title: Effect of renal impairment and haemodialysis on the pharmacokinetics of gemigliptin (LC15-0444).
abstract: 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.
authors.affiliation: Department of Pharmacology, Inje University College of Medicine, Busan, South Korea; Department of Clinical Pharmacology and Clinical Trial Center, Busan Paik Hospital, Busan, South Korea.
authors.forename: J H
authors.initials: JH
authors.lastname: Shon
authors.forename: N
authors.initials: N
authors.lastname: Kim
authors.forename: S J
authors.initials: SJ
authors.lastname: Park
authors.forename: M K
authors.initials: MK
authors.lastname: Oh
authors.forename: E Y
authors.initials: EY
authors.lastname: Kim
authors.forename: S H
authors.initials: SH
authors.lastname: Lee
authors.forename: Y H
authors.initials: YH
authors.lastname: Kim
authors.forename: J G
authors.initials: JG
authors.lastname: Shin
mesh_terms: D019540:Area Under Curve; D003404:Creatinine / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D008297:Male; D008657:Metabolic Clearance Rate / Q000187:drug effects; D010881:Piperidones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011743:Pyrimidines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006435:Renal Dialysis; D051437:Renal Insufficiency / Q000378:metabolism / Q000628:therapy*
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; C534891:LC15-0444; D010881:Piperidones; D011743:Pyrimidines; D003404:Creatinine
keywords: DPP-4 inhibitor; gemigliptin; haemodialysis; pharmacokinetics; renal impairment; type 2 diabetes