Investigation of a High-Dose pH-Dependent-Release Mesalazine on the Induction of Remission in Active Crohn’s Disease

INTRODUCTION The effect of mesalazine in treating active Crohn's disease (CD) remains controversial, possibly due to the various formulae of mesalazine used to treat inflammation located in different regions of the digestive tract. METHODS This exploratory, multicenter, uncontrolled, open-label study included 17 patients with active CD. The inclusion criteria were patients with a CD activity index (CDAI) of ≥ 200 and <350, and in whom mucosal lesions were observed in the area from the terminal ileum to the rectum using colonoscopy (CS). Each patient was treated with pH-dependent-release mesalazine at 4.8 g/day. The drug was administered three times daily for 12 weeks. Efficacy was evaluated by the change in CDAI at the time of final observation (at week 12 or at discontinuation), and safety was evaluated by the incidence of adverse events (AEs) and adverse drug reactions (ADRs). RESULTS In the full analysis set (n = 17), the change in CDAI at the time of final observation was -67.4, and the mean change in CDAI from baseline was -49.3 at week 2, -61.8 at week 4, -78.3 at week 8, and -101.1 at week 12. A statistically significant improvement was observed from week 2 to week 12 compared with baseline, and the incidences of AEs and ADRs were 94.1 and 58.8%, respectively. All events were known events, as the results suggested, which is in line with the known safety profile of pH-dependent-release mesalazine. CONCLUSIONS The results suggest that the administration of pH-dependent-release mesalazine 4.8 g/day for 12 weeks could be an effective and highly safe treatment option for patients with mild to moderately active CD in whom mucosal lesions were observed in the area from the terminal ileum to the rectum. TRIAL REGISTRATION NUMBER JapicCTI-111460.