68Ga-labeled DOTA-Peptides and 68Ga-labeled Radiopharmaceuticals for Positron Emission Tomography: Current Status of Research, Clinical Applications, and Future Perspectives

In this review we give an overview of current knowledge of Ga-68-labeled pharmaceuticals, with focus on imaging receptor-mediated processes. A major advantage of a Ge-68/Ga-68 generator is its continuous source of Ga-68, 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 Ga-68-labeled pharmaceuticals with major clinical impact. Ga-68-labeled pharmaceuticals have the potential to cover all today's clinical options with Tc-99m, with the concordant higher resolution of positron emission tomography (PET) in comparison with single photon emission computed tomography. Ga-68-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 Ga-68-labeled pharmaceuticals. All the above-mentioned items in favor of successful application of Ga-68-labeled radiopharmaceuticals for imaging in patients are strong arguments for the development of a Ge-68/Ga-68 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 Ga-68-radiopharmaceutical is available. As soon as these are achieved, a whole new radiopharmacy providing PET radiopharmaceuticals might develop. Semin Nucl Med 41:314-321 (C) 2011 Elsevier Inc. All rights reserved.