The development of new drug therapy is an evolutionary process progressing from clinical success with current treatments through an understanding of interactions in the immune and inflammatory events that culminate in the tissue injury of IBD. The basic immunoinflammatory response is reviewed, with identification of the recognized and potential sites of activity of current therapies. Potential sites and implications for future interventions by newer therapies are discussed as we anticipate the discovery of the etiology and eventual cure for ulcerative colitis and Crohn's disease.