Red yeast rice is a kind of traditional health foods, which is made through fermenting rice with red yeast mold. It is rich in a variety of active ingredients, such as red yeast pigment, red yeast polysaccharides, lovastatin, γ-aminobutyric acid and ergosterol, which endows the rice with various biological functions. Previous studies have found that red yeast rice has lipid-lowering, antihypertensive and antibacterial effects. Recent studies revealed that red yeast rice and its main active ingredients potentially have anticancer effects, which can affect apoptosis, cell cycle and cell invasion as well as reverse drug resistance of cancer cells. In this paper, the status of domestic and international research, is systematically summarized, the research progress on the anti-cancer effects of red yeast rice and its main active ingredients is reviewed, and the corresponding molecular mechanisms are described and classfied in detail. As a traditional food with a high market value, in-depth studies of its anticancer effect and associated molecular mechanisms will help the improvement of its industrial value and provide a theoretical basis for the processing and development of red yeast rice into functional foods with chemopreventive effects against cancer.