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J Nucl Med. 2008; 49 (Supplement 1):292P
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Radiopharmaceutical Chemistry: New Chemistry-Oncology

New Chemistry-Oncology Posters

Development of 153Sm-HYNIC-angiostatin as an anti-cancer agent and its in vivo distribution

Joon-Kee Yoon1, Bok-Nam Park1, Ul Jae Park2, Sun-Ju Choi2, Bong-Hoi Choi1, Sun-Pyo Hong1, Young-Sil An1, Seok-Nam Yoon1 and Chul-Woo Joh1

1 Nuclear Medicine and Molecular Imaging, Ajou University, Suwon, South Korea; 2 Korea Atomic Energy Research Institute, Daejeon, South Korea

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Objectives: Samarium-153 (153Sm) has been widely used for bone pain palliation of various cancers. We developed 153Sm-labeled angiostatin as an anti-cancer agent and evaluated its biodistribution in small animals.

Methods: 153SmCl3 was produced by irradiation of 152Sm2O3 in a nuclear reactor, and incubated with 4 µCi HYNIC and 1 mg tricine. 153Sm-HYNIC was incubated with 32 µg angiostatin, and then loaded through PD-10 column. After calculation of labeling efficiency, 153Sm-HYNIC-angiostatin was injected to rats via tail vein (n=6, 2 mCi/rat). At 2, 24 and 48 hour, gamma camera images were acquired and each organ was removed for measurement of radioactivity.

Results: The labeling efficiency of 153Sm-HYNIC-angiostatin was 66%. Most of the injected radioactivity was delivered to the liver and kidney, which did not change until 48 hour (figure 1). Meanwhile, blood pool activity rapidly declined from 2 hour to 24 hour. After 24 hour, faint uptake on axial bones by free 153Sm was visualized. Radioactivities of heart, lung and muscle were minimal.

Conclusions: We successfully labeled 153Sm to angiostatin and evaluated its biodistribution. For use of 153Sm-HYNIC-angiostatin as an anti-cancer therapeutic agent, further pre-clinical and clinical evaluation are needed.

Research Support: This work was supported by Korea Science and Engineering Foundation (KOSEF) and Ministry of Science & Technology (MOST), Korean government, through its National Nuclear Technology Program (M20702000027-07B0200-02710).





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