Relative bioavailability of an empagliflozin 25-mg/linagliptin 5-mg fixed-dose combination tablet

Abstract

This study shows that the FDC of empagliflozin 25 mg/linagliptin 5 mg can be regarded as bioequivalent to the individual tablets. Administering the tablet after food or a tablet with a slow-dissolution profile did not have a clinically-relevant impact on the bioavailability of empagliflozin/linagliptin FDC tablets. .

Modeling the renoprotective mechanisms of SGLT2 inhibition in hypertensive chronic kidney disease

“…Maximum concentration (505 ± 130 nmol/L) and plasma half‐life (10 ± 2 h) after 25 mg empagliflozin were used to compare single‐dose studies in healthy subjects (Seman et al, 2013) (Figure 3). Also, maximum empagliflozin concentration in the model (830 nmol/L) was within range with a study examining normal fasted subjects (700–1400 nmol/L) (Glund et al, 2017). Cumulative urinary glucose responses from this study were also used to validate the SGLT2 inhibitor model (Figure 3).…”

Linagliptin as add‐on to empagliflozin in a fixed‐dose combination in Japanese patients with type 2 diabetes: Glycaemic efficacy and safety profile in a two‐part, randomized, placebo‐controlled trial

“…Empagliflozin/linagliptin FDC (Empa/Lina) is the first SGLT2 inhibitor/DPP‐4 inhibitor combination approved in the United States and Europe for the treatment of T2DM. Empa/Lina FDC tablets (Empa 10 mg/Lina 5 mg [Empa/Lina 10/5] and Empa 25 mg/Lina 5 mg [Empa/Lina 25/5]) are bioequivalent to the combination of empagliflozin and linagliptin administered separately, and can be administered with or without food . Phase III randomized controlled trials conducted outside Japan have demonstrated the safety and efficacy of Empa/Lina FDC for the treatment of T2DM in patients who had not received antidiabetic therapy for approximately 12 weeks and in patients using metformin .…”

“…6 Because of the complementary mechanisms of action of SGLT2 and DPP-4 inhibitors, dual therapy improves glycaemic control in patients with T2DM without increasing the risk of hypoglycaemia or weight gain, 4 administered with or without food. 7 Phase III randomized controlled trials conducted outside Japan have demonstrated the safety and efficacy of Empa/Lina FDC for the treatment of T2DM in patients who had not received antidiabetic therapy for approximately 12 weeks and in patients using metformin. [8][9][10] The objective of this two-part study was to evaluate the efficacy and safety of Empa/Lina FDC in Japanese patients with T2DM who switched from empagliflozin monotherapy.…”