Effect of renal impairment and haemodialysis on the pharmacokinetics of gemigliptin (LC15-0444).
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 (AUCinf) [maximum plasma concentration (Cmax)] 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.
['Shon|J H|JH|', 'Kim|N|N|', 'Park|S J|SJ|', 'Oh|M K|MK|', 'Kim|E Y|EY|', 'Lee|S H|SH|', 'Kim|Y H|YH|', 'Shin|J G|JG|']
D019540:Area Under Curve D003404:Creatinine D054873:Dipeptidyl-Peptidase IV Inhibitors D005260:Female D006801:Humans D008297:Male D008657:Metabolic Clearance Rate D010881:Piperidones D011743:Pyrimidines D006435:Renal Dialysis D051437:Renal Insufficiency
renal impairment haemodialysis pharmacokinetics gemigliptin DPP-4 inhibitor type 2 diabetes