CETP Inhibition: Past Failures and Future Hopes.
CETP Inhibition: Past Failures and Future Hopes.
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DOI：
10.4137/cmc.s32667
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发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Vittorio TJ
中科院分区：
文献类型：
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作者：
Kosmas CE;DeJesus E;Rosario D;Vittorio TJ
高密度脂蛋白胆固醇（HDL-C）在心血管疾病中的动脉粥样硬化保护作用已经明确确立，流行病学数据已经清楚地表明HDL-C水平与心血管事件风险之间存在很强的负相关关系，这与低密度脂蛋白胆固醇（LDL-C）水平无关。因此，假设HDL-C升高可能会导致心血管风险的降低是合乎逻辑的。胆固醇酯转移蛋白（CETP）促进胆固醇酯从高密度脂蛋白向极低密度脂蛋白和低密度脂蛋白的转移。因此，CETP抑制提高HDL-C水平，降低LDL-C水平。第一次使用CETP抑制剂的试验未能显示心血管事件的减少。然而，新的CETP抑制剂对脂质有更有利的作用，目前正在临床试验中进行测试，希望它们的使用可能导致心血管风险的降低。这篇综述旨在提供目前关于CETP抑制的证据，以及与正在开发的新的CETP抑制剂有关的临床和科学数据。
The atheroprotective role of high-density lipoprotein cholesterol (HDL-C) in cardiovascular disease has been unequivocally established, and epidemiological data have clearly demonstrated a strong inverse relationship between HDL-C levels and the risk of cardiovascular events, which is independent of the low-density lipoprotein cholesterol (LDL-C) levels. Thus, it would be logical to hypothesize that raising HDL-C might potentially lead to a reduction of cardiovascular risk. Cholesteryl ester transfer protein (CETP) promotes the transfer of cholesteryl esters from HDL to very low-density lipoprotein and LDL. Therefore, CETP inhibition raises HDL-C levels and decreases LDL-C levels. The first trials with CETP inhibitors failed to show a reduction in cardiovascular events. However, newer CETP inhibitors with more favorable effects on lipids are presently being tested in clinical trials with the hope that their use may lead to a reduction in cardiovascular risk. This review aims to provide the current evidence regarding CETP inhibition, as well as the clinical and scientific data pertaining to the new CETP inhibitors in development.