Hypercholesterolemia is a risk factor of cardiovascular diseases, which have been managed using statin drugs. Red yeast rice (RYR) as a traditional food in the Eastern Asia countries has anti-hyperlipidemia activity. Recently, a variety of food supplement products containing RYR have been developed to lower blood cholesterol, which is attributed to the presence of monacolins, especially monacolin K (lovastatin, a statin drug). This review was aimed to summarize the clinical trials using RYR products to investigate their effects on lipid profiles in humans. Relevant articles of human clinical trials were retrieved from PubMed and discussed here. Results showed that RYR and its extracts have been included in commercially available products alone and in combinations with various other materials, which include bioactive compounds such as coenzyme Q10 and berberine, vitamins, extracts from other plants such as phytosterols, polyunsaturated fatty acids or even probiotics. The durations of the trials ranged from 4 weeks to 60 months. The content of monacolin K ranged from 0.32 mg/pack to 10 mg/pack. The data of these human clinical trials demonstrated that these RYR supplement products were sufficient to reduce blood cholesterol in different populations. However, the inclusions of certain materials might not have additive effect. Additionally, studies including a lovastatin only positive control group with the equivalent dose as that of monacolin K in the RYR products remain to be done. Furthermore, variations of monacolin K contents and presence of toxic citrinin are still concerns. Last, bioactivities of other components in RYR should be investigated as well. More future studies will certainly help to fully explore the potentials of this traditional food in the combat against cardiovascular and other metabolic diseases.