Effects of renal impairment on the pharmacokinetics and pharmacodynamics of a novel dipeptidyl peptidase-4 inhibitor, evogliptin (DA-1229)

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• 作者：Jaeseong Oh ; Andrew HyoungJin Kim ; SeungHwan Lee ; Hyunjeong Cho ; Yon Su Kim ; Mi Young Bahng ; Seo Hyun Yoon ; Joo-Youn Cho ; In-Jin Jang and Kyung-Sang Yu
• 刊名：Diabetes, Obesity and Metabolism
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：19
• 期：2
• 页码：294-298
• 全文大小：395K
• ISSN：1463-1326

文摘

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.