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Re-186 Radiotherapeutical Agent for Bone Tumor Metastases and Bone Pain Palliation Radiotherapy

Re-186 放射治疗剂用于骨肿瘤转移和骨痛缓解放射治疗

基本信息

批准号：
13670932
负责人：
FUKUDA Satoshi
金额：
$ 2.24万
依托单位：
National Institue of Radiological Sciences (2002)Kyoto University (2001)
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2001
资助国家：
日本
起止时间：
2001 至 2002
项目状态：
已结题

项目摘要

In recent years, deficiency of Tc-bone imaging in oncology patients is lack of specificity on osteoclastic (bone destruction)(OC) or osteoblastic (bone formation) (OB) bone metastases differenciation. Uniqueness of pentavalent polynuclear Tc-complex of dimercaptosuccinic acid (Tc(V)-DMS) to accumulate in bone pathologies are of interest. In this project, studies on the osteotropic character at cellular level and in OC and OB animal models were performed. At cellular level, the great affinity of Tc(V)-DMS for the osteoclastic cells was demonstrated. Comparative studies with the well known bisphosphonate (BBP) agent, Tc HMDP, showed lack of affinity in any OC or OB cells. In the OC type of animal model, by the VX2 implant in rabbit, clear affinity of Tc(V)-DMS for the metastatic area demonstrated by SPECT studies, the ARG (186Re(V)-DMS, 186Re-HMSDP) and histological studies confirmed the radioactivity accumulation in areas abundant in OC. The Tc-HMDP showed lack of accumulation in the OC model, but this agent accumulated 10-1 5 times with higher avidity in bone injured rats (OB model), demonstrated by preliminary injection of tetracycline, a fluorescent agent to accumulate in recently formed injured bone, superimposed to the radioactive region. The distinctive Tc(V)-DMS accumulation in OC bone tumor indicated the potentiality of this agent in the differentiation of OC from OB metastases and its plausible use in radiotherapy and bone pain palliation.

近年来，肿瘤患者Tc-骨显像的不足之处在于对骨破坏（OC）或成骨细胞（OB）骨转移的鉴别缺乏特异性。二巯基丁二酸的五价多核Tc-络合物（Tc（V）-DMS）在骨病变中蓄积的唯一性是令人感兴趣的。本课题从细胞水平和OC、OB动物模型两个方面研究了其向骨的特性。在细胞水平上，Tc（V）-DMS对成骨细胞有很强的亲和力。与众所周知的双膦酸盐（BBP）试剂Tc HMDP的比较研究表明，在任何OC或OB细胞中缺乏亲和力。在OC型动物模型中，通过在兔体内植入VX 2，SPECT研究、ARG（186 Re（V）-DMS、186 Re-HMSDP）和组织学研究证实了Tc（V）-DMS对转移区域的明确亲和力，证实了OC丰富区域的放射性蓄积。Tc-HMDP在OC模型中显示缺乏积累，但该试剂在骨损伤大鼠（OB模型）中积累10- 15倍，具有更高的亲合力，这通过预先注射四环素（一种荧光剂）来证明，四环素在最近形成的损伤骨中积累，叠加到放射性区域。OC骨肿瘤中独特的Tc（V）-DMS蓄积表明该药物在区分OC和OB转移瘤中的潜力，以及其在放射治疗和骨痛缓解中的合理用途。