由于其多方面的治疗方式，具有明确结构的离散有机金属配合物在对抗恶性肿瘤方面正在迅速发展。许多创新的优点，如高抗肿瘤活性、极低的全身毒性、活性靶向能力和增强的细胞摄取能力，使其在临床应用中比各个前体更有竞争力。特别是有机荧光配体的配位诱导发光和光物理性质调控已经展示出及时评估治疗效果、实现协同光动力疗法（PDT）或光热疗法（PTT）的重要潜力。本综述强调了基于自组装金属环/金属笼的多模式放射化学治疗平台用于癌症消融的有指导意义的例子，并按照功能以逐步方式进行分类。最后，本文还介绍了癌症治疗领域的基本需求和一些可行的展望。© 2023 Wiley-VCH GmbH.

Discrete organometallic complexes with defined structures are proceeding rapidly in combating malignant tumors due to their multipronged treatment modalities. Many innovative superiorities, such as high antitumor activity, extremely low systemic toxicity, active targeting ability, and enhanced cellular uptake, make them more competent for clinical applications than individual precursors. In particular, coordination-induced regulation of luminescence and photophysical properties of organic light-emitting ligands has demonstrated significant potential in the timely evaluation of therapeutic efficacy by bioimaging and enabled synergistic photodynamic therapy (PDT) or photothermal therapy (PTT). This review highlights instructive examples of multimodal radiochemotherapy platforms for cancer ablation based on self-assembled metallacycles/metallacages, which would be classified by functions in a progressive manner. Finally, the essential demands and some plausible prospects in this field for cancer therapy are also presented.© 2023 Wiley-VCH GmbH.