The use of non-specific anti-inflammatory drugs such as the glucocorticoids is the foundation of medical therapy for inflammatory bowel disease. Although conventional steroid drugs are highly effective, their use is associated with the adverse effects of Cushing's syndrome. However, the therapeutic index of these drugs can be improved by chemical modification of the steroid nucleus and the use of new drug delivery systems that target the bowel wall as the pharmacokinetic compartment of interest. Budesonide is a novel glucocorticoid compound that illustrates the potential of this approach to identify effective and safe new treatments. Regional therapy for inflammatory bowel disease is an important pharmacological concept for the future development of the new glucocorticoids and other classes of drugs.