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Development and clinical potential of 18F-PSiMA for prostate cancer PET imaging

Prostate-specific membrane antigen (PSMA) is a key target for diagnosing prostate cancer through positron emission tomography (PET). While 68Ga-labeled PSMA compounds are widely used, 18F-labeled PSMA inhibitors have gained traction for clinical tumor imaging. We previously investigated PSMA-targeti...

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Main Authors: Gower-Fry, Lexi (Author) , Bailey, Justin J. (Author) , Wuest, Melinda (Author) , Pike, Susan (Author) , Kostikov, Alexey (Author) , Dorian, Andreas (Author) , Wängler, Carmen (Author) , Wuest, Frank (Author) , Schirrmacher, Ralf (Author)
Format: Article (Journal)
Language:English
Published: 09 May 2025
In: RSC medicinal chemistry
Year: 2025, Volume: 16, Issue: 8, Pages: 3633-3644
ISSN:2632-8682
DOI:10.1039/D5MD00275C
Online Access:Verlag, kostenfrei, Volltext: https://doi.org/10.1039/D5MD00275C
Verlag, kostenfrei, Volltext: https://pubs.rsc.org/en/content/articlelanding/2025/md/d5md00275c
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Author Notes:Lexi Gower-Fry, Justin J. Bailey, Melinda Wuest, Susan Pike, Alexey Kostikov, Andreas Dorian, Carmen Wängler, Frank Wuest and Ralf Schirrmacher
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Summary:Prostate-specific membrane antigen (PSMA) is a key target for diagnosing prostate cancer through positron emission tomography (PET). While 68Ga-labeled PSMA compounds are widely used, 18F-labeled PSMA inhibitors have gained traction for clinical tumor imaging. We previously investigated PSMA-targeting compounds based on the Lys-urea-Glu motif, incorporating a silicon fluoride-acceptor (SiFA) and chemical auxiliaries to enhance in vivo biodistribution. This led to the development of 18F-PSiMA, a SiFA-based radiotracer with an optimized linker exhibiting favorable PSMA potency (IC50 = 154 ± 47 nM in LNCaP cells). 18F-PSiMA radiosynthesis with low to high concentrations of 18F and precursor achieved molar activities (Am) of 10.9-82.5 GBq μmol−1 and showed a 24-38% increase in tumor uptake in LNCaP tumors (SUV60min 1.56 ± 0.18; 7.23 ± 0.75% ID per g at lower Am and SUV60min 1.90 ± 0.29; 9.62 ± 1.29% ID per g at higher Am) compared to our previous lead, 18F-SiFA-Asp2-PEG3-PSMA. PSMA specificity was confirmed by a 20 ± 10% reduction in SUV60min upon co-injection with DCFPyl. These promising in vitro and in vivo results support further clinical translation of 18F-PSiMA for prostate cancer PET imaging.
Item Description:Zuerst veröffentlicht: 09. Mai 2025
Gesehen am 17.09.2025
Im Titel ist die Zahl "18" hochgestellt
Physical Description:Online Resource
ISSN:2632-8682
DOI:10.1039/D5MD00275C

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