エゼチミブ

用途エゼチミブ（Ezetimibe）は、小腸からのコレステロール吸収を抑制し、血中コレステロール値を低下させる医薬品である。他のコレステロール低下薬に不忍容の場合に単剤で用いられるほか、スタチン単剤でのコントロールが悪い場合に併用される。

来歴Ezetimibe (brand name Zetia) was approved by the FDA in October 2002 for lowering levels of total cholesterol and LDL (bad) cholesterol in the blood. Zetia is used to treat high cholesterol in people whose cholesterol levels cannot be controlled by diet and exercise alone. It is sometimes given in combination with other cholesterol-lowering drugs, including fenofibrate, or statins, such as atorvastatin, lovastatin, simvastatin, pravastatin, or fluvastatin.

使用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.

一般的な説明Ezetimibe, (3R,4S)-1-(4-fluorophenyl)-3-((3S)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)-2-azetidinone (Zetia), is an antihyperlipidemicagent that has usefulness in lowering cholesterol levels. Itacts by decreasing cholesterol absorption in the intestine byblocking the absorption of the sterol at the Brush boarder.Specifically, the -lactam binds to the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract that isresponsible for cholesterol absorption. Although it may beused alone, it is marketed as a combination product withsimvastatin under the trade name Vytorin.