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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 Following Single Doses in Healthy, Young Japanese and White Male Subjects
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Pharmacokinetics and Pharmacodynamics of Anacetrapib Following Single Doses in Healthy, Young Japanese and White Male Subjects

机译：在健康，年轻日本和白人科目中单剂量后anacetrapib的药代动力学和药效学

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摘要

Abstract Anacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor being developed for the treatment of mixed dyslipidemia. The aim of the study was to evaluate the pharmacokinetic, pharmacodynamic, and safety characteristics of anacetrapib following single doses in healthy, young Japanese men. In a double‐blind, randomized, placebo‐controlled, 3‐panel, single‐rising‐dose study, 6 healthy young Japanese male or white male subjects (aged 19 to 44 years) received single oral doses of 5 to 500 mg anacetrapib, and 2 received placebo. Plasma and urine drug concentrations were measured 0–168 hours postdose, and plasma CETP inhibition was measured 0–24 hours postdose. Urinary anacetrapib levels were all below quantitation limits. Plasma concentrations of anacetrapib increased approximately less than dose‐proportionally. Consumption of a traditional Japanese breakfast prior to dosing increased the plasma pharmacokinetics of anacetrapib in Japanese subjects compared with fasted conditions, to a similar extent as in white subjects. CETP activity measured over 0–24 hours postdose resulted in significant inhibition. Anacetrapib was generally well tolerated, and there were no serious adverse experiences. No clinically meaningful differences in PK and CETP inhibition parameters were found between Japanese and white subjects.
机译：摘要Anacetrapib是一种用于治疗混合血脂血症的胆固醇酯转移蛋白（CETP）抑制剂。该研究的目的是评估在健康的年轻日本男性中单剂量后anacetrapib的药代动力学，药物动力学和安全特性。在双盲，随机，安慰剂控制，3面板，单升级剂量研究中，6名健康年轻的日本男性或白人男性受试者（年龄19至44岁）接受单次口服剂量为5至500 mg anacetrapib，和2个接受的安慰剂。测量血浆和尿液药物浓度为0-168小时，滴定0-24小时测量血浆CETP抑制。尿肛门蛋白酶水平均低于定量限制。血浆浓度的Anacetrapib增加大约小于剂量。在给药之前消耗传统日本早餐在日本受试者中增加了胸腺嘧啶的血浆药代动力学与禁食条件相比，与白色受试者相似。在0-24小时后测量的CETP活性导致显着的抑制作用。 Anacetrapib通常耐受良好，并且没有严重的不利经验。在日本和白色受试者之间发现了PK和CETP抑制参数的临床上有意义的差异。

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