Evaluation of the pharmacokinetics of the DPP-4 inhibitor gemigliptin when coadministered with rosuvastatin or irbesartan to healthy subjects. (February 2015)

• Record Type: Journal Article
• Authors: Choi, Hee Youn; Lim, Hyeong-Seok; Kim, Yo Han; Jeon, Hae Sun; Kim, Mi Jo; Lee, Shi Hyang; Jung, Jong Hyuk; Lee, Young Kyoung; Kim, Hyun Jeong; Bae, Kyun-Seop
• Is Part Of: Current medical research and opinion. Volume 31:Number 2(2015:Feb.)
• Page Start: 229
• Page End: 241
• Publication Date: 2015-02
• Subjects: Clinical medicine -- Periodicals; Therapeutics -- Periodicals; 615.5
• DOI: 10.1185/03007995.2014.980886
• Languages: English
• ISSNs: 0300-7995

Abstract

<abstract> <title>Abstract</title> <sec id="ss1"> <title>Objective:</title> <p>Gemigliptin is a selective DPP4 inhibitor used to treat type 2 diabetes. The objective of this study was to evaluate the pharmacokinetics (PKs) of gemigliptin, rosuvastatin, and irbesartan monotherapies and combination therapies.</p> </sec> <sec id="ss2"> <title>Research design and methods:</title> <p>Randomized, open-label, three-treatment, six-sequence, three-period, crossover studies were performed on healthy male volunteers. The three treatments were: 50 mg gemigliptin alone; 20 mg rosuvastatin (part A) or 300 mg irbesartan alone (part B); and rosuvastatin or irbesartan with concomitant gemigliptin. Each drug was administered as part of once daily, 7 day, repeated dosing regimens with a 14 day washout period.</p> </sec> <sec id="ss3"> <title>Clinical trial registration:</title> <p>NCT01823133 (part A) and NCT01825850 (part B).</p> </sec> <sec id="ss4"> <title>Main outcome measures:</title> <p>The primary PK parameters – <italic>C<sub>max</sub></italic> and <italic>AUC<sub>τ</sub></italic> – were compared to the geometric mean ratios (GMRs) and 90% confidence intervals (90% CIs) that were determined for the combination therapies and monotherapies.</p> </sec> <sec id="ss5"> <title>Results:</title> <p>A total of 60 participants were administered the study drugs, and 52 participants (27 participants in part A; 25 participants in part B) were analyzed as part of the PK dataset. In part A, the GMRs (gemigliptin + rosuvastatin/gemigliptin) of the <italic>C<sub>max</sub></italic> and <italic>AUC<sub>τ</sub></italic> values of gemigliptin were 0.955 (90% CI = 0.874–1.044) and 1.023 (90% CI = 0.991–1.057), and those of rosuvastatin were 1.012 (90% CI = 0.946–1.084) and 1.086 (90% CI = 1.032–1.142), respectively. In part B, the GMRs of the <italic>C<sub>max</sub></italic> and <italic>AUC<sub>τ</sub></italic> values of gemigliptin were 1.046 (90% CI = 0.964–1.134) and 1.035 (90% CI = 1.005–1.065), and those of irbesartan were 0.966 (90% CI = 0.897–1.040) and 1.050 (90% CI = 0.993–1.111), respectively. The limitations of this study include its relatively short treatment period and small sample size, as only healthy participants were included.</p> </sec> <sec id="ss6"> <title>Conclusions:</title> <p>Gemigliptin does not affect the PK properties of rosuvastatin or irbesartan; also, rosuvastatin and irbesartan do not affect the PKs of gemigliptin.</p> </sec> </abstract>