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首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Re-188-labeled bisphosphonates as potential bifunctional agents for therapy in patients with bone metastases
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Re-188-labeled bisphosphonates as potential bifunctional agents for therapy in patients with bone metastases

机译：Re-188标记的双膦酸盐可作为潜在的双功能药物治疗骨转移患者

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Two new bisphosphonates have been examined for their ability to bind Re-188 and deliver it selectively to bone. The bisphosphonates are prototype compounds with potential to deliver rhenium radionuclides and a second therapy modality to bone metastases. A conjugate between diethylenetriaminepentaacetic acid and bisphosphonate (DTPA/BP) and a conjugate between 5-fluorouracil and bisphosphonate (5-FU/BP) were prepared and labeled at high radiochemical purity with Re-188 and biodistribution studies were carried out in normal Balb/C mice. The compounds showed rapid blood clearance and elimination from soft tissues with substantial retention of activity in the bone comparable to Re-188-hydroxyethylidine diphosphonate used as a control. At 8 h bone activity was 3.51% of injected dose for Re-188-DTPA/BP and 6.38% of injected dose for Re-188-5-FU/BP representing 69.6% and 80.6% of total body radioactivity, respectively. The two compounds show the potential for combination therapy of painful bone metastases. (C) 2004 Elsevier Ltd. All rights reserved.
机译：已经研究了两种新的双膦酸酯结合Re-188并将其选择性递送至骨骼的能力。双膦酸盐是具有将to放射性核素和第二种治疗方式递送至骨转移瘤的潜力的原型化合物。制备了二亚乙基三胺五乙酸和双膦酸酯（DTPA / BP）之间的结合物以及5-氟尿嘧啶和双膦酸酯（5-FU / BP）之间的结合物，并用Re-188标记了高放射化学纯度，并在正常的Balb / C小鼠。与用作对照的Re-188-羟乙啶二膦酸酯相比，该化合物显示出快速的血液清除和从软组织中清除的能力，并且在骨骼中的活性基本上得以保留。在8 h时，骨活性分别为Re-188-DTPA / BP注射剂量的3.51％和Re-188-5-FU / BP注射剂量的6.38％，分别占人体总放射性的69.6％和80.6％。这两种化合物显示出联合治疗疼痛的骨转移瘤的潜力。 （C）2004 Elsevier Ltd.保留所有权利。

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