Safety, Tolerability and Pharmacokinetics of Single Rising Oral Doses (40 to 400 mg) of KUC-7483 Tablets in Healthy Male Volunteers (Double-blind at Each Dose Level, Randomised, Placebo Controlled Study) as Well as Food Effects at 80 mg (Intraindividual Testing in the Same Volunteers)
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 50
- 主要终点
- Number of subjects with clinically significant changes in special laboratory parameters
研究概览
简要总结
Study to investigate safety, tolerability and pharmacokinetics of KUC 7483
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- Double
入排标准
- 年龄范围
- 30 Years 至 60 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy males according to the following criteria:
- •Based upon a complete medical history, including the physical examination, vital signs (BP, PR), 12-lead ECG, clinical laboratory tests
- •No finding deviating from normal and of clinical relevance
- •No evidence of a clinically relevant concomitant disease
- •Age ≥30 and Age ≤60 years
- •BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index)
- •Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice and the local legislation
排除标准
- •Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
- •Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
- •History of relevant orthostatic hypotension, fainting spells or blackouts
- •Chronic or relevant acute infections
- •History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
- •Intake of drugs with a long half-life (> 24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
- •Use of drugs which might reasonably influence the results of the trial based on the knowledge at the time of protocol preparation within 10 days prior to administration or during the trial
- •Participation in another trial with an investigational drug within two months prior to administration or during the trial
- •Smoker (> 10 cigarettes or > 3 cigars of > 3 pipes/day)
- •Inability to refrain from smoking on trial days
- •Alcohol abuse (more than 60 g/day)
- •Drug abuse
- •Blood donation (more than 100 mL within four weeks prior to administration or during the trial)
- •Excessive physical activities (within one week prior to administration or during the trial)
- •Any laboratory value outside the reference range of clinical relevance
研究组 & 干预措施
KUC 7483 CL
single rising doses
干预措施: KUC 7483 CL (Drug)
KUC 7483 CL, fed
dosing after high fat meal
干预措施: KUC 7483 CL (Drug)
KUC 7483 CL, fed
dosing after high fat meal
干预措施: High fat meal (Other)
Placebo
干预措施: Placebo (Drug)
结局指标
主要结局
Number of subjects with clinically significant changes in special laboratory parameters
时间窗: up to 24 hours after drug administration
Tropanin I, Insulin, C-Peptide, Glucagon, free fatty acids and faecal occult blood testing
Number of subjects with clinically significant findings in physical examination
时间窗: up to 8 days after last drug administration
Number of subjects with clinically significant changes in vital signs
时间窗: up to 8 days after last drug administration
Blood pressure, Pulse Rate, Respiratory Rate, body temperature, orthostatic testing
Number of subjects with clinically significant findings in 12-lead ECG (electrocardiogram)
时间窗: up to 8 days after last drug administration
Number of subjects with clinically significant changes in laboratory parameters
时间窗: up to 8 days after last drug administration
Number of subjects with adverse events
时间窗: up to 8 days after last drug administration
Assessment of tolerability by investigator on a 3-point rating scale
时间窗: within 8 days after last drug administration
次要结局
- tmax (time from dosing to the maximum concentration of the analyte in plasma)(up to 48 hours after drug administration)
- AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point)(up to 48 hours after drug administration)
- MRTpo (mean residence time of the analyte in the body after oral administration)(up to 48 hours after drug administration)
- Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)(up to 48 hours after drug administration)
- Cmax (maximum measured concentration of the analyte in plasma)(up to 48 hours after drug administration)
- AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)(up to 48 hours after drug administration)
- λz (terminal rate constant of the analyte constant in plasma)(up to 48 hours after drug administration)
- CLR,t1-t2 (renal clearance of the analyte determined from the time point t1 until time point t2)(up to 48 hours after drug administration)
- CL/F (apparent clearance of the analyte in the plasma after extravascular administration)(up to 48 hours after drug administration)
- t1/2 (terminal half-life of the analyte in plasma)(up to 48 hours after drug administration)
- Aet1-t2 (amount of the analyte that is eliminated in urine from the time point t1 until time point t2)(up to 48 hours after drug administration)
- fet1-t2 (fraction of administered drug excreted unchanged in urine from the time point t1 until time point t2)(up to 48 hours after drug administration)