The statin drugs (‘statins’) potently inhibit hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase by competitively blocking the active site of the enzyme. Statins decrease de novo cholesterol biosynthesis and thereby reduce plasma cholesterol levels. Statins exhibit “pleiotropic” properties that are independent of their lipid-lowering effects. For example, preclinical evidence suggests that statins inhibit tumor growth and induce apoptosis in specific cancer cell types. Furthermore, statins show chemo-sensitizing effects by impairing Ras family GTPase signaling. However, whether statins have clinically meaningful anti-cancer effects remains an area of active investigation. Both preclinical and clinical studies on the potential mechanisms of action of statins in several cancers have been reviewed in the literature. Considering the contradictory data on their efficacy, we present an up-to-date summary of the pleiotropic effects of statins in cancer therapy and review their impact on different malignancies. We also discuss the synergistic anti-cancer effects of statins when combined with other more conventional anti-cancer drugs to highlight areas of potential therapeutic development.

他汀类药物（“他汀类药物”）通过竞争性阻断羟甲基戊二酰辅酶 A (HMG-CoA) 还原酶的活性位点来有效抑制该酶。他汀类药物可减少胆固醇的从头生物合成，从而降低血浆胆固醇水平。他汀类药物表现出与其降脂作用无关的“多效性”特性。例如，临床前证据表明他汀类药物可抑制肿瘤生长并诱导特定癌细胞类型的细胞凋亡。此外，他汀类药物通过损害 Ras 家族 GTP 酶信号传导而显示出化疗增敏作用。然而，他汀类药物是否具有临床意义的抗癌作用仍然是一个积极研究的领域。文献综述了他汀类药物在多种癌症中潜在作用机制的临床前和临床研究。考虑到其疗效的相互矛盾的数据，我们提出了他汀类药物在癌症治疗中多效作用的最新总结，并回顾了它们对不同恶性肿瘤的影响。我们还讨论了他汀类药物与其他更传统的抗癌药物联合使用时的协同抗癌作用，以突出潜在的治疗开发领域。