Evaluation of the pharmacokinetics of the DPP-4 inhibitor gemigliptin when coadministered with rosuvastatin or irbesartan to healthy subjects

Choi, Hee Youn; Lim, Hyeong‐Seok; Kim, Yo Han; Jeon, Hoonbae; Kim, Mi Jo; Lee, Shi Hyang; Jung, Jong Hyuk; Lee, Young Kyoung; Bae, Kyun‐Seop

doi:10.1185/03007995.2014.980886

Cited by 10 publications

(4 citation statements)

References 33 publications

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“…The washout period of this study was 14 days, which is long enough to eliminate carryover effects considering previously reported half-lives of 17 h for gemigliptin, 27 h for LC15-0636, and 19 h for rosuvastatin. 9,15,21 However, one case of carryover effect for gemigliptin and rosuvastatin was observed at pre-dose in the second period after washout. However, PK analysis was performed without any adjustments because both of gemigliptin and rosuvastatin concentrations were less than 5% of C max .…”

Section: Discussionmentioning

confidence: 99%

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

Kim

Park

Jang

et al. 2019

DDDT

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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 noncompartmental 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 C max and AUC last 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 I max and AUEC last 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.

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Section: Discussionmentioning

confidence: 99%

“…14 According to a previous study, pharmacokinetic properties of rosuvastatin are not altered by gemigliptin and vice versa. 15 The maximum daily dose of gemigliptin approved by the Ministry of Food and Drug Safety (Republic of Korea) is 50 mg (Zemiglo ® , LG Chem. 2017).…”

Section: Introductionmentioning

confidence: 99%

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

Kim

Park

Jang

et al. 2019

DDDT

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“…Studies also revealed that gemigliptin did not alter the pharmacokinetics of most commonly used antidiabetic agents (metformin, glimepiride, and pioglitazone), antihypertensives, and lipid lowering agents. [ 18 19 20 21 ] Ketoconazole, a CYP3A4 inhibitor, moderately increased gemigliptin exposure while it was reduced when coadministered with rifampicin, a CYP3A4 inducer. [ 22 ]…”

Section: P Harmacokinetics D Osage mentioning

confidence: 99%

Gemigliptin: Newer promising gliptin for type 2 diabetes mellitus

Gutch

Joshi

Kumar

et al. 2017

Indian J Endocr Metab

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The dipeptidyl peptidase-4 (DPP-4) inhibitors have facilitated the management of type 2 diabetes mellitus (T2DM) owing to their superior efficacy and safety with low incidence of adverse effects. Gemigliptin is a new member of this family of drugs, and studies have revealed certain advantages of gemigliptin use compared to its previous congeners. Besides, this drug has also been studied for the treatment of T2DM as monotherapy, in combination with metformin or other oral antidiabetic drugs and in T2DM with moderate-to-severe renal failure. In this review, we explore the published data highlighting the pharmacology, efficacy, and safety of gemigliptin along with its recommendations for use in patients with T2DM.

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“…In several drug-drug interaction studies, gemigliptin did not meaningfully alter pharmacokinetics of co-medications frequently used to treat T2DM, such as antidiabetic agents (metformin, pioglitazone, and glimepiride), and antihypertensive and lipid-lowering agents (irbesartan and rosuvastatin) [ 30 31 32 33 ]. Although co-administration of ketoconazole, a potent inhibitors of CYP3A4, resulted in a moderate increase in gemigliptin exposure (1.9-fold as total active moiety of gemigliptin), no dosage adjustment should be required when gemigliptin is co-administered with ketoconazole.…”

Section: Characteristics Of Gemigliptinmentioning

confidence: 99%

Gemigliptin: An Update of Its Clinical Use in the Management of Type 2 Diabetes Mellitus

Kim¹,

Yoo²,

Lee

et al. 2016

Diabetes Metab J

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Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antidiabetic agent for the treatment of type 2 diabetes mellitus. They increase endogenous levels of incretin hormones, which stimulate glucose-dependent insulin secretion, decrease glucagon secretion, and contribute to reducing postprandial hyperglycemia. Although DPP-4 inhibitors have similar benefits, they can be differentiated in terms of their chemical structure, pharmacology, efficacy and safety profiles, and clinical considerations. Gemigliptin (brand name: Zemiglo), developed by LG Life Sciences, is a potent, selective, competitive, and long acting DPP-4 inhibitor. Various studies have shown that gemigliptin is an optimized DPP-4 inhibitor in terms of efficacy, safety, and patient compliance for treatment of type 2 diabetes mellitus. In this review, we summarize the characteristics of gemigliptin and discuss its potential benefits in clinical practice.

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Evaluation of the pharmacokinetics of the DPP-4 inhibitor gemigliptin when coadministered with rosuvastatin or irbesartan to healthy subjects

Abstract: Gemigliptin does not affect the PK properties of rosuvastatin or irbesartan; also, rosuvastatin and irbesartan do not affect the PKs of gemigliptin.

Cited by 10 publications

References 33 publications

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

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

Gemigliptin: Newer promising gliptin for type 2 diabetes mellitus

Gemigliptin: An Update of Its Clinical Use in the Management of Type 2 Diabetes Mellitus

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