Fully Automated GMP-Compliant Synthesis of [18F]FE-PE2I

Bratteby, Klas; Denholt, Charlotte Lund; Lehel, Szabolcs; Petersen, Ida Nymann; Madsen, Jacob; Erlandsson, Maria; Ohlsson, Tomas; Herth, Matthias M.; Gillings, Nic

doi:10.3390/ph14070601

Cited by 5 publications

(3 citation statements)

References 18 publications

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“…The [ 18 F]FE-PE2I containing fraction was collected through a 0.22 µm sterile filter directly in the final product vial containing 15 ml sterile sodium phosphate buffer, thus providing the final product solution (23 mL) containing approximately 6% ethanol. Further details are reported elsewhere [ 27 ].…”

Section: Methodsmentioning

confidence: 99%

[18F]FE-PE2I PET is a feasible alternative to [123I]FP-CIT SPECT for dopamine transporter imaging in clinically uncertain parkinsonism

et al. 2022

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Background Dopamine transporter (DAT) imaging of striatum is clinically used in Parkinson’s disease (PD) and neurodegenerative parkinsonian syndromes (PS) especially in the early disease stages. The aim of the present study was to evaluate the diagnostic performance of the recently developed tracer for DAT imaging [18F]FE-PE2I PET/CT to the reference standard [123I]FP-CIT SPECT. Methods Ninety-eight unselected patients referred for DAT imaging were included prospectively and consecutively and evaluated with [18F]FE-PE2I PET/CT and [123I]FP-CIT SPECT on two separate days. PET and SPECT scans were categorized independently by two blinded expert readers as either normal, vascular changes, or mixed. Semiquantitative values were obtained for each modality and compared regarding effect size using Glass’ delta. Results Fifty-six of the [123I]FP-CIT SPECT scans were considered abnormal (52 caused by PS, 4 by infarctions). Using [18F]FE-PE2I PET/CT, 95 of the 98 patients were categorized identically to SPECT as PS or non-PS with a sensitivity of 0.94 [0.84–0.99] and a specificity of 1.00 [0.92–1.00]. Inter-reader agreement for [18F]FE-PE2I PET with a kappa of 0.97 [0.89–1.00] was comparable to the agreement for [123I]FP-CIT SPECT of 0.96 [0.76–1.00]. Semiquantitative values for short 10-min reconstructions of [18F]FE-PE2I PET/CT were comparable to longer reconstructions. The effect size for putamen/caudate nucleus ratio was significantly increased using PET compared to SPECT. Conclusions The high correspondence of [18F]FE-PE2I PET compared to reference standard [123I]FP-CIT SPECT establishes [18F]FE-PE2I PET as a feasible PET tracer for clinical use with favourable scan logistics.

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Section: Methodsmentioning

confidence: 99%

[18F]FE-PE2I PET is a feasible alternative to [123I]FP-CIT SPECT for dopamine transporter imaging in clinically uncertain parkinsonism

et al. 2022

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“…The radiosynthesis of [ 18 F]-FE-PE2I was described previously [ 14 ]. No patients or controls took medications containing amphetamine, modafinil, or other dopamine transporter ligands prior to the [ 18 F]-FE-PE2I PET/CT.…”

Section: Methodsmentioning

confidence: 99%

Dopaminergic Dysfunction Is More Symmetric in Dementia with Lewy Bodies Compared to Parkinson’s Disease

Fedorova

Knudsen

Horsager

et al. 2023

Journal of Parkinson’s Disease

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Background: The α-syn Origin site and Connectome model (SOC) proposes that α-synucleinopathies can be divided into two categories: the asymmetrical brain-first, and more symmetrical body-first Lewy body disease. We have hypothesized that most patients with dementia with Lewy bodies (DLB) belong to the body-first subtype, whereas patients with Parkinson’s disease (PD) more often belong to the brain-first subtype. Objective: To compare asymmetry of striatal dopaminergic dysfunction in DLB and PD patients using [18F]-FE-PE2I positron emission tomography (PET). Methods: We analyzed [18F]-FE-PE2I PET data from 29 DLB patients and 76 PD patients who were identified retrospectively during a 5-year period at Dept. of Neurology, Aarhus University Hospital. Additionally, imaging data from 34 healthy controls was used for age-correction and visual comparison. Results: PD patients showed significantly more asymmetry in specific binding ratios between the most and least affected putamen (p < 0.0001) and caudate (p = 0.003) compared to DLB patients. PD patients also had more severe degeneration in the putamen compared to the caudate in comparison to DLB patients (p < 0.0001) who had a more universal pattern of striatal degeneration. Conclusion: Patients with DLB show significantly more symmetric striatal degeneration on average compared to PD patients. These results support the hypothesis that DLB patients may be more likely to conform to the body-first subtype characterized by a symmetrical spread of pathology, whereas PD patients may be more likely to conform to the brain-first subtype with more lateralized initial propagation of pathology.

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“…[14] Moreover, a recent study adapted this one-step synthesis method of [ 18 F]FE-PE2I for an automated cassette-based radiochemistry module (Synthera® + , IBA). [15] The goal of the current work was to enable large-scale production of [ 18 F]FE-PE2I to meet the increasing clinical demand for an 18 F-labelled DAT PET imaging agent. Herein, we report the fully automated radiosynthesis of [ 18 F]FE-PE2I performed under good manufacturing procedure (GMP) conditions using a commercial radio uorination module (GE TRACERLab FX2 N) and its comprehensive validation for clinical routine human use.…”

Section: Introductionmentioning

confidence: 99%

GMP Production of [18F]FE-PE2I on a TRACERLab FX2 N synthesis module, a Radiotracer for in vivo PET Imaging of the Dopamine Transport

Ferrat,

Moein,

Cananau

et al. 2024

Preprint

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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 minutes, and the molar activity was 925.3 ± 763 GBq/µmol (250 ± 20 Ci/µmol). The produced [18F]FE-PE2I was stable over 6 hours at room temperature. Conclusion The protocol reliably provides a sterile and pyrogen–free GMP-compliant product.

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Fully Automated GMP-Compliant Synthesis of [18F]FE-PE2I

Cited by 5 publications

References 18 publications

[18F]FE-PE2I PET is a feasible alternative to [123I]FP-CIT SPECT for dopamine transporter imaging in clinically uncertain parkinsonism

[18F]FE-PE2I PET is a feasible alternative to [123I]FP-CIT SPECT for dopamine transporter imaging in clinically uncertain parkinsonism

Dopaminergic Dysfunction Is More Symmetric in Dementia with Lewy Bodies Compared to Parkinson’s Disease

GMP Production of [18F]FE-PE2I on a TRACERLab FX2 N synthesis module, a Radiotracer for in vivo PET Imaging of the Dopamine Transport

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