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Etude (Study) Phase I Enox - UnFractionated Heparin (UFH)

Phase 1
Completed
Conditions
Thrombosis
Interventions
Registration Number
NCT00622115
Lead Sponsor
Sanofi
Brief Summary

Primary objective:

* to characterize the pharmacokinetic and the pharmacodynamic profile after intravenous bolus injection of unfractionated heparin (UFH) after repeated sc 100 IU anti-Xa/kg (corresponding to 1 mg/kg) twice a day during 2.5 days (every 12±2hrs) administrations of enoxaparin in Caucasian healthy subjects.

Secondary objective(s):

* to compare the pharmacokinetic and the pharmacodynamic profile between 3 different timing of administration of the UFH

* to assess the tolerability of the different anticoagulation protocols

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
72
Inclusion Criteria
  • Caucasian
  • Male and female subjects, between 40 and 60 years of age
  • Body weight between 50 kg and 90 kg if male and between 40 and 80 kg if female with Body Mass Index (BMI) between 18 and 29 kg/m2

Health Status:

  • Certified as healthy by a comprehensive clinical assessment (detailed medical history and complete physical examination)

  • Subject with hypertension, hypo- or hyperthyroidism or dyslipidemia will be included if their concomitant pathology is well-controlled by treatment for at least one year

  • Normal vital signs after 10 minutes resting in supine position:

    • 95 mmHg < systolic blood pressure (SBP) < 140 mmHg;
    • 45 mmHg < diastolic blood pressure (DBP) < 90 mmHg;
    • 40 bpm < heart rate < 100 bpm.
  • Normal 12-lead electrocardiogram (ECG); 120 ms < PR < 220 ms, QRS < 120 ms, QTc ≤ 430 ms for male, 450 ms for female or not considered as clinically significant by the investigator

  • Laboratory parameters within the normal range unless the Investigator considers an abnormality to be clinically irrelevant for healthy subjects; hepatic enzymes (aspartate amino-transferase or AST, alanine amino-transferase or ALT) should be strictly below the upper laboratory norm.

  • Platelets ≥ 150 000 / mm3

  • Mean corpuscular volume (MCV) and gamma glutamyl-transferase (GGT) should be strictly in the normal range of the laboratory

  • Activated partial thromboplastin time (aPTT) ratio should be comprised between 0.95 and 1.15

  • Estimated Creatinine clearance by Cockroft formula should be higher than 50 mL/min

  • Non smoker or smoking the equivalent or less than 5 cigarettes a day and able not to smoke during the study hospitalization

  • Normal gynecological examination no longer than 12 months before inclusion.

  • For female with childbearing potential using an effective contraception method (e.g. intra-uterine device, hormonal contraception, diaphragm and condom) except if postmenopausal for more than 12 months or sterilized for more than three months

  • Subject with coagulation test and blood count (including platelets) within the physiological ranges)

Regulations:

  • Having given written informed consent prior to any procedure related to the study
  • Covered by Health Insurance System and/or in compliance with the recommendations of National Law in force relating to biomedical research
  • Not under any administrative or legal supervision
Exclusion Criteria

Medical history and clinical status:

  • Contra-indication to anticoagulant therapy
  • Subject with known increased bleeding time, hemophilia, thrombocytopenia, and/or history of any vascular purpura
  • Subject with detectable antibody against heparin in the blood
  • Any history or presence of clinically relevant cardiovascular, gynecologic (for women), pulmonary, gastro-intestinal, hepatic, renal, metabolic, hematological, neurologic, psychiatric, systemic, ocular or infectious disease that is capable of altering the absorption, metabolism, or elimination of drugs, or of constituting a risk factor when taking the study medication; any acute infectious disease or signs of acute illness; except subject with hypertension, hypo- or hyperthyroidism or dyslipidemia if well-controlled by treatment for at least one year.
  • Subject with diabetes or other cardiovascular or metabolic disease
  • Subject with INR > 1.5
  • Frequent headaches and/or migraine, recurrent nausea and/or vomiting (more than twice a month)
  • Blood donation or blood loss within one month before administration
  • Symptomatic hypotension whatever the decrease in blood pressure or asymptomatic postural hypotension defined by a decrease in SBP equal to or greater than 20 mmHg within three minutes when changing from the supine to the standing position
  • Presence or history of drug allergy, or allergic disease diagnosed and treated by a physician
  • History or presence of drug or alcohol abuse (alcohol consumption > 40 grams/day)
  • Smoking more than 5 cigarettes or equivalent/day, or unable to stop smoking during the study
  • Excessive consumption of beverages with xanthine bases (> 4 cups or glasses/day)
  • Pregnancy (defined as positive beta-HCG plasma test that can not be explicated by menopauses), breast-feeding for female, any history or presence of clinically relevant gynecologic disease

Interfering substance:

  • Any medication (including St John's Wort) within 14 days before administration, or within 5 times the elimination half-life of that drug, except for hormonal contraception or replacement therapy, and allowed therapy for stable pathology
  • Anti-inflammatory treatments and anti-aggregant treatments are strictly forbidden during the whole study period

General conditions:

  • Subject who, in the judgment of the Investigator, is likely to be non-compliant during the study, or unable to cooperate because of a language problem or poor mental development
  • Subject in exclusion period of a previous study according to applicable regulations
  • Subject who cannot be contacted in case of emergency
  • Subject is the investigator or any sub-investigator, research assistant, pharmacist, study coordinator, other staff thereof, directly involved in the conduct of the protocol or any other protocol of the Investigating Center
  • Subject is an employee of the Investigating Center

Biological status:

  • Positive reaction to any of the following tests: HBs antigen, anti-HCV antibodies, anti-HIV1 antibodies, anti-HIV2 antibodies, anti-LMWH antibodies
  • Positive results on urine drug screen (amphetamines/metamphetamines, barbiturates, benzodiazepines, cannabinoids)
  • Positive alcohol breath or plasma test

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
CEnoxaparin70 U/kg of UnFractionated Heparin (UFH) administered intravenously at 10 hours following the last injection of enoxaparin
AEnoxaparin70 U/kg of UnFractionated Heparin (UFH) administered intravenously at 4 hours following the last injection of enoxaparin
BEnoxaparin70 U/kg of UnFractionated Heparin (UFH) administered intravenously at 6 hours following the last injection of enoxaparin
Primary Outcome Measures
NameTimeMethod
Concentration-time profiles of anti-Xa and anti-IIa levelsAt baseline (Day 2) after the morning enoxaparin injection and at day 3 from pre-dose of enoxaparin and lasting until 14 hours after the enoxaparin injection.
Secondary Outcome Measures
NameTimeMethod
Effect-time profiles of ACT, TGTppp and TGTprpAt baseline (Day 2) after the morning enoxaparin sc injection and at day 3 from pre-dose of enoxaparin and lasting until 14 hours after the enoxaparin injection.
PFA100 levels measuredAt pre-dose, 4h and 14h post dose of enoxaparin
Documentation of adverse event, physical examination, clinical laboratory safety, vital signs and ECG recording at prespecified time-points.during the entire study

Trial Locations

Locations (1)

Sanofi-Aventis Administrative Office

🇫🇷

Paris, France

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