胆固醇酯转移蛋白抑制剂anacetrapib.pdfVIP

现代药物与临床 Drugs Clinic 第 26 卷 第 2 期 2011 年 3 月 • 153 • 胆固醇酯转移蛋白抑制剂 Anacetrapib 肖桂芝，贺 星，田 红，陈常青 天津药物研究院 医药信息中心，天津 300193 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。 关键词：Anacetrapib ；胆固醇酯转移蛋白抑制剂；动脉粥样硬化；高密度脂蛋白；低密度脂蛋白 中图分类号：R972.6 文献标志码：A 文章编号：1674 - 5515(2011) - 0153 - 04 Cholesterol ester transfer protein inhibitor Anacetrapib XIAO Gui-zhi, HE Xing, TIAN Hong, CHEN Chang-qing Centre of Pharmaceutical Information, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China Abstract: 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. Key words: Anacetrapib; cholesterol ester transfer protein (CETP) inhibitors; atherosclerosis; high-density lipoprotein (HDL); low-density lipoprotein (LDL) 1 药物概况