The use of Monascus has a history of over 1000 years in China and it is commonly used for making red yeast rice and fermented bean curd. Its metabolites demonstrate broad application potential in the fields of food, health products and medicine. This review summarizes recent advances in research on the metabolites of Monascus in terms of their antibacterial, anti-inflammatory, lipid-lowering, blood glucose-lowering, and blood pressure-lowering effects. Studies indicate that Monascus metabolites contain various functional components, such as Monascus pigments, monacolin K and γ-aminobutyric acid (GABA), which exhibit their biological activities through multiple mechanisms. Some Monascus pigments have antibacterial properties, monacolin K is an ideal lipid-lowering agent, and GABA shows a significant blood pressure-lowering effect. Additionally, Monascus metabolites demonstrate good anti-inflammatory activity and blood glucose-lowering effects, and show significant anti-inflammatory effects in inflammation models. In conclusion, Monascus metabolites have broad application prospects, but further research is needed to elucidate the mechanism of their health benefits. This review will promote their development and application in the food, health and medical fields.