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Effects of renal impairment on the pharmacokinetics and pharmacodynamics of a novel dipeptidyl peptidase-4 inhibitor, evogliptin (DA-1229).
- Source :
-
Diabetes, obesity & metabolism [Diabetes Obes Metab] 2017 Feb; Vol. 19 (2), pp. 294-298. Date of Electronic Publication: 2016 Nov 24. - Publication Year :
- 2017
-
Abstract
- Evogliptin is a novel potent and selective dipeptidyl peptidase-4 (DPP-4) inhibitor. The aim of the present study was to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of evogliptin in participants with renal impairment (RI). An open-label, parallel-group clinical study was conducted in participants with mild, moderate and severe RI and in matched participants with normal renal function (NRF). A single oral 5-mg dose of evogliptin was administered and serial blood and urine samples were obtained to assess the PK and PD characteristics of evogliptin. Baseline urine samples were collected to evaluate endogenous CYP3A metabolic markers. The plasma exposure to evogliptin and degree of DPP-4 activity inhibition increased with decreasing renal function. The mean areas under the concentration-time curves from 0 to 120 hours were increased 1.2-, 1.8- and 1.98-fold in the mild, moderate and severe RI groups, respectively, compared with the NRF group. The levels of CYP3A metabolic markers were lower in the RI group than in the NRF group. The increase in the plasma concentration of evogliptin is unlikely to result in changes in its efficacy or safety, considering the results of previous clinical studies.<br /> (© 2016 John Wiley & Sons Ltd.)
- Subjects :
- Adult
Aged
Chromatography, Liquid
Cortisone analogs & derivatives
Cortisone metabolism
Cytochrome P-450 CYP3A metabolism
Dipeptidyl Peptidase 4 metabolism
Dipeptidyl-Peptidase IV Inhibitors blood
Dipeptidyl-Peptidase IV Inhibitors urine
Female
Glomerular Filtration Rate
Humans
Hydrocortisone analogs & derivatives
Hydrocortisone metabolism
Hydroxycholesterols metabolism
Male
Middle Aged
Piperazines blood
Piperazines urine
Republic of Korea
Severity of Illness Index
Tandem Mass Spectrometry
Dipeptidyl-Peptidase IV Inhibitors pharmacology
Piperazines pharmacology
Renal Insufficiency, Chronic metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1463-1326
- Volume :
- 19
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Diabetes, obesity & metabolism
- Publication Type :
- Academic Journal
- Accession number :
- 27761990
- Full Text :
- https://doi.org/10.1111/dom.12813