A Phase I, Drug-drug Interaction Study Between Oral Doses of GLPG1205 and a Cocktail of CYP2C9, CYP2C19 and CYP1A2 Substrates in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Galapagos NV
- 入组人数
- 14
- 试验地点
- 1
- 主要终点
- The time of occurrence of Cmax (tmax) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo
研究概览
简要总结
This will be a Phase I, randomized, double-blind, placebo-controlled, 2 period cross-over, drug-drug interaction study to evaluate the effect of multiple oral doses of GLPG1205 or placebo (daily from Day 1 to Day 12) on a single dose pharmacokinetic profile of a cocktail of CYP450 substrates administered to healthy male subjects. The cocktail of CYP450 substrates will consist of 10 mg warfarin (CYP2C9 substrate), 20 mg omeprazole (CYP2C19 substrate) and 100 mg caffeine (CYP1A2 substrate).
Fourteen healthy male subjects will receive during two treatment periods from Day 1 to Day 12 a daily dose of GLPG1205 or placebo. On Day 13, a single dose of the cocktail of CYP450 substrates will be co-administered either with GLPG1205 or with placebo. The two treatment periods will be separated by a wash-out period of at least 28 days.
Also, the safety and tolerability of multiple oral doses of GLPG1205 administered with or without a cocktail of CYP450 substrates in healthy male subjects will be evaluated.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Treatment
- 盲法
- Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)
入排标准
- 年龄范围
- 18 Years 至 50 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •healthy male, age 18-50 years
- •BMI between 18-30 kg/m2
排除标准
- •Poor or moderate metabolizer for CYP2C9 or CYP2C19 as determined by genotyping
- •Having a contraindication as indicated in the respective Summary of Product Characteristics (or Package Leaflets) for warfarin, omeprazole or caffeine
- •Intake of nutraceuticals within 3 weeks prior to dosing or within 6 times the elimination half life
- •Intake of enzyme inducing or enzyme inhibiting drugs within 3 months prior to dosing
- •Intake of vitamin K within 3 weeks prior to dosing
- •Any condition that might interfere with the procedures or tests in this study
- •Drug or alcohol abuse
研究组 & 干预措施
GLPG1205 and single CYP450 substrate cocktail dose
Daily GLPG1205 administration from Day 1 to Day 12 Single GLPG1205 co-administration on Day 13 with CYP450 substrate cocktail
干预措施: GLPG1205 (Drug)
GLPG1205 and single CYP450 substrate cocktail dose
Daily GLPG1205 administration from Day 1 to Day 12 Single GLPG1205 co-administration on Day 13 with CYP450 substrate cocktail
干预措施: Cocktail of CYP450 substrates (Drug)
Placebo and single CYP450 substrate cocktail dose
Daily Placebo administration from Day 1 to Day 12 Single Placebo co-administration on Day 13 with CYP450 substrate cocktail
干预措施: Placebo (Drug)
Placebo and single CYP450 substrate cocktail dose
Daily Placebo administration from Day 1 to Day 12 Single Placebo co-administration on Day 13 with CYP450 substrate cocktail
干预措施: Cocktail of CYP450 substrates (Drug)
结局指标
主要结局
The time of occurrence of Cmax (tmax) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo
时间窗: Between Day 13 and 7 days after the last dose
To characterize the time of occurrence of Cmax (tmax) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects
The area under the plasma concentration versus time curve (AUC) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo
时间窗: Between Day 13 and 7 days after the last dose
To characterize the area under the plasma concentration versus time curve (AUC) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects
The maximum observed concentration (Cmax) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo
时间窗: Between Day 13 and 7 days after the last dose
To characterize the maximum observed concentration (Cmax) of CYP450 substrates in plasma over time after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects
The apparent terminal half-life (t1/2) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo
时间窗: Between Day 13 and 7 days after the last dose
To characterize the apparent terminal half-life (t1/2) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects
The metabolite over parent AUC ratio (R) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo
时间窗: Between Day 13 and 7 days after the last dose
To characterize the metabolite over parent AUC ratio (R) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects
次要结局
- Number of adverse events(Between Screening and 7 days after the last dosing)
- Changes in vital signs as measured by heart rate, blood pressure, respiratory rate and oral body temperature(Between Screening and 7 days after the last dosing)
- Changes in 12-lead ECG measures(Between Screening and 7 days after the last dosing)
- Changes in physical examination measures(Between Screening and 7 days after the last dosing)
- Changes in blood safety lab parameters(Between Screening and 7 days after the last dosing)
- Changes in urine safety lab parameters(Between Screening and 7 days after the last dosing)