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      No Relevant Pharmacokinetic Drug–Drug Interaction Between the Sodium-Glucose Co-Transporter-2 Inhibitor Empagliflozin and Lobeglitazone, a Peroxisome Proliferator-Activated Receptor-γ Agonist, in Healthy Subjects

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          Abstract

          Purpose

          Combination therapy with insulin-independent sodium-glucose cotransporter 2 inhibitors and thiazolidinedione drugs, such as lobeglitazone, has been reported to elicit potential additive efficacy in glycemic control in type 2 diabetes mellitus. This study was conducted to evaluate the pharmacokinetic (PK) drug–drug interactions between empagliflozin and lobeglitazone in healthy subjects.

          Subjects and Methods

          A randomized, open-label, multiple-dose study was conducted in 30 healthy subjects using a three-treatment, six-sequence, three-way crossover design. Subjects received one of the following treatments once daily for 5 days in each period: 25 mg empagliflozin, 0.5 mg lobeglitazone sulfate, or a combination. Serial blood sampling before every dose and up to 24 h after the last dose was performed during each treatment period. The PK parameters were estimated using noncompartmental methods with the plasma empagliflozin and lobeglitazone concentrations. The absence of a PK interaction was construed as the 90% confidence interval (90% CI) of maximum concentration at steady state (C max,ss) and area under the concentration-time curve over the dosing interval (AUC tau) for combination therapy-to-monotherapy ratios within the limits of 0.80–1.25.

          Results

          The steady-state plasma empagliflozin and lobeglitazone concentration-time profiles of combination therapy and monotherapy were comparable in the 25 subjects who completed the study. Coadministration of empagliflozin with lobeglitazone did not affect empagliflozin PK (with 90% CIs of 0.956–1.150 and 0.945–1.133 for C max,ss and AUC tau, respectively). Likewise, empagliflozin did not affect lobeglitazone C max,ss or AUC tau (with 90% CIs of 0.869–0.995 and 0.851–1.018, respectively). All treatment groups tolerated mild adverse events well.

          Conclusion

          The lack of PK interactions between lobeglitazone and empagliflozin in combination therapy, along with their good tolerability, indicates that the two drugs can be coadministered without dose adjustment.

          Trial Registration Number

          NCT02854748, Registered on August 7, 2016.

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          Most cited references 38

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          World Medical Association Declaration of Helsinki: ethical principles for medical research involving human subjects.

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            Epidemic obesity and type 2 diabetes in Asia.

            The proportions of people with type 2 diabetes and obesity have increased throughout Asia, and the rate of increase shows no sign of slowing. People in Asia tend to develop diabetes with a lesser degree of obesity at younger ages, suffer longer with complications of diabetes, and die sooner than people in other regions. Childhood obesity has increased substantially and the prevalence of type 2 diabetes has now reached epidemic levels in Asia. The health consequences of this epidemic threaten to overwhelm health-care systems in the region. Urgent action is needed, and advocacy for lifestyle changes is the first step. Countries should review and implement interventions, and take a comprehensive and integrated public-health approach. At the level of primary prevention, such programmes can be linked to other non-communicable disease prevention programmes that target lifestyle-related issues. The cost of inaction is clear and unacceptable.
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              Global Prevalence of Diabetes: Estimates for the year 2000 and projections for 2030

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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                dddt
                dddt
                Drug Design, Development and Therapy
                Dove
                1177-8881
                28 April 2021
                2021
                : 15
                : 1725-1734
                Affiliations
                [1 ]Department of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital , Cheongju, Republic of Korea
                [2 ]Department of Pharmacology and Clinical Pharmacology, Dong-A University College of Medicine, Dong-A University Hospital , Busan, Republic of Korea
                Author notes
                Correspondence: Min Kyu Park Department of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital , 776, 1 Sunhwan-ro, Seowon-gu, Cheongju-si, Chungcheongbuk-do, 28644, Republic of KoreaTel +82 43 269 8708Fax +82 43 269 8724 Email mk_park@cbnuhctc.com
                [*]

                These authors contributed equally to this work

                Article
                302215
                10.2147/DDDT.S302215
                8089085
                © 2021 Kim et al.

                This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms ( https://www.dovepress.com/terms.php).

                Page count
                Figures: 4, Tables: 5, References: 39, Pages: 10
                Funding
                Funded by: Chong Kun Dang Pharm;
                This study was sponsored by Chong Kun Dang Pharm.
                Categories
                Original Research

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