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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

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Received: 20 February 2014; in revised form: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

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(7):779-796.

Chicago/Turabian Style

Eder, Matthias; Neels, Oliver; Müller, Miriam; Bauder-Wüst, Ulrike; Remde, Yvonne; Schäfer, Martin; Hennrich, Ute; Eisenhut, Michael; Afshar-Oromieh, Ali; Haberkorn, Uwe; Kopka, Klaus. 2014. "Novel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC: A New PET Tracer for Imaging of Prostate Cancer." Pharmaceuticals 7, no. 7: 779-796.



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