Kadsura coccinea (Lem.) A.C.Smith, a plant in the Schisandraceae family, has high medicinal and nutritional value. Tetracyclic triterpenoids are one of the major bioactive components in K. coccinea, exhibiting diverse biological activities such as wind-dampness dispelling, anti-inflammatory, anti-cancer and anti-viral function, and immune modulation. In order to identify effective substances for preventing and treating diseases from K. coccinea, researchers have focused their attention on its tetracyclic triterpenoids due to their structural diversity. However, the pharmacological basis and action mechanisms of K. coccinea’s tetracyclic triterpenoids remain to be further elucidated. This paper systematically reviews the structural characteristics, biological activity and mechanism of action of the effective tetracyclic triterpenoids in K. coccinea, aiming to provide a theoretical foundation for the development and utilization of high-value-added products from K. coccinea, expand its application fields and promote the sustainable and healthy development of the K. coccinea industry.