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Journal of Nuclear Medicine Vol. 48 No. 1 122-127
© 2007 by Society of Nuclear Medicine

Basic Science Investigation

Therapeutic Effects of a 186Re-Complex–Conjugated Bisphosphonate for the Palliation of Metastatic Bone Pain in an Animal Model

Kazuma Ogawa1,2, Takahiro Mukai1,3, Daigo Asano1, Hidekazu Kawashima1, Seigo Kinuya4, Kazuhiro Shiba2, Kazuyuki Hashimoto5, Hirofumi Mori2 and Hideo Saji1

1 Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan; 2 Division of Tracer Kinetics, Advanced Science Research Center, Kanazawa University, Kanazawa, Japan; 3 Department of Biomolecular Recognition Chemistry, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan; 4 Department of Biotracer Medicine, Graduate School of Medical Sciences, Kanazawa University, Kanazawa, Japan; and 5 Japan Atomic Energy Agency, Tokai-mura, Ibaraki, Japan

Correspondence: For correspondence or reprints contact: Hideo Saji, PhD, Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan. E-mail: hsaji{at}pharm.kyoto-u.ac.jp

Previously, based on the concept of bifunctional radiopharmaceuticals, we developed a highly stable 186Re-mercaptoacetylglycylglycylglycine (MAG3) complex–conjugated bisphosphonate, [[[[(4-hydroxy-4,4-diphosphonobutyl)carbamoylmethyl]carbamoylmethyl]carbamoylmethyl]carbamoylmethanethiolate] oxorhenium(V) (186Re-MAG3-HBP), for the treatment of painful bone metastases. This agent showed a superior biodistribution as a bone-seeking agent in normal mice when compared with 186Re-1-hydroxyethylidene-1,1-diphosphonate (186Re-HEDP). In this study, we evaluated the therapeutic effects of 186Re-MAG3-HBP using an animal model of bone metastasis. Methods: The model was prepared by injecting syngeneic MRMT-1 mammary tumor cells into the left tibia of female Sprague–Dawley rats. 186Re-MAG3-HBP (55.5, 111, or 222 MBq/kg) or 186Re-HEDP (55.5 MBq/kg) was then administered intravenously 21 d later. To evaluate the therapeutic effects and side effects, tumor size and peripheral blood cell counts were determined. Palliation of bone pain was evaluated by a von Frey filament test. Results: In the rats treated with 186Re-HEDP, tumor growth was comparable with that in untreated rats. In contrast, when 186Re-MAG3-HBP was administered, tumor growth was significantly inhibited. Allodynia induced by bone metastasis was attenuated by treatment with 186Re-MAG3-HBP or 186Re-HEDP, but 186Re-MAG3-HBP tended to be more effective. Conclusion: These results indicate that 186Re-MAG3-HBP could be useful as a therapeutic agent for the palliation of metastatic bone pain.

Key Words: bone metastases • internal radiotherapy • bisphosphonate • pain • radiopharmaceutical

COPYRIGHT © 2006 by the Society of Nuclear Medicine, Inc.


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