Mesalazine preparations for the treatment of ulcerative colitis: Are all created equal?

Abstract

Oral mesalazine (also known as mesalamine) is a 5-aminosalicylic acid compound used in the treatment of mild to moderate ulcerative colitis, with high rates of efficacy in induction and maintenance of remission. The therapeutic effect of mesalazine occurs topically at the site of diseased colonic mucosa. A myriad of oral mesalazine preparations have been formulated with various drug delivery methods to minimize systemic absorption and maximise drug availability at the inflamed colonic epithelium. It remains unclear whether different oral mesalazine formulations are bioequivalent. This review aims to evaluate the differences between mesalazine formulations based on the currently available literature and explore factors which may influence the selection of one agent above another.

Keywords: Colitis; Drug delivery systems; Mesalamine; Sulfasalazine; Therapeutic equivalency; Ulcerative.

Figure 1

Proposed mechanism of action of mesalazine at the colonic mucosa. IL: Interleukin; NF κB: Nuclear factorκB; PPAR: Peroxisome proliferative activated receptor; TNF: Tumour necrosis factor.

Figure 2

Algorithm for selection of mesalazine formulations. Anti-TNF: Anti-tumour necrosis factor; AEs: Adverse events; MMX: Multi-matrix system; OD: Once daily; CRP: C-reactive protein.