Rheumatoid arthritis (RA) is a persistent autoimmune ailment that is typified by the development of pannus, proliferation of synovial lining cells, microvascular neogenesis, infiltration of interstitial inflammatory cells, and destruction of cartilage and bone tissue. The disease not only imposes physical pain and economic burden on patients, but also results in a significant decline in their quality of life, rendering it a leading cause of disability. General treatment and drugs are commonly employed to alleviate the condition and symptoms of RA. Cyclooxygenase (COX), janus kinase (JAK), glucocorticoid receptor (GR) et al. have been identified as the main therapeutic targets for RA. This article provides a comprehensive review of the clinical applications and synthetic routes of 26 representative drugs for the treatment of RA, with the aim of facilitating the discovery of more effective new drugs for the treatment of this debilitating disease.