Concomitant treatment of radiotherapy and chemotherapy is widely used in cancer therapy. The search for highly efficient radiochemotherapy drugs for tumor targeting therapy under image-guiding is of considerable interest. Herein we report an Ir-based prodrug Ir-NB with high sensitization efficiency for in vivo tumor microenvironment responsive cancer-targeted bioimaging radiochemotherapy. To the best of our knowledge, the sensitivity enhancement ratio (SER) of the Ir-NB prodrug is the highest among those reported for radiotherapy metal complex drugs. From detailed action mechanism study, we provide evidence that the prodrug is effectively suppresses the tumor growth through inducing mitochondrial dysfunction, and eventually amplifies the apoptotic signal pathway. This study provides an approach for the development of cancer theranostic agents for tumor radiotherapy.

中文翻译：

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高度X射线敏感的铱前药，用于可视化肿瘤放化疗

放射疗法和化学疗法的伴随治疗被广泛用于癌症治疗。在图像引导下寻找用于肿瘤靶向治疗的高效放射化学治疗药物引起了极大的兴趣。本文中，我们报告了一种基于Ir的前药Ir-NB，对体内肿瘤微环境响应性癌症靶向的生物成像放射化学疗法具有很高的敏化效率。据我们所知，Ir-NB的灵敏度增强比（SER）前体药物在放射疗法金属复合药物的报道中最高。通过详细的作用机制研究，我们提供证据表明前药可通过诱导线粒体功能障碍有效抑制肿瘤生长，并最终放大细胞凋亡信号通路。这项研究提供了开发用于肿瘤放疗的癌症治疗药物的方法。