Efficacy and tolerability of
sitagliptin, a dipeptidyl peptidase-4 inhibitor, were assessed in Japanese patients with
type 2 diabetes. In a multicenter, double-blind, randomized, placebo-controlled trial in Japan, 151 patients with inadequate
glycemic control [HbA(1c) > or =6.5% to <10%, fasting plasma
glucose (FPG) > or =126 to < or =240 mg/dL] were randomized to once-daily
sitagliptin 100mg or placebo for 12 weeks. After 12 weeks, the least squares (LS) mean change from baseline HbA(1c) was -0.65% (95% CI: -0.80, -0.50) with
sitagliptin versus 0.41% (0.26, 0.56) with placebo [between-group difference=-1.05% (-1.27, -0.84); p<0.001]. LS mean change from baseline FPG was -22.5mg/dL (95% CI: -28.0, -17.0) with
sitagliptin versus 9.4 mg/dL (3.9, 14.9) with placebo [between-group difference=-31.9 mg/dL (95% CI: -39.7,-24.1); p<0.001]. More patients achieved HbA(1c) <7% or <6.5% with
sitagliptin than with placebo (p<0.001). Following a meal tolerance test, 2-h postprandial
glucose was significantly reduced with
sitagliptin relative to placebo. Clinical and laboratory adverse experiences were similar between treatments, with no reported
hypoglycemia adverse events with
sitagliptin.
Body weight was unchanged relative to baseline in the
sitagliptin group (-0.1 kg), but significantly (p<0.01) different relative to the placebo group (-0.7 kg). In this study, once-daily
sitagliptin 100mg for 12 weeks improved fasting and postprandial
glycemic control and was generally well tolerated in Japanese patients with
type 2 diabetes.