| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
Experimental Therapeutics, Preclinical Pharmacology |
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, Missouri 63110 [J. S. L., M. R. L., P. D. C., S. W. S., M. M. M., C. J. A.]; Division of Biostatistics, Washington University School of Medicine, St. Louis, Missouri 63110 [J. P. M.]; and Mallinckrodt, Inc., Hazelwood, Missouri 63042 [A. S., M. A. S.]
64Cu [T1/2= 12.8 h; 
+ = 0.655 MeV (19%); - = 0.573 MeV (40%)] has shown promise as a radioisotope for targeted radiotherapy. It has been demonstrated previously that the somatostatin analogue 64Cu-TETA-octreotide (64Cu-TETA-OC, where TETA is 1,4,8,11-tetraazacyclotetradecane-N,N',N'',N'''-tetraacetic acid) significantly inhibited the growth of somatostatin receptor-positive CA20948 rat pancreatic tumors in Lewis rats (C. J. Anderson et al., J. Nucl. Med., 39: 1944–1951, 1998). In this study, we evaluated the radiotherapeutic efficacy of a new 64Cu-labeled somatostatin analogue, 64Cu-TETA-Tyr3-octreotate (64Cu-TETA-Y3-TATE), in CA20948 tumor-bearing rats. A single dose of 15 mCi (555 MBq) of 64Cu-TETA-Y3-TATE was shown to be more effective in reducing tumor burden than the same dose of 64Cu-TETA-OC. In multiple dose experiments, tumor-bearing rats were administered three doses of either 10 or 20 mCi (370 or 740 MBq) of 64Cu-TETA-Y3-TATE at 48-h intervals. Rats given 3 x 10 mCi (3 x 370 MBq) showed extended mean survival times compared with rats given a single dose; however, no complete regressions occurred. Complete regression of tumors was observed for all rats treated with 3 x 20 mCi (3 x 740 MBq), with no palpable tumors for 
10 days; moreover, the mean survival time of these rats was nearly twice that of controls. Toxicity was determined by physical appearance and hematological and enzyme analysis, which revealed no overt toxicity and only transient changes in blood and liver chemistry. Absorbed dose estimates showed the dose-limiting organ to be the kidneys. The radiotherapy results, along with absorbed dose estimates to target and clearance organs, confirm that 64Cu-labeled somatostatin analogues warrant continued consideration as agents for targeted radiotherapy.
This article has been cited by other articles:
|
|
 |
|
  M. Eiblmaier, R. Andrews, R. Laforest, B. E. Rogers, and C. J. Anderson Nuclear Uptake and Dosimetry of 64Cu-Labeled Chelator Somatostatin Conjugates in an SSTr2-Transfected Human Tumor Cell Line J. Nucl. Med., August 1, 2007; 48(8): 1390 - 1396. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
Y. Wu, X. Zhang, Z. Xiong, Z. Cheng, D. R. Fisher, S. Liu, S. S. Gambhir, and X. Chen microPET Imaging of Glioma Integrin {alpha}v{beta}3 Expression Using 64Cu-Labeled Tetrameric RGD Peptide J. Nucl. Med., October 1, 2005; 46(10): 1707 - 1718. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 Y. Miao, M. Hylarides, D. R. Fisher, T. Shelton, H. Moore, D. W. Wester, A. R. Fritzberg, C. T. Winkelmann, T. Hoffman, and T. P. Quinn Melanoma Therapy via Peptide-Targeted {alpha}-Radiation Clin. Cancer Res., August 1, 2005; 11(15): 5616 - 5621. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
Y. Miao, N. K. Owen, D. R. Fisher, T. J. Hoffman, and T. P. Quinn Therapeutic Efficacy of a 188Re-Labeled {alpha}-Melanocyte-Stimulating Hormone Peptide Analog in Murine and Human Melanoma-Bearing Mouse Models J. Nucl. Med., January 1, 2005; 46(1): 121 - 129. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
D. J. Buchsbaum, T. R. Chaudhuri, and K. R. Zinn Radiotargeted Gene Therapy J. Nucl. Med., January 1, 2005; 46(1_suppl): 179S - 186S. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. E. Sprague, Y. Peng, X. Sun, G. R. Weisman, E. H. Wong, S. Achilefu, and C. J. Anderson Preparation and Biological Evaluation of Copper-64-Labeled Tyr3-Octreotate Using a Cross-Bridged Macrocyclic Chelator Clin. Cancer Res., December 15, 2004; 10(24): 8674 - 8682. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Schmitt, P. Bernhardt, O. Nilsson, H. Ahlman, L. Kolby, H. R. Maecke, and E. Forssell-Aronsson Radiation Therapy of Small Cell Lung Cancer with 177Lu-DOTA-Tyr3-Octreotate in an Animal Model J. Nucl. Med., September 1, 2004; 45(9): 1542 - 1548. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. Schottelius, T. Poethko, M. Herz, J.-C. Reubi, H. Kessler, M. Schwaiger, and H.-J. Wester First 18F-Labeled Tracer Suitable for Routine Clinical Imaging of sst Receptor-Expressing Tumors Using Positron Emission Tomography Clin. Cancer Res., June 1, 2004; 10(11): 3593 - 3606. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. L. Aft, J. S. Lewis, F. Zhang, J. Kim, and M. J. Welch Enhancing Targeted Radiotherapy by Copper(II)diacetyl- bis(N4-methylthiosemicarbazone) Using 2-Deoxy-D-Glucose Cancer Res., September 1, 2003; 63(17): 5496 - 5504. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. R. Lewis, M. Wang, D. B. Axworthy, L. J. Theodore, R. W. Mallet, A. R. Fritzberg, M. J. Welch, and C. J. Anderson In Vivo Evaluation of Pretargeted 64Cu for Tumor Imaging and Therapy J. Nucl. Med., August 1, 2003; 44(8): 1284 - 1292. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. S. Lewis, J. M. Connett, J. R. Garbow, T. L. Buettner, Y. Fujibayashi, J. W. Fleshman, and M. J. Welch Copper-64-pyruvaldehyde-bis(N4-methylthiosemicarbazone) for the Prevention of Tumor Growth at Wound Sites following Laparoscopic Surgery: Monitoring Therapy Response with microPET and Magnetic Resonance Imaging Cancer Res., January 1, 2002; 62(2): 445 - 449. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. de Jong, W. A.P. Breeman, B. F. Bernard, W. H. Bakker, T. J. Visser, P. P.M. Kooij, A. van Gameren, and E. P. Krenning Tumor Response After [90Y-DOTA0,Tyr3]Octreotide Radionuclide Therapy in a Transplantable Rat Tumor Model Is Dependent on Tumor Size J. Nucl. Med., December 1, 2001; 42(12): 1841 - 1846. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
C. J. Anderson, F. Dehdashti, P. D. Cutler, S. W. Schwarz, R. Laforest, L. A. Bass, J. S. Lewis, and D. W. McCarthy 64Cu-TETA-Octreotide as a PET Imaging Agent for Patients with Neuroendocrine Tumors J. Nucl. Med., February 1, 2001; 42(2): 213 - 221. [Abstract] [Full Text]
|
|
|
|
 |
|
 J. S. Lewis, R. Laforest, T. L. Buettner, S.-K. Song, Y. Fujibayashi, J. M. Connett, and M. J. Welch Copper-64-diacetyl-bis(N4-methylthiosemicarbazone): An agent for radiotherapy PNAS, January 30, 2001; 98(3): 1206 - 1211. [Abstract] [Full Text] [PDF]
|
|
| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
| Cancer Research | Clinical Cancer Research |
| Cancer Epidemiology Biomarkers & Prevention | Molecular Cancer Therapeutics |
| Molecular Cancer Research | Cancer Prevention Research |
| Cancer Prevention Journals Portal | Cancer Reviews Online |
| Annual Meeting Education Book | Meeting Abstracts Online |
