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JAEA Reports

Radiation monitoring using manned helicopter around the Nuclear Power Station in the fiscal year 2020 (Contract research)

Futemma, Akira; Sanada, Yukihisa; Ishizaki, Azusa; Kawasaki, Yoshiharu*; Iwai, Takeyuki*; Hiraga, Shogo*; Sato, Kazuhiko*; Haginoya, Masashi*; Matsunaga, Yuki*; Kikuchi, Hikaru*; et al.

JAEA-Technology 2021-029, 132 Pages, 2022/02

JAEA-Technology-2021-029.pdf:24.58MB

By the nuclear disaster of Fukushima Daiichi Nuclear Power Station (FDNPS), Tokyo Electric Power Company (TEPCO), caused by the Great East Japan Earthquake and the following tsunami on March 11, 2011, a large amount of radioactive material was released from the FDNPS. After the nuclear disaster, airborne radiation monitoring using manned helicopter has been conducted around FDNPS. The results of the airborne radiation monitoring and the evaluation for temporal change of dose rate in the fiscal 2020 were summarized in this report. Analysis considering topographical effects was applied to the result of the airborne monitoring to improve the accuracy of conventional method. In addition, technique for discriminating gamma rays from the ground and those from the airborne Rn-progenies was also utilized to evaluate their effect on airborne radiation monitoring.

Journal Articles

Preparation and evaluation of an astatine-211-labeled sigma receptor ligand for $$alpha$$ radionuclide therapy

Ogawa, Kazuma*; Mizuno, Yoshiaki*; Washiyama, Koshin*; Shiba, Kazuhiro*; Takahashi, Naruto*; Kozaka, Takashi*; Watanabe, Shigeki; Shinohara, Atsushi*; Odani, Akira*

Nuclear Medicine and Biology, 42(11), p.875 - 879, 2015/11

 Times Cited Count:18 Percentile:69.85(Radiology, Nuclear Medicine & Medical Imaging)

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

 Times Cited Count:9 Percentile:33.73(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

Usefulness of competitive inhibitors of protein binding for improving the pharmacokinetics of $$^{186}$$Re-MAG3-conjugated bisphosphonate ($$^{186}$$Re-MAG3-HBP), an agent for treatment of painful bone metastases

Ogawa, Kazuma*; Mukai, Takahiro*; Kawai, Keiichi*; Takamura, Norito*; Hanaoka, Hirofumi*; Hashimoto, Kazuyuki; Shiba, Kazuhiro*; Mori, Hirofumi*; Saji, Hideo*

European Journal of Nuclear Medicine and Molecular Imaging, 36(1), p.115 - 121, 2009/01

 Times Cited Count:19 Percentile:55.39(Radiology, Nuclear Medicine & Medical Imaging)

We have developed a $$^{186}$$Re-MAG3 complex-conjugated bisphosphonate ($$^{186}$$Re-MAG3-HBP) for the treatment of painful bone metastases. We assumed competitive inhibitors of protein binding to be useful for procuring a favorable biodistribution of $$^{186}$$Re-MAG3-HBP because it has been reported that the concurrent administration of $$^{rm 99m}$$Tc-MAG3 and drugs with high affinity for serum protein enhanced total clearance and tissue distribution. The protein binding of $$^{186}$$Re-MAG3-HBP in a human serum albumin solution was significantly decreased by the addition of ceftriaxone. In the biodistribution experiments, pretreatment with ceftriaxone enhanced the clearance of the radioactivity of $$^{186}$$Re-MAG3-HBP in blood and nontarget tissues but had no effect on accumulation in bone. The findings suggested that the use of protein-binding competitive inhibitors would be effective in improving the pharmacokinetics of radiopharmaceuticals with high affinity for serum protein.

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.

Journal Articles

Assessment of $$^{186}$$Re chelate-conjugated bisphosphonate for the development of new radiopharmaceuticals for bones

Uehara, Tomoya*; Jin, Z. L.*; Ogawa, Kazuma*; Akizawa, Hiromichi*; Hashimoto, Kazuyuki; Nakayama, Morio*; Arano, Yasushi*

Nuclear Medicine and Biology, 34(1), p.79 - 87, 2007/01

 Times Cited Count:23 Percentile:59.1(Radiology, Nuclear Medicine & Medical Imaging)

In this study, a key factor affecting the pharmacokinetics of a chelate-conjugated BP was investigated to estimate the validity and the applicability of molecular design. Chemically inert and well-characterized [$$^{186}$$Re]CpTR-Gly was conjugated with 3-amino-1-hydroxypropylidene-1,1-bisphosphonate and purified by HPLC to prepare [$$^{186}$$Re]CpTR-Gly-APD. Plasma stability, plasma protein binding, hydroxyapatite (HA) binding and the pharmacokinetics of [$$^{186}$$Re]CpTR-Gly-APD were compared with those of $$^{186}$$Re 1-hydroxyethylidene-1,1-diphosphonate (HEDP). The HPLC-purified [$$^{186}$$Re]CpTR-Gly-APD showed higher plasma stability, higher HA binding, higher bone accumulation and lower plasma protein binding than did $$^{186}$$Re -HEDP. Although $$^{186}$$Re -HEDP possessed HA binding and bone accumulation similar to those of [$$^{186}$$Re]CpTR-Gly-APD, the specific activity of $$^{186}$$Re -labeled BPs was found to play a crucial role in bone accumulation and blood clearance. Thus, the molecular design of chelate-conjugated BP would be useful for the development of bone-seeking radiopharmaceuticals with a variety of radionuclides by selecting chelating molecules that provide high specific activities.

Journal Articles

Rhemium-186-monoaminemonoamidedithiol-conjugated bisphosphonate derivatives for bone pain palliation

Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Otaka, Akira*; Ueda, Masashi*; Uehara, Tomoya*; Magata, Yasuhiro*; Hashimoto, Kazuyuki; Saji, Hideo*

Nuclear Medicine and Biology, 33(4), p.513 - 520, 2006/05

 Times Cited Count:51 Percentile:80.77(Radiology, Nuclear Medicine & Medical Imaging)

To develop a radiopharmaceutical for the palliation of painful bone metastases based on the concept of bifunctional radiopharmaceuticals, we synthesized a bisphosphonate derivative labeled with rhenium-186 ($$^{186}$$Re) that contains a hydroxyl group at the central carbon of its bisphosphonate structure and attached a stable $$^{186}$$Re-MAMA chelate to the amino group of a 4-amino-butylidene-bisphosphonate derivative, $$^{186}$$Re-MAMA-HBP, and investigated the effect of a hydroxyl group at the central carbon of its bisphosphonate structure on the affinity for hydroxyapatite and biodistribution by conducting a comparative study with $$^{186}$$Re-MAMA-BP. $$^{186}$$Re-MAMA-HBP was prepared by a reaction with $$^{186}$$ReO$$_{4}$$$$^{-}$$ and SnCl$$_{2}$$ in citrate buffer after the deprotection of trityl groups of Tr-MAMA-HBP. After reversed phase HPLC, $$^{186}$$Re-MAMA-HBP had a radiochemical purity of over 95 %. Compared with $$^{186}$$Re-MAMA-BP, $$^{186}$$Re-MAMA-HBP showed a greater affinity for hydroxyapatite beads in vitro and accumulated a significantly higher level in the femur in vivo. Thus, the introduction of a hydroxyl group into $$^{186}$$Re complex-conjugated bisphosphonates would be effective in enhancing accumulation in bone. These findings provide useful information on the design of bone-seeking therapeutic radiopharmaceuticals.

Journal Articles

Development of a Rhenium-186-labeled MAG3-conjugated bisphosphonate for the palliation of metastatic bone pain based on the concept of bifunctional radiopharmaceuticals

Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Ono, Masahiro*; Hanaoka, Hirofumi*; Ishino, Seigo*; Hashimoto, Kazuyuki; Nishimura, Hiroshi*; Saji, Hideo*

Bioconjugate Chemistry, 16(4), p.751 - 757, 2005/07

 Times Cited Count:59 Percentile:87.42(Biochemical Research Methods)

Rhenium-186-1-hydroxyethylidene-1,1-diphosphonate ($$^{186}$$Re-HEDP) has been used for the palliation of metastatic bone pain. Delayed blood clearance and high gastric uptake of radioactivity have been observed upon injection, due to the instability of $$^{186}$$Re-HEDP in vivo. In this study, on the basis of the concept of bifunctional radiopharmaceuticals, we designed a stable $$^{186}$$Re-mercaptoacetylglycylglycylglycine (MAG3) complex-conjugated bisphosphonate ($$^{186}$$Re-MAG3-HBP). After purification by HPLC, $$^{186}$$Re-MAG3-HBP was synthesized with a radiochemical purity of over 95%. In biodistribution experiments, the radioactivity level of$$^{186}$$Re-MAG3-HBP in bone was significantly higher than that of $$^{186}$$Re-HEDP. Blood clearance of $$^{186}$$Re-MAG3-HBP was faster than that of $$^{186}$$Re-HEDP. In addition, the gastric accumulation of $$^{186}$$Re-MAG3-HBP radioactivity was lower than that of $$^{186}$$Re-HEDP. In conclusion, $$^{186}$$Re-MAG3-HBP is expected to be a useful radiopharmaceutical for the palliation of metastatic bone pain.

Journal Articles

Design of a radiopharmaceutical for the palliation of painful bone metastases; Rhenium-186-labeled bisphosphonate derivative

Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Hanaoka, Hirofumi*; Hashimoto, Kazuyuki; Nishimura, Hiroshi*; Saji, Hideo*

Journal of Labelled Compounds and Radiopharmaceuticals, 47(11), p.753 - 761, 2004/11

 Times Cited Count:27 Percentile:62.35(Biochemical Research Methods)

no abstracts in English

Journal Articles

Synthesis and evaluation of bisphosphonate derivative labeled with Rhenium-186 using monoaminemonoamidedithiols as a chelating group

Mukai, Takahiro*; Ogawa, Kazuma*; Arano, Yasushi*; Ono, Masahiro*; Fujioka, Yasushi*; Izumo, Mishiroku; Konishi, Junji*; Saji, Hideo*

Journal of Labelled Compounds and Radiopharmaceuticals, 44(Suppl.1), p.S617 - S618, 2001/05

no abstracts in English

Journal Articles

Labeling with radioactive rhenium for the purpose of the pain relief of cancerous bone metastasis

Ogawa, Kazuma*; Ono, Masahiro*; Fujioka, Yasushi*; Saji, Hideo*; Mukai, Takahiro*; Konishi, Junji*; Uehara, Tomoya*; Arano, Yasushi*; Onoma, Katsuyuki

Kaku Igaku, 37(5), P. 577, 2000/09

no abstracts in English

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

Control of biodistribution of Rhenium-186-MAG3-conjugated bisphosphonate using a competitive inhibitor of protein binding

Ogawa, Kazuma*; Mukai, Takahiro*; Kawai, Keiichi*; Takamura, Norito*; Hanaoka, Hirofumi*; Hashimoto, Kazuyuki; Saji, Hideo*

no journal, , 

Previously, based on the concept of bifunctional radiopharmaceuticals, we developed a highly stable$$^{186}$$Re-MAG3 complex conjugated bisphosphonate ($$^{186}$$Re-MAG3-HBP) for treatment of the painful bone metastases. We assumed that competitive inhibitors of protein binding might be useful for$$^{186}$$Re-MAG3-HBP because it has been reported that the concurrent administration between $$^{99m}$$Tc-MAG3 and drugs with high protein binding affinity produced competitive displacement at the specific binding sites and enhanced total clearance and tissue distribution. In this study, the displacement effect between $$^{186}$$Re-MAG3-HBP and several protein binding inhibitors were investigated. Effects of each competitive protein binding inhibitor were examined in in vitro human serum. Bucolome, ceftriaxione and cefazolin as displacers of human serum albumin (HSA) binding site I, and ibuprofen as a displacer of HSA binding site II were added to each serum before addition of $$^{186}$$Re-MAG3-HBP. As a result of in vitro study, the free fraction rate of $$^{186}$$Re-MAG3-HBP was significantly increased by the addition of ceftriaxone. In biodistribution studies, the loading ceftriaxone enhanced the clearance of radioactivity of $$^{186}$$Re-MAG3-HBP in blood and non-target tissues without the reduction of the bone accumulation. These findings suggested that the use of a protein binding competitive inhibitor would be effective for lowering the side effects of $$^{186}$$Re-MAG3-HBP.

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

15 (Records 1-15 displayed on this page)
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