163222-33-1

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What is the Ezetimibe ?

Ezetimibe is white powder, while it's Molecular Formula is C24H21F2NO3. Ezetimibe (9) was approved as the first hypolipidemic drug to act by blocking the absorption of dietary cholesterol. This drug was discovered by Schering-Plough and is codeveloped and co-marketed by Merck and Schering-Plough for the treatment of hypercholesterolemia and also two less common forms of hyperlipidemia: homozygous familial hypercholesterolemia and homozygous sitosterolemia.

What is the CAS number for Ezetimibe ?

The CAS number of Ezetimibe is 163222-33-1.

More information of Ezetimibe 163222-33-1 are:

What is Ezetimibe (163222-33-1) used for?

Ezetimibe is a once-daily orally active cholesterol absorption inhibitor, launched as a hypolipidemic agent. The one-step diastereo- and enantioselective formation of β-lactams starting from commercially available (3S)-hydroxy-y-lactone is the key point of the asymmetric synthesis of ezetimibe. The 2-azetidinone class was initially designed as acylcoenzyme A: cholesterol acyltransferase (ACAT) inhibitors but experimental data suggest that this compound acts in the intestinal wall to inhibit cholesterol through a novel mechanism with an as yet undiscovered target. Orally administered ezetimibe inhibited increases in plasma cholesterol in four cholesterol-fed animals species (hamster, rats, dogs and rhesus monkeys). In rats cannulated in the intestine and bile duct, [3H]-ezetimibe inhibited cholesterol absorption by more than 95%. In cholesterol-fed LDL receptor+apoE knockout mice, treatment with ezetimibe reduced atherosclerotic lesion cross sectional area by 48% in the aorta and 20% in the carotid artery. Moreover, the plasma cholesterol levels were reduced and the progression of lesions was inhibited. Ezetimibe is highly protein bound and is metabolized by the liver to its glucuronide metabolite, which represents 80-90% of circulating ezetimibe. About 90% of ezetimibe and/or the glucuronide metabolite are excreted in the feces and 10% in the urine. The parent compound and its glucuronide metabolite undergo enterohepatic recirculation; in consequence, the drug is slowly eliminated. In hypercholesterolemic patients, ezetimibe (10 mglday, 12 weeks) reduced LDL cholesterol by 18% and total cholesterol by 12%, with a similar safety profile to placebo. Co-administration of ezetimibe with statins or fenofibrate lowered LDL cholesterol levels more than either monotherapy. Ezetimibe was well tolerated and interaction studies provided evidence that ezetimibe had no significant effect on the activity of major CYP450 drug-metabolizing enzymes. Moreover, no pharmacokinetic/pharmacodynamic interactions were seen between ezetimibe and statins and others frequently administered drugs. .

InChI:InChI=1/C24H21F2NO3/c25-17-5-1-15(2-6-17)22(29)14-13-21-23(16-3-11-20(28)12-4-16)27(24(21)30)19-9-7-18(26)8-10-19/h1-12,21-23,28-29H,13-14H2

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