Radiolabelled RGD peptides for imaging and therapy

• Published in: European journal of nuclear medicine and molecular imaging Vol. 39; no. Suppl 1; pp. 126 - 138
• Main Authors: Gaertner, F. C., Kessler, H., Wester, H.-J., Schwaiger, M., Beer, A. J.
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer-Verlag 01.02.2012; Springer Nature B.V
• Subjects: Angiogenesis; Angiogenesis Inhibitors - therapeutic use; Cardiology; Copper Radioisotopes; Drug therapy; Galactose - analogs & derivatives; Gallium Radioisotopes; Humans; Imaging; Integrins - metabolism; Medical imaging; Medicine; Medicine & Public Health; Neoplasms - blood supply; Neoplasms - diagnostic imaging; Neoplasms - metabolism; Neoplasms - radiotherapy; Neovascularization, Pathologic - diagnostic imaging; Neovascularization, Pathologic - metabolism; Neovascularization, Pathologic - radiotherapy; Nuclear Medicine; Oligopeptides - therapeutic use; Oncology; Orthopedics; Peptides; Peptides, Cyclic; Polyethylene Glycols; Radiology; Radiopharmaceuticals - therapeutic use; Review Article; Technetium; Tomography, Emission-Computed, Single-Photon; Molecular imaging; Angiogenesis; RGD peptides
• ISSN: 1619-7070; 1619-7089
• DOI: 10.1007/s00259-011-2028-1

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 α v β 3 . 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 α v β 3 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.