The fermentation products of Monascus, especially those produced by solid-state fermentation of rice, have been used as food and health remedies for over 1000 years in China. Monascus rice products (MRPs) are currently being used as health foods in the United States and many Asian countries such as Japan, Taiwan, China, Korea, Thailand, the Philippines, and Indonesia. Many studies have shown that Monascus spp. produce commercially viable metabolites, including food colorants, cholesterol-lowering agents, and antibiotics. The most important bioactive compound isolated from Monascus is monacolin K, which is identical to the potent cholesterol-lowering, antiatherosclerotic drug lovastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor. Several species of the genus Monascus also produce citrinin, a mycotoxin harmful to the hepatic and renal systems. Monacolin K and citrinin are polyketide fungal metabolites. The biosynthetic pathways leading to the formation of polyketides, including monacolin K and citrinin, have been elucidated in Aspergillus and Monascus. The concern for safety is, therefore, high for the development of MRPs as health foods. Other attractive applications for MRPs are likely, as supported by recent studies that indicate that MRPs contain other substances (flavonoids, polyunsaturated fats, phytosterols, pyrrolinic compounds, and others) with a wide variety of biological activities and pharmacological potentials. Their effects in lowering blood sugar and triacylglycerol while raising HDL-C are more pronounced than those of monacolin K alone. Beyond cholesterol lowering, MRP may also be an ideal candidate for the treatment of metabolic syndrome.