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Effect of renal impairment and haemodialysis on the pharmacokinetics of gemigliptin ( LC15 ‐0444)
Author(s) -
Shon J.H.,
Kim N.,
Park S.J.,
Oh M.K.,
Kim E.Y.,
Lee S.H.,
Kim Y.H.,
Shin J.G.
Publication year - 2014
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/dom.12292
Subject(s) - pharmacokinetics , medicine , pharmacology
This study evaluated the effects of renal impairment ( RI ) and haemodialysis ( HD ) on the pharmacokinetics of gemigliptin, a novel dipeptidyl peptidase‐4 ( DPP ‐4) inhibitor. After a 100 mg administration to subjects with normal renal function (n = 23) or RI (n = 24), plasma, urine or dialysate samples were analysed. Control subjects were matched to patients based on age, gender and body mass index. Patients with mild, moderate, severe RI and end‐stage renal disease ( ESRD ) showed 1.20, 2.04, 1.50 and 1.66‐fold (1.10, 1.49, 1.22 and 1.21‐fold) increase of mean area under the time‐plasma concentration curve from 0 to infinity (AUC inf ) [maximum plasma concentration (C max )] of gemigliptin, respectively. Pharmacokinetics of gemigliptin was comparable between HD and non‐ HD periods in ESRD patients. Less than 4% of the dose was removed by 4 h HD . RI appeared to have modest effect on the gemigliptin disposition. No dose adjustment in patients with RI is proposed on the basis of exposure–response relationship. Impact of HD on the removal of gemigliptin was negligible.