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机构地区:[1]天津药物研究院医药信息中心,天津300193
出 处:《现代药物与临床》2011年第2期153-156,共4页Drugs & Clinic
摘 要:高密度脂蛋白-胆固醇(HDL-C)低于正常水平是诱发心血管疾病的因素之一,升高较低水平的HDL-C能够降低患心血管疾病的风险。一些代谢疾病,如胰岛素耐受、高三酰甘油血症都会增强胆固醇酯转移蛋白的活性,高活性的胆固醇酯转移蛋白可诱发动脉粥样硬化和增加患心血管疾病的风险。因此,抑制胆固醇酯转移蛋白是治疗动脉粥样硬化症的新靶点。Aanncetrapib是一小分子唑烷酮类选择性胆固醇酯转移蛋白抑制剂,能很好地作用于低密度脂蛋白-胆固醇(LDL-C)和HDL-C,安全有效地调节冠状动脉心脏病患者以及冠状动脉心脏病高危患者的脂质水平。Subnormal plasma levels of high-density lipoprotein cholesterol (HDL-C) constitute a major cardiovascular risk factor. Raising low HDL-C levels may therefore reduce the residual cardiovascular risk that frequently presents in dyslipidaemic subjects. The activity of Cholesteryl ester transfer protein (CETP) is levated in the dyslipidaemias of metabolic disease involving insulin resistance, hypertriglyceridaemia, and leads premature atherosclerosis and high cardiovascular risk. CETP inhibition therefore is regarded as a potential target for elevation of HDL-C and reduction in atherosclerosis. Treatment with Anacetrapib that a CETP inhibitor had strong effects on low-density lipoprotein (LDL) and HDL-C, according to recent study. Further studies of Anacetrapib, specifically in long-term, large-scale outcome trials, will provide essential information on its safety and efficacy in reducing residual cardiovascular risk.
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