Pharmacokinetics, Pharmacodynamics, and Tolerability of Betrixaban Administered Orally in Subjects With Normal and Reduced Renal Function.
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 32
- 试验地点
- 1
- 主要终点
- Area Under The Plasma Concentration-Time Curve From Time Zero To 24 Hours (AUC0-24) Postdose Of Oral Doses Of Betrixaban On Day 8
研究概览
简要总结
The purpose of the study is to compare the pharmacokinetics, pharmacodynamics, and tolerability of betrixaban in patients with mild, moderate, and severe renal impairment to healthy volunteers.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 80 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Able to understand and sign the written informed consent.
- •Subjects should have either normal renal function or have stable renal disease
排除标准
- •Subjects require dialysis
- •Evidence of active bleeding or bleeding disorder
- •Unstable or clinically significant other disorders such as respiratory, hepatic, metabolic, psychiatric or gastrointestinal disorder
研究组 & 干预措施
Group C
Patients with severe renal impairment
干预措施: Betrixaban (Drug)
Group H
Healthy subjects matched to the renal impairment groups
干预措施: Betrixaban (Drug)
Group A
Patients with mild renal impairment
干预措施: Betrixaban (Drug)
Group B
Patients with moderate renal impairment
干预措施: Betrixaban (Drug)
结局指标
主要结局
Area Under The Plasma Concentration-Time Curve From Time Zero To 24 Hours (AUC0-24) Postdose Of Oral Doses Of Betrixaban On Day 8
时间窗: Predose up to 168 hours postdose
Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2. Results were reported in nanogram multiplied by hour per milliliter (ng\*h/mL).
Maximum Observed Plasma Concentration (Cmax) Following Administration Of Oral Doses Of Betrixaban On Day 8
时间窗: Predose, up to 168 hours postdose
Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2. Results were reported in nanogram per milliliter (ng/mL).
Plasma Terminal Elimination Half-Life (T½) Following Administration Of Oral Doses Of Betrixaban On Day 8
时间窗: Predose, up to 168 hours postdose
Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2. Harmonic mean and Jackknife standard deviation was used to report this outcome and results were reported in hour.
Total Plasma Clearance (CL/F) Following Administration Of Oral Doses Of Betrixaban On Day 8
时间窗: Predose, up to 168 hours postdose
Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2. Results were reported in milliliter per minute (mL/min).
Volume Of Distribution During The Terminal Phase (Vz/F) Following Administration Of Oral Doses Of Betrixaban On Day 8
时间窗: Predose, up to 168 hours postdose
Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2. Results were reported in liter.
Thrombin Generation Following Administration Of Oral Doses Of Betrixaban On Day 8
时间窗: Day 1: predose; Day 8: 2, 3, 4, 8, 24, and 48 hours postdose
Blood samples were collected at the protocol-specified time points. Plasma samples were assayed for measurement of thrombin generation for all participants.
Anti-Factor Xa (fXa) Activity Following Administration Of Oral Doses Of Betrixaban On Day 8
时间窗: Day 8: 2, 3, 4, 8, 24, and 48 hours postdose
Blood samples were collected at the protocol-specified time points. Plasma samples were assayed for measurement of anti-fXa activity at baseline and steady state for all participants. Results were reported in international units per milliliter (IU/mL).
Percentage Of Dose Excreted In Urine From 0-24 (fe0-24) Postdose Of Oral Doses Of Betrixaban On Day 8
时间窗: Predose, up to 24 hours postdose
Blood and urine samples for pharmacokinetic analysis were collected and determined from the plasma and urine concentrations of betrixaban using non-compartmental procedures in WinNonlin Enterprise Version 5.2. Results were reported in percentage.
Percentage Of Betrixaban Bound To Plasma Proteins On Day 8
时间窗: 4 hours Postdose at Day 8
Blood samples were collected for measurement of plasma protein binding for betrixaban for all participants. Results of protein binding assays were summarized by sample time and eGFR group. Results were reported in percent (%).
次要结局
未报告次要终点