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Exploring the clinical pharmacokinetics and pharmacodynamics of SGLT2 inhibitor, empagliflozin: a systematic review

Saleem T, Rasool MF, Saeed H, Alqahtani F

Drug metabolism reviews, 2026

Abstract

Abstract Empagliflozin is a potent, highly selective antihyperglycemic agent indicated for the treatment of adults with type 2 diabetes mellitus. This review aims to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) parameters of empagliflozin in healthy and diseased subjects. Google Scholar, PubMed, and Cochrane Library databases were systematically searched for PK and PD studies on empagliflozin. Of the 1,340 articles identified, 28 studies met the eligibility criteria and were involved in this systematic review. PK analysis showed dose-proportional increases in area under the curve for empagliflozin from 0 to infinity (AUC0–∞), similar bioavailability across formulations, and reduced absorption under fed conditions. In healthy subjects, urinary glucose excretion (UGE) after an evening dose of empagliflozin was approximately 1.7-fold higher compared with morning administration. The AUC0-∞ for empagliflozin in patients with severe renal impairment was significantly higher than in subjects with normal renal function, i.e. 7485.1 ng.hr/mL vs. 4779.646 ng.hr/mL. The maximum plasma concentration (Cmax) of empagliflozin was 1.4-fold greater in patients with severe liver impairment. The AUC0-∞ in the fasting condition was significantly greater than that of the fed state. Furthermore, empagliflozin exhibited a Cmax that was 1.1-fold greater when administered alone but decreased in the presence of linagliptin. This systematic review consolidates all available PK and PD…

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