HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH RSS TABLE OF CONTENTS		QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:

This Article Figures Only Full Text Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Maecke, H. R. Articles by Haberkorn, U. Search for Related Content PubMed PubMed Citation Articles by Maecke, H. R. Articles by Haberkorn, U.

⁶⁸Ga-Labeled Peptides in Tumor Imaging

¹ Division of Radiological Chemistry, Department of Radiology, University Hospital Basel, Basel, Switzerland
² Department of Nuclear Medicine, Hannover Medical School, Hannover, Germany
³ Department of Nuclear Medicine, University of Heidelberg and Clinical Cooperation Unit Nuclear Medicine, German Cancer Research Center, Heidelberg, Germany

Radiolabeled peptides are of increasing interest in nuclear oncology. Special emphasis has been given to the development of peptides labeled with positron emitters. Among these, ⁶⁸Ga deserves special attention, because it is available from an inhouse generator rendering ⁶⁸Ga radiopharmacy independent of an onsite cyclotron. ⁶⁸Ga has a half-life of 68 min and decays by 89% through positron emission. The parent, ⁶⁸Ge, is accelerator produced and decays with a half-life of 270.8 d by electron capture. Currently, at least 1 commercial and several in-house generators are available. ⁶⁸Ge is strongly absorbed on metal oxides or organic material, making a ⁶⁸Ge-breakthrough highly unlikely. Several groups continue to further develop generators to remove cationic impurities from the eluate. Several bifunctional chelators based on 1,4,7-triazacyclononane-N,N',N''-triacetic acid and 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) macrocycles are available for coupling to peptides and other biomolecules. In addition to these hydrophilic chelators, a lipophilic tetradentate S₃N ligand was developed. Radiopeptides for ⁶⁸Ga labeling have been developed and tested preclinically for the targeting of somatostatin receptors, the melanocortin 1 receptor, and the bombesin receptor. Clinical studies were performed with ⁶⁸Ga-DOTA,Tyr³-octreotide, localizing neuroendocrine tumors with higher sensitivity than ¹¹¹In-diethylenetriaminepentaacetic acid-octreotide. In addition, ⁶⁸Ga-DOTA-based bombesin derivatives are being investigated with some success in patients with prostate cancer. Conclusion: Generator-produced ⁶⁸Ga and the development of small chelator-coupled peptides (and other small biomolecules) may open a new generation of freeze-dried, good manufacturing practice–produced, kit-formulated PET radiopharmaceuticals similar to ⁹⁹Mo-/^99mTc-generator–based, ^99mTc-labeled radiopharmaceuticals.

Key Words: oncology • ⁶⁸Ga • peptides • tumor imaging

This article has been cited by other articles:

				D. Putzer, M. Gabriel, B. Henninger, D. Kendler, C. Uprimny, G. Dobrozemsky, C. Decristoforo, R. J. Bale, W. Jaschke, and I. J. Virgolini Bone Metastases in Patients with Neuroendocrine Tumor: 68Ga-DOTA-Tyr3-Octreotide PET in Comparison to CT and Bone Scintigraphy J. Nucl. Med., August 1, 2009; 50(8): 1214 - 1221. [Abstract] [Full Text] [PDF]

				J. C. Reubi and H. R. Maecke Peptide-Based Probes for Cancer Imaging J. Nucl. Med., November 1, 2008; 49(11): 1735 - 1738. [Abstract] [Full Text] [PDF]

				P. T. Winnard Jr., A. P. Pathak, S. Dhara, S. Y. Cho, V. Raman, and M. G. Pomper Molecular Imaging of Metastatic Potential J. Nucl. Med., June 1, 2008; 49(Suppl_2): 96S - 112S. [Abstract] [Full Text] [PDF]

				O. Schillaci Somatostatin Receptor Imaging in Patients with Neuroendocrine Tumors: Not Only SPECT? J. Nucl. Med., April 1, 2007; 48(4): 498 - 500. [Full Text] [PDF]

				M. Cremonesi, M. Ferrari, L. Bodei, G. Tosi, and G. Paganelli Dosimetry in Peptide Radionuclide Receptor Therapy: A Review J. Nucl. Med., September 1, 2006; 47(9): 1467 - 1475. [Abstract] [Full Text] [PDF]

				L. E. Lantry, E. Cappelletti, M. E. Maddalena, J. S. Fox, W. Feng, J. Chen, R. Thomas, S. M. Eaton, N. J. Bogdan, T. Arunachalam, et al. 177Lu-AMBA: Synthesis and Characterization of a Selective 177Lu-Labeled GRP-R Agonist for Systemic Radiotherapy of Prostate Cancer J. Nucl. Med., July 1, 2006; 47(7): 1144 - 1152. [Abstract] [Full Text] [PDF]

				V. Tolmachev, F. Y. Nilsson, C. Widstrom, K. Andersson, D. Rosik, L. Gedda, A. Wennborg, and A. Orlova 111In-Benzyl-DTPA-ZHER2:342, an Affibody-Based Conjugate for In Vivo Imaging of HER2 Expression in Malignant Tumors J. Nucl. Med., May 1, 2006; 47(5): 846 - 853. [Abstract] [Full Text] [PDF]

				I. Velikyan, A. L. Sundberg, O. Lindhe, A. U. Hoglund, O. Eriksson, E. Werner, J. Carlsson, M. Bergstrom, B. Langstrom, and V. Tolmachev Preparation and Evaluation of 68Ga-DOTA-hEGF for Visualization of EGFR Expression in Malignant Tumors J. Nucl. Med., November 1, 2005; 46(11): 1881 - 1888. [Abstract] [Full Text] [PDF]

				E. P. Krenning, R. Valkema, D. J. Kwekkeboom, W. W. de Herder, C. H.J. van Eijck, M. de Jong, S. Pauwels, and J.-C. Reubi Molecular Imaging as In Vivo Molecular Pathology for Gastroenteropancreatic Neuroendocrine Tumors: Implications for Follow-Up After Therapy J. Nucl. Med., January 1, 2005; 46(1_suppl): 76S - 82S. [Abstract] [Full Text] [PDF]