PMID: 11323245Apr 27, 2001Paper

Radiotherapeutic efficacy of (153)Sm-CMDTPA-Tyr(3)-octreotate in tumor-bearing rats

Nuclear Medicine and Biology
J E BugajA Srinivasan

Abstract

A number of radiolabeled somatostatin analogs have been evaluated in animal tumor models for radiotherapeutic efficacy. The majority of the agents tested have used either high-energy beta-emitters, such as Y-90 or Re-188, or the Auger electron-emitting radionuclide, In-111. Because a medium-energy beta-emitter might have equivalent efficacy compared to high-energy emitters, and lower toxicity to non-target tissues, we have evaluated the therapeutic potential of the beta-emitting nuclide, Sm-153, chelated to the somatostatin analog, CMDTPA-Tyr(3)-octreotate. Using an in vitro binding assay, this octreotate derivative was shown to have high affinity for the somatostatin subtype-2 receptor (IC(50) = 2.7 nM). Biodistribution studies in CA20948 tumor-bearing Lewis rats demonstrate that the Sm-153 labeled compound has high uptake and retention in tumor tissue (1.7% injected dose/g tissue, 4 hrs post injection) and has rapid overall clearance properties from non-target tissue. Radiotherapy studies were carried out using (153)Sm-CMDTPA-Tyr(3)-octreotate and CA20948 tumor bearing Lewis rats at 7 days post implant. Dose regimens consisting of single and multiple i.v. injections of 5.0 mCi/rat (185 MBq) were employed over a time span of 7...Continue Reading

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Citations

Dec 18, 2001·International Journal of Cancer. Journal International Du Cancer·J S LewisC J Anderson
May 21, 2005·Pharmaceutical Research·Ali AzhdariniaE Edmund Kim
Jan 27, 2004·Nuclear Medicine and Biology·Qin WangWalter Mier
Aug 3, 2004·Cancer Biotherapy & Radiopharmaceuticals·Suzanne VerwijnenMarion de Jong
Aug 22, 2006·Cancer Biotherapy & Radiopharmaceuticals·Ludger M Dinkelborg, Joseph E Bugaj
Aug 22, 2006·Cancer Biotherapy & Radiopharmaceuticals·Emad F AzizRüdiger Lawaczeck
May 11, 2012·Neuroendocrinology·Eva Forssell-AronssonHåkan Ahlman
Jun 3, 2009·Dalton Transactions : an International Journal of Inorganic Chemistry·Sara LacerdaIsabel Santos
Apr 20, 2005·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Dik J KwekkeboomEric P Krenning
Jun 13, 2009·Journal of Receptor and Signal Transduction Research·Alex N Eberle, Gabriele Mild

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