A Single-center, Open-label, Randomized, Formulation Screening, Two-cohort, Four-period, Crossover Study for Selexipag Sustained Release in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 24
- 试验地点
- 1
- 主要终点
- Maximum Observed Analyte Concentration (Cmax) of Selexipag and ACT-333679
研究概览
简要总结
The purpose of this study is to evaluate the pharmacokinetic (PK) of selexipag and ACT-333679 following single oral administration of the matrix tablet and the encapsulated pellets of selexipag, each with 3 different release profiles, as compared to selexipag immediate release (IR) tablets in healthy male participants.
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
- None
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
- •Healthy on the basis of physical examination, medical history, vital signs, and 12-lead electrocardiogram (ECG) performed at screening
- •Healthy on the basis of clinical laboratory tests performed at screening. If the results of the serum chemistry panel, hematology, or urinalysis are outside the normal reference ranges, the participants may be included only if the investigator judges the abnormalities or deviations from normal to be not clinically significant. This determination must be recorded in the participant's source documents and initialed by the investigator
- •Must sign an informed consent form (ICF) indicating they understand the purpose of, and procedures required for, the study and is willing to participate in the study
- •Body mass index (BMI; weight (kilogram [kg]/height^2 [meter {m}]^2) between 18.0 and 28.0 kilogram per square centimeter (kg/m^2) (inclusive), and body weight not less than 50.0 kg at screening
- •Blood pressure (after the participant is supine for 5 minutes) between 90 and 145 millimeters of mercury (mmHg) systolic, inclusive, and no higher than 90 mmHg diastolic at screening. If blood pressure is out of range, up to 2 repeated assessments within the screening period are permitted, last assessment being conclusive
排除标准
- •Clinically significant abnormal values for hematology, biochemistry, or urinalysis at screening and on Day -1 of Treatment Period 1 as deemed appropriate by the investigator
- •Known allergies, hypersensitivity, or intolerance to selexipag or its excipients
- •Any contraindication included in the Summary of Product Characteristics (SmPC) of selexipag
- •History or clinical evidence of any disease and/or existence of any surgical or medical condition, which might interfere with the absorption, distribution, metabolism or excretion of the study treatments (appendectomy and herniotomy allowed, cholecystectomy not allowed)
- •Previous history of stroke, fainting, collapse, syncope, orthostatic hypotension, vasovagal reactions, head injury
研究组 & 干预措施
Cohort 1: Selexipag Matrix Tablets
Participants will receive oral doses of selexipag matrix tablets based on release profiles (IR=immediate release, F=fast release, M=medium release and S=slow release) in treatment sequence 1 (IR+F+M+S), treatment sequence 2 (F+S+IR+M), treatment sequence 3 (M+ IR+ S+F) and treatment sequence 4 (S+M+F+IR) in periods 1, 2, 3, and 4, respectively under fasted condition. A washout period of at least 7 days will be maintained between each treatment period.
干预措施: Selexipag matrix tablet (Drug)
Cohort 1: Selexipag Matrix Tablets
Participants will receive oral doses of selexipag matrix tablets based on release profiles (IR=immediate release, F=fast release, M=medium release and S=slow release) in treatment sequence 1 (IR+F+M+S), treatment sequence 2 (F+S+IR+M), treatment sequence 3 (M+ IR+ S+F) and treatment sequence 4 (S+M+F+IR) in periods 1, 2, 3, and 4, respectively under fasted condition. A washout period of at least 7 days will be maintained between each treatment period.
干预措施: Selexipag Immediate-release (IR) tablet (Drug)
Cohort 2: Selexipag Encapsulated Pellets
Participants will receive oral doses of selexipag encapsulated) pellets based on release profiles (IR=immediate release, F=fast release, M=medium release and S=slow release) in treatment sequence 1 (IR+F+M+S), treatment sequence 2 (F+S+IR+M), treatment sequence 3 (M+ IR+ S+F) and treatment sequence 4 (S+M+F+IR) in periods 1, 2, 3, and 4, respectively under fasted condition. A washout period of at least 7 days will be maintained between each treatment period.
干预措施: Selexipag encapsulated pellets (Drug)
Cohort 2: Selexipag Encapsulated Pellets
Participants will receive oral doses of selexipag encapsulated) pellets based on release profiles (IR=immediate release, F=fast release, M=medium release and S=slow release) in treatment sequence 1 (IR+F+M+S), treatment sequence 2 (F+S+IR+M), treatment sequence 3 (M+ IR+ S+F) and treatment sequence 4 (S+M+F+IR) in periods 1, 2, 3, and 4, respectively under fasted condition. A washout period of at least 7 days will be maintained between each treatment period.
干预措施: Selexipag Immediate-release (IR) tablet (Drug)
结局指标
主要结局
Maximum Observed Analyte Concentration (Cmax) of Selexipag and ACT-333679
时间窗: Predose and 0 to 72 hours postdose
The Cmax is the maximum observed analyte concentration.
Area Under Analyte Concentration From Time Zero to the Last Quantifiable Concentration (AUC [0-last]) of Selexipag and ACT-333679
时间窗: Predose and 0 to 72 hours postdose
AUC (0-last) defined as the area under the analyte concentration-time curve from time zero to time of the last measurable (non-BQL) analyte concentration, calculated by linear-linear trapezoidal summation.
Plasma analyte concentration 24 hours (C24) Post Dose of Selexipag and ACT-333679
时间窗: Predose and 0 to 72 hours postdose
C24 defined as plasma analyte concentration at 24 hours postdose.
Area Under the Analyte Concentration-Time Curve From Time Zero to Infinite Time (AUC [0-infinity])
时间窗: Predose and 0 to 72 hours postdose
AUC (0-infinity) is defined the area under the analyte concentration-time curve from time zero to infinity time, calculated as the sum of AUC (0-last) and C(last)/lambda(z); wherein AUC (0-last) is area under the plasma concentration-time curve from time zero to last measurable concentration, C(last) is the last observed measurable concentration, and lambda(z) is apparent terminal elimination rate constant.
次要结局
- Number of Participants with Adverse Events (AEs) as a Measure of Safety and Tolerability(Up to 50 Days)