{"title":"在模块化实验室标准中优化[68Ga]Ga-Pentixafor、[68Ga]Ga-FAPI-4 和 [68Ga]Ga-DOTATATE 的自动放射合成程序。","authors":"Sreeja Raj Menon, Arpit Mitra, Sudeep Sahu, Sangita Lad, Avik Chakraborty, Mukti Kanta Ray, Sharmila Banerjee","doi":"10.22038/AOJNMB.2024.77059.1545","DOIUrl":null,"url":null,"abstract":"<p><strong>Objectives: </strong>The present work describes the automated radiochemical synthesis of different PET tracers like [<sup>68</sup>Ga]Ga-Pentixafor, [<sup>68</sup>Ga]Ga-FAPI-4 and [<sup>68</sup>Ga]Ga-DOTATATE using optimized single protocol in the non-cassette based Eckert & Ziegler (EZ) Modular Lab (fixed tubing system) without any modification in the inbuilt human machine interface (HMI) software. Recently, PET agents viz. [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4 are gaining prominence for the diagnosis of overexpressed Chemokine Receptor-4 (CXCR4) and Fibroblast Activation Protein (FAP) receptor, respectively, in the microenvironment of numerous cancer types. The promising results observed with the clinical usage of [<sup>68</sup>Ga]Ga-DOTATATE produced using the automated protocol, provided impetus for the clinical translation of [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4 using the in-house developed automated radiolabeling protocol.</p><p><strong>Methods: </strong>Herein we report a single radiolabeling protocol for the automated preparation of [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4 in the non-cassette based EZ Modular-Lab Standard radiochemistry module, without any changes in schematic, graphical user interface (GUI) software and time list, from that used for routine production of [<sup>68</sup>Ga]Ga-DOTATATE in our centre, since 2015. Physico-chemical quality control and in-vitro stability analyses were carried out using radio-TLC and radio-HPLC.</p><p><strong>Results: </strong>The automated protocol yielded reliable and consistent non-decay corrected (ndc) radiochemical yield (RCY) of (84.4%±0.9%) and (85.5%±1.4%) respectively, for [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4, with RCP>98%, which are comparable to the RCY of (84.4%±1.2%) and RCP (99.1%±0.3%) for [<sup>68</sup>Ga]Ga-DOTATATE. The biological quality control studies confirmed the formulations to be of ready-to-use pharmaceutical grade.</p><p><strong>Conclusion: </strong>The consistent and reliable RCY and RCP of multiple <sup>68</sup>Ga-labeled PET tracers by single automated radiochemistry protocol exhibits the versatility of the EZ Modular Lab.</p>","PeriodicalId":8503,"journal":{"name":"Asia Oceania Journal of Nuclear Medicine and Biology","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11263773/pdf/","citationCount":"0","resultStr":"{\"title\":\"On the Optimization of the Protocol for Automated Radiosyntheses of [<sup>68</sup>Ga]Ga-Pentixafor, [<sup>68</sup>Ga]Ga-FAPI-4 and [<sup>68</sup>Ga]Ga-DOTATATE in a Modular-Lab Standard.\",\"authors\":\"Sreeja Raj Menon, Arpit Mitra, Sudeep Sahu, Sangita Lad, Avik Chakraborty, Mukti Kanta Ray, Sharmila Banerjee\",\"doi\":\"10.22038/AOJNMB.2024.77059.1545\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objectives: </strong>The present work describes the automated radiochemical synthesis of different PET tracers like [<sup>68</sup>Ga]Ga-Pentixafor, [<sup>68</sup>Ga]Ga-FAPI-4 and [<sup>68</sup>Ga]Ga-DOTATATE using optimized single protocol in the non-cassette based Eckert & Ziegler (EZ) Modular Lab (fixed tubing system) without any modification in the inbuilt human machine interface (HMI) software. Recently, PET agents viz. [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4 are gaining prominence for the diagnosis of overexpressed Chemokine Receptor-4 (CXCR4) and Fibroblast Activation Protein (FAP) receptor, respectively, in the microenvironment of numerous cancer types. The promising results observed with the clinical usage of [<sup>68</sup>Ga]Ga-DOTATATE produced using the automated protocol, provided impetus for the clinical translation of [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4 using the in-house developed automated radiolabeling protocol.</p><p><strong>Methods: </strong>Herein we report a single radiolabeling protocol for the automated preparation of [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4 in the non-cassette based EZ Modular-Lab Standard radiochemistry module, without any changes in schematic, graphical user interface (GUI) software and time list, from that used for routine production of [<sup>68</sup>Ga]Ga-DOTATATE in our centre, since 2015. Physico-chemical quality control and in-vitro stability analyses were carried out using radio-TLC and radio-HPLC.</p><p><strong>Results: </strong>The automated protocol yielded reliable and consistent non-decay corrected (ndc) radiochemical yield (RCY) of (84.4%±0.9%) and (85.5%±1.4%) respectively, for [<sup>68</sup>Ga]Ga-Pentixafor and [<sup>68</sup>Ga]Ga-FAPI-4, with RCP>98%, which are comparable to the RCY of (84.4%±1.2%) and RCP (99.1%±0.3%) for [<sup>68</sup>Ga]Ga-DOTATATE. The biological quality control studies confirmed the formulations to be of ready-to-use pharmaceutical grade.</p><p><strong>Conclusion: </strong>The consistent and reliable RCY and RCP of multiple <sup>68</sup>Ga-labeled PET tracers by single automated radiochemistry protocol exhibits the versatility of the EZ Modular Lab.</p>\",\"PeriodicalId\":8503,\"journal\":{\"name\":\"Asia Oceania Journal of Nuclear Medicine and Biology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11263773/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Asia Oceania Journal of Nuclear Medicine and Biology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.22038/AOJNMB.2024.77059.1545\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Asia Oceania Journal of Nuclear Medicine and Biology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.22038/AOJNMB.2024.77059.1545","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Medicine","Score":null,"Total":0}
引用次数: 0
摘要
目的：本工作描述了在不修改内置人机界面软件的情况下，在基于非盒式的 Eckert & Ziegler (EZ) 模块化实验室（固定管道系统）中使用优化的单一协议自动放射化学合成不同的 PET 示踪剂，如 [68Ga]Ga-Pentixafor、[68Ga]Ga-FAPI-4 和 [68Ga]Ga-DOTATATE。最近，[68Ga]Ga-Pentixafor 和[68Ga]Ga-FAPI-4 这两种正电子发射计算机断层显像剂在诊断多种癌症微环境中过度表达的趋化因子受体-4（CXCR4）和成纤维细胞活化蛋白（FAP）受体方面越来越受到重视。使用自动化方案生产的[68Ga]Ga-DOTATATE在临床应用中取得了良好的效果，这为使用内部开发的自动化放射性标记方案将[68Ga]Ga-Pentixafor和[68Ga]Ga-FAPI-4应用于临床提供了动力。方法：在此，我们报告了自2015年以来在非盒式EZ Modular-Lab标准放射化学模块中自动制备[68Ga]Ga-Pentixafor和[68Ga]Ga-FAPI-4的单一放射标记方案，与本中心用于常规生产[68Ga]Ga-DOTATATE的方案相比，该方案在原理图、图形用户界面（GUI）软件和时间列表方面没有任何变化。使用放射性-TLC和放射性-HPLC进行了理化质量控制和体外稳定性分析：结果：[68Ga]Ga-Pentixafor和[68Ga]Ga-FAPI-4的非衰变校正（ndc）放射化学收率（RCY）分别为（84.4%±0.9%）和（85.5%±1.4%），RCP>98%，与[68Ga]Ga-DOTATATE的RCY（84.4%±1.2%）和RCP（99.1%±0.3%）相当。生物质量控制研究证实这些制剂为即用药物级：结论：通过单个自动化放射化学方案实现多种 68Ga 标记 PET 示踪剂的一致、可靠的 RCY 和 RCP，展示了 EZ 模块化实验室的多功能性。
On the Optimization of the Protocol for Automated Radiosyntheses of [68Ga]Ga-Pentixafor, [68Ga]Ga-FAPI-4 and [68Ga]Ga-DOTATATE in a Modular-Lab Standard.
Objectives: The present work describes the automated radiochemical synthesis of different PET tracers like [68Ga]Ga-Pentixafor, [68Ga]Ga-FAPI-4 and [68Ga]Ga-DOTATATE using optimized single protocol in the non-cassette based Eckert & Ziegler (EZ) Modular Lab (fixed tubing system) without any modification in the inbuilt human machine interface (HMI) software. Recently, PET agents viz. [68Ga]Ga-Pentixafor and [68Ga]Ga-FAPI-4 are gaining prominence for the diagnosis of overexpressed Chemokine Receptor-4 (CXCR4) and Fibroblast Activation Protein (FAP) receptor, respectively, in the microenvironment of numerous cancer types. The promising results observed with the clinical usage of [68Ga]Ga-DOTATATE produced using the automated protocol, provided impetus for the clinical translation of [68Ga]Ga-Pentixafor and [68Ga]Ga-FAPI-4 using the in-house developed automated radiolabeling protocol.
Methods: Herein we report a single radiolabeling protocol for the automated preparation of [68Ga]Ga-Pentixafor and [68Ga]Ga-FAPI-4 in the non-cassette based EZ Modular-Lab Standard radiochemistry module, without any changes in schematic, graphical user interface (GUI) software and time list, from that used for routine production of [68Ga]Ga-DOTATATE in our centre, since 2015. Physico-chemical quality control and in-vitro stability analyses were carried out using radio-TLC and radio-HPLC.
Results: The automated protocol yielded reliable and consistent non-decay corrected (ndc) radiochemical yield (RCY) of (84.4%±0.9%) and (85.5%±1.4%) respectively, for [68Ga]Ga-Pentixafor and [68Ga]Ga-FAPI-4, with RCP>98%, which are comparable to the RCY of (84.4%±1.2%) and RCP (99.1%±0.3%) for [68Ga]Ga-DOTATATE. The biological quality control studies confirmed the formulations to be of ready-to-use pharmaceutical grade.
Conclusion: The consistent and reliable RCY and RCP of multiple 68Ga-labeled PET tracers by single automated radiochemistry protocol exhibits the versatility of the EZ Modular Lab.
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