Introducing a Novel Once-weekly Dipeptidyl Peptidase 4 Inhibitor: Trelagliptin in India.

India faces a growing burden of type 2 diabetes mellitus (T2DM), necessitating innovative treatments that improve glycemic control, reduce glycemic variability (GV), and enhance patient adherence. Dipeptidyl peptidase 4 (DPP-4) inhibitors are established antidiabetic agents; however, once- or twice-daily dosing often limits long-term compliance. Trelagliptin, a novel once-weekly DPP-4 inhibitor, addresses this issue with an extended half-life and superior molecular stability, enabling sustained DPP-4 inhibition and significant GV reduction. Improved glycemic control with trelagliptin can potentially lower the risk of macrovascular and microvascular complications associated with T2DM. Trelagliptin, developed and launched in India by Zuventus Healthcare Limited under the brand name Trelaglip®, offers prolonged efficacy and high selectivity in inhibiting the DPP-4 enzyme, helping minimize side effects. Development began with in-house active pharmaceutical ingredient (API) synthesis, followed by successful formulation and stability studies. A bioequivalence study confirmed pharmacokinetic equivalence with the reference product by Takeda, Japan. In a randomized phase 3 clinical trial involving patients with glycated hemoglobin (HbA1c) ≥8%, trelagliptin showed greater HbA1c reduction (-1.25%) as compared to vildagliptin (-1.15%) and a similar safety profile. Mild adverse events occurred in 6.67% of trelagliptin users compared to 9.17% with vildagliptin. This article outlines the development and regulatory journey leading to trelagliptin's first approval in India by the Central Drugs Standard Control Organization (CDSCO) in December 2024. Phase 4 real-world evidence studies are currently ongoing in India to assess long-term safety and efficacy.