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Long‐term treatment with empagliflozin, a novel, potent and selective SGLT‐2 inhibitor, improves glycaemic control and features of metabolic syndrome in diabetic rats
Author(s) -
Thomas L.,
Grempler R.,
Eckhardt M.,
Himmelsbach F.,
Sauer A.,
Klein T.,
Eickelmann P.,
Mark M.
Publication year - 2012
Publication title -
diabetes, obesity and metabolism
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.445
H-Index - 128
eISSN - 1463-1326
pISSN - 1462-8902
DOI - 10.1111/j.1463-1326.2011.01518.x
Subject(s) - empagliflozin , type 2 diabetes , medicine , diabetes mellitus , endocrinology , insulin , excretion , glucose clamp technique , pharmacology , insulin resistance , insulin sensitivity
Empagliflozin is a potent, selective sodium glucose co‐transporter‐2 inhibitor that is in development for the treatment of type 2 diabetes. This series of studies was conducted to assess the in vivo pharmacological effects of single or multiple doses of empagliflozin in Zucker diabetic fatty rats. Single doses of empagliflozin resulted in dose‐dependent increases in urinary glucose excretion and reductions in blood glucose levels. After multiple doses (5 weeks), fasting blood glucose levels were reduced by 26 and 39% with 1 and 3 mg/kg empagliflozin, respectively, relative to vehicle. After 5 weeks, HbA1c levels were reduced (from a baseline of 7.9%) by 0.3 and 1.1% with 1 and 3 mg/kg empagliflozin, respectively, versus an increase of 1.1% with vehicle. Hyperinsulinaemic–euglycaemic clamp indicated improved insulin sensitivity with empagliflozin after multiple doses versus vehicle. These findings support the development of empagliflozin for the treatment of type 2 diabetes.