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

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 recent...

Full description

Saved in:
Bibliographic Details
Published in:Pharmaceuticals (Basel, Switzerland) Switzerland), 2014-06, Vol.7 (7), p.779-796
Main Authors: Eder, Matthias, Neels, Oliver, Müller, Miriam, Bauder-Wüst, Ulrike, Remde, Yvonne, Schäfer, Martin, Hennrich, Ute, Eisenhut, Michael, Afshar-Oromieh, Ali, Haberkorn, Uwe, Kopka, Klaus
Format: Article
Language:English
Subjects:
68Ga-PET imaging
Antigens
Chelating agents
GMP
good manufacturing practice
HBED-CC
Medical imaging
Prostate cancer
PSMA
radiopharmaceutical production
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph7070779