The medical armamentarium for inflammatory bowel diseases continues to expand despite the uncertain etiologies of Crohn's disease and ulcerative colitis. To date, almost all of the medications in use have multiple sites of activity or are regarded as nonspecific suppressants of the chronic intestinal inflammatory response. Newer agents, such as cyclosporine, offer more focused, single-mediator activity, which still influence many ''down-stream'' cascades of inflammatory compounds. Whereas prior attempts to control these diseases have relied on corticosteroids, antibiotics, sulfasalazine, and dietary manipulations, these approaches have left many patients either resistant to, or intolerant of steroids while exposed to their long-term sequelae. The immunomodulatory agents offer new therapeutic options to many of these patients. Azathioprine, 6-mercaptopurine, cyclosporine, and methotrexate have all shown efficacy in Crohn's disease or ulcerative colitis, although in some cases the onset of action is slow, or potential side effects preclude generalized use outside of experienced centers. The success in achieving and maintaining remission in patients when other agents have failed, in reducing or eliminating steroids, and in avoiding surgery have made these agents important therapeutic alternatives. The spectrum of aminosalicylate formulations has already improved the quality of life for patients while similar advances in the site-specific delivery of novel steroids can be expected to improve the short- and long-term clinical outcomes. Novel agents continue to be applied to inflammatory bowel disease in hopes of both improving the therapeutic response and delineating pathogenic mechanisms.