OBJECTIVES: Empagliflozin is an orally available, potent and highly selective 
inhibitor of the sodium glucose cotransporter 2 (SGLT2). This study was 
undertaken to investigate the effect of food on the pharmacokinetics of 25 mg 
empagliflozin and to assess dose proportionality between 10 mg and 25 mg 
empagliflozin under fasted conditions.
MATERIALS AND METHODS: In this open-label, 3-way, cross-over study, 18 healthy 
volunteers received 3 single doses of empagliflozin in a randomized sequence (25 
mg empagliflozin under fasted conditions, 25 mg empagliflozin after a high-fat, 
high-calorie breakfast and 10 mg empagliflozin under fasted conditions), each 
separated by a washout period of at least 7 days. Serial plasma samples were 
collected at selected time points over a period of 72 hours.
RESULTS: Administration with food had no clinically relevant effect on the area 
under the plasma concentration-time curve (AUC0-∞) of empagliflozin (geometric 
mean ratio (GMR): 84.04, 90% confidence interval (CI): 80.86 - 87.34). The 
decrease observed in the maximum plasma concentrations (Cmax) of empagliflozin 
(GMR: 63.22, 90% CI: 56.74 - 70.44) when administered with food was not 
considered clinically meaningful. The increases in AUC0-∞ and Cmax for 10 mg vs. 
25 mg empagliflozin administered under fasting conditions were roughly 
dose-proportional, as demonstrated by the slope β of the regression lines being 
slightly less than 1 (slope β for AUC0-∞: 0.94, 95% CI: 0.90 - 0.97; slope β for 
Cmax: 0.91, 95% CI: 0.80 - 1.01). Empagliflozin was well tolerated under fed and 
fasting conditions.
CONCLUSIONS: The results support administration of empagliflozin tablets 
independently of food. Increases in empagliflozin exposure under fasting 
conditions were roughly dose-proportional between 10 mg and 25 mg empagliflozin.