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A Fixed-Dose Combination Of Gemigliptin And Rosuvastatin Exhibits Similar Pharmacokinetics, Pharmacodynamics, And Safety Compared To That Of A Loose Combination In Healthy Subjects

Authors Kim E, Park KR, Jang IJ, Yu KS, Lee S

Received 4 December 2018

Accepted for publication 25 March 2019

Published 13 November 2019 Volume 2019:13 Pages 3879—3885


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2

Editor who approved publication: Dr Sukesh Voruganti

Eunwoo Kim,1 Kyoung Ryun Park,1 In-Jin Jang,1 Kyung-Sang Yu,1 SeungHwan Lee1,2

1Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, Republic of Korea; 2Clinical Trials Center, Seoul National University Hospital, Seoul, Republic of Korea

Correspondence: SeungHwan Lee
Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, 101 Daehak-ro, Jongno-gu, Seoul 03080, Republic of Korea
Tel +82-2-2072-3520
Fax +82-2-742-9252

Purpose: Fixed-dose combination (FDC) of gemigliptin and rosuvastatin may improve medication compliance of patients with comorbid type 2 diabetes and dyslipidemia. Pharmacokinetics (PK), pharmacodynamics (PD), and safety of gemigliptin/rosuvastatin 50/20 mg FDC was compared with a loose combination of individual tablets in healthy subjects.
Patients and methods: A randomized, open-label, single-dose, two-period, two-sequence, two-treatment crossover study was conducted. Subjects received FDC or a loose combination of gemigliptin (50 mg) and rosuvastatin (20 mg) during each period, with a 14-day washout. Serial blood samples were collected up to 72 hrs after dosing to measure plasma concentrations of gemigliptin, its active metabolite LC15-0636, and rosuvastatin for PK assessment, and DPP-4 activity for PD assessment. PK and PD parameters were calculated using a non-compartmental method. Safety profiles were evaluated throughout the study.
Results: Thirty-seven subjects completed the study. The concentration-time profiles of gemigliptin, LC15-0636, and rosuvastatin were similar between FDC and loose combination, respectively. For each of the three compounds, the geometric mean ratios (90% confidence interval) of FDC to loose combination for Cmax and AUClast fell within the bioequivalence range of 0.8–1.25. Inhibition of DPP-4 activity–time profiles after administration of FDC and loose combination was overlapping, and Imax and AUEClast were similar. Both FDC and the loose combination were well tolerated.
Conclusion: PK, PD, and safety profiles of gemigliptin, its metabolite, and rosuvastatin were similar between FDC and loose combination. The FDC of gemigliptin (50 mg) and rosuvastatin (20 mg) can be used as an alternative to a loose combination, which is expected to improve patient compliance.

Keywords: DPP-4 inhibitor, statin, type 2 diabetes, dyslipidemia, pharmacokinetics

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