A Phase I Study to Evaluate the Pharmacokinetics, Pharmacodynamics and Safety in Healthy Subjects with Multiple Administration of Tiprogrel
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 14
- 试验地点
- 1
- 主要终点
- PK parameters： Cmax
研究概览
简要总结
This study is designed to evaluate the pharmacokinetics, pharmacodynamics and safety in healthy subjects with multiple administration of Tiprogrel.
详细描述
Tiprogrel is a novel oral P2Y12 receptor antagonist.This study is to evaluate the pharmacokinetics, pharmacodynamics and safety in healthy subjects with multiple administration of Tiprogrel, and compare pharmacokinetics /pharmacodynamic of Tiprogrel,Clopidogrel and Ticagrelor.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Sequential
- 主要目的
- Basic Science
- 盲法
- None
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
- •Male and female Healthy Subjects
- •Subject has the ability and willingness to comply with study procedures and follow-up examination.
- •3：18 to 50 years of age (including the threshold) 4: Body mass index (BMI) ≥ 19.0 to ≤ 28.0 kg/m2; total body weight of male subject ≥ 50 kg at Screening; total body weight of female subject ≥ 45 kg at Screening; 5：Medically healthy based on their medical history, and physical examination, clinical laboratory test results, ECGs, and vital sign measurements as determined by the Investigator at Screening; 6: Female subjects are not pregnant or breastfeeding, and the fertile female and male subjects must agree to follow instructions for method(s) of contraception.
排除标准
- •History or presence of metabolic, allergy, dermatology, liver, kidney, hematology, cardiovascular, gastrointestinal, nervous, respiratory, endocrine or psychiatric diseases.
- •History or presence of obviously active bleeding, or coagulation or bleeding disorders, or any skin petechiae, or thrombus, or spontaneous bleeding.
- •Subject with history of allergy to a variety of drugs, or has a known or suspected hypersensitivity to tiprogrel or other anti-platelet drugs
- •Subjects who had a history of major surgery within 3 months before the trial or planned to undergo surgery during the study period.
- •Subjects who have lost or donated ≥ 400 mL blood or received blood transfusion or used blood products within three months, or subjects with clinically significant anemia based on the judgment of the Investigator
- •Subjects with systolic blood pressure of > 140 mmHg or < 90 mmHg, diastolic blood pressure of > 90 mmHg or < 60 mmHg
- •Subjects with 12-lead ECG examination: QTcF > 450 msec
- •Platelet count (PLT) value, beyond the laboratory's reference range
- •Activated partial thromboplastin time (APTT) and Prothrombin Time (PT), beyond the laboratory's reference range
- •ALT, AST, γ-GGT, ALP and TBIL value >1.5 times the upper limit of normal value
- •Subjects with positive results at screening for HIV, syphilis, HBsAg, or HCV
- •Subjects who have taken aspirin/other nonsteroidal anti-inflammatory drugs (NSAIDs) or other drugs that may affect coagulation function within 2 weeks before the trial
- •Subjects who have taken prescription drugs/products or herbs within 2 weeks or 5 half-lives (whichever is longer) before the trial;or taken OTC drugs/products within 7 days before the trial.
- •Subjects who have received live or attenuated vaccines within 1 month prior to receiving the study drug or expected to receive vaccines during the study period
- •Subjects who have ingested investigational drug within 3 months or 5 half-lives prior to the first study drug dose
- •Subjects who have participated in another clinical trial within 3 months or 5 half-lives prior to the first study drug dose;
- •Consumption of any known liver enzyme inducers/inhibitors within 30 days prior to the first study drug dose;
- •Have a history of drug addiction or drug abuse within 1 year prior to screening;
- •Positive results for alcohol, or cotinine, or urine for drugs test in screening or admission;
- •Subject with alcohol consumption defined as > 21 units per week for men and > 14 units per week for woman;
- •Use of tobacco or nicotine-containing products within 1 month prior to screening;
- •CYP2C19 poor metabolizer;
- •Subjects with a history of fainting needle or blood;
- •Subjects who are not suitable to participate in this experiment.
研究组 & 干预措施
Tiprogrel-Clopidogrel-Ticagrelor
Period 1: Dose 1 Tiprogrel; Period 2: Dose 2 Tiprogrel ; Period 3: Clopidogrel; Period 4: Ticagrelor
干预措施: Tiprogrel (Drug)
Tiprogrel-Clopidogrel-Ticagrelor
Period 1: Dose 1 Tiprogrel; Period 2: Dose 2 Tiprogrel ; Period 3: Clopidogrel; Period 4: Ticagrelor
干预措施: Clopidogrel (Drug)
Tiprogrel-Clopidogrel-Ticagrelor
Period 1: Dose 1 Tiprogrel; Period 2: Dose 2 Tiprogrel ; Period 3: Clopidogrel; Period 4: Ticagrelor
干预措施: Ticagrelor (Drug)
结局指标
主要结局
PK parameters： Cmax
时间窗: Day 1 to Day 9 in each period
Maximum Concentration of Clopidogrel 's active metabolite
PK parameters： AUC
时间窗: Day 1 to Day 9 in each period
Area under the plasma concentration curve of Clopidogrel 's active metabolite
PK parameters： Tmax
时间窗: Day 1 to Day 9 in each period
Time to maximum concentration of Clopidogrel 's active metabolite
PK parameters： T1/2
时间窗: Day 1 to Day 9 in each period
Half life of Clopidogrel 's active metabolite
PD parameters: Adenosine Diphosphate(ADP)-induced P2Y12 Receptor-mediated platelet aggregation of Tiprogrel
时间窗: Day 1 to Day 14 in each period
ADP-induced platelet reaction unit represents the rate and extent of ADP-stimulated platelet aggregation
PD parameters: Adenosine Diphosphate(ADP)-induced P2Y12 Receptor-mediated platelet aggregation of Clopidogrel
时间窗: Day 1 to Day 14 in each period
ADP-induced platelet reaction unit represents the rate and extent of ADP-stimulated platelet aggregation
PD parameters: Adenosine Diphosphate(ADP)-induced P2Y12 Receptor-mediated platelet aggregation of Ticagrelor
时间窗: Day 1 to Day 14 in each period
ADP-induced platelet reaction unit represents the rate and extent of ADP-stimulated platelet aggregation
Safety parameters: Number of Participants With Treatment-Related Adverse Events
时间窗: Day 1 to Day 14 in each period
次要结局
未报告次要终点