Ezetimibe CAS 163222-33-1

White SolidEzetimibe is ananti-hyperlipidemic drug used for lowering the plasma cholesterol levels. It is indicated as an adjunctive therapy to diet for the reduction of high-level total-C, LDL-C, and ApoB in patients suffering primary (heterozygous familial and non-familial) hypercholesterolemia. It is also used in combination therapy with HMG-CoA reductase inhibitors.Ezetimibe does not inhibit the cholesterol synthesis in the liver, or increase bile acid excretion.It takes effect throughactin
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Ezetimibe is a beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer). It has a role as an anticholesteremic drug, an antilipemic drug and an antimetabolite. It is a member of azetidines, an organofluorine compound and a beta-lactam.|Ezetimibe is a lipid-lowering compound that inhibits intestinal cholesterol and phytosterol absorption. The discovery and research of this drug began in the early 1990s, after the intravenous administration of radiolabelled ezetimibe in rats revealed that it was being localized within enterocytes of the intestinal villi - this prompted studies investigating the effect of ezetimibe on intestinal cholesterol absorption. Ezetimibe is used as an adjunctive therapy to a healthy diet to lower cholesterol levels in primary hyperlipidemia, mixed hyperlipidemia, homozygous familial hypercholesterolemia (HoFH), and homozygous sitosterolemia (phytosterolemia). Unlike other classes of cholesterol-reducing compounds including statins and bile acid sequestrants, ezetimibe has a distinct mechanism of action involving the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1), and is unique in that it does not affect the absorption of fat-soluble nutrients such as fat-soluble vitamins, triglycerides, or bile acids. In genetically NPC1L1-deficient mice, a 70% reduction in intestinal cholesterol absorption was seen, and these mice were insensitive to ezetimibe treatment - it was determined based on these findings that NPC1L1 plays an essential role in promoting intestinal cholesterol uptake via an ezetimibe-sensitive pathway. By interfering with the intestinal uptake of cholesterol and phytosterols, ezetimibe reduces the delivery of intestinal cholesterol to the liver.|Ezetimibe is a Dietary Cholesterol Absorption Inhibitor. The physiologic effect of ezetimibe is by means of Decreased Cholesterol Absorption.|Ezetimibe is an inhibitor of intestinal cholesterol absorption that is widely used in the therapy of hypercholesterolemia, usually in combination with other agents. Ezetimibe therapy is associated with a low rate of serum aminotransferase elevations and clinically apparent liver injury due to ezetimibe occurs, but is rare.|Ezetimibe is an azetidinone derivative and a cholesterol absorption inhibitor with lipid-lowering activity. Ezetimibe appears to interact physically with cholesterol transporters at the brush border of the small intestine and inhibits the intestinal absorption of cholesterol and related phytosterols. As a result, ezetimibe causes a decrease in the level of blood cholesterol or an increase in the clearance of cholesterol from the bloodstream. Overall, the following effects observed are a reduction of hepatic cholesterol stores and a reduction of total cholesterol, LDL cholesterol, and other triglycerides in the blood.|An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.