Recently, budesonide (Entecort EC) has been approved for the treatment of mildly to moderately active Crohn's disease involving the ileum and/or ascending colon. Budesonide is a synthetic corticosteroid having a potent glucocorticoid and weak mineralocorticoid activity. In standard in vitro and animal models, budes-onide has an approximately 200-fold higher affinity for the glucocorticoid receptor and a 1000-fold higher topical antiinflammatory potency than cortisol. While budesonide is well absorbed from the GI tract, its oral bioavailability is low (about 10%), primarily because of extensive first-pass metabolism in the liver. Two major metabolites (16a-hydroxyprednisolone and 6p-
hydroxybudesonide) are formed via the cytochrome P450 3A enzyme. In vitro studies on the binding of the two primary metabolites to the corticosteroid receptor indicate that their affinity for the receptor is less than 1% of that of the parent compound. It is hoped that use of this drug will avoid the long-term adverse reactions seen with systemically active corticosteroids.
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