177Lu-DOTA-lanreotide: a novel tracer as a targeted agent for tumor therapy

Nuclear Medicine and Biology
Sharmila BanerjeeM R A Pillai

Abstract

177Lu of specific activity approximately 100-110 TBq/g and radionuclidic purity of approximately 100% was obtained by irradiation of enriched Lu2O3 (60.6% 176Lu) target for 7 days at a thermal neutron flux of 3 x 10(13)n/cm2/sec. The 177Lu labeling of a macrocyclic bifunctional chelating agent viz. 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) has been extensively studied. Lanreotide, [beta-naphthyl-Ala-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2] a disulfide-linked cyclic octapeptide and a somatostatin analog, reported to bind with a wide variety of tumors expressing somatostatin receptors, was conjugated with DOTA. The peptide-BFCA conjugate was characterized with the help of high-resolution two-dimensional proton NMR spectroscopy. The 177Lu labeling of the DOTA-lanreotide conjugate has been standardized to give a radiolabeling yield of 85%. The tracer showed specific binding with A-431 human epidermoid carcinoma and IMR-32 human brain neuroblastoma cells.

References

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Citations

Feb 17, 2006·Cancer Biotherapy & Radiopharmaceuticals·Subhani M Okarvi, Ibrahim A Jammaz
Dec 5, 2015·Expert Opinion on Pharmacotherapy·Muhammad Wasif Saif
Nov 18, 2006·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Tapas DasMeera Venkatesh
Jul 26, 2006·Dalton Transactions : an International Journal of Inorganic Chemistry·Thomas A Kaden
Mar 31, 2005·Chemistry : a European Journal·Andrei LeonovChristian Griesinger
Jun 3, 2009·Dalton Transactions : an International Journal of Inorganic Chemistry·Sara LacerdaIsabel Santos

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