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Novel preclinical and radiopharmaceutical aspects of (68Ga)Ga-PSMA-HBED-CC: a new PET tracer for imaging of prostate cancer

The detection of prostate cancer lesions by PET imaging of the prostate-specific membrane antigen (PSMA) has gained highest clinical impact during the last years. 68Ga-labelled Glu-urea-Lys(Ahx)-HBED-CC ([68Ga]Ga-PSMA-HBED-CC) represents a successful novel PSMA inhibitor radiotracer which has recen...

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Main Authors: Eder, Matthias (Author) , Kiß, Oliver (Author) , Müller, Miriam (Author) , Bauder-Wüst, Ulrike (Author) , Remde, Yvonne (Author) , Schäfer, Martin (Author) , Hennrich, Ute (Author) , Eisenhut, Michael (Author) , Afshar-Oromieh, Ali (Author) , Haberkorn, Uwe (Author) , Kopka, Klaus (Author)
Format: Article (Journal)
Language:English
Published: 30 June 2014
In: Pharmaceuticals
Year: 2014, Volume: 7, Issue: 7, Pages: 779-796
ISSN:1424-8247
DOI:10.3390/ph7070779
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.3390/ph7070779
Verlag, lizenzpflichtig, Volltext: https://www.mdpi.com/1424-8247/7/7/779
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Author Notes:Matthias Eder, Oliver Neels, Miriam Müller, Ulrike Bauder-Wüst, Yvonne Remde, Martin Schäfer, Ute Hennrich, Michael Eisenhut, Ali Afshar-Oromieh, Uwe Haberkorn and Klaus Kopka
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Summary:The detection of prostate cancer lesions by PET imaging of the prostate-specific membrane antigen (PSMA) has gained highest clinical impact during the last years. 68Ga-labelled Glu-urea-Lys(Ahx)-HBED-CC ([68Ga]Ga-PSMA-HBED-CC) represents a successful novel PSMA inhibitor radiotracer which has recently demonstrated its suitability in individual first-in-man studies. The radiometal chelator HBED-CC used in this molecule represents a rather rarely used acyclic complexing agent with chemical characteristics favourably influencing the biological functionality of the PSMA inhibitor. The simple replacement of HBED-CC by the prominent radiometal chelator DOTA was shown to dramatically reduce the in vivo imaging quality of the respective 68Ga-labelled PSMA-targeted tracer proving that HBED-CC contributes intrinsically to the PSMA binding of the Glu-urea-Lys(Ahx) pharmacophore. Owing to the obvious growing clinical impact, this work aims to reflect the properties of HBED-CC as acyclic radiometal chelator and presents novel preclinical data and relevant aspects of the radiopharmaceutical production process of [68Ga]Ga-PSMA-HBED-CC.
Item Description:Im Titel steht der Ausdruck (68Ga) in eckiger Klammer, die Zahl 68 ist dabei hochgestellt
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Physical Description:Online Resource
ISSN:1424-8247
DOI:10.3390/ph7070779

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