在 TRACERLab FX2 N 合成模块上用 GMP 生产[18F]FE-PE2I，这是一种用于多巴胺转运体内 PET 成像的放射性示踪剂

IF 4.4 Q1 CHEMISTRY, INORGANIC & NUCLEAR EJNMMI Radiopharmacy and Chemistry Pub Date : 2024-05-02 DOI:10.1186/s41181-024-00269-9

Mélodie Ferrat, Mohammad M. Moein, Carmen Cananau, Tetyana Tegnebratt, Paul Saliba, Fredrik Norman, Carsten Steiger, Klas Bratteby, Erik Samén, Kenneth Dahl, Thuy A. Tran

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引用次数: 0

摘要

背景帕金森病是一种以多巴胺能系统退化为特征的神经退行性疾病。多巴胺转运体（DAT）正电子发射断层扫描（PET）成像已成为量化活体大脑多巴胺能功能的一种强大而无创的方法。PET放射性配体[18F]FE-PE2I是一种可卡因化学衍生物，在DAT的活体PET成像中表现出良好的特性，包括对DAT的高亲和性和选择性、良好的脑通透性和有利的新陈代谢。本研究的目的是扩大[18F]FE-PE2I 的生产规模，以满足临床上对这种示踪剂日益增长的需求。结果使用市售的放射合成模块 GE TRACERLab FX2 N 开发出了符合 GMP 标准的全自动生产程序。合成时间为 70 分钟，摩尔活度为 925.3 ± 763 GBq/µmol（250 ± 20 Ci/µmol）。在室温下，生成的[18F]FE-PE2I 在 6 小时内保持稳定。

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GMP production of [18F]FE-PE2I on a TRACERLab FX2 N synthesis module, a radiotracer for in vivo PET imaging of the dopamine transport

Background

Parkinson's disease is a neurodegenerative disorder that is characterized by a degeneration of the dopaminergic system. Dopamine transporter (DAT) positron emission tomography (PET) imaging has emerged as a powerful and non-invasive method to quantify dopaminergic function in the living brain. The PET radioligand, [¹⁸F]FE-PE2I, a cocaine chemical derivative, has shown promising properties for in vivo PET imaging of DAT, including high affinity and selectivity for DAT, excellent brain permeability, and favorable metabolism. The aim of the current study was to scale up the production of [¹⁸F]FE-PE2I to fulfil the increasing clinical demand for this tracer.

Results

Thus, a fully automated and GMP-compliant production procedure has been developed using a commercially available radiosynthesis module GE TRACERLab FX2 N. [¹⁸F]FE-PE2I was produced with a radiochemical yield of 39 ± 8% (n = 4, relative [¹⁸F]F⁻ delivered to the module). The synthesis time was 70 min, and the molar activity was 925.3 ± 763 GBq/µmol (250 ± 20 Ci/µmol). The produced [¹⁸F]FE-PE2I was stable over 6 h at room temperature.