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Pharmaceuticals 2014, 7(7), 779-796; doi:10.3390/ph7070779
Article

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

1,2,†,* , 1,2,†
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1 German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany 2 German Cancer Consortium (DKTK), Im Neuenheimer Feld 280, Heidelberg 69120, Germany 3 Department of Nuclear Medicine, University of Heidelberg, Im Neuenheimer Feld 400, Heidelberg 69120, Germany The authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 20 February 2014 / Revised: 11 June 2014 / Accepted: 12 June 2014 / Published: 30 June 2014
(This article belongs to the Special Issue Radiopharmaceutical Chemistry between Imaging and Radioendotherapy)
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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.
Keywords: 68Ga-PET imaging; PSMA; HBED-CC; prostate cancer; radiopharmaceutical production; good manufacturing practice; GMP 68Ga-PET imaging; PSMA; HBED-CC; prostate cancer; radiopharmaceutical production; good manufacturing practice; GMP
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Eder, M.; Neels, O.; Müller, M.; Bauder-Wüst, U.; Remde, Y.; Schäfer, M.; Hennrich, U.; Eisenhut, M.; Afshar-Oromieh, A.; Haberkorn, U.; Kopka, K. Novel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC: A New PET Tracer for Imaging of Prostate Cancer. Pharmaceuticals 2014, 7, 779-796.

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