Pharmacodynamic and Pharmacokinetic Study of 2 Different Dose Regimen of Clopidogrel in CYP2C19 Genotyped Healthy Subjects

A Randomized, Double-blind, Double-dummy, Two Period, Two Treatment Cross-over Pharmacodynamic and Pharmacokinetic Study of Clopidogrel Given as 5-day Repeated Oral Doses (300 mg Loading Dose Followed by 75 mg/Day and 600 mg Loading Dose Followed by 150 mg/Day) in 4 Different Groups of CYP2C19 Genotyped Healthy Male and Female Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01123824

Enrollment

Registered

2010-05-14

Start date

2009-04-30

Completion date

2009-08-31

Last updated

2011-12-15

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Keywords

healthy subjects

Brief summary

Primary Objective: * Investigate the possible role of the CYP2C19 genotype in Adenosine diphosphate (ADP)-induced platelet aggregation after administration of a standard dose regimen of clopidogrel (300 mg loading dose followed by 75 mg/day for 4 days) in healthy male and female subjects Secondary Objectives: * Assess the pharmacodynamic activity of a higher dose regimen of clopidogrel (600 mg loading dose followed by 150 mg/day for 4 days) * Compare the pharmacokinetic profiles of clopidogrel active metabolite between the selected groups of genotyped subjects and the 2 dose regimen

Detailed description

The total study duration per subject is 10-12 weeks broken down as follows: * Screening: 2 to 40 days before the first dosing * Period 1: 7 days including 5 days treatment * Washout: At least 14 days after the last dosing * Period 2: 7 days including 5 days treatment * End of study: 7 to 10 days after the last dosing

Interventions

DRUGCLOPIDOGREL

Pharmaceutical form: tablets Route of administration: oral

DRUGplacebo

Pharmaceutical form: matching tablets Route of administration: oral

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

BASIC_SCIENCE

Masking

DOUBLE (Subject, Investigator)

Eligibility

Sex/Gender

ALL

Age

18 Years to 65 Years

Healthy volunteers

Yes

Inclusion criteria

Healthy subject in good health, as determined by a medical history, physical examination including vital signs and clinical laboratory tests: * with a body weight between 45 kg and 95 kg if male, between 40 kg and 85 kg if female, and with a Body Mass Index (BMI) between 18 and 30 kg/m² * classified into one of the 4 groups of metabolizers according to his/her CYP2C19 genotype: * Ultrarapid Metabolizers (UMs, CYP2C19\*1/\*17 and CYP2C19\*17/\*17) * homozygous Extensive Metabolizers (homoEMs, CYP2C19\*1/\*1) * heterozygous Extensive Metabolizers (heteroEMs, CYP2C19\*1/\*2 and CYP2C19\*1/\*3) * Poor Metabolizers (PMs, CYP2C19\*2/\*2 and CYP2C19\*2/\*3)

Exclusion criteria

* Evidence of inherited disorder of coagulation/hemostasis functions * Subject smoking more than 10 cigarettes or equivalent per day * Unability to abstain from intake of any drug affecting hemostasis throughout the whole study duration The above information is not intended to contain all considerations relevant to a patient's potential participation in a clinical trial.

Design outcomes

Primary

Measure	Time frame
Maximum platelet aggregation intensity (MAI) induced by Adenosine diphosphate (ADP) 5 µM after 5 days treatment	Day 5 of each period

Secondary

Measure	Time frame
Maximum platelet aggregation intensity (MAI) induced by ADP 20 µM after 5 days treatment	Day 5 of each period
Platelet reactivity index -Vasodilator-stimulated phosphoprotein test (PRI-VASP) after 5 days treatment	Day 5 of each period
Clopidogrel active metabolite pharmacokinetic parameters (Cmax, tmax, AUC0-24, AUClast) after 5 days treatment	Up to 24 hours postdose on Day 5 for each period

Countries

Germany

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026