Safety, Tolerability, and Pharmacokinetics of Multiple Rising Doses of BI 425809 Tablets Given Orally Once Daily for 12 Days to Young and Elderly Healthy Male and Female Volunteers (Randomised, Double-blind, Placebo-controlled Within Dose Groups Phase I Study)(Part 1) and Comparison of Pharmacokinetics of a Single Oral Dose of BI 425809 After Oral Administration in the Morning Versus Oral Administration in the Evening in Young Healthy Male and Female Volunteers (Randomised, Two-sequence, Open, Two Period, Two-way Cross Over) (Part 2)
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 96
- 试验地点
- 1
- 主要终点
- Percentage of Subjects With Drug Related Adverse Events (AEs) in Part I
研究概览
简要总结
The aim of the study is to investigate the safety, tolerability, and pharmacokinetics of multiple rising doses of BI 425809 tablets given orally once daily for 12 days to young and elderly healthy male and female volunteers and to compare single dose pharmacokinetics of BI 425809 given in the morning and in the evening.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- Double
入排标准
- 年龄范围
- 18 Years 至 50 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Healthy male or female subjects according to the investigator´s assessment, based on a complete medical history including a physical examination, vital signs (blood pressure (BP), pulse rate (PR), 12-lead electrocardiogram (ECG), and clinical laboratory tests
- •age of 18 to 50 years (incl.) for young healthy volunteers or age of 65 to 80 years (incl.) for elderly healthy volunteers
- •Body mass index (BMI) of 18.5 to 29.9 kg/m2 (incl.)
- •Signed and dated written informed consent prior to admission to the study in accordance with good clinical practice (GCP) and local legislation
- •Female subjects who meet any of the following criteria:
- •Surgically sterilised
- •Postmenopausal, defined as at least 1 year of spontaneous amenorrhea (in questionable cases a blood sample with simultaneous levels of follicle stimulating hormone (FSH) above 40 U/L and estradiol below 30 ng/L is confirmatory)
排除标准
- •Any finding in the medical examination (including BP, PR or ECG) is deviating from normal and judged as clinically relevant by the investigator
- •Repeated measurement of systolic blood pressure outside the range of 90 to 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg in young subjects, and systolic blood pressure greater than 150 mmHg, diastolic blood pressure greater than 95 mmHg in elderly subjects, or pulse rate outside the range of 50 to 90 bpm
- •Any laboratory value outside the reference range that the investigator considers to be of clinical relevance
- •Any evidence of a concomitant disease judged as clinically relevant by the investigator
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- •Surgery of the gastrointestinal tract that could interfere with kinetics of the trial medication
- •Diseases of the central nervous system (including but not limited to any kind of seizures or stroke), and other relevant neurological or psychiatric disorders
- •History of relevant orthostatic hypotension, fainting spells, or blackouts
- •Chronic or relevant acute infections
- •Further exclusion criteria may apply
研究组 & 干预措施
Placebo - part I
Part I only - placebo tablet, oral administration with 240ml water, over 14 days
干预措施: Placebo (Drug)
BI 425809 low dose - part II
Part II - one low dose tablet on day 1 of visit 2 and 2a
BI 425809 low dose - part I
Part I - low dose tablet, oral administration with 240 ml water, over 14 days
干预措施: BI 425809 (Drug)
BI 425809 high dose -part I
Part I only - high dose tablet, oral administration with 240 ml water, over 14 days
干预措施: BI 425809 (Drug)
BI 425809 very low dose - part I
Part I only - very low dose tablet, oral administration with 240 ml water, over 14 days
干预措施: BI 425809 (Drug)
BI 425809 medium dose - part I
Part I only - medium dose tablet, oral administration with 240 ml water, over 14 days
干预措施: BI 425809 (Drug)
BI 425809 very high dose -part I
Part I only - very high dose tablet, oral administration with 240 ml water, over 14 days
干预措施: BI 425809 (Drug)
结局指标
主要结局
Percentage of Subjects With Drug Related Adverse Events (AEs) in Part I
时间窗: From first dose of study medication until 11 days after the last dose of study medication, up to 25 days
Percentage of subjects with drug related adverse events (AEs) in part I is reported
Area Under the Concentration-time Curve of the BI 425809 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) Part II
时间窗: PK samples were taken at: 0, 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48, 72, 96 hours after drug administration
Area under the concentration-time curve of the BI 425809 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) part II is reported.
Maximum Measured Concentration of the BI 425809 in Plasma (Cmax) Part II
时间窗: PK samples were taken at: 0, 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48, 72, 96 hours after drug administration
Maximum measured concentration of the BI 425809 in plasma (Cmax) part II.
次要结局
- Percentage of Subjects With Drug Related Adverse Events (AEs) in Part II(From first dose of study medication until 11 days after the last dose of study medication, up to 12 days)
- Area Under the Concentration-time Curve of the BI 425809 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC 0-infinity) Part II(PK samples were taken at: 0, 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48, 72, 96 hours after drug administration)
- Area Under the Concentration-time Curve of the BI 425809 in Plasma Over the Time Interval From 0 to 24 Hours (AUC0-24) Part I(PK plasma samples were taken at: 2 hours before drug administration and 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24 hours after the drug administration in YH and EH population)
- Area Under the Concentration-time Curve of the BI 425809 in Plasma at Steady State Over a Uniform Dosing Interval τ (AUCτ,ss) Part I(Up to 528 hours. The details are described in description.)
- Maximum Measured Concentration of the BI 425809 in Plasma (Cmax) Part I(PK plasma samples were taken at: 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48 and 58 hours after drug administration.)
- Maximum Measured Concentration of the BI 425809 in Plasma at Steady State Over a Uniform Dosing Interval τ (Cmax,ss) Part I(Up to 528 hours. The details are described in description.)