novel preclinical and radiopharmaceutical aspects of [68ga]ga-psma-hbed-cc: a new pet tracer for imaging of prostate cancer

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ID: 183767
2014
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Abstract
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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eder2014pharmaceuticalsnovel Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Matthias Eder, Oliver Neels, Miriam Müller, Ulrike Bauder-Wüst, Yvonne Remde, Martin Schäfer, Ute Hennrich, Michael Eisenhut, Ali Afshar-Oromieh, Uwe Haberkorn, Klaus Kopka
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Journal journal of cerebral blood flow and metabolism
Year 2014
DOI
10.3390/ph7070779
URL
http://www.mdpi.com/1424-8247/7/7/779
Keywords
prostate cancer psma

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