Clinical Medicine Insights: Therapeutics

MMXTM mesalazine is a novel delayed release mesalazine formulation with a high-strength 1.2 g tablet for the treatment of active mild to moderate colitis and maintenance of remission. In vitro and in vivo studies show initiation of drug release in the terminal ileum and caecum with gradual release of 5-ASA as the tablet passes through the colon. Pharmacokinetic data are comparable to other 5-ASA formulations with low systemic absorption and high levels in feces and in mucosal biopsies in the left colon. Clinical trials have shown high rates of clinical and endoscopic remission in active mild to moderate colitis over 8 weeks with a 2.4 g once daily dose. There do not appear to be higher remission rates with the 4.8 g dose. Prolongation of treatment with a further 8 weeks of 2.4 g twice daily can induce remission in those failing the initial 8 weeks of therapy. A maintenance study enrolling patients who achieved remission in the acute studies showed high rates of remission maintained at one year with 1.2 g twice daily (68.5%) and 2.4 g once daily (64.4%) using the strict definition of remission (including mucosal healing) that was used in the active treatment trials. The drug is safe and effective in colitis. The high tablet strength, and once-daily dosage make this formulation a welcome addition to therapy options for patients with colitis.