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Advances in Drug Design of Radiometal-Based Imaging Agents for Bone Disorders

机译：基于放射性金属的骨病成像剂药物设计的新进展

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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 and99mTc-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 the99mTc-mononuclear complex-conjugated bisphosphonate compounds showed superior biodistribution in preclinical studies. Moreover, the drug design concept could be applied to68Ga 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.
机译：核医学骨成像已成为检测骨疾病的最佳诊断方法，因为在出​​现症状和影像学改变之前就可以检测到病变。在过去的三十年中，尽管从化学和药学的角度来看，它们远非最佳，但99mTc-MDP和99mTc-HMDP由于其出色的生物分布特性而被用作骨闪烁显像剂。近来，已经提出了更合乎逻辑的药物设计作为双功能放射性药物的概念，其中载体分子（双膦酸酯）和放射性金属螯合基团在分子内，特别是99mTc-单核复合物-缀合的双膦酸酯是分开的。在临床前研究中，某些99mTc-单核复合物-共轭双膦酸酯化合物表现出优异的生物分布。而且，该药物设计概念可以应用于68Ga PET骨显像剂。这些研究将为开发基于放射性金属的影像学和治疗骨疾病（如骨转移）的治疗剂提供有用的信息。

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