Ferrat Mélodie, Moein Mohammad M, Cananau Carmen, Tegnebratt Tetyana, Saliba Paul, Norman Fredrik, Steiger Carsten, Bratteby Klas, Samén Erik, Dahl Kenneth, Tran Thuy A
Department of Radiopharmacy, Karolinska University Hospital, 171 76, Stockholm, Sweden.
Department of Oncology and Pathology, Karolinska Institutet, 171 76, Stockholm, Sweden.
EJNMMI Radiopharm Chem. 2024 May 2;9(1):35. doi: 10.1186/s41181-024-00269-9.
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, [F]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 [F]FE-PE2I to fulfil the increasing clinical demand for this tracer.
Thus, a fully automated and GMP-compliant production procedure has been developed using a commercially available radiosynthesis module GE TRACERLab FX2 N. [F]FE-PE2I was produced with a radiochemical yield of 39 ± 8% (n = 4, relative [F]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 [F]FE-PE2I was stable over 6 h at room temperature.
The protocol reliably provides a sterile and pyrogen-free GMP-compliant product.
帕金森病是一种神经退行性疾病，其特征是多巴胺能系统退化。多巴胺转运体（DAT）正电子发射断层扫描（PET）成像已成为一种强大的非侵入性方法，用于量化活体大脑中的多巴胺能功能。PET放射性配体[F]FE-PE2I是一种可卡因化学衍生物，已显示出在DAT的体内PET成像方面具有良好的特性，包括对DAT具有高亲和力和选择性、出色的脑通透性以及良好的代谢。本研究的目的是扩大[F]FE-PE2I的生产规模，以满足对该示踪剂日益增长的临床需求。
因此，使用市售的放射性合成模块GE TRACERLab FX2 N开发了一种全自动且符合GMP标准的生产程序。[F]FE-PE2I的放射化学产率为39±8%（n = 4，输送到模块的相对[F]F）。合成时间为70分钟，摩尔活度为925.3±763 GBq/µmol（250±20 Ci/µmol）。所生产的[F]FE-PE2I在室温下6小时内稳定。
该方案可靠地提供了一种无菌、无热原且符合GMP标准的产品。
