A Phase 1, Open-Label, Randomized, 3-Period Crossover Study to Assess the Effect of Low-Fat Food on Pexidartinib Pharmacokinetics in Healthy Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 24
- 试验地点
- 1
- 主要终点
- Maximum Observed Concentration in Plasma (Cmax) of Pexidartinib
研究概览
简要总结
All participants in this study are healthy volunteers.
Throughout the study, healthy volunteers will have physical exams, electrocardiograms and clinical laboratory tests. The study staff will keep track of symptoms, diet, and what medications they are taking.
Each participant will get all three treatments (A, B and C). Only the order in which they receive them will be different.
There are six groups based on the order: ABC, ACB, BAC, BCA, CAB, or CBA. Participants have an equal chance of being assigned to any of these groups.
For each treatment period, participants will:
- fast overnight
- receive the assigned treatment with or without food
- have a small tube of blood drawn prior to treatment
- after dosing, additional blood samples will be drawn at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours
- have a break from treatment for 6 days between each treatment period
All participants must reside in the clinic for a total of 20 days.
详细描述
The primary objectives of this study are:
- To assess the effect of low-fat food on the pharmacokinetics (PK) of pexidartinib following a single oral dose of 400 mg administered in healthy subjects
- To assess the PK of pexidartinib following a single oral dose of 200 mg administered with low-fat food in healthy subjects
The secondary objective of this study is:
- To characterize the safety and tolerability of pexidartinib in healthy subjects following administration of a single oral dose of pexidartinib with low fat food and without food
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Sequential
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 60 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Is healthy at screening visit
- •Is not pregnant or lactating
- •Is surgically or naturally unable to reproduce, or agrees to remain sexually abstinent or to use double barrier methods of contraception from check-in until 90 days after the final dose of pexidartinib
- •Has a Body Mass Index (BMI) of 18-30 kg/m^2, inclusive
- •Has negative test results for protocol-defined drugs and diseases at screening and/or check-in
- •Is willing to avoid food or beverages before check-in until the end of the study:
- •containing caffeine/xanthine or alcohol from 48 hours before check-in
- •containing grapefruit or Seville oranges 6 days before check-in
排除标准
- •Per protocol or in the opinion of the investigator at screening and/or check-in, has something that would preclude participation:
- •has a clinically significant disorder, disease or lab value
- •consumes a prohibited drug, drink or food
- •is unable to consume the standard meal
- •Is an employee of the clinic or their family member
研究组 & 干预措施
Sequence ABC
Healthy volunteers will receive Treatments A, then B, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment A - 400 mg Fasting (Drug)
Sequence ABC
Healthy volunteers will receive Treatments A, then B, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment B - 400 mg Fed (Drug)
Sequence ABC
Healthy volunteers will receive Treatments A, then B, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment C - 200 mg Fed (Drug)
Sequence ACB
Healthy volunteers will receive Treatments A, then C, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment A - 400 mg Fasting (Drug)
Sequence ACB
Healthy volunteers will receive Treatments A, then C, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment B - 400 mg Fed (Drug)
Sequence ACB
Healthy volunteers will receive Treatments A, then C, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment C - 200 mg Fed (Drug)
Sequence BAC
Healthy volunteers will receive Treatments B, then A, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment A - 400 mg Fasting (Drug)
Sequence BAC
Healthy volunteers will receive Treatments B, then A, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment B - 400 mg Fed (Drug)
Sequence CAB
Healthy volunteers will receive Treatments C, then A, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment C - 200 mg Fed (Drug)
Sequence BAC
Healthy volunteers will receive Treatments B, then A, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment C - 200 mg Fed (Drug)
Sequence BCA
Healthy volunteers will receive Treatments B, then C, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment A - 400 mg Fasting (Drug)
Sequence BCA
Healthy volunteers will receive Treatments B, then C, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment B - 400 mg Fed (Drug)
Sequence BCA
Healthy volunteers will receive Treatments B, then C, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment C - 200 mg Fed (Drug)
Sequence CAB
Healthy volunteers will receive Treatments C, then A, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment A - 400 mg Fasting (Drug)
Sequence CAB
Healthy volunteers will receive Treatments C, then A, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment B - 400 mg Fed (Drug)
Sequence CBA
Healthy volunteers will receive Treatments C, then B, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment A - 400 mg Fasting (Drug)
Sequence CBA
Healthy volunteers will receive Treatments C, then B, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment B - 400 mg Fed (Drug)
Sequence CBA
Healthy volunteers will receive Treatments C, then B, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days
干预措施: Treatment C - 200 mg Fed (Drug)
结局指标
主要结局
Maximum Observed Concentration in Plasma (Cmax) of Pexidartinib
时间窗: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdose
Mean Cmax of pexidartinib is calculated for each treatment period
Time to Cmax (Tmax)
时间窗: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdose
Median Tmax of pexidartinib is calculated for each treatment period
Area Under the Concentration-time Curve From Time of Dosing to Last Measurable Concentration (AUClast) and to Infinity (AUCinf)
时间窗: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdose
Mean AUClast and AUCinf for pexidartinib are calculated for each treatment period
Terminal Half-life (t1/2)
时间窗: Baseline, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours postdose
Mean t1/2 for pexidartinib is calculated for each treatment period
次要结局
未报告次要终点