Abstract: Rheumatoid arthritis （RA） is a chronic inflammatory autoimmune disease characterized by the destruction of joints. Currently, an efficacious and safe drug for RA is still lacking. Artesunate, a first-line drug for malaria, was recently found to have potential in treating autoimmune diseases, especially RA. In this article, the pharmacological mechanism of artesunate in the treatment of RA was summarized. The findings demonstrated that artesunate could not only regulate the immune function of T cells and B cells and suppress the formation of autoantibodies, but also directly affect the fibroblast-like synoviocytes and osteoclasts, inhibit the synovitis, neovascularization and osteoclastogenesis, and then suppress joint inflammation and bone destruction of RA. Therefore, artesunate might be a potential drug for RA in clinical practice.