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Imaging Characteristics and First Experience of [68Ga]THP-PSMA, a Novel Probe for Rapid Kit-Based Ga-68 Labeling and PET Imaging: Comparative Analysis with [68Ga]PSMA I&T

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Abstract

Purpose

[68Ga]Trishydroxypyridinone (THP)–prostate-specific membrane antigen (PSMA) is a novel tracer that can be labeled in one step by cold reconstitution of a kit with unprocessed generator eluate, targeting PSMA via the lysine-urea-glutamate (KuE) motif. The aim of this study was to evaluate the human imaging characteristics of [68Ga]THP-PSMA.

Procedures

[68Ga]THP-PSMA positron emission tomography (PET)/x-ray computed tomography (CT) was performed in 25 patients with biochemical recurrence after radical prostatectomy for prostate cancer. Urinary and biliary excretion and tumor lesion uptake were quantified using standardized uptake values (SUVs). Imaging characteristics were assessed in terms of non-target organ uptake, background activity, target-to-background ratios (TBRs) of tumor lesions, and frequency of bladder halo artifacts. Findings were compared to a matched cohort of 25 patients undergoing PET/CT with the established agent [68Ga]PSMA I&T.

Results

Physiologic uptake of [68Ga]THP-PSMA was significantly lower in salivary glands (P < 0.0001), liver (P < 0.0001), spleen (P < 0.0001), and kidneys (P < 0.0001) than with [68Ga]PSMA I&T. While biliary tracer excretion of [68Ga]THP-PSMA was negligible, urinary tracer excretion of [68Ga]THP-PSMA was fast, and significantly higher than for [68Ga]PSMA I&T, contributing to a higher frequency of bladder artifacts. Malignant lesion uptake of [68Ga]THP-PSMA assessed as either SUV or TBR was significantly lower than with [68Ga]PSMA I&T.

Conclusion

[68Ga]THP-PSMA yields suitable in vivo uptake characteristics. The simplified synthesis method for [68Ga]THP-PSMA may facilitate wider application and higher patient throughput with PSMA imaging. However, direct intraindividual comparison studies are needed to assess the relative performance of [68Ga]THP-PSMA vs other PSMA ligands in terms of clinical detection rate and image quality.

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Authors and Affiliations

  1. Department of Nuclear Medicine, Hannover Medical School, Carl-Neuberg-Str. 1, 30625, Hannover, Germany

    Thorsten Derlin, Sebastian Schmuck, Sophie M. Schneefeld, Almut C. A. Walte, James T. Thackeray, Tobias L. Ross & Frank M. Bengel

  2. Rotop Pharmaka GmbH, Dresden, Germany

    Cathleen Juhl, Steffi Teichert & Johanna Zörgiebel

  3. Pharmaceutical Radiochemistry, Technische Universität München, Garching, Germany

    Hans-Jürgen Wester

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  1. Thorsten Derlin
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Correspondence to Thorsten Derlin.

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Conflicts of Interest and Sources of Funding

Dr. Hans-Jürgen Wester is a shareholder of Scintomics. THP-PSMA was provided by ROTOP Pharmaka GmbH under an academic agreement, and Dr. Cathleen Juhl, Steffi Teichert, and Dr. Johanna Zörgiebel are employees of ROTOP Pharmaka GmbH. No other potential conflict of interest relevant to this article was reported.

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Derlin, T., Schmuck, S., Juhl, C. et al. Imaging Characteristics and First Experience of [68Ga]THP-PSMA, a Novel Probe for Rapid Kit-Based Ga-68 Labeling and PET Imaging: Comparative Analysis with [68Ga]PSMA I&T. Mol Imaging Biol 20, 650–658 (2018). https://doi.org/10.1007/s11307-018-1160-8

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