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J Nucl Med. 2008; 49 (Supplement 1):294P
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Radiopharmaceutical Chemistry: New Chemistry-Oncology

New Chemistry-Oncology Posters

99mTc(CO)3 Labeled ErbB-2 avid peptides for breast cancer imaging

H. Balter1, P. Cabral1, Jp. Gambini1, V. Trindade1, M. Fernandez1, V. Calzada1, M. Tassano1, X. Zhang2, S. Deutscher2 and Thomas Quinn2

1 Nuclear Research Center, Univ of the Republica, Montevideo, Uruguay; 2 Univ of Missouri, Columbia, Missouri

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Objectives: The erbB-2 avid peptide KCCYSL was radiolabeled using two 99mTc(CO)3 approaches and examined for radiolabeling efficiency and radiochemical stability and for its biodistribution and imaging properties in normal and tumor bearing rodents.

Methods: The synthesis of 99mTc(CO)3-DAP-GSG-KCCYSL and 99mTc(CO)3-Hys(Ac)-GSG-KCCYSL was performed by the addition of 100 ug of the respective peptide into 0.8 mL of neutralized [99mTc(CO)3(H2O)3]+ produced from an IsoLink kit and incubated 1h at 75 C. Characterization of labeled peptides were performed on a C18 column using a 0.05 M TEAP (pH 2):Methanol gradient. Biodistribution studies were carried out in normal mice. Scintigraphy was performed in rats bearing N-nitroso-N-methylurea (NMU) induced mammary tumors and also in mice with spontaneous adenocarcinoma.

Results: Radiochemical purity was greater than 92% for 99mTc-DAP-GSG-KCCYSL and 99% for and 99mTc(CO)3-Hys(Ac)-GSG-KCCYSL with a excellent stability up to 6 hours. Biodistribution profiles showed uptake of 99mTc(CO)3-DAP-GSG-KCCYSL in liver 9.02±2.01% ID/g, kidneys 9.77±6.36% ID/g and intestines 3.02±0.23% ID/g, with urinary excretion of 46.38±11.38% ID at 2 h post injection, while 99mTc(CO)3-Hys(Ac)-GSG-KCCYSL exhibited uptake in liver 3.26±1.12% ID/g, kidneys 2.35±0.47% ID/g, intestines 7.74±1.82% ID/g and 72.74±6.68% ID excreted in the urine. NMU induced mammary tumors in rats and spontaneous adenocarcinoma tumors in mice were visualized with scintigraphy using both 99mTc-tricarbonyl labeled peptides.

Conclusions: Rapid whole body clearance coupled with selective tumor imaging highlight the potential of the 99mTc(CO)3-erbB-2 avid peptides for breast cancer imaging.

Research Support: CSIC, IAEA, PEDECIBA, P50 CA103130 Mallinckrodt Tyco (IsoLink kits)





This Article
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Right arrow Articles by Quinn, T.