Study to Assess Pharmacokinetics, Pharmacodynamics and Safety of Tiprogrel in Healthy Subjects

NCT06584812 | Completed Phase 1

• 1 other identifier: TY601A-P1-03
• Study Type: interventional
• Target: 14
• Locations: 1 country
• Sites: 1

Brief Summary

This study is designed to evaluate the pharmacokinetics, pharmacodynamics and safety in healthy subjects with multiple administration of Tiprogrel.

Conditions

Acute Coronary Syndrome; Ischemic Stroke

Outcome Measures

Primary Outcomes (12)

• 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

  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

Study Arms (1)

Tiprogrel-Clopidogrel-Ticagrelor

OTHER

Period 1: Dose 1 Tiprogrel; Period 2: Dose 2 Tiprogrel ; Period 3: Clopidogrel; Period 4: Ticagrelor

Drug: Tiprogrel; Drug: Clopidogrel; Drug: Ticagrelor

Interventions

Tiprogrel DRUG

Period 1: Dose 1 Tiprogrel, loading dose of Tiprogrel followed by daily maintenance dose until Day 8.

Tiprogrel-Clopidogrel-Ticagrelor

Clopidogrel DRUG

Period 3: Clopidogrel; loading dose of Clopidogrel followed by daily maintenance dose until Day 8.

Tiprogrel-Clopidogrel-Ticagrelor

Ticagrelor DRUG

Period 4: Ticagrelor; loading dose of Ticagrelor followed by daily maintenance dose until Day 8.

Tiprogrel-Clopidogrel-Ticagrelor

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male and female Healthy Subjects
• Subject has the ability and willingness to comply with study procedures and follow-up examination.
• ：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.

You may not qualify if:

• 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

Sponsors & Collaborators

• Tianjin Institute of Pharmaceutical Research Co., Ltd: lead

Study Sites (1)

Beijing Tiantan Hosptial, Capital Medical University

Beijing, China

Location

MeSH Terms

Conditions

Acute Coronary Syndrome; Ischemic Stroke

Interventions

Clopidogrel; Ticagrelor

Condition Hierarchy (Ancestors)

Myocardial Ischemia; Heart Diseases; Cardiovascular Diseases; Vascular Diseases; Stroke; Cerebrovascular Disorders; Brain Diseases; Central Nervous System Diseases; Nervous System Diseases

Intervention Hierarchy (Ancestors)

Ticlopidine; Thienopyridines; Thiophenes; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Adenosine; Purine Nucleosides; Purines; Nucleosides; Nucleic Acids, Nucleotides, and Nucleosides; Ribonucleosides

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SEQUENTIAL
• Sponsor Type: OTHER GOV
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 29, 2024
• First Posted: September 5, 2024
• Study Start: September 9, 2024
• Primary Completion: December 5, 2024
• Study Completion: December 17, 2024
• Last Updated: January 6, 2025

Record last verified: 2025-01

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)