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依泽替米贝是先灵普劳公司与默克公司共同研制开发的一种新型的降脂药,美国FDA于2002年批准上市。它作用于小肠刷状缘的NPC1L1、膜联蛋白2小凹蛋白1、氨肽酶N等蛋白质,起着抑制胆固醇吸收的作用。它的作用机制与他汀类药物互补,后者可以抑制体内胆固醇合成。临床试验表明,依泽替米贝无论是单用还是与他汀类联合应用,都能收到很好的降脂效果,并且降脂的同时能降低低密度脂蛋白胆固醇水平,升高高密度脂蛋白胆固醇水平。另外,依泽替米贝对一些难治性的遗传性高胆固醇血症如家族型纯合子高脂血症有很好的疗效。
Ezetimibe is a new lipid-lowering drug jointly developed by Schering-Plow and Merck. The FDA approved the drug market in 2002. It acts on the brush border of the small intestine NPC1L1, annexin 2 small caveolin 1, aminopeptidase N and other proteins, play a role in the inhibition of cholesterol absorption. Its mechanism of action is complementary to statins, which inhibit the cholesterol synthesis in the body. Clinical trials have shown that ezetimibe can receive good lipid-lowering effects either alone or in combination with statins, and that lipid lowering can reduce LDL cholesterol levels and increase high-density lipids Protein cholesterol levels. In addition, ezetimibe for some refractory hereditary hypercholesterolemia such as familial homozygous hyperlipidemia has a good effect.