Production of ィイD1105ィエD1Rh and application of this nuclide to therapeutic radiopharmaceuticals
| Project/Area Number |
10670833
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 一般 |
|---|
| Research Field |
Radiation science
|
|---|
| Research Institution | Kanazawa University |
|---|
Principal Investigator |
ANDO Atsushi Faculty of Medicine, Kanazawa University Professor, 医学部, 教授 (50019915)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
ONOGUCHI Masahisa Faculty of Medicine, Kanazawa University Assistant, 医学部, 助手 (30283120)
OISHI Shigeo Faculty of Medicine, Kanazawa University Assistant, 医学部, 助手 (30272983)
|
|---|
| Project Period (FY) |
1998 – 1999
|
| Project Status |
Completed (Fiscal Year 1999)
|
| Budget Amount *help |
¥2,000,000 (Direct Cost: ¥2,000,000)
Fiscal Year 1999: ¥900,000 (Direct Cost: ¥900,000)
Fiscal Year 1998: ¥1,100,000 (Direct Cost: ¥1,100,000)
|
|---|
| Keywords | Radiotherapeutic nuclide / Rhodium-105 / EDTMP / Rh-105-EDTMP / Bone metastases / 疼痛緩和剤 / 治療用放射性医薬品 / ^<105>Rh / ブレオマイシン / ^<105>Rh-ブレオマイシン |
|---|
| Research Abstract |
Rhodium-105(ィイD1105ィエD1Rh) has favorable physical characteristics as a radiotherapeutic nuclide. Carrier-free ィイD1105ィエD1Rh can be produced by the neutron activation of ィイD1104ィエD1Ru followed by beta decay of ィイD1105ィエD1Ru. It was clarified that carrier-free ィイD1105ィエD1Rh can be produced in quantities and the purity necessary for chemical and clinical investigations of its use as a nuclide for radiotherapy.
ィイD157ィエD1Co-bleomycin is selectively accumulated in some cancer. However, the long half-life of ィイD157ィエD1Co(270 days) poses contamination problems which preclude its widespread clinical use. Kono suggested from the similarity of chemical property between cobalt and rhodium and from the in vitro study that Rh-bleomycin would have tumor affinity. Bleomycin-hydrochloride was added the solution of ィイD1105ィエD1Rh(II) and heated for 5 min in boiling water. ィイD1105ィエD1Rh-bleomycin(BLM) was separated from the reaction mixture by thin-layer chromatography on silica gel plate using the solvent system, MeOH : 10% CHィイD23ィエD2COONHィイD24ィエD2 in HィイD22ィエD20(1:1). Tumor affinity of ィイD1105ィエD1Rh-BLM was examined with Ehrlich tumor-bearing mice. In this experiment, ィイD1105ィエD1Rh-BLM did not accumulated in tumor tissue.
On the other hand, we produced ィイD1105ィエD1Rh-EDTMP for therapeutic bone agent. ィイD1105ィエD1Rh-EDTMP was simply obtained from ィイD1105ィエD1RhィイD13+ィエD1 and EDTMP by heating for 30 min in boiling water, giving a radiochemical yield of > 99 %. Dissociation of radioactivity assessed by paperchromatography was negligible for up to 5 days after its preparation. In animals, ィイD1105ィエD1Rh-EDTMP showed rapid blood clearance and selective uptake in the bone.
Hence, ィイD1105ィエD1Rh-EDTMP is thought to be a promising therapeutic agent for the treatment of pain due to bone metastases.
|
Report
(3 results)
Research Products
(3 results)
