3-part Study to Assess Safety, Tolerability, PK and PD of Single and Multiple Ascending Doses of EXS21546, and to Evaluate the Relative Bioavailability of 2 Formulations, in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 64
- 试验地点
- 1
- 主要终点
- EXS21546 and Metabolite Area under the plasma concentration versus time curve (AUC)
研究概览
简要总结
A 3-part Study to Assess Safety, Tolerability, PK and PD of Single (Part 1) and Multiple (Part 2) Ascending Doses of EXS21546, and to Evaluate the Relative Bioavailability of a Solid Dose Formulation Compared to a Powder for Oral Suspension (Part 3), in Healthy Male Subjects.
详细描述
Part 1 is a randomised, double-blind, placebo-controlled, SAD study with a food effect assessment.
Part 2 is a randomised, double-blind, placebo controlled, MAD study over 14 days. In order to explore the potential CYP3A4 inducer effect, midazolam will also be administered in one cohort.
Part 3 is a 3-period, open label, randomised, sequential study. Each subject will receive solid dose formulation and powder for oral suspension in a randomised manner.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Sequential
- 主要目的
- Treatment
- 盲法
- Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)
盲法说明
Part 1 and Part 2 are double blind. Part 3 is open label.
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •BMI 18.0 to 30.0 kg/m2
- •Weight ≥60 kg
- •Must adhere to contraception requirements
排除标准
- •Subjects who have received any IMP in a clinical research study within the 90 days prior to Day 1
- •Subjects who have previously been administered IMP in this study.
- •Evidence of current SARS-CoV-2 infection
- •History of any drug or alcohol abuse in the past 2 years
- •Regular alcohol consumption in males >21 units per week
- •A confirmed positive alcohol breath test at screening or admission
- •Current smokers and those who have smoked within the last 12 months. A confirmed breath carbon monoxide reading of greater than 10 ppm at screening or admission
- •Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months
- •Subjects with pregnant or lactating partners
- •Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) antibody results
- •Regimen L only: History of sleep apnea
- •Subjects with a history of cholecystectomy or gall stones
- •Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients
- •Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hay fever is allowed unless it is active
- •Donation of blood or plasma within the previous 3 months or loss of greater than 400 mL of blood
研究组 & 干预措施
Placebo
Placebo Powder for Oral Suspension
干预措施: Food Effect (Other)
EXS21546 Powder for Oral Suspension
EXS21546 Powder for Oral Suspension
干预措施: EXS21546 Powder for Oral Suspension (Drug)
EXS21546 Powder for Oral Suspension
EXS21546 Powder for Oral Suspension
干预措施: Midazolam (Other)
EXS21546 Powder for Oral Suspension
EXS21546 Powder for Oral Suspension
干预措施: Food Effect (Other)
Placebo
Placebo Powder for Oral Suspension
干预措施: Midazolam (Other)
Placebo
Placebo Powder for Oral Suspension
干预措施: Placebo Powder for Oral Suspension (Other)
EXS21546 Granule in Capsule
EXS21546 Granule in Capsule
干预措施: EXS21546 Granule in Capsule (Drug)
EXS21546 Granule in Capsule
EXS21546 Granule in Capsule
干预措施: Food Effect (Other)
结局指标
主要结局
EXS21546 and Metabolite Area under the plasma concentration versus time curve (AUC)
时间窗: 17 days
EXS21546 and Metabolite Area under the plasma concentration versus time curve (AUC)
EXS21546 and Metabolite Peak Plasma Concentration (Cmax)
时间窗: 17 days
EXS21546 and Metabolite Peak Plasma Concentration (Cmax)
Number of participants with treatment emergent Adverse Events
时间窗: 1 month
Number of participants with treatment emergent Adverse Events
次要结局
未报告次要终点