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: | , , , , , , , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
30 June 2014
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| 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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| 520 | |a 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. | ||
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