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A microdose clinical trial to evaluate [18F]Florastamin as a positron emission tomography imaging agent in patients with prostate cancer

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European Journal of Nuclear Medicine and Molecular Imaging Aims and scope Submit manuscript

Abstract

Purpose

To evaluate the biodistribution of [18F]Florastamin, a novel 18F-labelled positron emission tomography (PET) tracer for prostate-specific membrane antigen (PSMA) for the diagnosis of prostate cancer.

Methods

PET was performed for five healthy controls and 10 patients with prostate cancer at 0, 10, 30, 70, and 120 mins after injecting 370 MBq of [18F]Florastamin. The maximum standardised uptake value (SUVmax) was evaluated in the primary tumour. The mean SUVmax (SUVmean) was evaluated in normal organs. Furthermore, the residence time was evaluated by assessing radioactivity in each organ. The internal radiation dosimetry was calculated using the OLINDA/EXM software.

Results

The SUVmax in primary tumours increased with time. A favourable tumour to background ratio was also observed over time. Multiple lymph nodes and bone metastases were also evaluated and showed a similar pattern to SUVmax in the primary tumour. In one patient, a tiny lymph node metastasis was identified using [18F]Florastamin PET, which was not observed using other modalities, and was histologically confirmed. The highest absorbed dose was observed in the kidney (0.062 ± 0.015 mGy/MBq), followed by the bladder (0.032 ± 0.013 mGy/MBq), liver (0.022 ± 0.006 mGy/MBq), and salivary gland (0.018 ± 0.006 mGy/MBq). The effective dose with a 370 MBq injection of [18F]Florastamin was 1.81 mSv. No adverse events related to [18F]Florastamin were reported.

Conclusion

We identified a novel PSMA-targeted PET ligand, [18F]Florastamin, for imaging prostate cancer. [18F]Florastamin showed a high SUVmax and relatively high tumour to background ratio in both primary tumour and metastatic lesions, which suggests its high sensitivity to detect tumours without any adverse events.

Trial registration

KCT0003924 registered at https://cris.nih.go.kr/.

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Data availability

The datasets generated during and/or analysed during the current study are available from the corresponding author on reasonable request.

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Funding

This study was supported by a grant from the Korea Institute of Radiological and Medical Sciences (KIRAMS), funded by the Ministry of Science, ICT (MSIT), Republic of Korea (No. 50547-2020) and in part with a grant from the National Research Foundation of Korea (NRF), funded by the Ministry of Science, ICT (MSIT), Republic of Korea (No. 2019M2D2A1A02057204). [18F]Florastamin was supported by FutureChem Co., Ltd.

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Authors and Affiliations

  1. Department of Nuclear Medicine, Korea Cancer Centre Hospital, Korea Institute of Radiological and Medical Sciences, 75, Nowon-ro, Nowon-gu, Seoul, South Korea

    Inki Lee, Ilhan Lim, Byung Hyun Byun, Byung Il Kim, Chang Woon Choi & Sang Moo Lim

  2. Division of Applied RI, Research Institute of Radiological & Medical Sciences, Korea Institutes of Radiological & Medical Sciences, Seoul, South Korea

    Sang-Keun Woo, Kyo Chul Lee & Joo Hyun Kang

  3. Research Institute of Labeling, FutureChem Co., Ltd., Seoul, South Korea

    Hee Seup Kil, Chansoo Park & Dae Yoon Chi

  4. Department of Chemistry, Sogang University, Seoul, South Korea

    Dae Yoon Chi

  5. Department of Urology, Korea Cancer Centre Hospital, Korea Institute of Radiological and Medical Sciences, 75, Nowon-ro, Nowon-gu, Seoul, South Korea

    Jongwook Park & Kanghyon Song

Authors
  1. Inki Lee
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  2. Ilhan Lim
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  3. Byung Hyun Byun
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  7. Kyo Chul Lee
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  12. Jongwook Park
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  13. Kanghyon Song
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  14. Sang Moo Lim
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Contributions

All authors contributed to the study conception and design of this study. Inki Lee, Chansoo Park, Jongwook Park, and Kanghyon Song contributed to the collection and assembly of data. Inki Lee, Ilhan Lim, Byung Hyun Byun, Byung Il Kim, Chang Woon Choi, Sang-Keun Woo, Kyo Chul Lee, and Joo Hyun Kang contributed to the data analysis and interpretation. Inki Lee, Ilhan Lim, Sang-Keun Woo, and Hee Seup Kil contributed to drafting the work and revising it critically for important content and all authors commented on previous versions of the manuscript. All authors read and approved the final manuscript.

Corresponding authors

Correspondence to Ilhan Lim or Kanghyon Song.

Ethics declarations

Conflict of interest

Hee Seup Kil and Chansoo Park are employees of FutureChem Co., Ltd., Republic of Korea. Dae Yoon Chi is now an employee of FutureChem Co., Ltd. as Chief executive officer. The other authors declare no conflicts of interest.

Ethics approval

This study was approved by the by the Korean Ministry of Food and Drug Safety (MFDS), and the Institutional Review Board of KIRAMS (IRB No.: KIRAMS 2018-12-006-003). All procedures were performed following the 1964 Helsinki Declaration and its later amendments or comparable ethical standards. This clinical trial has been registered with the Clinical Research Information Service (https://cris.nih.go.kr), registration number KCT0003924.

Consent to participate

Informed consent was obtained from all individual participants included in the study.

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Publisher’s note

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Kanghyon Song and Ilhan Lim should be considered joint corresponding authors.

This article is part of the Topical Collection on Oncology - Genitourinary.

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Lee, I., Lim, I., Byun, B.H. et al. A microdose clinical trial to evaluate [18F]Florastamin as a positron emission tomography imaging agent in patients with prostate cancer. Eur J Nucl Med Mol Imaging 48, 95–102 (2021). https://doi.org/10.1007/s00259-020-04883-y

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  • DOI: https://doi.org/10.1007/s00259-020-04883-y

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