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Pharmacokinetics and safety of evogliptin in hepatically impaired patients

 Taegon Hong  ;  Byung Hak Jin  ;  Choon Ok Kim  ;  Byung Won Yoo  ;  Dasohm Kim  ;  Jung Il Lee  ;  Beom Kyung Kim  ;  Sang Hoon Ahn  ;  Do Young Kim  ;  Jun Yong Park  ;  Min Soo Park 
 BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, Vol.87(7) : 2.757-2.766, 2021-07 
Journal Title
Issue Date
Area Under Curve ; Diabetes Mellitus, Type 2* / drug therapy ; Dipeptidyl-Peptidase IV Inhibitors* / adverse effects ; Female ; Humans ; Hypoglycemic Agents / adverse effects ; Liver Diseases* ; Male ; Piperazines
DPP-4 inhibitor ; Type 2 diabetes mellitus ; evogliptin ; hepatic impairment ; pharmacokinetics
Aims: Evogliptin is a potent and selective dipeptidyl peptidase-4 inhibitor for glycaemic control in patients with type 2 diabetes mellitus. Since evogliptin is mainly eliminated through hepatic metabolism, we investigated the pharmacokinetics (PKs) and safety characteristics of evogliptin in Korean patients with mild or moderate hepatic impairment.

Methods: An open-label, parallel-group study was conducted in patients with mild or moderate hepatic impairment and healthy control subjects matched to each patient for sex, age and body mass index. A single dose (5 mg) of evogliptin was administered orally, and serial blood samples were collected over 120 h to assess the PK profile of evogliptin and its main metabolites (M7 and M8).

Results: Patients with mild hepatic impairment and their matched healthy controls showed similar maximum concentration (Cmax ) and area under the concentration-time curve values from 0 to 120 h (AUClast ); the geometric mean ratio (GMR) and 90% confidence interval (CI) were 1.04 (0.80, 1.35) and 1.01 (0.90, 1.14), respectively. Exposure to evogliptin (Cmax and AUClast ) was increased by about 40% in patients with moderate hepatic impairment-the GMR and 90% CI were 1.37 (1.09, 1.72) and 1.44 (1.18, 1.75), respectively. The metabolic ratios of M7 and M8 were lower in patients with moderate hepatic impairment than in matched healthy controls. Evogliptin was well tolerated by both patients and healthy subjects.

Conclusion: Although evogliptin exposure was increased in patients with moderate hepatic impairment, the increase is unlikely to affect safety and efficacy adversely, and no dose adjustment is warranted.
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6. Others (기타) > Dept. of Clinical Pharmacology (임상시험센터) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Internal Medicine (내과학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Pediatrics (소아과학교실) > 1. Journal Papers
Yonsei Authors
Kim, Do Young(김도영)
Kim, Beom Kyung(김범경) ORCID logo https://orcid.org/0000-0002-5363-2496
Kim, Choon Ok(김춘옥) ORCID logo https://orcid.org/0000-0002-2319-1108
Yoo, Byung Won(류병원) ORCID logo https://orcid.org/0000-0001-6895-1484
Park, Min Soo(박민수) ORCID logo https://orcid.org/0000-0002-4395-9938
Park, Jun Yong(박준용) ORCID logo https://orcid.org/0000-0001-6324-2224
Ahn, Sang Hoon(안상훈) ORCID logo https://orcid.org/0000-0002-3629-4624
Lee, Jung Il(이정일) ORCID logo https://orcid.org/0000-0002-0142-1398
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