Sulfasalazine and 5-Aminosalicylates for Ulcerative Colitis

Sulfasalazine was first identified in 1940 as a treatment for arthritis, and was found serendipitously to be beneficial in the treatment of ulcerative colitis. Since then, sulfasalazine and 5-aminosalicylic acid (5-ASA) derivatives have played an important role in the treatment of patients with mild to moderate disease activity (Moshkovska and Mayberry, World J Gastroenterol 13:4310–4315, 2007). Over the years, several 5-ASA formulations have been manufactured to enhance delivery to the colon, while minimizing adverse effects. Furthermore, evidence has suggested a role for these agents in cancer chemoprevention. Despite their established role in the treatment of ulcerative colitis, sulfasalazine and 5-ASA derivatives continue to be the subject of active research and advancement.Here the chemical structure and pharmacokinetics, mechanism of action, formulations, efficacy, and safety of sulfasalazine and 5-ASA are reviewed. The roles of rectal and oral delivery, dose response, and optimal duration of therapy are discussed. Finally, the potential of 5-ASA in chemoprevention and the cost-effectiveness of prolonged therapy are addressed.