Pharmacokinetics of otamixaban, a direct factor Xa inhibitor, in healthy male subjects: pharmacokinetic model development for phase 2/3 simulation of exposure.

Paccaly A; Frick A; Rohatagi S; Liu J; Shukla U; Rosenburg R; Hinder M; Jensen BK

首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Pharmacokinetics of otamixaban, a direct factor Xa inhibitor, in healthy male subjects: pharmacokinetic model development for phase 2/3 simulation of exposure.

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Pharmacokinetics of otamixaban, a direct factor Xa inhibitor, in healthy male subjects: pharmacokinetic model development for phase 2/3 simulation of exposure.

机译：otamixaban（一种直接因子Xa抑制剂）在健康男性受试者中的药代动力学：为暴露的2/3期模拟开发药代动力学模型。

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The pharmacokinetics of otamixaban was investigated in healthy male subjects over a wide range of intravenous doses, with duration of administration varying between 1-minute infusions (bolus dose) and 24-hour infusions, using noncompartmental and multicompartmental methods. A global compartmental analysis (2 and 3 compartments) generated a single set of pharmacokinetic parameters, regardless of infusion rate and duration, and took into account the 30% decrease in clearance and volume of distribution observed over the dose range. The 2-compartment model was retained to predict bolus plus 3-hour-infusion doses of otamixaban for future phase (2/3) studies. Otamixaban exhibited in healthy subjects several interesting pharmacokinetic features in view of its potential therapeutic use in coronary thrombosis: a rapid plasma distribution and elimination, a well-described dose-exposure relationship, a low intersubject variability in plasma exposure, and a mixed renal and biliary excretion with constant renal clearance.

机译：使用非隔室和多室方法，在健康的男性受试者中，对大范围静脉内剂量的otamixaban的药代动力学进行了研究，给药时间在1分钟输注（推注剂量）和24小时输注之间变化。无论输注速度和持续时间如何，整体隔室分析（2和3个隔室）都会生成一组药代动力学参数，并考虑到在剂量范围内观察到的清除率和分布体积减少了30％。保留2室模型以预测推注加3小时输注otamixaban的剂量，以用于将来的阶段（2/3）研究。鉴于其在冠状动脉血栓形成中的潜在治疗用途，Otamixaban在健康受试者中表现出几个有趣的药代动力学特征：快速的血浆分布和消除，良好描述的剂量-暴露关系，血浆暴露中受试者之间的低变异性以及肾和胆汁混合排泄，肾脏清除率恒定。

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《The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology》 |2006年第1期|共8页
作者
Paccaly A; Frick A; Rohatagi S; Liu J; Shukla U; Rosenburg R; Hinder M; Jensen BK;
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正文语种 eng
中图分类药学;
关键词
Infusion; NOS; Male gender; model development; simulation; bolus;

机译：输液;NOS;男性;模型开发;模拟;推注;

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1. Pharmacokinetics of otamixaban, a direct factor Xa inhibitor, in healthy male subjects: pharmacokinetic model development for phase 2/3 simulation of exposure. [J] . Paccaly A, Frick A, Rohatagi S, The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology . 2006,第1期

机译：otamixaban（一种直接因子Xa抑制剂）在健康男性受试者中的药代动力学：为暴露的2/3期模拟开发药代动力学模型。
2. Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939-an oral, direct Factor Xa inhibitor-after multiple dosing in healthy male subjects. [J] . Kubitza D, Becka M, Wensing G, European journal of clinical pharmacology . 2005,第12期

机译：在健康男性受试者中多次给药后，BAY 59-7939（一种口服直接Xa抑制剂）的安全性，药效学和药代动力学。
3. Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939—an oral, direct Factor Xa inhibitor—after multiple dosing in healthy male subjects [J] . Dagmar Kubitza, Michael Becka, Georg Wensing, European Journal of Clinical Pharmacology . 2005,第12期

机译：在健康男性受试者中多次给药后，BAY 59-7939（口服直接Xa因子抑制剂）的安全性，药效学和药代动力学
4. Interaction of subcutaneous lixisenatide 20 μg QD on pharmacokinetic and pharmacodynamic properties of oral ramipril 5 mg QD in steady state in young healthy males and females [C] . Dahmen R, Steinstraesser A, Poitiers F, European Association for Clinical Pharmacology and Therapeutics . 2011

机译：皮下丽西齐肽的相互作用20μgQD对年轻健康男性稳态口腔ramipril 5mg qd的药代动力学和药物动力学性质
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6. Apixaban an oral direct factor Xa inhibitor: single dose safety pharmacokinetics pharmacodynamics and food effect in healthy subjects [O] . Charles Frost, Jessie Wang, Sunil Nepal, 2013

机译：口服直接因子Xa抑制剂Apixaban：健康受试者的单剂量安全性药代动力学药效学和食物效应
7. Safety, pharmacokinetics and pharmacodynamics of single/multiple doses of the oral, direct Factor Xa inhibitor rivaroxaban in healthy Chinese subjects [O] . Zhao, Xia, Sun, Peihong, Zhou, Ying, 2009

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Pharmacokinetics of otamixaban, a direct factor Xa inhibitor, in healthy male subjects: pharmacokinetic model development for phase 2/3 simulation of exposure.

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