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This study is designed to evaluate the pharmacokinetics, pharmacodynamics and safety in healthy subjects with multiple administration of Tiprogrel.
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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Tiprogrel-Clopidogrel-Ticagrelor | Other | Period 1: Dose 1 Tiprogrel; Period 2: Dose 2 Tiprogrel ; Period 3: Clopidogrel; Period 4: Ticagrelor |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Tiprogrel | Drug | Period 1: Dose 1 Tiprogrel, loading dose of Tiprogrel followed by daily maintenance dose until Day 8. |
|
| Measure | Description | Time Frame |
|---|---|---|
| PK parameters: Cmax | Maximum Concentration of Tiprogrel 's active metabolite | Day 1 to Day 9 in each period |
| PK parameters: Cmax | Maximum Concentration of Clopidogrel 's active metabolite | Day 1 to Day 9 in each period |
| PK parameters: AUC | Area under the plasma concentration curve of Tiprogrel 's active metabolite | Day 1 to Day 9 in each period |
| PK parameters: AUC | Area under the plasma concentration curve of Clopidogrel 's active metabolite | Day 1 to Day 9 in each period |
| PK parameters: Tmax | Time to maximum concentration of Tiprogrel 's active metabolite | Day 1 to Day 9 in each period |
| PK parameters: Tmax | Time to maximum concentration of Clopidogrel 's active metabolite | Day 1 to Day 9 in each period |
| PK parameters: T1/2 | Half life of Tiprogrel 's active metabolite | Day 1 to Day 9 in each period |
| PK parameters: T1/2 | Half life of Clopidogrel 's active metabolite |
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Inclusion Criteria:
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.
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Beijing Tiantan Hosptial, Capital Medical University | Beijing | China |
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| ID | Term |
|---|---|
| D054058 | Acute Coronary Syndrome |
| D000083242 | Ischemic Stroke |
| ID | Term |
|---|---|
| D017202 | Myocardial Ischemia |
| D006331 | Heart Diseases |
| D002318 | Cardiovascular Diseases |
| D014652 | Vascular Diseases |
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| ID | Term |
|---|---|
| D000077144 | Clopidogrel |
| D000077486 | Ticagrelor |
| ID | Term |
|---|---|
| D013988 | Ticlopidine |
| D058924 | Thienopyridines |
| D013876 | Thiophenes |
| D013457 | Sulfur Compounds |
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| Tiprogrel | Drug | Period 2: Dose 2 Tiprogrel ; loading dose of Tiprogrel followed by daily maintenance dose until Day 8. |
|
| Clopidogrel | Drug | Period 3: Clopidogrel; loading dose of Clopidogrel followed by daily maintenance dose until Day 8. |
|
| Ticagrelor | Drug | Period 4: Ticagrelor; loading dose of Ticagrelor followed by daily maintenance dose until Day 8. |
|
| Day 1 to Day 9 in each period |
| PD parameters: Adenosine Diphosphate(ADP)-induced P2Y12 Receptor-mediated platelet aggregation of Tiprogrel | ADP-induced platelet reaction unit represents the rate and extent of ADP-stimulated platelet aggregation | Day 1 to Day 14 in each period |
| PD parameters: Adenosine Diphosphate(ADP)-induced P2Y12 Receptor-mediated platelet aggregation of Clopidogrel | ADP-induced platelet reaction unit represents the rate and extent of ADP-stimulated platelet aggregation | Day 1 to Day 14 in each period |
| PD parameters: Adenosine Diphosphate(ADP)-induced P2Y12 Receptor-mediated platelet aggregation of Ticagrelor | ADP-induced platelet reaction unit represents the rate and extent of ADP-stimulated platelet aggregation | Day 1 to Day 14 in each period |
| Safety parameters: Number of Participants With Treatment-Related Adverse Events | Day 1 to Day 14 in each period |
| D020521 |
| Stroke |
| D002561 | Cerebrovascular Disorders |
| D001927 | Brain Diseases |
| D002493 | Central Nervous System Diseases |
| D009422 | Nervous System Diseases |
| D009930 |
| Organic Chemicals |
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D000241 | Adenosine |
| D011684 | Purine Nucleosides |
| D011687 | Purines |
| D009705 | Nucleosides |
| D009706 | Nucleic Acids, Nucleotides, and Nucleosides |
| D012263 | Ribonucleosides |