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BioMed Research International
Volume 2014 (2014), Article ID 871609, 17 pages
Review Article

PET Radiopharmaceuticals for Imaging Integrin Expression: Tracers in Clinical Studies and Recent Developments

1Department of Nuclear Medicine, Innsbruck Medical University, Anichstraße 35, 6020 Innsbruck, Austria
2Molecular Imaging and Radiochemistry, Department of Nuclear Medicine, Friedrich-Alexander University, Schwabachanlage 6, 91054 Erlangen, Germany

Received 25 March 2014; Accepted 29 April 2014; Published 11 June 2014

Academic Editor: Patrick Riss

Copyright © 2014 Roland Haubner et al. 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.


Noninvasive determination of integrin expression has become an interesting approach in nuclear medicine. Since the discovery of the first 18F-labeled cyclic RGD peptide as radiotracer for imaging integrin expression in vivo, there have been carried out enormous efforts to develop RGD peptides for PET imaging. Moreover, in recent years, additional integrins, including and , came into the focus of pharmaceutical radiochemistry. This review will discuss the tracers already evaluated in clinical trials and summarize the preliminary outcome. It will also give an overview on recent developments to further optimize the first-generation compounds such as [18F]Galacto-RGD. This includes recently developed 18F-labeling strategies and also new approaches in 68Ga-complex chemistry. Furthermore, the approaches to develop radiopharmaceuticals targeting integrin and will be summarized and discussed.