(68)Ga-labeled DOTA-peptides and (68)Ga-labeled radiopharmaceuticals for positron emission tomography: current status of research, clinical applications, and future perspectives

Semin Nucl Med. 2011 Jul;41(4):314-21. doi: 10.1053/j.semnuclmed.2011.02.001.


In this review we give an overview of current knowledge of (68)Ga-labeled pharmaceuticals, with focus on imaging receptor-mediated processes. A major advantage of a (68)Ge/(68)Ga generator is its continuous source of (68)Ga, independently from an on-site cyclotron. The increase in knowledge of purification and concentration of the eluate and the complex ligand chemistry has led to (68)Ga-labeled pharmaceuticals with major clinical impact. (68)Ga-labeled pharmaceuticals have the potential to cover all today's clinical options with (99m)Tc, with the concordant higher resolution of positron emission tomography (PET) in comparison with single photon emission computed tomography. (68)Ga-labeled analogs of octreotide, such as DOTATOC, DOTANOC, and DOTA-TATE, are in clinical application in nuclear medicine, and these analogs are now the most frequently applied of all (68)Ga-labeled pharmaceuticals. All the above-mentioned items in favor of successful application of (68)Ga-labeled radiopharmaceuticals for imaging in patients are strong arguments for the development of a (68)Ge/(68)Ga generator with Marketing Authorization and thus to provide pharmaceutical grade eluate. Moreover, now not one United States Food and Drug Administration-approved or European Medicines Agency-approved (68)Ga-radiopharmaceutical is available. As soon as these are achieved, a whole new radiopharmacy providing PET radiopharmaceuticals might develop.

Publication types

  • Review

MeSH terms

  • Forecasting
  • Gallium Radioisotopes / chemistry
  • Gallium Radioisotopes / pharmacokinetics*
  • Humans
  • Molecular Structure
  • Neuroendocrine Tumors / diagnostic imaging
  • Octreotide / analogs & derivatives
  • Octreotide / chemistry
  • Octreotide / pharmacokinetics
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacokinetics
  • Peptides / chemistry
  • Peptides / pharmacokinetics*
  • Positron-Emission Tomography / methods*
  • Positron-Emission Tomography / trends
  • Radioactivity
  • Radionuclide Generators
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics*
  • United States


  • 68Ga-DOTANOC
  • Gallium Radioisotopes
  • Organometallic Compounds
  • Peptides
  • Radiopharmaceuticals
  • gallium Ga 68 dotatate
  • Octreotide
  • Edotreotide