Ezetimibe improves postprandial hyperlipidaemia in patients with type IIb hyperlipidaemia

Masuda, Daisuke; Nakagawa-Toyama, Yumiko; Nakatani, Kazuhiro; Inagaki, Miwako; Tsubakio-Yamamoto, Kazumi; Sandoval, Jose C.; Ohama, Tohru; Nishida, Makoto; Ishigami, Masato; Yamashita, Shizuya

doi:10.1111/j.1365-2362.2009.02163.x

Cited by 78 publications

(68 citation statements)

References 24 publications

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“…Indeed, increased levels of RLP-C are significant and independent risk factor of CAD and predict future coronary events in patients with CAD and type II DM [15]. As shown in the present study as well as in previous studies [16], ezetimibe appears to decrease RLP. The observed reduction in LDL-C correlated with improved references…”

Section: Discussionsupporting

confidence: 68%

Comparative study between high-dose fluvastatin and low-dose fluvastatin and ezetimibe with regard to the effect on endothelial function in diabetic patients

et al. 2011

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Section: Discussionsupporting

confidence: 68%

Comparative study between high-dose fluvastatin and low-dose fluvastatin and ezetimibe with regard to the effect on endothelial function in diabetic patients

et al. 2011

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“…On the other hand, postprandial serum FFA excursion, a risk factor for cardiovascular disease, was unaffected by ezetimibe administration and showed a J-curve in this study. Whenever serum insulin and plasma glucose increase during OGTT, serum FFA decreases in the opposite direction; however, a previous study 15) reported that serum FFA increased after a lipid-rich meal and that ezetimibe inhibited the increment of serum FFA excursion. The discrepancy between our study and the previous study may be explained by insulin-stimulated lipoprotein lipase (LPL) activity derived from the presence or absence of carbohydrates, although we did not measure LPL activity in this study.…”

Section: Safety and Tolerabilitymentioning

confidence: 83%

“…The discrepancy between our study and the previous study may be explained by insulin-stimulated lipoprotein lipase (LPL) activity derived from the presence or absence of carbohydrates, although we did not measure LPL activity in this study. Another possibility is that our model meal contained more carbohydrates than the meal in the previous study 15) . Postprandial glucose and insulin excursion and serum incretin levels were not affected by ezetimibe significantly (Fig.…”

Section: Safety and Tolerabilitymentioning

confidence: 86%

“…2d, 3d). Postprandial serum TG excursion after oral fat loading is reportedly reduced by ezetimibe in patients with type Ⅱb hyperlipidaemia 15) . Our results were essentially consistent with this previous report.…”

Section: Discussionmentioning

confidence: 99%

“…Clinically, the administration of ezetimibe has been shown to reduce fasting levels of total cholesterol (TC) and LDL-C in patients with primary hypercholesterolemia in both Japan and the United States 13,14) . In addition, ezetimibe has been reported to reduce postprandial hypertriglyceridaemia and inflammation and to improve insulin sensitivity 15,16) . In animals experiments, ezetimibe reversed dietinduced obesity 17,18) , liver steatosis [17][18][19][20] , and insulin resistance 19) .…”

Section: Measurement Of Serum Samplesmentioning

confidence: 99%

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Double-Blind Randomized Clinical Trial of the Effects of Ezetimibe on Postprandial Hyperlipidaemia and Hyperglycaemia

Kikuchi

Nezu

Inazumi

et al. 2012

JAT

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Aim: Ezetimibe selectively blocks intestinal cholesterol absorption by inhibiting Niemann-Pick C1-like 1 (NPC1L1) and reducing LDL cholesterol (LDL-C). In animals, ezetimibe reversed dietinduced obesity, liver steatosis, and insulin resistance. In humans, its potential effects on liver steatosis and insulin resistance have been suggested. We investigated the effects of ezetimibe on postprandial hyperlipidaemia and hyperglycaemia in obese subjects with dyslipidaemia in a double-blind randomized crossover trial. Methods: Twenty obese men with hypertriglyceridaemia were assigned randomly to an ezetimibe-or a placebo-precedence-treated group. Subjects in the ezetimibe group were treated with ezetimibe (10 mg/day) for the first 4 weeks, followed by a 4-week interval and then treated with placebo for another 4 weeks. The placebo group received these treatments in reverse order. Subjects were requested to fast for at least 12 hours and then received a standard meal. Blood samples were collected at 0, 30, 60, 120, 240, 360 and 480 minutes after the meal on Days 0, 28, 56 and 84 and were used to measure the lipid and glucose metabolism markers. Results: Ezetimibe significantly decreased the postprandial serum triglyceride excursion (p=0.01) and fasting serum LDL-C, remnant-like particles(RLP) and ApoB48 levels (p＜0.05). Postprandial glucose excursion, serum insulin levels, serum glucose-dependent insulinotropic polypeptide (GIP) and active glucagon-like peptide-1 (GLP-1) were not significantly affected by ezetimibe treatment. Conclusion: Ezetimibe restored the postprandial dysregulation of lipid but did not affect glucose metabolism in a double-blind randomized crossover trial.

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Antidyslipidemic potential of a novel farnesoid X receptor antagonist in a hamster model of dyslipidemia: Comparative studies of other nonstatin agents

Shinozawa

Amano

Yamakawa

et al. 2018

Pharmacology Res & Perspec

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We attempted to clarify the therapeutic capability of antagonists of the farnesoid X receptor (FXR), a nuclear receptor that regulates lipid and bile acid metabolism. Herein, we report the antidyslipidemic effects of a novel synthesized FXR antagonist, compound‐T1, utilizing a dyslipidemic hamster model. Compound‐T1 selectively inhibited chenodeoxycholic acid‐induced FXR activation (IC 50, 2.1 nmol·L−1). A hamster model of diet‐induced hyperlipidemia was prepared to investigate the antidyslipidemic effects of compound‐T1 through comparative studies of the nonstatin lipid‐modulating agents ezetimibe, cholestyramine, and torcetrapib. In the hamster model, compound‐T1 (6 mg·kg−1·day−1, p.o.) increased the level of plasma high‐density lipoprotein (HDL)‐cholesterol (+22.2%) and decreased the levels of plasma non‐HDL‐cholesterol (−43.6%) and triglycerides (−31.1%). Compound‐T1 also increased hepatic cholesterol 7α‐hydroxylase expression and fecal bile acid excretion, and decreased hepatic cholesterol content. Moreover, the hamster model could reflect clinical results of other nonstatin agents. Torcetrapib especially increased large HDL particles compared with compound‐T1. Additionally, in the human hepatoma Huh‐7 cells, compound‐T1 enhanced apolipoprotein A‐I secretion at a concentration close to its IC 50 value for FXR. Our results indicated the usefulness of the hamster model in evaluating FXR antagonists and nonstatin agents. Notably, compound‐T1 exhibited beneficial effects on both blood non‐HDL‐cholesterol and HDL‐cholesterol, which are thought to involve enhancement of cholesterol catabolism and apolipoprotein A‐I production. These findings aid the understanding of the antidyslipidemic potential of FXR antagonists with a unique lipid and bile acid modulation.

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Ezetimibe improves postprandial hyperlipidaemia in patients with type IIb hyperlipidaemia

Abstract: These findings suggest that ezetimibe improves fasting lipoprotein profiles and postprandial hyperlipidaemia by suppressing intestinal CM production in patients with type IIb hyperlipidaemia and such treatment may prove to be effective in reducing atherosclerosis.

Cited by 78 publications

References 24 publications

Comparative study between high-dose fluvastatin and low-dose fluvastatin and ezetimibe with regard to the effect on endothelial function in diabetic patients

Comparative study between high-dose fluvastatin and low-dose fluvastatin and ezetimibe with regard to the effect on endothelial function in diabetic patients

Double-Blind Randomized Clinical Trial of the Effects of Ezetimibe on Postprandial Hyperlipidaemia and Hyperglycaemia

Antidyslipidemic potential of a novel farnesoid X receptor antagonist in a hamster model of dyslipidemia: Comparative studies of other nonstatin agents

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