Radiometals possess an exceptional breadth of decay properties and have been applied to medicine with great success for several decades. The majority of current clinical use involves diagnostic procedures, which use either positron-emission tomography (PET) or single-photon imaging to detect anatomic abnormalities that are difficult to visualize using conventional imaging techniques (e.g., MRI and X-ray). The potential of therapeutic radiometals has more recently been realized and relies on ionizing radiation to induce irreversible DNA damage, resulting in cell death. In both cases, radiopharmaceutical development has been largely geared toward the field of oncology; thus, selective tumor targeting is often essential for efficacious drug use. To this end, the rational design of four-component radiopharmaceuticals has become popularized. This Review introduces fundamental concepts of drug design and applications, with particular emphasis on bifunctional chelators (BFCs), which ensure secure consolidation of the radiometal and targeting vector and are integral for optimal drug performance. Also presented are detailed accounts of production, chelation chemistry, and biological use of selected main group and rare earth radiometals.

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用于成像和治疗的放射性主族和稀土金属

放射性金属具有非凡的衰变特性，几十年来已成功应用于医学领域。当前大多数临床用途涉及诊断程序，该程序使用正电子发射断层扫描（PET）或单光子成像来检测难以使用常规成像技术（例如MRI和X射线）可视化的解剖异常。治疗性放射性金属的潜力最近已经实现，并依靠电离辐射诱导不可逆的DNA损伤，从而导致细胞死亡。在这两种情况下，放射性药物的开发都主要针对肿瘤学领域。因此，选择性靶向肿瘤对于有效使用药物常常是必不可少的。为此，四组分放射性药物的合理设计已经普及。这篇综述介绍了药物设计和应用的基本概念，特别强调了双功能螯合剂（BFCs），它们可确保放射性金属和靶向载体的安全整合，并且是实现最佳药物性能所不可或缺的。还介绍了选定主要族和稀土放射性金属的生产，螯合化学和生物用途的详细情况。