Abstract
Red yeast rice (RYR) is an Asian indigenous medicine that ferments Oryza sativa grains using the Monascus fungi, specifically Monascus purpureus. Monacolins, pigments, phenols, sterols, and benzopyrans, such as the mycotoxin citrinin, were proven to be present in RYR, contributing to its numerous effects. This study aims to provide a thorough overview of the in vitro and in vivo pharmacological activities of M. purpureus red yeast rice, its studies in humans, and a summary of recent case reports. A literature search was conducted on the PubMed database, using the keywords: "pharmacology activity of red yeast rice" filtered to free full text and articles published from 2014 to 2024 for in vitro and in vivo studies, to ensure the newest developments. In vitro and in vivo pharmacological activity studies of RYR and/or metabolites have confirmed antidyslipidemia, anti-inflammatory, and anticancer activities, whereas studies in humans have evidenced its activity in improving lipid profiles. Furthermore, case reports on red yeast rice supplements, published between 2020 and 2025, revealed Fanconi syndrome and kidney dysfunction as the main adverse events, mostly reported from Japan.