Preclinical Evaluation of Radiolabeled Peptides for PET Imaging of Glioblastoma Multiforme

Molecules. 2019 Jul 8;24(13):2496. doi: 10.3390/molecules24132496.


In this study, we have compared four 68Ga-labeled peptides (three Arg-Gly-Asp (RGD) peptides and substance-P) with two 18F-tracers clinically approved for tumor imaging. We have studied in vitro and in vivo characteristics of selected radiolabeled tracers in a glioblastoma multiforme tumor model. The in vitro part of the study was mainly focused on the evaluation of radiotracers stability under various conditions. We have also determined in vivo stability of studied 68Ga-radiotracers by analysis of murine urine collected at various time points after injection. The in vivo behavior of tested 68Ga-peptides was evaluated through ex vivo biodistribution studies and PET/CT imaging. The obtained data were compared with clinically used 18F-tracers. 68Ga-RGD peptides showed better imaging properties compared to 18F-tracers, i.e., higher tumor/background ratios and no accumulation in non-target organs except for excretory organs.

Keywords: 18F-FDG; 18F-FLT; PET; RGD peptides; biodistribution; gallium-68; glioblastoma multiforme.

MeSH terms

  • Animals
  • Brain Neoplasms / diagnostic imaging*
  • Brain Neoplasms / metabolism
  • Cell Line, Tumor
  • Female
  • Fluorine Radioisotopes
  • Gallium Radioisotopes / chemistry*
  • Glioblastoma / diagnostic imaging*
  • Glioblastoma / metabolism
  • Humans
  • Mice, SCID
  • Neoplasm Transplantation
  • Oligopeptides / chemistry*
  • Positron Emission Tomography Computed Tomography
  • Positron-Emission Tomography / methods
  • Radiopharmaceuticals / chemistry*
  • Tissue Distribution
  • Tomography, X-Ray Computed


  • Fluorine Radioisotopes
  • Gallium Radioisotopes
  • Oligopeptides
  • Radiopharmaceuticals
  • arginyl-glycyl-aspartic acid
  • Fluorine-18