Abstract

Purpose[18F]PR04.MZ is a new PET imaging agent for dopamine transporters, providing excellent image quality and allowing for the evaluation of patients with movement disorders such as Parkinson’s disease. The objective of this study was to evaluate the biodistribution and radiation dosimetry of [18F]PR04.MZ by serial PET imaging.MethodsSix healthy subjects (n = 3 males, n = 3 females) were enrolled in this study. A series of 14 whole-body PET/CT scans were acquired until 5.5 h post-injection of 200 ± 11 MBq of [18F]PR04.MZ. After rigid co-registration, volumes of interest were outlined either on CT or PET images. Time-integrated activity coefficients were calculated for selected source organs. Organ absorbed doses, and the effective dose were calculated using IDAC-Dose 2.1.ResultsPhysiological uptake of [18F]PR04.MZ was mainly observed in the striatum, brain, liver, gall bladder, intestine, red marrow and cortical bone. [18F]PR04.MZ was primarily excreted via hepatobiliary clearance and, to a lower extent, via renal clearance. The normalized absorbed doses were highest in gall bladder wall (32.2 ± 6.4 µGy/MBq), urinary bladder wall (27.2 ± 4.5 µGy/MBq), red marrow (26.5 ± 1.4 µGy/MBq), cortical bone surface (26.3 ± 2.5 µGy/MBq), liver (22.5 ± 1.8 µGy/MBq) and kidneys (21.8 ± 1.1 µGy/MBq). The effective dose according to ICRP 60 and 103 was 16.3 ± 1.1 and 16.6 ± 1.5 µSv/MBq, respectively.Conclusion[18F]PR04.MZ has a favourable dosimetry profile, comparable to those of other 18F-labelled PET tracers, and is suitable for larger clinical applications.Trial registration CEC SSM Oriente, Santiago, Chile, permit 20140520.

Highlights

  • The presynaptic dopamine transporter (DAT) modulates the extracellular dopamine concentration in the brain

  • Striatum and red marrow, peak uptake of 0.017 and 0.005%IA/g was observed around 15 and 25 min p.i., respectively. ­[18F]PR04.MZ was primarily cleared via the hepatobiliary pathway and, to a lower a

  • In this study, six healthy subjects were enrolled and whole-body Positron Emission Tomography (PET)/CT scans were acquired over 5.5 h post-injection to evaluate the biodistribution and dosimetry of ­[18F]PR04.MZ

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Summary

Introduction

The presynaptic dopamine transporter (DAT) modulates the extracellular dopamine concentration in the brain. DAT imaging is used to differentiate essential tremor from tremor due to PS for which the Single Photon Emission Computed Tomography (SPECT) tracer DaTscanTM (Ioflupane I-123), Lehnert et al EJNMMI Research (2022) 12:1 approved by the FDA and EMA, is the standard of care [5]. DAT PET imaging with 18F-labelled tracers such as ­[18F]FP-CIT, ­[18F]FE-CNT, ­[18F]FE-PE2I, ­[18F]LBT-999 is a viable alternative when precise quantification for clinical research is necessary or where DaTscanTM is not available [6,7,8,9,10]. The diagnostic potential of this new tracer was highlighted by the excellent imaging properties in a case study of Holmes Tremor [14] and the clinical validation for detection of nigro-striatal degeneration in patients under evaluation for movement disorders [15]

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