Balsalazide: a review of its therapeutic use in mild-to-moderate ulcerative colitis.

Abstract

The aminosalicylate balsalazide is a prodrug which is metabolised by bacterial azo reductases in the colon to release its therapeutically active moiety mesalazine [mesalamine (US) or 5-aminosalicylic acid] and an inert carrier molecule. The systemic absorption of balsalazide and its metabolites is not required for the therapeutic efficacy of the drug, and has been demonstrated to be limited. Data from well designed trials with a duration of 8 to 12 weeks show that oral balsalazide 6.75 g/day is as effective as (two trials) or more effective than (one trial) oral delayed-release (pH-dependent) mesalazine 2.4 g/day and appears to be as effective as oral sulfasalazine 3 g/day in the treatment of active mild-to-moderate ulcerative colitis. In addition, balsalazide appears to have a faster onset of action than mesalazine. Furthermore, balsalazide was as effective as delayed-release mesalazine (dosages used were 1.2 and 1.5 g/day, where 1.6 g/day is recommended) and oral sulfasalazine 2 g/day (recommended dosage) in the prevention of relapse in ulcerative colitis in remission after 6 to 12 months of treatment; the balsalazide dosage was 3 g/day versus mesalazine and 2 g/day versus sulfasalazine. Although not well established, additional benefits may be achieved with balsalazide dosages up to 6 g/day. Data from well designed, 2- to 12-month trials show that balsalazide is well tolerated by patients with ulcerative colitis in both acute and maintenance indications, and is better tolerated than standard formulations of sulfasalazine at therapeutically relevant dosages. Balsalazide is a well tolerated and effective first-line therapeutic option for patients with ulcerative colitis, both for the treatment of active mild-to-moderate disease and as maintenance therapy to prevent disease relapse.