Mesalamine Delayed Release Tablets (Lialda™)
Pharmacology Update
Mesalamine Delayed Release Tablets (Lialda™)
Dr. Elliott is Chair, Formulary Committee, Northern California Kaiser Permanente; Assistant Clinical Professor of Medicine, University of California, San Francisco; Dr. Chan is Pharmacy Quality and Outcomes Manager, Kaiser Permanente, Oakland, CA. Drs. Chan and Elliott report no financial relationship to this field of study.
The first once-daily mesalamine formulation has been approved for the treatment of ulcerative colitis. The formulation uses the Multi Matrix System (MMX) technology designed to deliver the drug throughout the colon. Lialda is under license from Guiliani SpA Italy and marketed by Shire Pharmaceuticals, Inc.
Indications
Mesalamine (MMX) is indicated for the induction of remission in patients with active, mild to moderate ulcerative colitis.1
Dosage
The recommended dose is two to four 1.2 g tablets taken once daily. Tablets may be taken whole and without regard to meals.1
Mesalamine (MMX) is available as 1.2 g tablets.
Potential Advantages
Mesalamine MMX can be given once-daily while other mesalamine products (Pentasa Asacol) and pro-drugs (sulfasalazine, balsalazide) require dosing 2 to 4 times a day.
Potential Disadvantages
Treatment duration longer than 8 weeks has not been studied.1 Mesalamine MMX is currently not FDA approved for Crohn's disease or for maintenance of disease remission.
Comments
Mesalamine MMX is a delivery system that uses lipophilic and hydrophilic matrices in a coating that resists gastric pH. The coating begins to dissolve at a pH of 7 or higher and slowly releases mesalamine in the colonic lumen beginning in the distal ileum.2 Efficacy was shown in two randomized, double-blind, placebo-controlled studies in adult patients (n = 517) with active, mild to moderate ulcerative colitis. This was defined as a score of 4-10 on a modified ulcerative disease activity index (UC-DAI) and sigmoidoscopy score.1 Remission was defined as a UC-DAI score of 1 and 1-point reduction in sigmoidoscopy score.1,2 Remission rates at 8 weeks, in the first study, were 34.1%, 29.2% and 12.9% for 1.2 g twice daily, 4.8 g once daily and placebo. In the second study, rates were 40.5%, 41.2%, and 22.1% for 2.4 g once daily, 4.8 g once daily, and placebo.1,2 In the second study, Asacol (2.4 g three times a day), as an active comparator, showed a remission rate of 33.6% but not significantly different from placebo.2 A larger trial would be needed to validate whether mesalamine MMX is more efficacious. Mesalamine MMX appears to be well tolerated. Adverse events include headache (3.4% to 5.6% vs 0.6% for placebo), flatulence (2.8% to 4% vs 2.8%), pruritus (0.6% to 1.1% vs 0%), and increase in ALT (0.6% to 1.1% vs 0%). The relative efficacy compared to other mesalamine formulations is not known. The wholesale cost for mesalamine MMX is $219 to $438 per month compared to about $170 for Asacol and Pentasa for induction of remission.
Clinical Implications
Ulcerative colitis is a chronic disease with a prevalence of about 250 per 100,000 individuals per year in the US.3 Sulfasalazine and mesalamine are the mainstays of therapy for mild-moderate active colitis that is not limited to the distal colon.4 However, mesalamine is generally better tolerated than sulfasalazine.5 Regimen complexity, tablet quantity and dose frequency are key factors associated with poor adherence in these patients.6 Mesalamine MMX provides a once-daily formulation with a low pill burden (2 to 4 tablets per day) that may be beneficial in patients in whom adherence is problematic.
References
1. Lialda Product Information. Shire Pharmaceutical, Inc. January 2007.
2. Kamm MA, et al. Gastroenterology. 2007;132:66-75.
3. http://digestive.niddk.nih.gov/statistics. Accessed 3/8/07.
4. Kornbluth A, et al. Am J Gastroenterol. 2004;99:1371-1385
5. Sutherland L, et al. Cochrane Database Syst Rev 2006 Apri 19;(2):CD000543.
6. Kane SV. Aliment Pharmacol Ther. 2006;23:577-585.
The first once-daily mesalamine formulation has been approved for the treatment of ulcerative colitis. The formulation uses the Multi Matrix System (MMX) technology designed to deliver the drug throughout the colon.Subscribe Now for Access
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