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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Pharmacokinetics and Pharmacodynamics of Anacetrapib in Black and White Healthy Subjects
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Pharmacokinetics and Pharmacodynamics of Anacetrapib in Black and White Healthy Subjects

机译:黑白健康受试者厌氧筛的药代动力学和药效学

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摘要

Abstract Anacetrapib is a cholesteryl ester transfer protein inhibitor intended for the treatment of dyslipidemia. A phase 1 study was conducted to examine the pharmacokinetics and pharmacodynamics of multiple doses of anacetrapib in black compared to white healthy subjects. Although there was no apparent race‐related pharmacokinetic effect, attenuation of the lipid response was observed in black subjects. Specifically, high‐density lipoprotein cholesterol percentage increased 18.1% (absolute percentage points) less in black subjects (89.9%) when compared to increases in white subjects (108.0%). Similarly, the decrease in low‐density lipoprotein cholesterol was 17.8% (absolute percentage points) less in blacks (–21.2%) relative to whites (–39.0%). In contrast, there were no apparent race‐related differences in cholesteryl ester transfer protein mass or activity. Anacetrapib was generally well tolerated in this study. The results of this study suggest that there may be race‐related differences in pharmacodynamics of anacetrapib independent of pharmacokinetics.
机译:摘要anacetrapib是一种用于治疗血脂血症的胆固醇酯转移蛋白抑制剂。进行了一期研究,以检查黑色中多剂量anacetrapib的药代动力学和药效学,与白色健康受试者相比。虽然没有明显的种族相关的药代动力学效果,但在黑色受试者中观察到脂质反应的衰减。具体而言,与白色受试者增加(108.0%)增加时,高密度脂蛋白胆固醇百分比增加18.1%(89.9%)的黑色受试者(89.9%)。类似地,相对于白人(-39.0%-39.0%),低密度脂蛋白胆固醇的降低为17.8%(绝对百分点)(-21.2%)(-39.0%)。相比之下,胆固醇酯转移蛋白质或活性没有明显的种族相关差异。在本研究中,anacetrapib通常耐受良好。该研究的结果表明,无关的药代动力学,Anacetrapib的药效学有关的差异。

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