A Phase 1, Single-Center, Open-Label Study to Evaluate the Pharmacokinetics and Tolerability of Rilzabrutinib (PRN1008) in Japanese and Caucasian Healthy Male and Female Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 23
- 试验地点
- 1
- 主要终点
- Time from dosing to maximum measured concentration of total rilzabrutinib in plasma (tmax)
研究概览
简要总结
This is a single-dose and multiple doses study to assess the Pharmacokinetics (PK) of rilzabrutinib as well as to evaluate the tolerability of rilzabrutinib in Japanese and Caucasian Healthy Male and Female subjects.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 75 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Japanese subjects must have both biological parents and all four grandparents of Japanese ancestry and born in a Japanese country of origin.
- •Caucasian subjects must have four Caucasian grandparents (Hispanics of white race can be considered Caucasian).
- •Healthy adult male or non-pregnant non-lactating females, 18 to 75 years of age (inclusive) at the time of screening.
- •Body mass index (BMI) ≥18 and ≤35 (kg/m2), inclusive, and a minimum body weight of 45 kg.
- •Additional inclusion criteria might apply.
排除标准
- •Symptoms consistent with COVID-19 such as fever, cough, and shortness of breath within 14 days before Day
- •Positive test for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) at screening or check-in (Day -1).
- •Known previous COVID-19 infection.
- •Use of any prescription or over-the-counter (OTC) medication, herbal products, or dietary supplements within the 7 days or 5 half-lives, whichever is longer, prior to the first study drug administration. Use of hormonal contraception is allowed prior to and during the study.
- •Additional exclusion criteria might apply.
研究组 & 干预措施
Cohort 1: Rilzabrutinib
干预措施: Rilzabrutinib (Drug)
Cohort 2: Rilzabrutinib
干预措施: Rilzabrutinib (Drug)
结局指标
主要结局
Time from dosing to maximum measured concentration of total rilzabrutinib in plasma (tmax)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Maximum measured concentration of total rilzabrutinib in plasma (Cmax)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Area under the concentration-time curve of total rilzabrutinib in plasma from 0 to the last measurable concentration (AUC0-last)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Terminal Half-Life of total rilzabrutinib in Plasma (t1/2)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Apparent volume of distribution after oral administration (Vd/F)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Accumulation ratio (Rac)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Apparent Total Clearance of rilzabrutinib in the plasma after oral administration (CL/F)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Dose proportionality of rilzabrutinib
时间窗: Up to 48 hours after the last rilzabrutinib dose
Area under the concentration-time curve of total rilzabrutinib in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf)
时间窗: Up to 48 hours after the last rilzabrutinib dose
Area under the plasma concentration-time curve of total rilzabrutinib from zero during the dosage interval (AUC0-tau)
时间窗: Up to 48 hours after the last rilzabrutinib dose
次要结局
- Incidence of potentially clinically significant laboratory test, vital signs, and electrocardiogram (ECGs) abnormalities(Up to 14 days after rilzabrutinib dosing)
- Number of Adverse Events (AE) / Serious Adverse Events (SAE)(From date of signed ICF, up to 47 days)
- Terminal Half-Life of rilzabrutinib metabolites in Plasma (t1/2)(Up to 48 hours after the last rilzabrutinib dose)
- Bruton's Tyrosine Kinase (BTK) Occupancy characterization(Up to 48 hours after the last rilzabrutinib dose)
- Area under the concentration-time curve of rilzabrutinib metabolites in plasma from 0 to the last measurable concentration (AUC0-last)(Up to 48 hours after the last rilzabrutinib dose)
- Maximum measured concentration of rilzabrutinib metabolites in plasma (Cmax)(Up to 48 hours after the last rilzabrutinib dose)
- Time from dosing to maximum measured concentration of rilzabrutinib metabolites in plasma (tmax)(Up to 48 hours after the last rilzabrutinib dose)
- Area under the concentration-time curve of rilzabrutinib metabolites in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf)(Up to 48 hours after the last rilzabrutinib dose)
- Area under the plasma concentration-time curve of rilzabrutinib metabolites from zero during the dosage interval (AUC0-tau)(Up to 48 hours after the last rilzabrutinib dose)