Drug repurposing or repositioning has been well-known to refer to the therapeutic applications of a drug for another indication other than it was originally approved for. Repurposing non-oncology small-molecule drugs has been increasingly becoming an attractive approach to improve cancer therapy, with potentially lower overall costs and shorter timelines. Several non-oncology drugs approved by FDA have been recently reported to treat different types of human cancers, with the aid of some new emerging technologies, such as omics sequencing and artificial intelligence to overcome the bottleneck of drug repurposing. Therefore, in this review, we focus on summarizing the therapeutic potential of non-oncology drugs, including cardiovascular drugs, microbiological drugs, small-molecule antibiotics, anti-viral drugs, anti-inflammatory drugs, anti-neurodegenerative drugs, antipsychotic drugs, antidepressants, and other drugs in human cancers. We also discuss their novel potential targets and relevant signaling pathways of these old non-oncology drugs in cancer therapies. Taken together, these inspiring findings will shed new light on repurposing more non-oncology small-molecule drugs with their intricate molecular mechanisms for future cancer drug discovery.

众所周知，药物再利用或重新定位是指药物在最初批准之外的其他适应症的治疗应用。重新利用非肿瘤小分子药物已越来越成为改善癌症治疗的一种有吸引力的方法，可能会降低总体成本并缩短时间。最近有报道称，FDA 批准的几种非肿瘤药物可用于治疗不同类型的人类癌症，借助一些新兴技术，如组学测序和人工智能，以克服药物再利用的瓶颈。因此，在这篇综述中，我们重点总结了非肿瘤药物的治疗潜力，包括心血管药物、微生物药物、小分子抗生素、抗病毒药物、抗炎药物、抗神经退行性药物、抗精神病药物、抗抑郁药和其他治疗人类癌症的药物。我们还讨论了这些旧的非肿瘤药物在癌症治疗中的新潜在靶点和相关信号通路。总而言之，这些鼓舞人心的发现将为重新利用更多具有复杂分子机制的非肿瘤小分子药物提供新的启示，以用于未来的癌症药物发现。