[18F]SynVesT-1 的良好制造程序生产，一种用于突触小泡糖蛋白 2A 体内正电子发射断层扫描成像的放射性配体,Journal of Labelled Compounds and Radiopharmaceuticals

当前位置： X-MOL 学术 › J. Label. Comp. Radiopharm. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

[18F]SynVesT-1 的良好制造程序生产，一种用于突触小泡糖蛋白 2A 体内正电子发射断层扫描成像的放射性配体
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2022-08-31 , DOI: 10.1002/jlcr.4002
Kenneth Dahl _{1,

2} , Stefan Larsson ₁ , Peter Bonn ₁ , Anita Wallin ₁ , Oleksiy Itsenko _{1,

2} , Michael Schöll _{1,

2,

3}

Affiliation

[ ¹⁸ F]SynVesT-1（也称为 [ ¹⁸ F]SDM-8 或 [ ¹⁸ F]MNI-1126）是一种有效的选择性突触小泡糖蛋白 2 (SV2A) 正电子发射断层扫描 (PET) 显像剂。为了满足对¹⁸ F 标记的 SV2A PET 配体日益增长的临床需求，我们开发了一种全自动程序，以提供 [ ¹⁸ F]SynVesT-1的无菌和无热原良好生产程序 (GMP) 合规产品适用于人体临床研究。[ ¹⁸F]SynVesT-1 通过快速铜介导的放射性氟化方案合成。该程序是在市售模块 TracerMaker（ScanSys Laboratorieteknik ApS，丹麦哥本哈根）上开发和建立的，这是一个最初开发用于进行碳 11 放射化学的合成平台。从 ~130 GBq（轰击结束）开始，我们新开发的程序使我们能够以14,220 ± 800 MBq ( n = 3)的孤立放射性产量制备 [ ¹⁸ F]SynVesT-1 ，这对应于放射化学产量 ( RCY) 为 19.5 ± 0.5%。每个最终配制批次的放射化学纯度 (RCP) 和对映体纯度均超过 98%。总合成时间为 90 分钟，摩尔活性为 330 ± 60 GBq/μmol (8.9 ± 1.6 Ci/μmol)。产生的 [ ¹⁸F]SynVesT-1 在室温下稳定超过 8 小时，适用于人体受试者的体内 PET 成像研究。

"点击查看英文标题和摘要"

Good manufacturing procedure production of [18F]SynVesT-1, a radioligand for in vivo positron emission tomography imaging of synaptic vesicle glycoprotein 2A

[¹⁸F]SynVesT-1 (also known as [¹⁸F]SDM-8 or [¹⁸F]MNI-1126) is a potent and selective synaptic vesicle glycoprotein 2 (SV2A) positron emission tomography (PET) imaging agent. In order to fulfill the increasing clinical demand of an ¹⁸F-labeled SV2A PET ligand, we have developed a fully automated procedure to provide a sterile and pyrogen-free good manufacturing procedure (GMP)-compliant product of [¹⁸F]SynVesT-1 suitable for clinical studies in humans. [¹⁸F]SynVesT-1 is synthesized via a rapid copper-mediated radiofluorination protocol. The procedure was developed and established on a commercially available module, TracerMaker (ScanSys Laboratorieteknik ApS, Copenhagen, Denmark), a synthesis platform originally developed to conduct carbon-11 radiochemistry. From ~130 GBq (end-of-bombardment), our newly developed procedure enabled us to prepare [¹⁸F]SynVesT-1 in an isolated radioactivity yield of 14,220 ± 800 MBq (n = 3), which corresponds to a radiochemical yield (RCY) of 19.5 ± 0.5%. The radiochemical purity (RCP) and enantiomeric purity of each of the final formulated batches exceeded 98%. The overall synthesis time was 90 min and the molar activity was 330 ± 60 GBq/μmol (8.9 ± 1.6 Ci/μmol). The produced [¹⁸F]SynVesT-1 was stable over 8 h at room temperature and is suitable for in vivo PET imaging studies in human subjects.

更新日期：2022-08-31

点击分享查看原文

点击收藏

阅读更多本刊新发论文