• 제목/요약/키워드: e-Clinical Trials

검색결과 152건 처리시간 0.03초

Enhancement of radiation effect using beta-lapachone and underlying mechanism

  • Ahn, Ki Jung;Lee, Hyung Sik;Bai, Se Kyung;Song, Chang Won
    • Radiation Oncology Journal
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    • 제31권2호
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    • pp.57-65
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    • 2013
  • Beta-lapachone (${\beta}$-Lap; 3,4-dihydro-2, 2-dimethyl-2H-naphthol[1, 2-b]pyran-5,6-dione) is a novel anti-cancer drug under phase I/II clinical trials. ${\beta}$-Lap has been demonstrated to cause apoptotic and necrotic death in a variety of human cancer cells in vitro and in vivo. The mechanisms underlying the ${\beta}$-Lap toxicity against cancer cells has been controversial. The most recent view is that ${\beta}$-Lap, which is a quinone compound, undergoes two-electron reduction to hydroquinone form utilizing NAD(P)H or NADH as electron source. This two-electron reduction of ${\beta}$-Lap is mediated by NAD(P)H:quinone oxidoreductase (NQO1), which is known to mediate the reduction of many quinone compounds. The hydroquinone forms of ${\beta}$-Lap then spontaneously oxidizes back to the original oxidized ${\beta}$-Lap, creating futile cycling between the oxidized and reduced forms of ${\beta}$-Lap. It is proposed that the futile recycling between oxidized and reduced forms of ${\beta}$-Lap leads to two distinct cell death pathways. First one is that the two-electron reduced ${\beta}$-Lap is converted first to one-electron reduced ${\beta}$-Lap, i.e., semiquinone ${\beta}$-Lap $(SQ)^{{\cdot}-}$ causing production of reactive oxygen species (ROS), which then causes apoptotic cell death. The second mechanism is that severe depletion of NAD(P)H and NADH as a result of futile cycling between the quinone and hydroquinone forms of ${\beta}$-Lap causes severe disturbance in cellular metabolism leading to apoptosis and necrosis. The relative importance of the aforementioned two mechanisms, i.e., generation of ROS or depletion of NAD(P)H/NADH, may vary depending on cell type and environment. Importantly, the NQO1 level in cancer cells has been found to be higher than that in normal cells indicating that ${\beta}$-Lap may be preferentially toxic to cancer cells relative to non-cancer cells. The cellular level of NQO1 has been found to be significantly increased by divergent physical and chemical stresses including ionizing radiation. Recent reports clearly demonstrated that ${\beta}$-Lap and ionizing radiation kill cancer cells in a synergistic manner. Indications are that irradiation of cancer cells causes long-lasting elevation of NQO1, thereby sensitizing the cells to ${\beta}$-Lap. In addition, ${\beta}$-Lap has been shown to inhibit the repair of sublethal radiation damage. Treating experimental tumors growing in the legs of mice with irradiation and intraperitoneal injection of ${\beta}$-Lap suppressed the growth of the tumors in a manner more than additive. Collectively, ${\beta}$-Lap is a potentially useful anti-cancer drug, particularly in combination with radiotherapy.

미숙아 빈혈에 대한 Recombinant Human Erythropoietin의 효과 : 예비연구 (Effect of Recombinant Human Erythropoietin in the Anemia of Prematurity : a Pilot Study)

  • 이경아;신손문;박용훈;하정옥
    • Journal of Yeungnam Medical Science
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    • 제11권1호
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    • pp.115-126
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    • 1994
  • 1991년 1월부터 1993년 2월까지 영남대학교 의과대학 부속병원에서 출생하여 신생아 중환자실에서 치료 받았던 12명의 미숙아를 대상으로 무작위로 대조군과 rHuEPO투여군으로 나누어 체중 kg당 100unit의 rHuEPO을 1주간 3회씩 4주동안 피하주사하고 rHuEPO투여 시작과 같이 체중 kg당 3mg의 elemental iron을 매일 경구투여 하였고 출생 후 수유가 가능할 때 부터 25unit씩의 비타민 E를 매일 경구투여 하였다. 망상적혈구, 혈색소치, 백혈구수, 혈소판수, 혈청 철, ferritin, 총 철결합능, erythropoietin농도, 활력징후, 체중, 간기능, 신장기능 및 피하주사부 위의 국소 부작용을 비교해 본 결과 치료 시작전 erythropoietin의 농도는 대조군과 rHuEPO투여군 사이에 차이는 없었으며 모두 정상 범위에 속했고 rHuEPO투여군에서는 치료 1주에서 3주사이에 급격한 망상적혈구의 경향이 관찰되었고 전반적으로 혈색소치, 백혈구수, 혈소판수, 혈청 철, ferritin, TIBC등에서는 차이가 없었다. 그리고 체중증가 및 활력증상, 간기능, 신장기능에서도 대조군과 rHuEPO투여군 사이에서 차이가 없었고 rHuEPO 투여 기간 동안 계속 정상적으로 유지되었다. 결론적으로 우리의 연구에서는 rHuEPO치료로 뚜렷한 혈색소치 및 헤마토크리의 증가를 볼 수 없었지만 망상적혈구가 치료 초기에 증가되는 경향이 관찰되었고 치료로 인한 특이할 만한 부작용이 없었으므로 첫째, 치료 기간 중의 예견할 수 없이 발생하는 패혈증, 무시할 수 없는 채혈량과 spontaneous endogenous erythropoietin생산이 rHuEPO의 반응에 미치는 영향, 둘째. rHuEPO의 가장 높은 효과를 얻기 위한 보다 적절한 투여용량, 기간 및 rHuEPO의 투여를 출생 후부터 바로 예방 목적으로 할 것인지 또는 출생 몇 주 후부터 rescue therapy로 할 것인지 투여 시작 시기, 셋째, 용량의 증가 및 감소에 동반되는 부작용의 정도등을 고려해서 앞으로 더 많은 미숙아를 대상으로 지속적인 연구를 한다면 rHuEPO을 이용해 더욱 더 활발하고 효과적으로 미숙아 빈혈을 치료할 수 있으리라 기대한다.

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『동의보감(東醫寶鑑)』에 수록된 파킨슨병 치료 처방(處方) 후보군 선별 연구 (Research on prescription candidates for Parkinson's disease in 『Dongeuibogam』)

  • 황민섭;박혜진;김시원;백진웅
    • 대한한의학방제학회지
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    • 제26권1호
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    • pp.65-80
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    • 2018
  • Objectives : This study aims to sort out prescription candidates for four major symptoms of Parkinson's disease from Korean traditional medical publication, "Dongeuibogam". Methods : Medical terms related to four major symptoms of Parkinson's disease were primarily selected from "Dongeuibogam". Prescriptions that include at least one or more medical terms which are selected above were classified by the four major symptoms of Parkinson's disease, and finally analyzed to sort the most effective candidates. Results & Conclusions : 1. There are 18 medical terms in efficacy ($ch{\grave{i}}$ $z{\grave{o}}ng$, $j{\bar{u}}$ $lu{\acute{a}}n$, $j{\bar{i}}ng$${\check{u}}$ $ju{\check{a}}n$($ju{\check{a}}n$, $qu{\acute{a}}n$) $lu{\acute{a}}n$, $j{\bar{i}}ng$${\check{u}}$ $lu{\acute{a}}n$($lu{\acute{a}}n$) $t{\grave{o}}ng$, $j{\bar{i}}n$ $lu{\acute{a}}n$, $j{\bar{i}}n$ $t{\grave{i}}$, $sh{\check{o}}u$ $zh{\grave{e}}n$, $y{\acute{a}}ng$ $sh{\check{o}}u$, $lu{\acute{a}}n$ $j{\acute{i}}$, $lu{\acute{a}}n$ $b{\grave{i}}$, $r{\grave{o}}u$ $r{\acute{u}}n$, $zh{\grave{a}}n$ $di{\grave{a}}o$, $zh{\grave{a}}n$ $y{\acute{a}}o$, $zh{\grave{i}}$ $z{\acute{u}}$, $ch{\grave{e}}$ $t{\grave{o}}ng$, $ch{\bar{o}u}$ $ch{\grave{e}}$, $f{\bar{e}}ng$ $ch{\grave{u}}$, $ch{\grave{u}}$ $nu{\grave{o}}$) related to tremor, one of four major symptoms of Parkinson's disease. 2. There are 9 medical terms in efficacy ($qi{\acute{a}}ng$ $j{\acute{i}}$, $qi{\acute{a}}ng$ $zh{\acute{i}}$, $qi{\acute{a}}ng$ $t{\grave{o}}ng$, $j{\bar{u}}$ $j{\acute{i}}$, $j{\bar{i}}n$ $j{\acute{i}}$, $sh{\bar{e}}n$ $qi{\acute{a}}ng$, $lu{\acute{a}}n$ $j{\acute{i}}$, $y{\bar{a}}o$ $j{\acute{i}}$ $qi{\acute{a}}ng$, $xi{\grave{a}}ng$ $qi{\acute{a}}ng$) related to rigidity, one of four major symptoms of Parkinson's disease. 3. 38 prescription candidates (jiaweishouxingyuan, jiaweilonghusan, gehuajiexingtang, qiangfutang, qianghuoxuduantang, dawugongsan, duhuojishengtang, mahuangzuojingtang, fangfengbaizhumulitang, fangfengtongshengsan, baizhutang, buxinwan, fulingtang, binsusan, xieqingwan, sanbitang, shengdiqinliantang, shujinbaoansan, xingxiangsan, xiaotanfulingwan, shengjunwan, shenmizuojingtang, wuyaoshunqisan, yuzhenwan, wenjingyiyuantang, yiziqingjinsan, ziyinningshentang, shaoyaogancaotang, dingtongsan, zhushazhijiasan, cangzusan, chuanxiongfulingtang, tiedanyuan, choubaowan, duomingsan, xuanhusuosan, xuefengtang, huoluodan) were selected for tremor, one of the four major symptoms of Parkinson's disease. 4. 21 prescription candidates (qianghuoshengshitang, guizhiqianghuotang, guizhifuzitang, jiuweiqianghuotang(qianghuochonghetang), xiongzhixiangsusan, daqianghuotang, mahuangguizhitang, muguajian, fuzilizhongtang, shenzhusan, lianqiaobaidusan, yuzhensan, niuhuangjinhudan, renshenbaidusan, shaoyaogancaotang, jiuzhumuguazhou, cangzusan, shenxiangtianmatang, xiangjiaosan, xuefengtang, huishousan) were selected for rigidity, one of the four major symptoms of Parkinson's disease. 5. The results in this study ought to be verified by subsequent studies and clinical trials.

비인강암의 방사선치료성적 (Radiation Therapy of Nasopharyngeal Cancers)

  • 신세원;김성규;김명세
    • Journal of Yeungnam Medical Science
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    • 제9권2호
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    • pp.312-320
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    • 1992
  • 1986년 4월부터 1992년 3월까지 6년간 영남대학교 의과대학 부속병원 치료방사선과에 내원하여 근치적인 방사선치료를 시행한 후 6개월 이상 추적조사가 가능하였던 31명의 치료성적은 다음과 같다. 대상환자 31명중 남자가 22명으로 여자보다 2.4배 많았으며 30세미만 3명을 제외하면 30대에서 60대까지 고른분포를 보였다. 병리조직학적 분류상 편평세포암이 13명, 미분화세포암이 18명이었다. 임상적병기는 I기 1명, II기 2명, III기 6명, IV기 22명이었다. 31명중 방사선치료만 시행된 경우가 11명, 항암제등과 병합치료를 시행한 경우가 20명이었다. 편평세포암 환자 11명중 6명에서 방사선치료만을 시행하였고 5명에서 병합치료를 시행하였으나, 미분화세포암에서는 18명중 5명은 방사선치료만을 시행하였고 13명은 병합치료를 실시하였다. 치료에 대항 반응은 치료방법에 따른 차이가 없었으나, 방사선치료만 시행한 경우에 편평세포암 6명중 3명이 완전관해를 보인 반면에, 미분화세포암 5명 모두 완전관해를 보여 큰 차이를 보였으나 병합치료에서는 세포형태에 따른 차이가 소실되었다. 치료 후 1년 생존율은 치료방법에 따른 차이가 없었다. 완전관해를 보인 환자 22명중에서 방사선치료만 시행한 8명중 6명에서 재발을 보였으며 그중 3명은 원격전이를 동반하였으나, 병합치료를 시행한 14명중에서 3명만이 재발을 보였으며 그중2명은 원격전이를 보였다. 이상의 결과에서 치료방법에 따른 관해율은 비슷하였으나 치료 후 추적과정에서 발생하는 재발은 방사선치료만 시행한 경우보다 병합치료를 실시한 경우에 현저히 줄어듬을 보여주어 비인강암에 대한병합치료가 국소재발의 감소 및 원격전이의 감소를 통하여 생존율의 향상에도 기여하리라 사료된다.

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Bioequivalence of Hana Loxoprofen Sodium Tablet to Dongwha Loxonin® Tablet (Loxoprofen Sodium 60 mg)

  • Kang, Hyun-Ah;Cho, Hea-Young;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • 제41권2호
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    • pp.117-123
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    • 2011
  • Loxoprofen sodium, a 2-phenylpropionate non-steroidal anti-inflammatory drug (NSAID), has marked analgesic and antipyretic activities and relatively weak gastrointestinal ulcerogenicity. The purpose of the present study was to evaluate the bioequivalence of two loxoprofen sodium tablets, Hana loxoprofen sodium tablet (Hana Pharm. Co., Ltd.) and Dongwha Loxonin$^{(R)}$ tablet (Dongwha Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The in vitro release of loxoprofen from the two loxoprofen sodium formulations was tested using KP IX Apparatus II method with various dissolution media. Twenty four healthy Korean male volunteers, $22.83{\pm}1.862$ years in age and $69.92{\pm}9.14$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After a single tablet containing 60 mg as loxoprofen sodium was orally administered, blood samples were taken at predetermined time intervals and the concentrations of loxoprofen in serum were determined using a online column-switching HPLC method with UV/Vis detection. The dissolution profiles of two formulations were similar in all tested dissolution media. The pharmacokinetic parameters such as $AUC^t$, $C_{max}$ and $T_{max}$ were calculated, and computer programs (Equiv Test and K-BE Test 2002) were utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and un-transformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Dongwha Loxonin$^{(R)}$ tablet, were 2.03, 2.99 and -9.49% for $AUC_t$, $C_{max}$, and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log0.8 to log1.25 (e.g., log0.9831~log1.0535 and log0.9455~log1.1386 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Hana loxoprofen sodium tablet was bioequivalent to Dongwha Loxonin$^{(R)}$ tablet.

Feasibility and Effects of a Postoperative Recovery Exercise Program Developed Specifically for Gastric Cancer Patients (PREP-GC) Undergoing Minimally Invasive Gastrectomy

  • Cho, In;Son, Younsun;Song, Sejong;Bae, Yoon Jung;Kim, Youn Nam;Kim, Hyoung-Il;Lee, Dae Taek;Hyung, Woo Jin
    • Journal of Gastric Cancer
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    • 제18권2호
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    • pp.118-133
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    • 2018
  • Purpose: Exercise intervention after surgery has been found to improve physical fitness and quality of life (QOL). The purpose of this study was to investigate the feasibility and effects of a postoperative recovery exercise program developed specifically for gastric cancer patients (PREP-GC) undergoing minimally invasive gastrectomy. Materials and Methods: Twenty-four patients treated surgically for early gastric cancer were enrolled in the PREP-GC. The exercise program comprised sessions of In-hospital Exercise (1 week), Home Exercise (1 week), and Fitness Improvement Exercise (8 weeks). Adherence and compliance to PREP-GC were evaluated. In addition, body composition, physical fitness, and QOL were assessed during the preoperative period, after the postoperative recovery (2 weeks after surgery), and upon completing the PREP-GC (10 weeks after surgery). Results: Of the 24 enrolled patients, 20 completed the study without any adverse events related to the PREP-GC. Adherence and compliance rates to the Fitness Improvement Exercise were 79.4% and 99.4%, respectively. Upon completing the PREP-GC, patients also exhibited restored cardiopulmonary function and muscular strength, with improved muscular endurance and flexibility (P<0.05). Compared to those in the preoperative period, no differences were found in symptom scale scores measured using the European Organization for Research and Treatment of Cancer (EORTC) Core Quality of Life Questionnaire (QLQ-C30) and Quality of Life Questionnaire-Stomach Cancer-Specific Module (QLQ-STO22); however, higher scores for global health status and emotional functioning were observed after completing the PREP-GC (P<0.05). Conclusions: In gastric cancer patients undergoing minimally invasive gastrectomy, PREP-GC was found to be feasible and safe, with high adherence and compliance. Although randomized studies evaluating the benefits of exercise intervention during postoperative recovery are needed, surgeons should encourage patients to participate in systematic exercise intervention programs in the early postoperative period (Registered at the ClinicalTrials.gov, NCT01751880).

Efficacy of Different Number of XELOX or SOX Chemotherapy Cycles After D2 Resection for Stage III Gastric Cancer

  • Yu, Yuanyuan;Zhang, Zicheng;Meng, Qianhao;Wang, Ke;Li, Qingwei;Ma, Yue;Yao, Yuanfei;Sun, Jie;Wang, Guangyu
    • Journal of Gastric Cancer
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    • 제22권2호
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    • pp.107-119
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    • 2022
  • Purpose: We aimed to explore whether the prognosis of patients treated with capecitabine and oxaliplatin (XELOX) or S-1 and oxaliplatin (SOX) regimens who received fewer cycles of chemotherapy after D2 radical resection for gastric cancer (GC) would be non-inferior to that of patients who received the standard number of cycles of chemotherapy. Materials and Methods: Data on patients who received XELOX or SOX chemotherapy after undergoing D2 radical resection at Harbin Medical University Cancer Hospital between January 2011 and May 2016 were collected. Results: In patients who received 4, 6, and 8 cycles of chemotherapy, the 5-year overall survival (OS) rates were 59.4%, 64.8%, and 62.7%, respectively. Compared to patients who received 4 cycles of chemotherapy, those who received 6 cycles (hazard ratio [HR], 0.882; 95% confidence interval [CI], 0.599-1.299; P=0.52) or 8 cycles (HR, 0.882; 95% CI, 0.533-1.458; P=0.62) of chemotherapy did not exhibit significantly prolonged OS. The 3-year disease-free survival (DFS) rate of patients who received 4, 6, and 8 cycles of chemotherapy was 62.1%, 67.2%, and 60.8%, respectively. Compared to patients who received 4 cycles of chemotherapy, those who received 6 cycles (HR, 0.835; 95% CI, 0.572-1.221; P=0.35) or 8 cycles (HR, 0.972; 95% CI, 0.606-1.558; P=0.91) of chemotherapy did not show significantly prolonged DFS. However, the 3-year DFS and 5-year OS rates of patients who received 6 cycles of chemotherapy appeared to be superior to those of patients who received 4 and 8 cycles of chemotherapy. Conclusions: For patients with stage III GC, 4 to 6 cycles of XELOX or SOX chemotherapy may be a favorable option. This study provides a rationale for further randomized clinical trials.

Efficacy and Safety of Trastuzumab Deruxtecan and Nivolumab as Third- or Later-Line Treatment for HER2-Positive Advanced Gastric Cancer: A Single-Institution Retrospective Study

  • Keitaro Shimozaki;Izuma Nakayama ;Daisuke Takahari;Kengo Nagashima;Koichiro Yoshino ;Koshiro Fukuda;Shota Fukuoka ;Hiroki Osumi ;Mariko Ogura ;Takeru Wakatsuki;Akira Ooki ;Eiji Shinozaki;Keisho Chin ;Kensei Yamaguchi
    • Journal of Gastric Cancer
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    • 제23권4호
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    • pp.609-621
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    • 2023
  • Purpose: Determination of optimal treatment strategies for HER2-positive advanced gastric cancer (AGC) in randomized trials is necessary despite difficulties in direct comparison between trastuzumab deruxtecan (T-DXd) and nivolumab as third or later-line treatments. Materials and Methods: This single-institution, retrospective study aimed to describe the real-world efficacy and safety of T-DXd and nivolumab as ≥ third line treatments for HER2-positive AGC between March 2016 and May 2022. Overall, 58 patients (median age, 64 years; 69% male) were eligible for the study (T-DXd group, n=20; nivolumab group, n=38). Results: Most patients exhibited a HER2 3+ status (72%) and presented metastatic disease at diagnosis (66%). The response rates of 41 patients with measurable lesions in the T-DXd and nivolumab groups were 50% and 15%, respectively. The T-DXd and nivolumab groups had a median progression-free survival of 4.8 months (95% confidence interval [CI], 3.3, 7.0) and 2.3 months (95% CI, 1.5, 3.5), median overall survival (OS) of 10.8 months (95% CI, 6.9, 23.8) and 11.7 months (95% CI, 7.6, 17.1), and grade 3 or greater adverse event rates of 50% and 2%, respectively. Overall, 64% patients received subsequent treatment. Among 23 patients who received both regimens, the T-DXd-nivolumab and nivolumab-T-DXd groups had a median OS of 14.0 months (95% CI, 5.0, not reached) and 19.3 months (95% CI, 9.5, 25.1), respectively. Conclusions: T-DXd and nivolumab showed distinct efficacy and toxicity profiles as ≥ third line treatments for HER2-positive AGC. Considering the distinct features of each regimen, they may help clinicians personalize optimal treatment approaches for these patients.

하나로 원자로 BNCT 열중성자 조사장치에 대한 선량특성연구 (Dosimetric Characteristics of a Thermal Neutron Beam Facility for Neutron Capture Therapy at HANARO Reactor)

  • 이동한;서소희;지영훈;최문식;박재홍;김금배;류성렬;김명섭;이병철;천기정;조재원;김미숙
    • 한국의학물리학회지:의학물리
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    • 제18권2호
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    • pp.87-92
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    • 2007
  • 최대출력 30 MW, 하나로(HANARO) 다목적 연구용 원자로의 접선 중성자공에 붕소중성자포획치료(Boron Neutron Capture Therapy, BNCT)를 위한 열중성자 조사장치가 개발되었다. BNCT 조사장치에서는 서로 다른 물리적 특성과 생물학적 효과비를 가진 여러 성분의 방사선이 방출되기 때문에 정확한 투여선량을 결정하기 위해서는 각 성분의 정량적 분석이 필수적이다. 따라서 본 연구에서는 방사화 분석, 열형광선량계 및 이온전리함 등 여러 유형의 검출기를 사용하여 BNCT 조사장치에서 방출되는 열중성자 및 감마선 혼합장의 선량 성분을 분리, 측정하였다. 선량측정은 물 속에 함유된 불순물과 중성자의 이차반응을 최소화하기 위해 증류수를 채운 물팬텀을 이용하였다. 그리고 측정 결과는 MCNP4B 전산계산의 결과와 상호 비교하였다. 측정 결과 열중성자속은 물팬텀 10 mm와 20 mm 깊이에서 각각 $1.02E9n/cm^2{\cdot}s$$6.07E8n/cm^2{\cdot}s$이었고, 고속중성자선량율은 10 mm 깊이에서 0.11 Gy/hr로 미세하였다. 감마선량률은 물팬텀 20 mm 깊이에서 5.10 Gy/hr로 나타났다. 측정된 중성자와 감마선량값은 MCNP의 결과와 5% 이내로 잘 일치하였고, 열중성자속은 14%의 비교오차를 나타내었다. 이러한 결과들은 중성자 검출의 난이도를 고려할 때 충분히 신뢰할 수 있는 수준이라 판단되며, BNCT 임상 연구를 위한 선량평가 자료로 활용할 수 있을 것으로 사료된다.

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$[^{123}I]$Idoxifene 합성과 유방암의 세포섭취에 관한 연구 (Study for the Synthesis of $[^{123}I]$Idoxifene and Its Uptake in the Breast Cancer Cell)

  • 조영섭;양승대;서용섭;전권수;안순혁;임수정;임상무;유국현
    • 대한핵의학회지
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    • 제34권5호
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    • pp.410-417
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    • 2000
  • 목적: 현재 유방암 치료제로서 임상실험 제 2단계에 들어간 idoxifene은 항에스트로겐 의약품으로서 기존의 tamoxifen보다도 많은 장점을 가지고 있는 것으로 연구결과 밝혀졌다. 또한 방사성 동위원소 $[^{123}I]$를 표지한 $[^{123}I]$idoxifene은 SPECT을 이용한 유방암세포를 영상화하여 조기에 진단할 수 있는 진단시약으로서 널리 각광 받고 있다. 따라서 본 연구에서는 idoxifene의 전구체를 합성하고 $[^{123}I]$를 표지하여 세포 내 섭취론 관찰하였다. 대상 및 방법: $[^{123}I]$idoxifene을 위한 전구체는 McCague가 연구 발표한 자료를 바탕으로 (2-chloroethoxy)benzene과 2-phenylbutanoic acid를 출발물질로 하여 합성하였다. 표지는 $[^{123}I]$를 사용하였으며 분리는 Silica Sep-Pak을 사용하였으며 세포 내 섭취실험은 에스트로겐 리셉터를 가진 MCF-7과 대조군으로서 에스트로겐 리셉터가 없는 MDA-MB-468을 이용하였다. 결과 및 결론: Idoxifene의 전구체인 4-stannylated 화합물의 합성수율은 약 30%이었으며, $[^{123}I]$ 표지는 60분 경과에서 $90{\sim}92%$로 최대의 표지수율을 보였으며 방사화학적 순도는 98%이상이었다. 또한 세포 내 섭취실험에서 실험군과 대조군 사이에 섭취비율은 180분에서 1.7:1로 나타나 idoxifence은 항에스트로겐 효과가 아주 높은 것으로 판명되었다. 이를 바탕으로 배양세포와 동물모델을 이용한 추가적인 실험이 필요하며, 유방암 환자에게도 임상이용이 기대된다.

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