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

Pharmaceuticals

Matthias Eder¹  Oliver Neels¹  Miriam Müller¹  Ulrike Bauder-Wüst¹  Yvonne Remde¹  Martin Schr¹  Ute Hennrich¹  Michael Eisenhut¹  Ali Afshar-Oromieh²  Uwe Haberkorn² 

[1] German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, Heidelberg 69120, Germany; E-Mails:;Department of Nuclear Medicine, University of Heidelberg, Im Neuenheimer Feld 400, Heidelberg 69120, Germany; E-Mails:

关键词: ⁶⁸Ga-PET imaging;    PSMA;    HBED-CC;    prostate cancer;    radiopharmaceutical production;    good manufacturing practice;    GMP;   

DOI  :  10.3390/ph7070779

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
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