Teresa Scotognella, Daria Maccora, Isabella Bruno, Marco Chinol, Massimo Castagnola, Francesco Collamati, Carlo Mancini-Terraciano, Silvio Morganti, Valerio Bocci, Elena Solfaroli Camillocci, Dante Rotili, Antonella Cartoni, Ilaria Fratoddi, Federica Marini, Iole Venditti, Riccardo Faccini, Alessandro Giordano
{"title":"90Y-DOTA-Nimotuzumab:一种有前途的β-放射性药物的合成。","authors":"Teresa Scotognella, Daria Maccora, Isabella Bruno, Marco Chinol, Massimo Castagnola, Francesco Collamati, Carlo Mancini-Terraciano, Silvio Morganti, Valerio Bocci, Elena Solfaroli Camillocci, Dante Rotili, Antonella Cartoni, Ilaria Fratoddi, Federica Marini, Iole Venditti, Riccardo Faccini, Alessandro Giordano","doi":"10.2174/1874471013999210104220031","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (<sup>90</sup>Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.</p><p><strong>Methods: </strong>The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50-fold excess of DOTA and then labelled with 90Y3+. The <sup>90</sup>Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the <sup>90</sup>Y-DOTA-nimotuzumab stability was evaluated in human plasma.</p><p><strong>Results: </strong>The radioimmunoconjugate <sup>90</sup>Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.</p><p><strong>Conclusions: </strong>The optimized conditions for a mild and easy preparation of <sup>90</sup>Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":"15 1","pages":"32-39"},"PeriodicalIF":1.5000,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"<sup>90</sup>Y-DOTA-Nimotuzumab: Synthesis of a Promising β- Radiopharmaceutical.\",\"authors\":\"Teresa Scotognella, Daria Maccora, Isabella Bruno, Marco Chinol, Massimo Castagnola, Francesco Collamati, Carlo Mancini-Terraciano, Silvio Morganti, Valerio Bocci, Elena Solfaroli Camillocci, Dante Rotili, Antonella Cartoni, Ilaria Fratoddi, Federica Marini, Iole Venditti, Riccardo Faccini, Alessandro Giordano\",\"doi\":\"10.2174/1874471013999210104220031\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (<sup>90</sup>Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.</p><p><strong>Methods: </strong>The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50-fold excess of DOTA and then labelled with 90Y3+. The <sup>90</sup>Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the <sup>90</sup>Y-DOTA-nimotuzumab stability was evaluated in human plasma.</p><p><strong>Results: </strong>The radioimmunoconjugate <sup>90</sup>Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.</p><p><strong>Conclusions: </strong>The optimized conditions for a mild and easy preparation of <sup>90</sup>Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.</p>\",\"PeriodicalId\":10991,\"journal\":{\"name\":\"Current radiopharmaceuticals\",\"volume\":\"15 1\",\"pages\":\"32-39\"},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2022-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current radiopharmaceuticals\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2174/1874471013999210104220031\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current radiopharmaceuticals","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/1874471013999210104220031","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
90Y-DOTA-Nimotuzumab: Synthesis of a Promising β- Radiopharmaceutical.
Background: Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (90Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.
Methods: The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50-fold excess of DOTA and then labelled with 90Y3+. The 90Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the 90Y-DOTA-nimotuzumab stability was evaluated in human plasma.
Results: The radioimmunoconjugate 90Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.
Conclusions: The optimized conditions for a mild and easy preparation of 90Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.
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