Abstract
ReO (4) (-) has similar kinetics regarding the sodium iodide symporter (NIS) to I- and TcO (4) (-) in NIS-expressing tissue. We investigated the therapeutic potential of (ReO)-Re-186 (4) (-) in NIS-transfected neuroendocrine tumour tissue. For experiments, the stably NIS-transfected pancreatic neuroendocrine cancer cell line Bon1C was used. NIS-mediated internalization and externalization ...
Abstract
ReO (4) (-) has similar kinetics regarding the sodium iodide symporter (NIS) to I- and TcO (4) (-) in NIS-expressing tissue. We investigated the therapeutic potential of (ReO)-Re-186 (4) (-) in NIS-transfected neuroendocrine tumour tissue. For experiments, the stably NIS-transfected pancreatic neuroendocrine cancer cell line Bon1C was used. NIS-mediated internalization and externalization experiments in vitro and a biodistribution study in nude mice bearing Bon1C xenografts were performed. A therapy study was also conducted consecutively in nude mice xenografted with Bon1C in which the mice were injected intravenously with (NaReO4)-Re-186. In vitro studies showed exponential internalization and efflux kinetics of (ReO)-Re-186 (4) (-) in the cell line. The biodistribution study showed high uptake of (ReO)-Re-186 (4) (-) in NIS-expressing tumours. Tumour growth inhibition was significant after injection of (ReO4)-Re-186 in two groups of animals treated with activity levels below the determined maximum tolerable activity as compared to controls. These results indicate that the use of (ReO)-Re-186 (4) (-) in the treatment of NIS-expressing neuroendocrine tumours is feasible and support the concept of using NIS as a therapeutic target for (ReO)-Re-186 (4) (-) .
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