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Trials and Tribulations of CETP Inhibitors
Circulation Research ( IF 16.5 ) Pub Date : 2018-01-05 , DOI: 10.1161/circresaha.117.311978
Alan R. Tall 1 , Daniel J. Rader 1
Affiliation  

The development of CETP (cholesteryl ester transfer protein) inhibitors has had a long and difficult course with 3 compounds failing in phase III clinical trials. Finally, the REVEAL (Randomized Evaluation of the Effects of Anacetrapib through Lipid modification) trial has shown that the CETP inhibitor anacetrapib decreased coronary heart disease when added to statin therapy. Although the result is different to earlier studies, this is likely related to the size and duration of the trial. The benefit of anacetrapib seems to be largely explained by lowering of non-HDL-C (high-density lipoprotein cholesterol), rather than increases in HDL-C. Although the magnitude of benefit for coronary heart disease appeared to be moderate, in part this may have reflected aspects of the trial design. Anacetrapib treatment was associated with a small increase in blood pressure, but was devoid of major side effects and was also associated with a small reduction in diabetes mellitus. Treatment with CETP inhibitors, either alone or in combination with statins, could provide another option for patients with coronary disease who require further reduction in LDL (low-density lipoprotein) and non-HDL-C.


中文翻译:

CETP抑制剂的试验和研究

CETP(胆固醇酯转移蛋白)抑制剂的开发过程漫长而艰难,其中有3种化合物在III期临床试验中均未通过。最后,REVEAL(通过脂质修饰对乙酰丙酮酸效果的随机评估)试验表明,CETP抑制剂醋氨苄酸在他汀类药物治疗中可降低冠心病。尽管结果与早期研究不同,但这可能与试验的规模和持续时间有关。减少非HDL-C(高密度脂蛋白胆固醇)而不是增加HDL-C似乎可以很大程度上解释anacetrapib的益处。尽管对冠心病的获益程度似乎是中等的,但这在一定程度上可能反映了试验设计的各个方面。Anacetrapib治疗与血压的小幅升高相关,但没有重大副作用,并且与糖尿病的小幅降低相关。单独或与他汀类药物联合使用CETP抑制剂治疗可为需要进一步降低LDL(低密度脂蛋白)和非HDL-C的冠心病患者提供另一种选择。
更新日期:2018-01-05
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