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Radiolabelled RGD peptides for imaging and therapy

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Abstract

Imaging of angiogenesis has become increasingly important with the rising use of targeted antiangiogenic therapies like bevacizumab (Avastin). Non-invasive assessment of angiogenic activity is in this respect interesting, e.g. for response assessment of such targeted antiangiogenic therapies. One promising approach of angiogenesis imaging is imaging of specific molecular markers of the angiogenic cascade like the integrin αvβ3. For molecular imaging of integrin expression, the use of radiolabelled peptides is still the only approach that has been successfully translated into the clinic. In this review we will summarize the current data on imaging of αvβ3 expression using radiolabelled RGD peptides with a focus on tracers already in clinical use. A perspective will be presented on the future clinical use of radiolabelled RGD peptides including an outlook on potential applications for radionuclide therapy.

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Authors and Affiliations

  1. Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaningerstr. 22, 81675, Munich, Germany

    F. C. Gaertner, M. Schwaiger & A. J. Beer

  2. Institute for Advanced Study and Center of Integrated Protein Science, Department of Chemistry, Technische Universität München, Garching, Germany

    H. Kessler

  3. Chemistry Department, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah, 21589, Saudi Arabia

    H. Kessler

  4. Institute for Pharmaceutical Radiochemistry, Walther-Meissner-Str.3, 85748, Garching, Germany

    H.-J. Wester

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  1. F. C. Gaertner
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Gaertner, F.C., Kessler, H., Wester, HJ. et al. Radiolabelled RGD peptides for imaging and therapy. Eur J Nucl Med Mol Imaging 39 (Suppl 1), 126–138 (2012). https://doi.org/10.1007/s00259-011-2028-1

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