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      Somatostatin receptor PET ligands - the next generation for clinical practice

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          Somatostatin receptors (SSTRs) are variably expressed by a variety of malignancies. Using radiolabeled somatostatin analogs (SSAs), the presence of SSTRs on tumor cells may be exploited for molecular imaging and for peptide receptor radionuclide therapy. 111In-DTPA-octreotide has long been the standard in SSTR scintigraphy. A major leap forward was the introduction of gallium-68 labeled SSAs for positron emission tomography (PET) offering improved sensitivity. Tracers currently in clinical use are 68Ga-DOTA-Tyr 3-octreotide ( 68Ga-DOTATOC), 68Ga-DOTA-Tyr 3-octreotate ( 68Ga-DOTATATE) and 68Ga-DOTA-1-NaI 3-octreotide ( 68Ga-DOTANOC), collectively referred to as 68Ga-DOTA-peptides. 68Ga-DOTA-peptide PET has superseded 111In-DTPA-octreotide scintigraphy as the modality of choice for SSTR imaging. However, implementation of 68Ga-DOTA-peptides in routine clinical practice is often limited by practical, economical and regulatory factors related to the use of the current generation of 68Ge/ 68Ga generators. Centralized production and distribution is challenging due to the low production yield and relatively short half-life of gallium-68. Furthermore, gallium-68 has a relatively long positron range, compromising spatial resolution on modern PET cameras. Therefore, possibilities of using other PET radionuclides are being explored. On the other hand, new developments in SSTR PET ligands are strongly driven by the need for improved lesion targeting, especially for tumors with low SSTR expression. This may be achieved by using peptide vectors having a higher affinity for the SSTR or a broader affinity profile for the different receptor subtypes or by using compounds recognizing more binding sites, such as SSTR antagonists. This review gives an overview of recent developments leading to the next generation of clinical PET tracers for SSTR imaging.

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          Author and article information

          Am J Nucl Med Mol Imaging
          Am J Nucl Med Mol Imaging
          American Journal of Nuclear Medicine and Molecular Imaging
          e-Century Publishing Corporation
          20 October 2018
          : 8
          : 5
          : 311-331
          [1 ] Nuclear Medicine, University Hospitals Leuven Leuven, Belgium
          [2 ] Nuclear Medicine and Molecular Imaging, Department of Imaging and Pathology, KU Leuven Leuven, Belgium
          [3 ] Radiopharmaceutical Research, Department of Pharmacy and Pharmacology, KU Leuven Leuven, Belgium
          Author notes
          Address correspondence to: Christophe M Deroose, Nuclear Medicine, University Hospitals Leuven, UZ Leuven, Campus Gasthuisberg, Nucleaire Geneeskunde, Herestraat 49, BE-3000 Leuven, Belgium. Tel: +32 16 34 37 15; Fax: +32 16 34 37 59; E-mail: christophe.deroose@ 123456uzleuven.be
          PMC6261874 PMC6261874 6261874
          AJNMMI Copyright © 2018
          Review Article


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