薬理と治療

Abstract

Background and Aim Anagliptin, a novel dipeptidyl peptidase-4 inhibitor, has been used in monotherapy and combination therapy with α-glucosidase inhibitors, biguanides, sulfonylureas, or thiazolidinediones for patients with type 2 diabetes in Japan. We investigated the efficacy and safety of anagliptin add to insulin therapy in a multi-center, randomized, placebo controlled, double-blind, parallel-group study with an open-label, 40 weeks extension in Japanese patients with type 2 diabetes mellitus. Methods A total of 123 subjects with type 2 diabetes receiving insulin therapy were treated with 100 mg of anagliptin or placebo twice a day for 12 weeks. Thereafter, all subjects continued on anagliptin 100 mg twice a day in an open-label extension for 40 weeks. Patients who did not achieve the HbA1c goal（less than 7.0％）at either visit from week 28 to week 40 were placed on anagliptin 200 mg twice a day. The primary endpoint was the change in HbA1c from baseline to the end of the double-blind period（week 12）. Results After 12 weeks, HbA1c in anagliptin-treated group were significantly decreased compared to those in placebo-treated group. This significant reduction of HbA1c was observed with any type of insulin therapy. Postprandial glucose, area under the curve（AUC）of glucose, 1,5-AG, glycoalbumin in anagliptin-treated group were also significantly improved compared to those in the placebo-treated group. Significant reductions of HbA1c from baseline were sustained through 52 weeks. The most frequent adverse event is hypoglycemia which was not statistically different in the placebo-treated group and anagliptin-treated group. We did not observe any clinically important adverse events else. Conclusions We demonstrated that anagliptin was effective and well tolerated in the treatment of the patients with type 2 diabetes mellitus receiving insulin therapy. These results suggest that anagliptin is a useful add-on insulin therapy in type 2 diabetes.