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动脉粥样硬化(AS)是引起心肌梗死、脑梗死及冠心病等心脑血管疾病死亡的主要原因。近来对胆固醇酯转移蛋白(CETP)的抑制作用已成为治疗AS的新靶点,torcetrapib是治疗AS和脂蛋白紊乱的新的CETP抑制剂。家兔实验表明,torcetrapib对CETP活性的抑制达70%~80%,且能使HDL-C水平增加50%~100%。临床试验表明,torcetrapib单独服用或伍用其他抑制剂,均能使HDL-C水平增加,LDL-C水平降低,达到AS的治疗目标。
Atherosclerosis (AS) is the main cause of death from cardiovascular and cerebrovascular diseases such as myocardial infarction, cerebral infarction and coronary heart disease. Recent inhibition of cholesteryl ester transfer protein (CETP) has become a new target for the treatment of AS and torcetrapib is a novel CETP inhibitor for the treatment of AS and lipoprotein disorders. Rabbit experiments showed that torcetrapib inhibited CETP activity by 70% -80% and increased HDL-C by 50% -100%. Clinical trials show that torcetrapib alone or in combination with other inhibitors, can make HDL-C levels, LDL-C levels lower, to achieve the therapeutic goals of AS.