Artesunate (ART) is a derivative of artemisinin. Compared with artemisinin, ART has excellent water solubility, high stability and oral bioavailability. In this review, the application of ART in classic autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus and ulcerative colitis is summarized. ART exhibited similar or even better efficacy than other highly effective immunosuppressive agents, such as methotrexate and cyclophosphamide. In addition, ART exerts its pharmacological effects mainly by inhibiting the production of inflammatory factors, reactive oxygen species, autoantibodies and the migration of cells to reduce damage to tissues or organs. Moreover, ART widely affected the NF-κB, PI3K/Akt, JAK/STAT and MAPK pathways to exert pharmacological effects.