Carolline M. Ntihabose, Maryana Handula, Amber Piet, Savanne Beekman, Louise van Dalen, Negin Eskandari, Asude Aydogan, Debra Stuurman, Corrina de Ridder, Mark Konijnenberg, Yann Seimbille, Erik de Blois
{"title":"铽-161标记放射性药物的潜力和实际挑战","authors":"Carolline M. Ntihabose, Maryana Handula, Amber Piet, Savanne Beekman, Louise van Dalen, Negin Eskandari, Asude Aydogan, Debra Stuurman, Corrina de Ridder, Mark Konijnenberg, Yann Seimbille, Erik de Blois","doi":"10.1186/s41181-025-00390-3","DOIUrl":null,"url":null,"abstract":"<div><h3>Background</h3><p>Due to promising preclinical studies and clinical case reports, Tb-161 labeled radiopharmaceuticals for targeted radionuclide therapy (TRT) have gained interest. Unlike Lu-177, Tb-161 not only emits β<sup>−</sup> particles, but also Auger and conversion electrons, which may improve the current therapeutic efficacy of TRT. However, before implementing Tb-161 for clinical use, several steps are required (E.g., development, optimization, validation). Therefore, this study focuses on the purity of Tb-161 as well as the detection and quantification of Tb–Tb-161-labeled radiopharmaceuticals. As multiple studies are currently aiming to determine the therapeutic effect of Tb-161 labeled radiopharmaceuticals, standardizing and evaluating Tb-161 is essential to be able to compare its therapeutic potential against Lu-177 and other radionuclides. Therefore, we established accurate detection methods, impurity measurements, radiolabeling protocols, and quality control for Tb-161 labeled pharmaceuticals. Parameters of Tb-161 labeled radiopharmaceuticals were investigated and exemplified by [<sup>161</sup> Tb]Tb-DOTA-TATE, in comparison with [<sup>177</sup>Lu]Lu-DOTA-TATE.</p><h3>Results</h3><p>Analysis of Tb-161 stock solution demonstrated the presence of metal impurities (ΣFe, Zn, Cu, Gd, and Dy) at the reference day and increased over time. The geometric effect of vial type demonstrated a decrease in activity when a vial was used without point-source. For both Lu-177 and Tb-161 labeled DOTA-TATE, high radiochemical yield and purity (> 95%) were obtained and remained stable (> 90%) up to 24 h in solution.</p><h3>Conclusion</h3><p>Analysis of Tb-161 stock showed an increase in metal impurities over time, which could interfere with the production of Tb-161 labeled radiopharmaceuticals. The low gamma energy (48.9 keV and 74.6 keV) of Tb-161 needs to be considered in (pre)clinical applications when quantifying activity. For Tb-161 labeled pharmaceuticals, similar radiolabeling conditions as Lu-177 have been shown to be successful and highly stable.</p></div>","PeriodicalId":534,"journal":{"name":"EJNMMI Radiopharmacy and Chemistry","volume":"10 1","pages":""},"PeriodicalIF":4.4000,"publicationDate":"2025-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ejnmmipharmchem.springeropen.com/counter/pdf/10.1186/s41181-025-00390-3","citationCount":"0","resultStr":"{\"title\":\"Potentials and practical challenges of terbium-161 labeled radiopharmaceuticals\",\"authors\":\"Carolline M. Ntihabose, Maryana Handula, Amber Piet, Savanne Beekman, Louise van Dalen, Negin Eskandari, Asude Aydogan, Debra Stuurman, Corrina de Ridder, Mark Konijnenberg, Yann Seimbille, Erik de Blois\",\"doi\":\"10.1186/s41181-025-00390-3\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Background</h3><p>Due to promising preclinical studies and clinical case reports, Tb-161 labeled radiopharmaceuticals for targeted radionuclide therapy (TRT) have gained interest. Unlike Lu-177, Tb-161 not only emits β<sup>−</sup> particles, but also Auger and conversion electrons, which may improve the current therapeutic efficacy of TRT. However, before implementing Tb-161 for clinical use, several steps are required (E.g., development, optimization, validation). Therefore, this study focuses on the purity of Tb-161 as well as the detection and quantification of Tb–Tb-161-labeled radiopharmaceuticals. As multiple studies are currently aiming to determine the therapeutic effect of Tb-161 labeled radiopharmaceuticals, standardizing and evaluating Tb-161 is essential to be able to compare its therapeutic potential against Lu-177 and other radionuclides. Therefore, we established accurate detection methods, impurity measurements, radiolabeling protocols, and quality control for Tb-161 labeled pharmaceuticals. Parameters of Tb-161 labeled radiopharmaceuticals were investigated and exemplified by [<sup>161</sup> Tb]Tb-DOTA-TATE, in comparison with [<sup>177</sup>Lu]Lu-DOTA-TATE.</p><h3>Results</h3><p>Analysis of Tb-161 stock solution demonstrated the presence of metal impurities (ΣFe, Zn, Cu, Gd, and Dy) at the reference day and increased over time. The geometric effect of vial type demonstrated a decrease in activity when a vial was used without point-source. For both Lu-177 and Tb-161 labeled DOTA-TATE, high radiochemical yield and purity (> 95%) were obtained and remained stable (> 90%) up to 24 h in solution.</p><h3>Conclusion</h3><p>Analysis of Tb-161 stock showed an increase in metal impurities over time, which could interfere with the production of Tb-161 labeled radiopharmaceuticals. The low gamma energy (48.9 keV and 74.6 keV) of Tb-161 needs to be considered in (pre)clinical applications when quantifying activity. For Tb-161 labeled pharmaceuticals, similar radiolabeling conditions as Lu-177 have been shown to be successful and highly stable.</p></div>\",\"PeriodicalId\":534,\"journal\":{\"name\":\"EJNMMI Radiopharmacy and Chemistry\",\"volume\":\"10 1\",\"pages\":\"\"},\"PeriodicalIF\":4.4000,\"publicationDate\":\"2025-10-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://ejnmmipharmchem.springeropen.com/counter/pdf/10.1186/s41181-025-00390-3\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"EJNMMI Radiopharmacy and Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://link.springer.com/article/10.1186/s41181-025-00390-3\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, INORGANIC & NUCLEAR\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"EJNMMI Radiopharmacy and Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://link.springer.com/article/10.1186/s41181-025-00390-3","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
Potentials and practical challenges of terbium-161 labeled radiopharmaceuticals
Background
Due to promising preclinical studies and clinical case reports, Tb-161 labeled radiopharmaceuticals for targeted radionuclide therapy (TRT) have gained interest. Unlike Lu-177, Tb-161 not only emits β− particles, but also Auger and conversion electrons, which may improve the current therapeutic efficacy of TRT. However, before implementing Tb-161 for clinical use, several steps are required (E.g., development, optimization, validation). Therefore, this study focuses on the purity of Tb-161 as well as the detection and quantification of Tb–Tb-161-labeled radiopharmaceuticals. As multiple studies are currently aiming to determine the therapeutic effect of Tb-161 labeled radiopharmaceuticals, standardizing and evaluating Tb-161 is essential to be able to compare its therapeutic potential against Lu-177 and other radionuclides. Therefore, we established accurate detection methods, impurity measurements, radiolabeling protocols, and quality control for Tb-161 labeled pharmaceuticals. Parameters of Tb-161 labeled radiopharmaceuticals were investigated and exemplified by [161 Tb]Tb-DOTA-TATE, in comparison with [177Lu]Lu-DOTA-TATE.
Results
Analysis of Tb-161 stock solution demonstrated the presence of metal impurities (ΣFe, Zn, Cu, Gd, and Dy) at the reference day and increased over time. The geometric effect of vial type demonstrated a decrease in activity when a vial was used without point-source. For both Lu-177 and Tb-161 labeled DOTA-TATE, high radiochemical yield and purity (> 95%) were obtained and remained stable (> 90%) up to 24 h in solution.
Conclusion
Analysis of Tb-161 stock showed an increase in metal impurities over time, which could interfere with the production of Tb-161 labeled radiopharmaceuticals. The low gamma energy (48.9 keV and 74.6 keV) of Tb-161 needs to be considered in (pre)clinical applications when quantifying activity. For Tb-161 labeled pharmaceuticals, similar radiolabeling conditions as Lu-177 have been shown to be successful and highly stable.
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