Advances in drug design of radiometal-based imaging agents for bone disorders.
Advances in drug design of radiometal-based imaging agents for bone disorders.
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DOI：
10.1155/2011/537687
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发表时间：
2011
期刊：
影响因子：
--
通讯作者：
Saji H
中科院分区：
文献类型：
--
作者：
Ogawa K;Saji H
核医学骨显像已成为最佳的诊断骨疾病的检测，因为病变可以检测之前出现的症状和影像学变化。在过去的三十年中，99 mTc-MDP和99 mTc-HMDP由于其上级生物分布特性而被用作骨显像剂，尽管从化学和药学的角度来看它们远不是最佳的。最近，一个更合理的药物设计已被提出作为双功能放射性药物的概念，其中载体分子（双膦酸盐）和放射性金属螯合基团在分子内分离，特别是，99 mTc-单核络合物共轭双膦酸盐。一些99 mTc-单核络合物缀合的双膦酸盐化合物在临床前研究中显示出上级生物分布。此外，药物设计概念可应用于68 Ga PET骨显像剂。这些研究将为骨疾病（如骨转移）的放射性成像和治疗药物的开发提供有用的信息。
Nuclear medicine bone imaging has been the optimum diagnosis for the detection of bone disorders because the lesion could be detectable before the appearance of symptomatic and radiographic changes. Over the past three decades, 99mTc-MDP and 99mTc-HMDP have been used as bone scintigraphic agents because of their superior biodistribution characteristics, although they are far from optimal from a chemical and pharmaceutical point of view. Recently, a more logical drug design has been proposed as a concept of bifunctional radiopharmaceuticals in which the carrier molecules (bisphosphonates) and radiometal chelating groups are separated within a molecule, specifically, 99mTc-mononuclear complex-conjugated bisphosphonate. Some of the 99mTc-mononuclear complex-conjugated bisphosphonate compounds showed superior biodistribution in preclinical studies. Moreover, the drug design concept could be applied to 68Ga PET bone imaging agents. These studies would provide useful information for the development of radiometal-based imaging and therapeutic agents for bone disorders such as bone metastases.