초록 ▼

1. 연구개발목표 및 내용
<연구목표>
o 악성 및 양성 질환 진단 및 치료용 신규 방사성 의약품 개발 및 실용화
o 방사성 표지화합물을 이용한 약제의 체내 치료 검증법 확립
o 항암제가 함유된 신규 방사성 복합의약품 개발
<연구내용>
o 관상동맥 재협착 치료용 $^{166}$Ho-DTPA filled balloon 및 $^{166)$Ho-coated balloon의 유효성 검증
o 내부 방사선 치료용 $^{166}$Ho-

1. 연구개발목표 및 내용
<연구목표>
o 악성 및 양성 질환 진단 및 치료용 신규 방사성 의약품 개발 및 실용화
o 방사성 표지화합물을 이용한 약제의 체내 치료 검증법 확립
o 항암제가 함유된 신규 방사성 복합의약품 개발
<연구내용>
o 관상동맥 재협착 치료용 $^{166}$Ho-DTPA filled balloon 및 $^{166)$Ho-coated balloon의 유효성 검증
o 내부 방사선 치료용 $^{166}$Ho-CHICO의 치료응용 확대 연구
o 담도 폐색 및 식도암 치료용 $^{166}$Ho-Stent의 유효성 검증
o 뇌질환 진단용 $^{99m}$Tc 표지화합물 개발
o 종양 진단용 $^{99m}$Tc 표지화합물 개발
o $^{166}$Ho 함유 근접 방사선 치료기구 실용화
o Neuro receptor 및 $\beta$-amyloid 관련 뇌질환 진단용 Tc-99m 표지화합물 개발
o $^{166}$Ho-CHICO를 이용한 난치성 질환의 치료응용 확대연구

Abstract ▼

Due to the rapid development of imaging technology, the researches in the area of developing the radiopharmaceuticals for the early detection and treatment of diseases have been in more demand. For example, $^{131}$I, $^{90}$Y and $^{188}$Re complex have been introdu

Due to the rapid development of imaging technology, the researches in the area of developing the radiopharmaceuticals for the early detection and treatment of diseases have been in more demand. For example, $^{131}$I, $^{90}$Y and $^{188}$Re complex have been introduced as a preferred agents for the liver cancer control. However, these radionuclides was reported the limited value for tumor necrosis because it is carried Passively by blood flow via the hepatic artery Therefore, normal tissue would be irradiated in the same way tumor itself causing undesirable damages. In 1994 KAERI developed Holmium-166 chitosan complex ($^{166}$Ho-CHICO). This radionuclide was thought to be a desirable agent for liver cancer because of it's physical characteristics with high beta energy (1.84 Mev), adequate half-life with 26.83 hr and a good maximum penetration depth of 83 mm of tissues. Therefore, it's application into other diseases was positively expected as a good candidate for the therapeutic agents.
- applications of $^{166}$Ho-CHICO as radiopharmaceuticals : For the application of $^{166}$Ho-CHICO in case of liver cancer, animal was injected intraarterially with $^{166}$Ho-CHICO prior to the clinical application to evaluate the biodistribution and effects in dog. A clinical study was also designed to evaluate the effects and complications of $^{166}$Ho-CHICO in the treatment of liver cancer on the base of the clinical research of "percutaneous injection of $^{166}$Ho-CHICO in the small liver cancer whose size is fess than 3 Cm and animal experiment of intervertebral injection of $^{166}$Ho-CHICO. The clinical trials of $^{166}$Ho-CHICO in the treatment of rheumatoid knee synovitis was carried out by characterization of VAS of knee pain on walking and on rest, circumference of knee at mid point of the patella, ROM of knee and VAS of pain on ROM of knee· In addition, each patient had anteroposterior radiography taken followed by classification according to the Steinbrocker criteria. Also extrarticular leakage of $^{166}$Ho-CHICO was determined by scintigraphic evaluation into liver, groin and knee joints.
- Investigation of clinical application of newly developed $^{166}$Ho-CHICO
Patch : A radioactive patch containing holmium-166 was developed for a skin cancer treatment. And the other applications of $^{166}$Ho-CHICO to various types of skin diseases were also studied using skin cancer animal model. Further study related to $^{166}$Ho-CHICO Patch were investigated using Raman Spectrum for the process of changes in tissues of skin cancer which was irradiated by $^{166}$Ho (beta source). This study was carried out to develop the diagnostic method for the skin cancer especially in early phase of cancer
- Development of radioactive medical devices, $^{166}$Ho-stent and balloon, and clinical trials : Self-expandable metallic stents are widely used for palliative treatment of esophageal cancer, however, tumor overgrowth and short survival limit its long term effects. The purpose of the study was to evaluate tissue response of self-expandable metallic stent covered $^{166}$Ho in normal canine esophagus. Fluoroscopy was used for the confirmation of stents in esophagus without migration for two days. To develop a $^{166}$Ho liquid/coated balloon for occlusive coronary artery diseases, the effects of $^{166}$Ho on endovascular therapy for the prevention of restenosis after PTCA(percutaneous transluminal coronary angioplasty) or stenting for occlusive coronary artery disease were evaluated using angioplasty.
- Development of radiopharmaceuticals using $^{153}$Sm, $^{188}$Re and $^{99m}$Tc : To over come the limitations on application of $^{166}$Ho due to its short half life, $^{153}$Sm-CHICO developed and $^{188}$Re, well known as a cost-effective radionuclide, and its effects on pain perceptions were evaluated on metastatic bone cancer animal model using nude mouse. Further investigation was made to develop the radioisotope labelled compound serotonin neuroreceptor imaging agent which might be useful for the diagnosis of brain diseases For the study Arylpiperazine derivatives were synthesized followed by labelling with $^{99m}$Tc. And its diagnostic functions were studied using gamma camera on rabbit.

목차 Contents

• 제1장 연구개발과제의 개요...49
• 제2장 국내.외 기술개발 현황...52
• 제3장 연구개발 수행내용 및 결과...55
• 제1절 관상동맥 제협착 치료용 166Ho-DTPA filled balloon 및 166Ho-coated balloon의 유효성 검증...55
• 제2절 내부 방사선 치료용 166Ho-CHICO의 치료응용 확대 연구...104
• 제3절 담도 폐색 및 식도암 치료용 166Ho-Stent의 유효성 검증...160
• 제4절 뇌질환 진단용 99mTc 표지화합물 개발...167
• 제5절 종양 진단용 99mTc 표지화합물 개발...217
• 제4장 연구개발 목표 달성도 및 관련 분야에의 기여도...291
• 제5장 연구개발결과의 활용계획...298
• 제6장 연구개발과정에서 수집한 해외 과학기술정보...301