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The clinical safety, biodistribution and internal radiation dosimetry of [18F]fluciclovine in healthy adult volunteers

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Abstract

Purpose

We report on the biodistribution and internal radiation dosimetry in humans of [18F]fluciclovine, a synthetic L-leucine analogue being investigated as a potential diagnostic biomarker for neoplasia.

Methods

Whole-body positron emission tomography (PET) scans of 6 healthy volunteers were acquired at up to 16 time points up to about 5 h after a bolus administration of [18F]fluciclovine (153.8 ± 2.2 MBq). Venous blood samples were taken up to about 4 h post-injection from which 18F activity concentrations in whole blood and plasma were measured. Urine was collected as voided up to 4 h post-injection, from which the excreted 18F activity was measured. Absolute values of the 18F activity contained in up to 11 source regions (brain, salivary glands, lung, heart, pancreas, spleen, liver, red bone marrow, kidneys, uterus and urinary bladder contents) were determined directly from quantitative analysis of the images. For each source region, the 18F activity decay-corrected and normalised to that injected, as a function of time, was fit by an analytical function which was subsequently integrated to yield the cumulated activity normalised to the injected activity. These normalised cumulated activities were then used as input to the Organ Level INternal Dose Assessment/EXponential Modelling (OLINDA/EXM) package to calculate the internal radiation dosimetry of each subject following the Medical Internal Radiation Dose (MIRD) schema. An effective dose was then estimated for each subject.

Results

[18F]Fluciclovine was clinically well tolerated in this study. Very little 18F was excreted with only a mean value of 3.3 % present in the urine at about 4 h post-injection; no activity within the intestinal contents was noted. The highest mean initial uptakes were measured in the liver (13.8 %), red bone marrow (11.1 %) and lung (7.1 %). The highest mean radiation absorbed doses per unit administered activity were received by the pancreas (102.2 μGy/MBq), the cardiac wall (51.7 μGy/MBq) and the uterine wall (44.6 μGy/MBq). The mean effective dose per unit administered activity was 22.1 μSv/MBq.

Conclusion

The internal radiation dosimetry of [18F]fluciclovine appears acceptable for PET imaging.

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Conflicts of interest

This study was sponsored by GE Healthcare. BJMcP is an employee of GE Healthcare.

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Authors and Affiliations

  1. Imaging Technology Group, GE Healthcare Medical Diagnostics, The Grove Centre, White Lion Road, Amersham, Buckinghamshire, UK, HP7 9LL

    Brian J. McParland

  2. Section of Nuclear Medicine and PET, Department of Radiology, Oncology and Radiation Sciences, Uppsala University, Uppsala, Sweden

    Anders Wall & Jens Sørensen

  3. Section of Oncology, Department of Radiology, Oncology and Radiation Sciences, Uppsala University, Uppsala, Sweden

    Silvia Johansson

Authors
  1. Brian J. McParland
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  2. Anders Wall
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  3. Silvia Johansson
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  4. Jens Sørensen
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Correspondence to Brian J. McParland.

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McParland, B.J., Wall, A., Johansson, S. et al. The clinical safety, biodistribution and internal radiation dosimetry of [18F]fluciclovine in healthy adult volunteers. Eur J Nucl Med Mol Imaging 40, 1256–1264 (2013). https://doi.org/10.1007/s00259-013-2403-1

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  • DOI: https://doi.org/10.1007/s00259-013-2403-1

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