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Published online: 27 June 2015
© Springer International Publishing Switzerland 2015
Abstract Trelagliptin (Zafatek®) is an orally active dipeptidyl peptidase (DPP)-4 inhibitor developed by Takeda and approved in Japan for the treatment of type 2 diabetes mellitus (T2DM). Unlike other approved agents of its class, which are usually administered once daily, trelagliptin can be administered once weekly. Phase II development of trelagliptin was discontinued in the USA and EU, as Takeda considered that the costs associated with obtaining approval in these markets were prohibitive. This article summarizes the milestones in the development of trelagliptin leading to this first approval for T2DM.
1 Introduction
Trelagliptin (Zafatek) is a novel, orally active, highly selective dipeptidyl peptidase (DPP)-4 (also known as T-cell activation antigen CD26) inhibitor that has been approved for use in type 2 diabetes mellitus (T2DM) in Japan [1]. Currently, in the treatment of T2DM, DPP-4 inhibitors are recommended as add-on therapy with metformin when glycaemic goals are not achieved with metformin alone, or recommended for first-line therapy if metformin cannot be used [2]. The addition of a DPP-4 inhibitor is also recommended when glycaemic control has not been achieved with metformin plus a sulfonylurea, a thiazolidinedione, a sodium-glucose co-transporter 2 inhibitor or insulin [2].
Unlike other approved agents of its class (e.g. alogliptin, linagliptin, sitagliptin), which are usually administered once daily, trelagliptin is administered once weekly [1]. Adherence to treatment is often poor in patients with chronic conditions, including T2DM[3], and drug regimens with reduced dosing frequencies are usually preferred and are associated with improved treatment adherence compared with oncedaily dosing [4]. Therefore, the once-weekly administration regimen of trelagliptin may lead to improved adherence compared with once-daily gliptins, with the potential for improved glycaemic control in patients with T2DM.
The new drug application for trelagliptin in the treatment of T2DM in Japan was filed by Takeda in March 2014, and the drug was approved by the Japanese Ministry of Health, Labour and Welfare (MHLW) in March 2015 [1]. Approval was granted on the basis of positive results from phase III trials conducted in patients with T2DM.
Trelagliptin had undergone phase II trials outside of Japan; however, Takeda discontinued the development of trelagliptin in the USA and EU in October 2014 after considering the costs...