5-aminosalicylates remain the first-line treatment for patients with ulcerative colitis. A number of formulations are available for the treatment of active ulcerative colitis, including encapsulated mesalazine and mesalazine in combination with other molecules. Balsalazide is an aminosalicylate prodrug that releases mesalazine in the colon, thus exerting its multiple anti-inflammatory effects in areas of colitis. This review will examine the pharmacological and therapeutic features of balsalazide as an anti-inflammatory agent in ulcerative colitis. The introduction of novel aminosalicylate formulations and an appreciation of their molecular mode of action, has renewed interest in these agents in both maintenance of disease remission and cancer prevention.