Latest research on Ezetimibe

Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes.

Ezetimibe side effects

Mortality caused by atherosclerotic coronary artery disease is expected to remain high even with statins and Ezetimibe being used as a standard of care and a new antibody therapy against the proprotein convertase subtilisin/kexin 9 reaching the market (1). [source, 2016]
To define pharmacotherapy use, participants were asked to list all current medications, allowing determination of Acetylsalicylic acid, statin, Ezetimibe, fibrate, and RAS inhibitor use; history of side-effects, drug intolerance, and duration of therapy were not ascertained. [source, 2016]
Regarding Ezetimibe, G allele carriers exhibit an increased response to Ezetimibe compared with carriers who are homozygous for the common allele [10, 11]. [source, 2016]
Because of the suggested role of NPC1L1 in uptaking biliary cholesterol into hepatocytes in human [3], there are concerns that Ezetimibe treatment might induce gallstone formation through inhibition of hepatic NPC1L1. [source, 2016]
Very recently, the IMPROVE-IT study, after 6-year followed up, did not show increased incidence of gallstone disease by Ezetimibe treatment [34] either. [source, 2016]
Only Ezetimibe showed significant decrease of cardiovascular events from the recent randomized clinical trial: IMPROVE-IT, comparing simvastatin monotherapy and simvastatin plus Ezetimibe combination [7]. [source, 2015]
However, in light of recent findings regarding the increased incidence of new-onset diabetes and the impact on glucose parameters with the use of statins [2-7], it is important to assess any potential for these same issues with Ezetimibe use. [source, 2015]
Over the course of the 24 weeks of treatment, HbA1c significantly increased from baseline in both the Ezetimibe 10 mg and placebo groups (Figure 2). [source, 2015]
Several studies in animals have suggested that Ezetimibe may have positive effects on glycemic control, including reduced weight gain, diet-induced hyperglycemia and insulin resistance [22], improvement in insulin and plasma glucose response in obese fatty rats [23], and improvement in glucose tolerance, increased insulin sensitivity, and protecting the function of beta-cells in diabetic mice [24]. [source, 2015]
These results are consistent with those of the current trial, suggesting that Ezetimibe does not confer an increased risk of glucose dysregulation. [source, 2015]