https://orcid.org/0000-0001-8568-7320
![Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days]({"type":"image" , "src" : "/sda/5925/TOC-Subject-Sample-2021-Bioscience.jpg"})
Abstract
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.
Acknowledgment
This study was funded by LG Chem., Seoul, Republic of Korea.
Data Sharing Statement
The authors do not intend to share substantial data of this study, but they are ready to share de-identified file of substantial data in excel format and all other study-related documents, at any specific time for any period, if the editorial board requires.
Disclosure
Kyoung Ryun Park is currently employed by Boryung Co., Ltd. Her contribution to the manuscript was based on her prior employment, and the current manuscript does not reflect any position of Boryung Co., Ltd. The authors report no other conflicts of interest in this work.