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Effect of food on the pharmacokinetics of empagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor, and assessment of dose proportionality in healthy volunteers.
Int J Clin Pharmacol Ther. 2013 Nov; 51(11):873-9.IJ

Abstract

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.

Authors+Show Affiliations

Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT, USA, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach, and Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim, Germany.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24152604

Citation

Macha, Sreeraj, et al. "Effect of Food On the Pharmacokinetics of Empagliflozin, a Sodium Glucose Cotransporter 2 (SGLT2) Inhibitor, and Assessment of Dose Proportionality in Healthy Volunteers." International Journal of Clinical Pharmacology and Therapeutics, vol. 51, no. 11, 2013, pp. 873-9.
Macha S, Jungnik A, Hohl K, et al. Effect of food on the pharmacokinetics of empagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor, and assessment of dose proportionality in healthy volunteers. Int J Clin Pharmacol Ther. 2013;51(11):873-9.
Macha, S., Jungnik, A., Hohl, K., Hobson, D., Salsali, A., & Woerle, H. J. (2013). Effect of food on the pharmacokinetics of empagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor, and assessment of dose proportionality in healthy volunteers. International Journal of Clinical Pharmacology and Therapeutics, 51(11), 873-9.
Macha S, et al. Effect of Food On the Pharmacokinetics of Empagliflozin, a Sodium Glucose Cotransporter 2 (SGLT2) Inhibitor, and Assessment of Dose Proportionality in Healthy Volunteers. Int J Clin Pharmacol Ther. 2013;51(11):873-9. PubMed PMID: 24152604.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of food on the pharmacokinetics of empagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor, and assessment of dose proportionality in healthy volunteers. AU - Macha,Sreeraj, AU - Jungnik,Arvid, AU - Hohl,Kathrin, AU - Hobson,Dagmar, AU - Salsali,Afshin, AU - Woerle,Hans J, PY - 2013/10/25/entrez PY - 2013/10/25/pubmed PY - 2014/1/17/medline SP - 873 EP - 9 JF - International journal of clinical pharmacology and therapeutics JO - Int J Clin Pharmacol Ther VL - 51 IS - 11 N2 - 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. SN - 0946-1965 UR - https://www.unboundmedicine.com/medline/citation/24152604/Effect_of_food_on_the_pharmacokinetics_of_empagliflozin_a_sodium_glucose_cotransporter_2__SGLT2__inhibitor_and_assessment_of_dose_proportionality_in_healthy_volunteers_ L2 - http://www.dustri.com/nc/journals-in-english.html?artId=10927 DB - PRIME DP - Unbound Medicine ER -