Citrus fruits, renowned for their abundant of phytochemicals and bioactive compounds, hold a prominent position as commercially grown fruits with health-promoting properties. In this context, tangerine peel (Citri Reticulatae Pericarpium, CRP) is garnering attention as a byproduct of citrus fruits. Within the framework of the circular economy, CRP has emerged as a focal point due to its potential health benefits. CRP, extracted from Citrus reticulata cv. and aged for over three years, has attracted increasing attention for its diverse health-promoting effects, including its anticancer, cardiovascular-protecting, gastrointestinal-modulating, antioxidant, anti-inflammatory, and neuroprotective properties. Moreover, CRP positively impacts skeletal health and various physiological functions. This review delves into the therapeutic effects and molecular mechanisms of CRP. The substantial therapeutic potential of CRP highlights the need for further research into its applications in both food and medicine. As a value-added functional ingredient, CRP and its constituents are extensively utilized in the development of food and health supplements, such as teas, porridges, and traditional medicinal formulations.