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European Journal of Nuclear Medicine and Molecular Imaging
Published in: European Journal of Nuclear Medicine and Molecular Imaging 10/2023

16-05-2023 | Positron Emission Tomography | Original Article

Biodistribution and radiation dosimetry in cancer patients of the ascorbic acid analogue 6-Deoxy-6-[18F] fluoro-L-ascorbic acid PET imaging: first-in-human study

Authors: Yali Long, Chang Yi, Renbo Wu, Yuying Zhang, Bing Zhang, Xinchong Shi, Xiangsong Zhang, Zhihao Zha

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 10/2023

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Abstract

Purpose

Clinical studies on the use of ascorbic acid (AA) have become a hot spot in cancer research. There remains an unmet need to assess AA utilization in normal tissues and tumors. 6-Deoxy-6-[18F]fluoro-L-ascorbic acid ([18F]DFA) displayed distinctive tumor localization and similar distribution as AA in mice. In this study, to evaluate the distribution, tumor detecting ability and radiation dosimetry of [18F]DFA in humans, we performed the first-in-human PET imaging study.

Methods

Six patients with a variety of cancers underwent whole-body PET/CT scans after injection of 313–634 MBq of [18F]DFA. Five sequential dynamic emission scans in each patient were acquired at 5–60 min. Regions of interest (ROI) were delineated along the edge of the source-organ and tumor on the transverse PET slice. Tumor-to-background ratio (TBR) was obtained using the tumor SUVmax to background SUVmean. Organ residence times were calculated via time-activity curves, and human absorbed doses were estimated from organ residence time using the medical internal radiation dosimetry method.

Results

[18F]DFA was well tolerated in all subjects without serious adverse event. The high uptake was found in the liver, adrenal glands, kidneys, choroid plexus, and pituitary gland. [18F]DFA accumulated in tumor rapidly and the TBR increased over time. The average SUVmax of [18F]DFA in tumor lesions was 6.94 ± 3.92 (range 1.62–22.85, median 5.94). The organs with the highest absorbed doses were the liver, spleen, adrenal glands, and kidneys. The mean effective dose was estimated to be 1.68 ± 0.36 E−02 mSv/MBq.

Conclusions

[18F]DFA is safe to be used in humans. It showed a similar distribution pattern as AA, and displayed high uptake and retention in tumors with appropriate kinetics. [18F]DFA might be a promising radiopharmaceutical in identifying tumors with high affinity for SVCT2 and monitoring AA distribution in both normal tissues and tumors.

Trial registration

Chinese Clinical Trial Registry; Registered Number: ChiCTR2200057842​ (registered 19 March 2022).
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Metadata
Title
Biodistribution and radiation dosimetry in cancer patients of the ascorbic acid analogue 6-Deoxy-6-[18F] fluoro-L-ascorbic acid PET imaging: first-in-human study
Authors
Yali Long
Chang Yi
Renbo Wu
Yuying Zhang
Bing Zhang
Xinchong Shi
Xiangsong Zhang
Zhihao Zha
Publication date
16-05-2023
Publisher
Springer Berlin Heidelberg
Published in
European Journal of Nuclear Medicine and Molecular Imaging / Issue 10/2023
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI
https://doi.org/10.1007/s00259-023-06262-9

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