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Safety, tolerability, pharmacokinetics and pharmacodynamics following 4 weeks' treatment with empagliflozin once daily in patients with type 2 diabetes.
Diabetes Obes Metab. 2013 Jul; 15(7):613-21.DO

Abstract

AIM

To investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of empagliflozin in patients with type 2 diabetes following oral administration of 10, 25 or 100 mg doses once daily over 28 days.

METHODS

A total of 78 patients were assigned to empagliflozin 10 mg (n = 16), 25 mg (n = 16) or 100 mg (n = 30) or placebo (n = 16) for 28 days. Assessments included adverse events (AEs) and pharmacokinetic and pharmacodynamic endpoints.

RESULTS

Empagliflozin exposure increased dose-proportionally over the dose range 10-100 mg and showed linear pharmacokinetics with respect to time. Urinary glucose excretion (UGE) increased from baseline to day 1 by 74, 90 and 81 g with empagliflozin 10, 25 and 100 mg, respectively. The increases in UGE were maintained over 28 days with multiple dosing. Virtually no change in UGE was observed in the placebo group. Significant reductions from baseline in mean daily plasma glucose and fasting plasma glucose were observed with empagliflozin compared with placebo. The incidence of AEs was similar in the empagliflozin and placebo groups (50.0, 56.3 and 66.7% with empagliflozin rising doses and 62.5% with placebo). The most frequently reported AEs were pollakiuria (10.3%), nasopharyngitis (9.0%), constipation (9.0%) and headache (7.7%).

CONCLUSIONS

Oral administration of empagliflozin at doses of 10, 25 or 100 mg once daily over 28 days resulted in significant increases in UGE and reductions in blood glucose compared with placebo, and were well tolerated in patients with type 2 diabetes.

Authors+Show Affiliations

Profil, Hellersbergstrasse 9, Neuss, Germany. tim.heise@profil.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Multicenter Study
Randomized Controlled Trial

Language

eng

PubMed ID

23356556

Citation

Heise, T, et al. "Safety, Tolerability, Pharmacokinetics and Pharmacodynamics Following 4 Weeks' Treatment With Empagliflozin once Daily in Patients With Type 2 Diabetes." Diabetes, Obesity & Metabolism, vol. 15, no. 7, 2013, pp. 613-21.
Heise T, Seewaldt-Becker E, Macha S, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics following 4 weeks' treatment with empagliflozin once daily in patients with type 2 diabetes. Diabetes Obes Metab. 2013;15(7):613-21.
Heise, T., Seewaldt-Becker, E., Macha, S., Hantel, S., Pinnetti, S., Seman, L., & Woerle, H. J. (2013). Safety, tolerability, pharmacokinetics and pharmacodynamics following 4 weeks' treatment with empagliflozin once daily in patients with type 2 diabetes. Diabetes, Obesity & Metabolism, 15(7), 613-21. https://doi.org/10.1111/dom.12073
Heise T, et al. Safety, Tolerability, Pharmacokinetics and Pharmacodynamics Following 4 Weeks' Treatment With Empagliflozin once Daily in Patients With Type 2 Diabetes. Diabetes Obes Metab. 2013;15(7):613-21. PubMed PMID: 23356556.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Safety, tolerability, pharmacokinetics and pharmacodynamics following 4 weeks' treatment with empagliflozin once daily in patients with type 2 diabetes. AU - Heise,T, AU - Seewaldt-Becker,E, AU - Macha,S, AU - Hantel,S, AU - Pinnetti,S, AU - Seman,L, AU - Woerle,H J, Y1 - 2013/02/17/ PY - 2012/08/03/received PY - 2012/09/27/revised PY - 2012/12/28/accepted PY - 2013/1/30/entrez PY - 2013/1/30/pubmed PY - 2014/1/11/medline SP - 613 EP - 21 JF - Diabetes, obesity & metabolism JO - Diabetes Obes Metab VL - 15 IS - 7 N2 - AIM: To investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of empagliflozin in patients with type 2 diabetes following oral administration of 10, 25 or 100 mg doses once daily over 28 days. METHODS: A total of 78 patients were assigned to empagliflozin 10 mg (n = 16), 25 mg (n = 16) or 100 mg (n = 30) or placebo (n = 16) for 28 days. Assessments included adverse events (AEs) and pharmacokinetic and pharmacodynamic endpoints. RESULTS: Empagliflozin exposure increased dose-proportionally over the dose range 10-100 mg and showed linear pharmacokinetics with respect to time. Urinary glucose excretion (UGE) increased from baseline to day 1 by 74, 90 and 81 g with empagliflozin 10, 25 and 100 mg, respectively. The increases in UGE were maintained over 28 days with multiple dosing. Virtually no change in UGE was observed in the placebo group. Significant reductions from baseline in mean daily plasma glucose and fasting plasma glucose were observed with empagliflozin compared with placebo. The incidence of AEs was similar in the empagliflozin and placebo groups (50.0, 56.3 and 66.7% with empagliflozin rising doses and 62.5% with placebo). The most frequently reported AEs were pollakiuria (10.3%), nasopharyngitis (9.0%), constipation (9.0%) and headache (7.7%). CONCLUSIONS: Oral administration of empagliflozin at doses of 10, 25 or 100 mg once daily over 28 days resulted in significant increases in UGE and reductions in blood glucose compared with placebo, and were well tolerated in patients with type 2 diabetes. SN - 1463-1326 UR - https://www.unboundmedicine.com/medline/citation/23356556/Safety_tolerability_pharmacokinetics_and_pharmacodynamics_following_4_weeks'_treatment_with_empagliflozin_once_daily_in_patients_with_type_2_diabetes_ L2 - https://doi.org/10.1111/dom.12073 DB - PRIME DP - Unbound Medicine ER -