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Pharmaceuticals (Basel). 2014 Jun 30;7(7):779-96. doi: 10.3390/ph7070779.

Novel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC: A New PET Tracer for Imaging of Prostate Cancer.

Author information

  • 1German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. m.eder@dkfz.de.
  • 2German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. o.neels@dkfz.de.
  • 3German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. miriam.mueller@wak-gmbh.de.
  • 4German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. u.bauder-wuest@dkfz.de.
  • 5German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. y.remde@dkfz.de.
  • 6German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. martin.schaefer@dkfz.de.
  • 7German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. u.hennrich@dkfz.de.
  • 8German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. m.eisenhut@dkfz.de.
  • 9Department of Nuclear Medicine, University of Heidelberg, Im Neuenheimer Feld 400, Heidelberg 69120, Germany. Ali.Afshar@med.uni-heidelberg.de.
  • 10Department of Nuclear Medicine, University of Heidelberg, Im Neuenheimer Feld 400, Heidelberg 69120, Germany. Uwe.Haberkorn@med.uni-heidelberg.de.
  • 11German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany. k.kopka@dkfz.de.

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.

PMID:
24983957
PMCID:
PMC4113732
DOI:
10.3390/ph7070779
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