Radiolabelled RGD peptides for imaging and therapy

Eur J Nucl Med Mol Imaging. 2012 Feb:39 Suppl 1:S126-38. doi: 10.1007/s00259-011-2028-1.

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 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.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / therapeutic use
  • Copper Radioisotopes
  • Galactose / analogs & derivatives
  • Gallium Radioisotopes
  • Humans
  • Integrins / metabolism
  • Neoplasms / blood supply*
  • Neoplasms / diagnostic imaging
  • Neoplasms / metabolism
  • Neoplasms / radiotherapy
  • Neovascularization, Pathologic / diagnostic imaging*
  • Neovascularization, Pathologic / metabolism
  • Neovascularization, Pathologic / radiotherapy*
  • Oligopeptides / therapeutic use*
  • Peptides
  • Peptides, Cyclic
  • Polyethylene Glycols
  • Radiopharmaceuticals / therapeutic use*
  • Technetium
  • Tomography, Emission-Computed, Single-Photon

Substances

  • 18F-RGD-K5
  • AH 111585
  • Angiogenesis Inhibitors
  • Copper Radioisotopes
  • Gallium Radioisotopes
  • Integrins
  • Oligopeptides
  • Peptides
  • Peptides, Cyclic
  • Radiopharmaceuticals
  • fluorogalacto-RGD
  • Polyethylene Glycols
  • Technetium
  • arginyl-glycyl-aspartic acid
  • Galactose