Journal of Nuclear Medicine | |
Therapeutic Effects of a 186Re-Complex–Conjugated Bisphosphonate for the Palliation of Metastatic Bone Pain in an Animal Model | |
Daigo Asano1  Kazuma Ogawa1  Seigo Kinuya1  Hideo Saji1  Kazuyuki Hashimoto1  Kazuhiro Shiba1  Hidekazu Kawashima1  Hirofumi Mori1  Takahiro Mukai1  | |
关键词: bone metastases; internal radiotherapy; bisphosphonate; pain; radiopharmaceutical; | |
DOI : | |
学科分类:医学(综合) | |
来源: Society of Nuclear Medicine | |
【 摘 要 】
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.
【 授权许可】
Unknown
【 预 览 】
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