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Effect of a high‐fat meal on the pharmacokinetics of dapagliflozin, a selective SGLT2 inhibitor, in healthy subjects
Author(s) -
Kasichayanula S.,
Liu X.,
Zhang W.,
Pfister M.,
Reele S. B.,
Aubry A.F.,
LaCreta F. P.,
Boulton D. W.
Publication year - 2011
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.1463-1326.2011.01397.x
Subject(s) - dapagliflozin , cmax , pharmacokinetics , urine , crossover study , meal , medicine , endocrinology , chemistry , pharmacology , type 2 diabetes , diabetes mellitus , placebo , alternative medicine , pathology
Dapagliflozin is a potent and selective inhibitor of sodium–glucose co‐transporter type 2 that is being developed for the treatment of type 2 diabetes mellitus. This open‐label, randomized, two‐period, two‐treatment (single doses of 10‐mg dapagliflozin fasted or fed), crossover study was conducted to evaluate the effect of a high‐fat meal on the pharmacokinetics of dapagliflozin in 14 healthy subjects. Compared to the fasted state, a high‐fat meal decreased mean dapagliflozin maximum plasma concentrations (C max ) by 31%, increased the time to C max ( T max ) by 1 h, but did not affect overall dapagliflozin systemic exposure [area under the plasma concentration‐time curve (AUC)]. As the cumulative (daily) amount of glucose excreted in the urine induced by dapagliflozin is dependent upon dapagliflozin AUC, the effect of food on dapagliflozin C max is unlikely to have a clinically meaningful effect on dapagliflozin's efficacy. On the basis of these findings, dapagliflozin can be administered without regard to meals.