Rheumatoid arthritis (RA) is the most common inflammatory musculoskeletal disease and an important cause of diminished quality-of-life for the affected individuals and with a major impact on society because of decreased work-force participation. Treatment of RA has been advanced dramatically during the past two decades by the advent of biological therapies. A large number of such agents have been approved and several additional ones are in late-stage clinical developments. Because of the high price of biologics, pharmacoeconomical considerations have become an important part of the appraisal of such medications. Current therapeutic developments include the development of additional biologics with various specific targets, the development of small-molecule compounds with similar efficacies, and entirely new approaches to treat autoimmune inflammatory diseases such as RA.