188Re-labeled bisphosphonates as potential bifunctional agents for therapy in patients with bone metastases
188Re-labeled bisphosphonates as potential bifunctional agents for therapy in patients with bone metastases
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DOI：
10.1016/j.apradiso.2004.10.004
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发表时间：
2005-04-01
影响因子：
1.6
通讯作者：
Mercer, JR
中科院分区：
文献类型：
--
作者：
El-Mabhouh, A;Mercer, JR
两种新的双膦酸盐已被检查其结合Re-188并将其选择性地递送至骨的能力。双膦酸盐是具有递送放射性核素和骨转移的第二治疗方式的潜力的原型化合物。制备了二乙三胺五乙酸双膦酸盐偶联物（DTPA/BP）和5-氟尿嘧啶双膦酸盐偶联物（5-FU/BP），用Re-188标记，并在正常Balb/C小鼠体内进行了生物分布研究。这些化合物显示出快速的血液清除和从软组织中消除，在骨中的活性基本保留与用作对照的Re-188-羟基亚乙基二膦酸盐相当。在8 h时，Re-188-DTPA/BP和Re-188-5-FU/BP的骨活性分别为注射剂量的3.51%和6.38%，分别占全身放射性的69.6%和80.6%。这两种化合物显示出联合治疗疼痛性骨转移的潜力。(C)2004爱思唯尔有限公司保留所有权利。
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.