Ficus pumila L. has been used as a functional plant for a long time in East Asia, especially its fruits, as a dietary component in Japan and parts of China. A series of bioactive compounds, including phenolic acids, flavonoids, terpenoids, alcohols, and steroids, have been extracted from the stems, leaves, flowers, and fruits of Ficus pumila L. Accumulated studies have demonstrated that Ficus pumila L. has multiple therapeutic activities, including antioxidant, anti-inflammatory, antibacterial, antitumor, hypoglycemic, and cardiovascular protective effects. Moreover, Ficus pumila L. has extensive applications, such as in the food industry and ecological city construction. Herein, we summarize the latest knowledge about the bioactive compounds and therapeutic activities of Ficus pumila L., and its applications in the food industry and ecological city construction are also discussed. We hope that this comprehensive review can attract more attention to Ficus pumila L. and be helpful for its further applications.