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Journal Articles

Production and synthesis of a novel $$^{191}$$Pt-labeled platinum complex and evaluation of its biodistribution in healthy mice

Omokawa, Marina*; Kimura, Hiroyuki*; Hatsukawa, Yuichi*; Kawashima, Hidekazu*; Tsukada, Kazuaki; Yagi, Yusuke*; Naito, Yuki*; Yasui, Hiroyuki*

Bioorganic & Medicinal Chemistry, 97, p.117557_1 - 117557_6, 2024/01

https://doi.org/10.1016/j.bmc.2023.117557
 Times Cited Count：0 Percentile：0.01(Biochemistry & Molecular Biology)

Journal Articles

Preparation and evaluation of $$^{186/188}$$Re-labeled antibody (A7) for radioimmunotherapy with rhenium(I) tricarbonyl core as a chelate site

Ogawa, Kazuma*; Kawashima, Hidekazu*; Kinuya, Seigo*; Shiba, Kazuhiro*; Onoguchi, Masahisa*; Kimura, Hiroyuki*; Hashimoto, Kazuyuki; Odani, Akira*; Saji, Hideo*

Annals of Nuclear Medicine, 23(10), p.843 - 848, 2009/12

https://doi.org/10.1007/s12149-009-0319-4
 Times Cited Count：9 Percentile：31.33(Radiology, Nuclear Medicine & Medical Imaging)

Rhenium is one of the most valuable elements for internal radiotherapy because $$^{186/188}$$Re have favorable physical characteristics. However, there are problems when proteins such as antibodies are used as carriers of $$^{186/188}$$Re. Labeling methods require the complicated processes. Therefore, we planned the preparation by a simple method and evaluation of a stable $$^{186/188}$$Re-labeled antibody. For this purpose, we selected $$^{186/188}$$Re(I) tricarbonyl complex as a chelating site. A7 was used as a model protein. $$^{186/188}$$Re-labeled A7 was prepared by directly reacting a $$^{186/188}$$Re(I) tricarbonyl precursor with A7. $$^{186/188}$$Re-(CO)$$_{3}$$-A7 were prepared with radiochemical yields of 23-28%. After purification, $$^{186/188}$$Re-(CO)$$_{3}$$-A7 showed a radiochemical purity of over 95%. In biodistribution experiments, $$^{186/188}$$Re-labeled A7 showed high uptakes in the tumor.

Journal Articles

Therapeutic effects of a $$^{186}$$Re-complex-conjugated bisphosphonate for the palliation of metastatic bone pain in an animal model

Ogawa, Kazuma*; Mukai, Takahiro*; Asano, Daigo*; Kawashima, Hidekazu*; Kinuya, Seigo*; Shiba, Kazuhiro*; Hashimoto, Kazuyuki; Mori, Hirofumi*; Saji, Hideo*

Journal of Nuclear Medicine, 48(1), p.122 - 127, 2007/01

We developed a highly stable rhenium-186 ($$^{186}$$Re)-MAG3 complex-conjugated bisphosphonate, ($$^{186}$$Re-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 $$^{186}$$Re-HEDP. In this study, we evaluated the therapeutic effects of $$^{186}$$Re-MAG3-HBP using an animal model of bone metastasis. In the rats treated with $$^{186}$$Re-HEDP, tumor growth was comparable to that in untreated rats. In contrast, when $$^{186}$$Re-MAG3-HBP was administered, tumor growth was significantly inhibited. Allodynia induced by bone metastasis was attenuated by treatment with $$^{186}$$Re-MAG3-HBP or $$^{186}$$Re-HEDP, but $$^{186}$$Re-MAG3-HBP tended to be more effective. These results indicate that $$^{186}$$Re-MAG3-HBP could be useful as a therapeutic agent for the palliation of metastatic bone pain.

Oral presentation

Therapeutic effects of a new $$^{186}$$Re-labeled bisphosphonate in a rat model of bone metastasis

Ogawa, Kazuma*; Mukai, Takahiro*; Asano, Daigo*; Kawashima, Hidekazu*; Hashimoto, Kazuyuki; Shiba, Kazuhiro*; Mori, Hirofumi*; Saji, Hideo*

no journal, , 

no abstracts in English

Oral presentation

Preparation of $$^{188}$$Re-labeled antibody (A7) by a simple method using rhenium(I) tricarbonyl complex

Ogawa, Kazuma*; Kawashima, Hidekazu*; Kinuya, Seigo*; Yoshimoto, Mitsuyoshi*; Shiba, Kazuhiro*; Kimura, Hiroyuki*; Hashimoto, Kazuyuki; Mori, Hirofumi*; Saji, Hideo*

no journal, , 

$$^{188}$$Re is one of the most useful radionuclides for internal radiotherapy. However, there is a problem when protein such as antibody is used as a carrier of $$^{188}$$Re. The labeling method using bifunctional chelating agents require the conjugation of $$^{188}$$Re-complex to protein after radiolabeling with the bifunctional chelating agent. Then, we planned the preparation of a stable $$^{188}$$Re-labeled protein by a simple method. A7 monoclonal antibody was labeled by reacting $$^{188}$$Re(I) tricarbonyl precursor with A7 directly. $$^{188}$$Re labeled A7 was prepared with radiochemical yield of 23%. After purification, $$^{188}$$Re labeled A7 showed radiochemical purity over 98%. After 24 hours of incubation, about 93% of $$^{188}$$Re-A7 remained intact, which indicates $$^{188}$$Re-A7 is stable in vitro. In biodistribution experiment, 11.2% of the injected dose/g of $$^{188}$$Re-A7 accumulated in the tumor at 24 hours postinjection, and tumor to blood ratio was over 1.0 at the same time.

Oral presentation

Synthesis and evaluation of $$^{186}$$Re-labeled biotin as a labeling agent for antibodies

Hirasawa, Makoto*; Kawashima, Hidekazu*; Ogawa, Kazuma*; Kimura, Hiroyuki*; Ono, Masahiro*; Hashimoto, Kazuyuki; Saji, Hideo*

no journal, , 

no abstracts in English

Oral presentation

Pretargeted radioimmunotherapy of tumor using a novel radiorhenium-labeled biotin derivative and streptavidin conjugated anti-cytokeratin 19 monoclonal antibody

Kawashima, Hidekazu*; Hirasawa, Makoto*; Kimura, Hiroyuki*; Ono, Masahiro*; Hashimoto, Kazuyuki; Saji, Hideo*

no journal, , 

no abstracts in English

7 (Records 1-7 displayed on this page)
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