Ezetimibe and Reactive Oxygen Species

Title: Ezetimibe and Reactive Oxygen Species

Volume: 9 Issue: 1

Author(s): Minako Yamaoka-Tojo, Taiki Tojo, Naonobu Takahira, Takashi Masuda and Tohru Izumi

Affiliation:

Keywords: Reactive oxygen species, atherosclerosis, dyslipidemia, inflammation, cholesterol

Abstract: Ezetimibe is a potent inhibitor of cholesterol absorption that has been approved for the treatment of hypercholesterolemia. Statin, 3-hydroxy-3 methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, is an inhibitor of cholesterol synthesis. Statin is the first-choice drug to reduce low-density lipoprotein (LDL)-cholesterol for patients with hypercholesterolemia, due to its strong effect to lower the circulating LDL-cholesterol levels. Because a high dose of statins causes concern about rhabdomyolysis, it is sometimes difficult to achieve the guideline-recommended levels of LDLcholesterol in patients with high LDL-cholesterol treated with statin monotherapy. Ezetimibe has been reported to reduce LDL-cholesterol safely with both monotherapy and combination therapy with statins. Ezetimibe is especially expected to be the best pharmacological option for the treatment of patients unable to achieve LDL-cholesterol goals with statins. Reactive oxygen species (ROS) are produced at low levels to maintain physiological redox balance. Oxidative stress results when ROS production exceeds the ability of cells to detoxify ROS. Overproduction of ROS damages cellular components, including lipids, leading to decline in physiological function and cell death. Oxidative stress exacerbates atherosclerosis, the major risk factor for coronary artery disease and ischemic stroke, at every step involves the accumulation of oxidized LDL in the arteries, leading to foam cell formation, plaque development, and plaque rupture. This review focuses on the recent findings of ezetimibe-related atheroprotective effects in vasculature. Moreover, known and proposed mechanisms of how ezetimibe could improve ROS-induced pro-atherosclerotic conditions in vasculature are discussed; these effects may help to explain the mechanisms by which ezetimibe may protect vascular from atherosclerosis.

Cite this article as:

Yamaoka-Tojo Minako, Tojo Taiki, Takahira Naonobu, Masuda Takashi and Izumi Tohru, Ezetimibe and Reactive Oxygen Species, Current Vascular Pharmacology 2011; 9 (1) . https://dx.doi.org/10.2174/157016111793744652