PMID: 11340564May 8, 2001Paper

177Lu-DOTA(0),Tyr3] octreotate for somatostatin receptor-targeted radionuclide therapy

International Journal of Cancer. Journal International Du Cancer
M de JongE P Krenning

Abstract

Receptor-targeted scintigraphy using radiolabeled somatostatin analogs such as octreotate is being used with great success to demonstrate the in vivo presence of somatostatin receptors on various tumors. A new and promising application for these analogs is radionuclide therapy. Radionuclides suitable for this application include the Auger electron-emitter (111)In and the beta-emitters (90)Y (high energy) and (177)Lu (low energy). We investigated [DOTA(0),Tyr(3)]octreotate, labeled with the lanthanide (177)Lu, in biodistribution and radionuclide therapy experiments using male Lewis rats bearing the somatostatin receptor-positive rat CA20948 pancreatic tumor. Biodistribution studies in Lewis rats showed the highest uptake in the rat pancreatic CA20948 tumor and sst(2)-positive organs, which include the adrenals, pituitary and pancreas, of [(177)Lu-DOTA(0),Tyr(3)]octreotate in comparison with (88)Y- and (111)In-labeled analogs. Kidney uptake of [(177)Lu-DOTA(0),Tyr(3)]octreotate could be reduced by approximately 40% by co-injection of 400 mg/kg D-lysine. In radionuclide therapy studies, a 100% cure rate was achieved in the groups of rats bearing small (< or =1 cm(2)) CA20948 tumors after 2 doses of 277.5 MBq or after a single dose...Continue Reading

References

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Citations

Oct 18, 2002·Biopolymers·Sylvie Froidevaux, Alex N Eberle
Dec 18, 2001·International Journal of Cancer. Journal International Du Cancer·J S LewisC J Anderson
Mar 14, 2003·European Journal of Nuclear Medicine and Molecular Imaging·D J KwekkeboomE P Krenning
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