A Study to Assess the Effect Tasimelteon on the Cytochrome P450 3A4 and 2C8 Enzymes in Healthy Subjects
An Open-Label, Single-Sequence Study to Assess the Effect of Multiple Doses of Tasimelteon on the Cytochrome P450 3A4 and 2C8 Enzymes Using Midazolam and Rosiglitazone as Substrates in Healthy Subjects
研究概览
研究类型
注册 (实际的)
阶段
- 阶段1
联系人和位置
学习地点
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Missouri
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Springfield、Missouri、美国、65802
- Bio-Kinetic Clinical Applications
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参与标准
资格标准
适合学习的年龄
接受健康志愿者
有资格学习的性别
描述
Inclusion Criteria:
- Ability and acceptance to provide written informed consent;
- Subjects must be males or females between 18 and 55 years of age, inclusive;
Female subjects of childbearing potential must be non-pregnant and non-lactating and have a negative serum or urine pregnancy test at the Screening visit and at Check-in (Days -1) and agree not to attempt to become pregnant during the course of the study. Female subjects of childbearing potential (including peri-menopausal women who have had a menstrual bleeding within 1 year) must be using appropriate birth control (e.g. intrauterine device [IUD], diaphragm or condom with spermicidal jelly or foam or abstinence, or cervical cap) for a period of 35 days before the first dosing, for the duration of the study, and for one month after the last dose;
a. Note: Women are not permitted to use hormonal methods of birth control (e.g. oral contraceptives, hormonal intrauterine device [IUD], patch and steroids) and must use another acceptable method of birth control during the study and for one month after the last dose. Women currently taking oral contraceptives will be required to discontinue their regimen two weeks prior to first dosing.
- Subjects with Body Mass Index (BMI) of >18 and <35 kg/m2 (BMI = weight (kg)/ [height (m)]2);
Vital signs (after 3 minutes resting in a semi-supine position) which are within the ranges shown below:
- Body temperature between 35.0-37.5 °C;
- Systolic blood pressure between 90-150 mm Hg;
- Diastolic blood pressure between 50-95 mm Hg;
- Pulse rate between 50-100 bpm.
- Willing and able to comply with study requirements;
- Subjects must be in good health as determined by past medical history, physical examination, electrocardiogram, clinical laboratory tests and urinalysis;
Exclusion Criteria:
- History of recent (within six months) drug or alcohol abuse;
- Any major surgery within three months of Day 1 or any minor surgery within one month;
- Donation or loss of 400 mL or more of blood within two months prior to the Baseline Visit;
- History or current evidence of cardiovascular, hepatic, hematopoietic, renal, gastrointestinal or metabolic dysfunction judged by the Investigator to be clinically significant;
- Any condition requiring the regular use of medication;
- History of intolerance and/or hypersensitivity to drugs including midazolam, rosiglitazone or other 'glitazones', melatonin or melatonin agonists, or anyone who has taken a melatonin preparation chronically within the past two months prior to Day 1;
- History of or current evidence of hypoglycemia judged by the Investigator to be clinically significant;
- History of liver disease and/or positive for one or more of the following serological results: HCV, HIV, HBsAg
- Treatment with any drug known to cause major organ system toxicity (e.g., chloramphenicol or tamoxifen) during the 60 day preceding Day 1;
- Elevated (> 2 times the upper limit of normal) liver function tests (i.e. aspartate aminotransferase (AST [SGOT]), alanine aminotransferase (ALT [SGPT]), and total bilirubin);
- Inability to be venipunctured and/or tolerate venous access;
- Subjects who have used tobacco products 3 months prior to dosing.
- Exposure to any investigational drug within 30 days or 5 half lives (whichever is longer) of baseline, including placebo;
- Participation in a previous BMS-214778/VEC-162 trial;
- Use of prescription or OTC medication, including herbal products (e.g., St. John's Wort) within 2 weeks of Day 1;
- Use of any food or beverage containing alcohol, grapefruit or grapefruit juice, apple or orange juice, vegetables from the mustard green family (e.g. kale, broccoli, watercress, collard greens, kohlrabi, brussel sprouts, mustard) and charbroiled meats within 1 week before Day 1 and during the actual duration of the study;
- Any other sound medical reason as determined by the clinical Investigator.
学习计划
研究是如何设计的?
设计细节
- 主要用途:基础科学
- 分配:非随机化
- 介入模型:并行分配
- 屏蔽:无(打开标签)
武器和干预
参与者组/臂 |
干预/治疗 |
|---|---|
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实验性的:Steady State PK Group
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20mg daily dosing, Days 4-20
4mg, single dose, Days 3 and 20
其他名称:
10mg, single dose, Days 1 and 18
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实验性的:No steady state PK
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20mg daily dosing, Days 4-20
4mg, single dose, Days 3 and 20
其他名称:
10mg, single dose, Days 1 and 18
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研究衡量的是什么?
主要结果指标
结果测量 |
措施说明 |
大体时间 |
|---|---|---|
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CYP3A4 Pharmacokinetics
大体时间:Days 1 and 18
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Composite of 24 hour pharmacokinetic parameters of midazolam will be compared between Day 1 and Day 18.
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Days 1 and 18
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CYP2C8 Pharmacokinetics
大体时间:Days 3 and 20
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Composite of 24 hour pharmacokinetic parameters of rosiglitazone will be compared between Day 3 and 20.
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Days 3 and 20
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次要结果测量
结果测量 |
措施说明 |
大体时间 |
|---|---|---|
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Midazolam PK
大体时间:Days 1 and 17
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Composite pharmacokinetic parameters of midazolam and α-hydroxymidazolam will be compared between Day 1 and Day 18.
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Days 1 and 17
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Rosiglitazone PK
大体时间:Days 3 and 20
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Composite of 24 hour pharmacokinetic parameters of rosiglitazone will be compared between Day 3 and Day 20.
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Days 3 and 20
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Tasimelteon multiple dose pharmacokinetics
大体时间:Days 4-21
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Composite of 24 hour pharmacokinetic parameters of tasimelteon and tasimelteon metabolites M9, M11, M12, M13, and M14, at Days 5, 8, 11, 14 (Group 1 only), and Days 17 and 19 (Groups 1 and 2).
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Days 4-21
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Tasimelteon safety and tolerability
大体时间:Days 1-21
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Safety of multiple oral doses of 20 mg of tasimelteon alone and in combination with 10 mg of midazolam as measured by vital signs, ECG, and adverse event reporting.
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Days 1-21
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合作者和调查者
研究记录日期
研究主要日期
学习开始
初级完成 (实际的)
研究完成 (实际的)
研究注册日期
首次提交
首先提交符合 QC 标准的
首次发布 (估计)
研究记录更新
最后更新发布 (估计)
上次提交的符合 QC 标准的更新
最后验证
更多信息
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