOh-TUfC6S8aab5mMd-A3sHx7mdAn8YwMGq8jLHwC4e0ueGuihpTxuZWdcR2IrQxSJR3M0BQHuq5tq1pFj1oGWAa9huSh0WujZMpPY2R3MPhjpk0zGc_eF3NBzcCDcbAMOZMBENIpHa7I2Ub2UV8f9iW5fZy2Ykaz3udex7TKkkr3vXTa7-OK18jr-7oqq-If0V9Zb2z7</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2902959878</pqid></control><display><type>article</type><title>The Theranostic Optimization of PSMA-GCK01 Does Not Compromise the Imaging Characteristics of 99mTcTc-PSMA-GCK01 Compared to Dedicated Diagnostic 99mTcTc-EDDA/HYNIC-iPSMA in Prostate Cancer</title><source>SpringerNature Journals</source><creator>Mamlins, Eduards ; Scharbert, Lara ; Cardinale, Jens ; Krotov, Maria ; Winter, Erik ; Rathke, Hendrik ; Strodel, Birgit ; Ankrah, Alfred O ; Sathekge, Mike ; Haberkorn, Uwe ; Kratochwil, Clemens ; Giesel, Frederik L</creator><creatorcontrib>Mamlins, Eduards ; Scharbert, Lara ; Cardinale, Jens ; Krotov, Maria ; Winter, Erik ; Rathke, Hendrik ; Strodel, Birgit ; Ankrah, Alfred O ; Sathekge, Mike ; Haberkorn, Uwe ; Kratochwil, Clemens ; Giesel, Frederik L</creatorcontrib><description>Radiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.PURPOSERadiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.Two cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. The imaging data were retrospective analyzed for salivary gland, kidney, liver, soft tissue, and tumor uptake on a semi-automated ROI-analysis using HERMES Medical Solutions AB (HMS, Sweden).PROCEDURESTwo cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. The imaging data were retrospective analyzed for salivary gland, kidney, liver, soft tissue, and tumor uptake on a semi-automated ROI-analysis using HERMES Medical Solutions AB (HMS, Sweden).The data sets were semi-automated quantified on a ROI-based analysis. The tumor-to-background presented equal results of [99mTc]Tc-PSMA-GCK01 compared to [99mTc]Tc-EDDA/HYNIC-iPSMA. The physiological PSMA-positive organs like salivary gland presented also equal uptake in counts/MBq (salivary gland median 9.48 [99mTc]Tc-PSMA-GCK01 vs. median 9.11 [99mTc]Tc-EDDA/HYNIC-iPSMA), while liver-to-kidney ratio presented a slight shift to the liver parenchyma using [99mTc]Tc-PSMA-GCK01 (0.83) compared to [99mTc]Tc-EDDA/HYNIC-iPSMA (0.55) with no statistical significance. This is in agreement with the results from the docking study revealing only a minor difference in the docking scores for both ligands.RESULTSThe data sets were semi-automated quantified on a ROI-based analysis. The tumor-to-background presented equal results of [99mTc]Tc-PSMA-GCK01 compared to [99mTc]Tc-EDDA/HYNIC-iPSMA. The physiological PSMA-positive organs like salivary gland presented also equal uptake in counts/MBq (salivary gland median 9.48 [99mTc]Tc-PSMA-GCK01 vs. median 9.11 [99mTc]Tc-EDDA/HYNIC-iPSMA), while liver-to-kidney ratio presented a slight shift to the liver parenchyma using [99mTc]Tc-PSMA-GCK01 (0.83) compared to [99mTc]Tc-EDDA/HYNIC-iPSMA (0.55) with no statistical significance. This is in agreement with the results from the docking study revealing only a minor difference in the docking scores for both ligands.The novel theranostic tracer [99mTc]Tc/[188Re]Re-PSMA-GCK01 demonstrates comparable general imaging characteristic with the reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA. These results pave the way for the PSMA-targeting imaging and theranostic agents for a broader, rather low-cost, generator applied radio-ligand therapy utilization.CONCLUSIONSThe novel theranostic tracer [99mTc]Tc/[188Re]Re-PSMA-GCK01 demonstrates comparable general imaging characteristic with the reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA. These results pave the way for the PSMA-targeting imaging and theranostic agents for a broader, rather low-cost, generator applied radio-ligand therapy utilization.</description><identifier>ISSN: 1860-2002</identifier><identifier>EISSN: 1860-2002</identifier><identifier>DOI: 10.1007/s11307-023-01881-y</identifier><language>eng</language><ispartof>Molecular imaging and biology, 2024-02, Vol.26 (1), p.81</ispartof><rights>2023. The Author(s).</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,782,786,27931,27932</link.rule.ids></links><search><creatorcontrib>Mamlins, Eduards</creatorcontrib><creatorcontrib>Scharbert, Lara</creatorcontrib><creatorcontrib>Cardinale, Jens</creatorcontrib><creatorcontrib>Krotov, Maria</creatorcontrib><creatorcontrib>Winter, Erik</creatorcontrib><creatorcontrib>Rathke, Hendrik</creatorcontrib><creatorcontrib>Strodel, Birgit</creatorcontrib><creatorcontrib>Ankrah, Alfred O</creatorcontrib><creatorcontrib>Sathekge, Mike</creatorcontrib><creatorcontrib>Haberkorn, Uwe</creatorcontrib><creatorcontrib>Kratochwil, Clemens</creatorcontrib><creatorcontrib>Giesel, Frederik L</creatorcontrib><title>The Theranostic Optimization of PSMA-GCK01 Does Not Compromise the Imaging Characteristics of 99mTcTc-PSMA-GCK01 Compared to Dedicated Diagnostic 99mTcTc-EDDA/HYNIC-iPSMA in Prostate Cancer</title><title>Molecular imaging and biology</title><description>Radiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.PURPOSERadiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.Two cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. The imaging data were retrospective analyzed for salivary gland, kidney, liver, soft tissue, and tumor uptake on a semi-automated ROI-analysis using HERMES Medical Solutions AB (HMS, Sweden).PROCEDURESTwo cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. The imaging data were retrospective analyzed for salivary gland, kidney, liver, soft tissue, and tumor uptake on a semi-automated ROI-analysis using HERMES Medical Solutions AB (HMS, Sweden).The data sets were semi-automated quantified on a ROI-based analysis. The tumor-to-background presented equal results of [99mTc]Tc-PSMA-GCK01 compared to [99mTc]Tc-EDDA/HYNIC-iPSMA. The physiological PSMA-positive organs like salivary gland presented also equal uptake in counts/MBq (salivary gland median 9.48 [99mTc]Tc-PSMA-GCK01 vs. median 9.11 [99mTc]Tc-EDDA/HYNIC-iPSMA), while liver-to-kidney ratio presented a slight shift to the liver parenchyma using [99mTc]Tc-PSMA-GCK01 (0.83) compared to [99mTc]Tc-EDDA/HYNIC-iPSMA (0.55) with no statistical significance. This is in agreement with the results from the docking study revealing only a minor difference in the docking scores for both ligands.RESULTSThe data sets were semi-automated quantified on a ROI-based analysis. The tumor-to-background presented equal results of [99mTc]Tc-PSMA-GCK01 compared to [99mTc]Tc-EDDA/HYNIC-iPSMA. The physiological PSMA-positive organs like salivary gland presented also equal uptake in counts/MBq (salivary gland median 9.48 [99mTc]Tc-PSMA-GCK01 vs. median 9.11 [99mTc]Tc-EDDA/HYNIC-iPSMA), while liver-to-kidney ratio presented a slight shift to the liver parenchyma using [99mTc]Tc-PSMA-GCK01 (0.83) compared to [99mTc]Tc-EDDA/HYNIC-iPSMA (0.55) with no statistical significance. This is in agreement with the results from the docking study revealing only a minor difference in the docking scores for both ligands.The novel theranostic tracer [99mTc]Tc/[188Re]Re-PSMA-GCK01 demonstrates comparable general imaging characteristic with the reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA. These results pave the way for the PSMA-targeting imaging and theranostic agents for a broader, rather low-cost, generator applied radio-ligand therapy utilization.CONCLUSIONSThe novel theranostic tracer [99mTc]Tc/[188Re]Re-PSMA-GCK01 demonstrates comparable general imaging characteristic with the reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA. These results pave the way for the PSMA-targeting imaging and theranostic agents for a broader, rather low-cost, generator applied radio-ligand therapy utilization.</description><issn>1860-2002</issn><issn>1860-2002</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><recordid>eNqVjk1LAzEQhoMoWD_-gKc5eomdZNHdPZZstUWsBffiqYQ03UY2SU3Sg_43_5tZqNCrh2Fm4H1eHkJuGN4xxHIcGSuwpMgLiqyqGP06ISNWPSDliPz06D4nFzF-ILKS8WJEftqthjxBOh-TUfC6S8aab5mMd-A3sHx7mdAn8YwMGq8jLHwC4e0ueGuihpTxuZWdcR2IrQxSJR3M0BQHuq5tq1pFj1oGWAa9huSh0WujZMpPY2R3MPhjpk0zGc_eF3NBzcCDcbAMOZMBENIpHa7I2Ub2UV8f9iW5fZy2Ykaz3udex7TKkkr3vXTa7-OK18jr-7oqq-If0V9Zb2z7</recordid><startdate>20240201</startdate><enddate>20240201</enddate><creator>Mamlins, Eduards</creator><creator>Scharbert, Lara</creator><creator>Cardinale, Jens</creator><creator>Krotov, Maria</creator><creator>Winter, Erik</creator><creator>Rathke, Hendrik</creator><creator>Strodel, Birgit</creator><creator>Ankrah, Alfred O</creator><creator>Sathekge, Mike</creator><creator>Haberkorn, Uwe</creator><creator>Kratochwil, Clemens</creator><creator>Giesel, Frederik L</creator><scope>7X8</scope></search><sort><creationdate>20240201</creationdate><title>The Theranostic Optimization of PSMA-GCK01 Does Not Compromise the Imaging Characteristics of 99mTcTc-PSMA-GCK01 Compared to Dedicated Diagnostic 99mTcTc-EDDA/HYNIC-iPSMA in Prostate Cancer</title><author>Mamlins, Eduards ; Scharbert, Lara ; Cardinale, Jens ; Krotov, Maria ; Winter, Erik ; Rathke, Hendrik ; Strodel, Birgit ; Ankrah, Alfred O ; Sathekge, Mike ; Haberkorn, Uwe ; Kratochwil, Clemens ; Giesel, Frederik L</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-proquest_miscellaneous_29029598783</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mamlins, Eduards</creatorcontrib><creatorcontrib>Scharbert, Lara</creatorcontrib><creatorcontrib>Cardinale, Jens</creatorcontrib><creatorcontrib>Krotov, Maria</creatorcontrib><creatorcontrib>Winter, Erik</creatorcontrib><creatorcontrib>Rathke, Hendrik</creatorcontrib><creatorcontrib>Strodel, Birgit</creatorcontrib><creatorcontrib>Ankrah, Alfred O</creatorcontrib><creatorcontrib>Sathekge, Mike</creatorcontrib><creatorcontrib>Haberkorn, Uwe</creatorcontrib><creatorcontrib>Kratochwil, Clemens</creatorcontrib><creatorcontrib>Giesel, Frederik L</creatorcontrib><collection>MEDLINE - Academic</collection><jtitle>Molecular imaging and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mamlins, Eduards</au><au>Scharbert, Lara</au><au>Cardinale, Jens</au><au>Krotov, Maria</au><au>Winter, Erik</au><au>Rathke, Hendrik</au><au>Strodel, Birgit</au><au>Ankrah, Alfred O</au><au>Sathekge, Mike</au><au>Haberkorn, Uwe</au><au>Kratochwil, Clemens</au><au>Giesel, Frederik L</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The Theranostic Optimization of PSMA-GCK01 Does Not Compromise the Imaging Characteristics of 99mTcTc-PSMA-GCK01 Compared to Dedicated Diagnostic 99mTcTc-EDDA/HYNIC-iPSMA in Prostate Cancer</atitle><jtitle>Molecular imaging and biology</jtitle><date>2024-02-01</date><risdate>2024</risdate><volume>26</volume><issue>1</issue><spage>81</spage><pages>81-</pages><issn>1860-2002</issn><eissn>1860-2002</eissn><abstract>Radiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.PURPOSERadiolabeled PSMA-ligands play a major role in today's nuclear medicine. Since approval of [177Lu]Lu-PSMA-617 for therapy of metastatic prostate cancer, availability of 177Lu became bottleneck of supply due to the high demand. Recently, a theranostic PSMA-ligand, PSMA-GCK01, was developed which can be labeled either diagnostically with 99mTc or therapeutically with 188Re with both nuclides available from well-known generator systems. This novel tracer might aid to overcome aforementioned supply limitations. In this investigation, the biodistribution and general imaging characteristics of [99mTc]Tc-PSMA-GCK01 were compared with the diagnostic reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA in patients with advanced stage prostate cancer. In addition, the binding of both ligands to PSMA was analyzed at the molecular level using molecular docking.Two cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. The imaging data were retrospective analyzed for salivary gland, kidney, liver, soft tissue, and tumor uptake on a semi-automated ROI-analysis using HERMES Medical Solutions AB (HMS, Sweden).PROCEDURESTwo cohorts (n = 19 vs. n = 21) of patients with metastatic castration-resistant prostate cancer matched for age, tumor stage, and Gleason score underwent a planar gamma camera imaging with [99mTc]Tc-EDDA/HYNIC-iPSMA or [99mTc]Tc-PSMA-GCK01 prior to PSMA-ligand therapy for PSMA-phenotyping. The imaging data were retrospective analyzed for salivary gland, kidney, liver, soft tissue, and tumor uptake on a semi-automated ROI-analysis using HERMES Medical Solutions AB (HMS, Sweden).The data sets were semi-automated quantified on a ROI-based analysis. The tumor-to-background presented equal results of [99mTc]Tc-PSMA-GCK01 compared to [99mTc]Tc-EDDA/HYNIC-iPSMA. The physiological PSMA-positive organs like salivary gland presented also equal uptake in counts/MBq (salivary gland median 9.48 [99mTc]Tc-PSMA-GCK01 vs. median 9.11 [99mTc]Tc-EDDA/HYNIC-iPSMA), while liver-to-kidney ratio presented a slight shift to the liver parenchyma using [99mTc]Tc-PSMA-GCK01 (0.83) compared to [99mTc]Tc-EDDA/HYNIC-iPSMA (0.55) with no statistical significance. This is in agreement with the results from the docking study revealing only a minor difference in the docking scores for both ligands.RESULTSThe data sets were semi-automated quantified on a ROI-based analysis. The tumor-to-background presented equal results of [99mTc]Tc-PSMA-GCK01 compared to [99mTc]Tc-EDDA/HYNIC-iPSMA. The physiological PSMA-positive organs like salivary gland presented also equal uptake in counts/MBq (salivary gland median 9.48 [99mTc]Tc-PSMA-GCK01 vs. median 9.11 [99mTc]Tc-EDDA/HYNIC-iPSMA), while liver-to-kidney ratio presented a slight shift to the liver parenchyma using [99mTc]Tc-PSMA-GCK01 (0.83) compared to [99mTc]Tc-EDDA/HYNIC-iPSMA (0.55) with no statistical significance. This is in agreement with the results from the docking study revealing only a minor difference in the docking scores for both ligands.The novel theranostic tracer [99mTc]Tc/[188Re]Re-PSMA-GCK01 demonstrates comparable general imaging characteristic with the reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA. These results pave the way for the PSMA-targeting imaging and theranostic agents for a broader, rather low-cost, generator applied radio-ligand therapy utilization.CONCLUSIONSThe novel theranostic tracer [99mTc]Tc/[188Re]Re-PSMA-GCK01 demonstrates comparable general imaging characteristic with the reference compound [99mTc]Tc-EDDA/HYNIC-iPSMA. These results pave the way for the PSMA-targeting imaging and theranostic agents for a broader, rather low-cost, generator applied radio-ligand therapy utilization.</abstract><doi>10.1007/s11307-023-01881-y</doi></addata></record> |
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| title | The Theranostic Optimization of PSMA-GCK01 Does Not Compromise the Imaging Characteristics of 99mTcTc-PSMA-GCK01 Compared to Dedicated Diagnostic 99mTcTc-EDDA/HYNIC-iPSMA in Prostate Cancer |
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