High-dose potent statin therapy in combination with ezetimibe is now standard practice for the treatment of adult patients with heterozygous familial hypercholesterolemia (heFH), as the result of numerous studies in patients with primary hypercholesterolemia or heFH. These studies have shown the combination to be both effective and safe in the short to medium term. Recently, short-term ezetimib...

The combination of ezetimibe, an inhibitor of Niemann-Pick C1-like 1 protein (NPC1L1), and an HMG-CoA reductase inhibitor decreases cholesterol absorption and synthesis. In clinical trials, ezetimibe plus simvastatin produces greater LDL-cholesterol reductions than does monotherapy. The molecular mechanism for this enhanced efficacy has not been defined. Apolipoprotein B-100 (apoB-100) kinetics...

AIM High cholesterol absorption in the small intestine has been proposed to be a risk factor of atherosclerosis. In this study, we evaluated the effect of ezetimibe monotherapy on arterial stiffness in type 2 diabetic patients. METHODS Forty type 2 diabetes mellitus patients with high serum low-density lipoprotein cholesterol (LDL-C) were enrolled and treated with ezetimibe 10 mg/day for 6 mo...

BACKGROUND Ezetimibe, as a cholesterol absorption inhibitor, has been shown protecting against atherosclerosis when combined with statin. However, side by side comparison has not been made to evaluate the beneficial effects of ezetimibe alone versus statin. Herein, the study aimed to test whether ezetimibe alone would exhibit similar effects as statin and the combination therapy would be necess...

BACKGROUND Postprandial hyperlipidaemia is known to be a high-risk factor for atherosclerotic disease because of rapid and lasting accumulations of triglyceride-rich lipoproteins and remnants. The Niemann-Pick C1-Like 1 (NPC1L1) protein acts as an intestinal cholesterol transporter and ezetimibe, which inhibits NPC1L1, has been used in patients with hypercholesterolaemia. We investigated effect...

Human NPC1L1 protein mediates cholesterol absorption in the intestine and liver and is the target of the drug ezetimibe, which is used to treat hypercholesterolemia. Previous studies concluded that NPC1L1-GFP protein trafficking is regulated by cholesterol binding and that ezetimibe blocks NPC1L1-GFP function by inhibiting its endocytosis. We used cell surface biotinylation to monitor NPC1L1-GF...

Objective: The aim of this work was to investigate and compare various practical techniques to enhance dissolution of ezetimibe, a Class II Biopharmaceutics Classifi cation System compound. Ezetimibe is a poorly soluble compound with variable oral bioavailability. Nanosuspensions, hydroxypropyl-beta-cyclodextrin (HPβCD) complexes as well as combination of surfactant were techniques investigated...

Ezetimibe is a white, crystalline powder that is freely to very soluble in ethanol, methanol, and acetone and practically insoluble in water. Ezetimibe has a melting point of about 163°C and is stable at ambient temperature. ZETIA is available as a tablet for oral administration containing 10 mg of ezetimibe and the following inactive ingredients: croscarmellose sodium NF, lactose monohydrate N...

Hypercholesterolemic patients (n = 1,547) at high atherosclerotic cardiovascular disease risk with low-density lipoprotein cholesterol (LDL-C) levels ≥100 and ≤160 mg/dl while treated with atorvastatin 10 mg/day entered a multicenter, randomized, double-blind, active-controlled, clinical trial using two 6-week study periods. Period I compared the efficacy/safety of (1) adding ezetimibe 10 mg (e...

A simple, rapid and precise method is developed for the quantitative simultaneous determination of Ezetimibe and Simvastatin in combined pharmaceutical-dosage forms. Two methods are described for the simultaneous determination of Ezetimibe and Simvastatin. The first method was based on UVSpectrophotometric determination of two drugs, using simultaneous equation method. It involves absorbance me...