Long‐term safety and efficacy of a novel once‐weekly oral trelagliptin as monotherapy or in combination with an existing oral antidiabetic drug in patients with type 2 diabetes mellitus: A 52‐week open‐label, phase 3 study

AIMS/INTRODUCTION: Trelagliptin is a novel once‐weekly oral dipeptidyl peptidase‐4 inhibitor for type 2 diabetes mellitus that was first approved in Japan. We evaluated long‐term safety and efficacy of trelagliptin in Japanese patients with type 2 diabetes mellitus. MATERIALS AND METHODS: This was a phase 3, multicenter, open‐label study to evaluate long‐term safety and efficacy of trelagliptin. Patients with type 2 diabetes mellitus inadequately controlled despite diet/exercise or treatment with one of the existing oral antidiabetic drugs along with diet/exercise received trelagliptin 100 mg orally once weekly for 52 weeks as monotherapy or combination therapies. The primary end‐points were the safety variables, and the secondary end‐points were glycosylated hemoglobin and fasting plasma glucose. RESULTS: A total of 680 patients received the following antidiabetic therapies: trelagliptin monotherapy (n = 248), combination with a sulfonylurea (n = 158), a glinide (n = 67), an α‐glucosidase inhibitor (n = 65), a biguanide (n = 70), or a thiazolidinedione (n = 72). During the study, 79.8% of the patients experienced at least one adverse event for monotherapy, 87.3% for combination with a sulfonylurea, 77.6% for a glinide, 81.5% for an α‐glucosidase inhibitor, 64.3% for a biguanide, and 84.7% for a thiazolidinedione, respectively. Most of the adverse events were mild or moderate. The change in glycosylated hemoglobin from baseline at the end of the treatment period was −0.74 to −0.25% for each therapy. CONCLUSIONS: Once‐weekly oral trelagliptin provides well‐tolerated long‐term safety and efficacy in both monotherapy and combination therapies in Japanese patients with type 2 diabetes mellitus.