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Ticagrelor in Human Endotoxemia Response to Human Endotoxemia

Not Applicable
Completed
Conditions
Endotoxemia
Interventions
Drug: Placebo
Drug: Acetylsalicylic acid lysinate
Registration Number
NCT02612480
Lead Sponsor
Radboud University Medical Center
Brief Summary

Rationale:

In patients suffering a myocardial infarction the P2Y12 receptor antagonists prasugrel and ticagrelor improve outcome and prognosis compared to clopidogrel. Moreover, ticagrelor lowers mortality from pulmonary infections and sepsis, which cannot solely be explained by its platelet-inhibiting effect. An effect on the inflammatory response in the setting of acute myocardial might underlie this phenomenon and if substantiated support a novel beneficial mechanism of the new the P2Y12 receptor antagonists.

Objective:

To study whether ticagrelor, added to acetylsalicylic acid, modulates the inflammatory response to the administration of lipopolysaccharide (LPS) in humans in vivo, and to compare this effect with the P2Y12 antagonist clopidogrel.

Study design:

Prospective randomized placebo-controlled trial, according to a PROBE design (prospective randomized open blinded-endpoint study).

Study population:

Forty healthy male volunteers aged ≥ 18 and ≤ 35 years. Intervention (if applicable): Participants will be randomized to receive either placebo (twice daily), acetylsalicylic acid (80 mg once daily, after a loading dose of 160 mg) + placebo (once daily), acetylsalicylic acid (80 mg once daily, after a loading dose of 160 mg) + ticagrelor (90 mg twice daily, after a loading dose of 180 mg) or acetylsalicylic acid (80 mg once daily, after a loading dose of 160 mg)+ clopidogrel (75 mg once daily, after a loading dose of 300mg).

Main study parameters/endpoints:

Endpoints: area under the curve of the proinflammatory cytokines TNF-alpha, IL6, IL-10, IL1ra IL-8, IL-1β, MCP-1 MIP-1a, MIP-1b en IFN; peak concentrations of the various cytokines; plasma concentration of HMGP1; platelet-monocyte complex formation and markers of platelet function; plasma concentration of adenosine.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
40
Inclusion Criteria
  • Age ≥ 18 and ≤ 35 years
  • Male
  • No known current medical/psychiatric diseases
Exclusion Criteria
  • History, signs or symptoms of any cardiovascular disease

  • History of chronic obstructive pulmonary disease (COPD) or asthma

  • History of hemorrhagic diathesis, or any other disorder associated with increased risk of bleeding

  • Previous spontaneous vagal collapse

  • Use of any medication

  • Smoking

  • Liver enzyme abnormalities (defined as ALAT and/or ASAT > twice upper limit of normality)

  • Thrombocytopenia (<150*109

    /ml) or anemia (haemoglobin < 8.0 mmol/L)

  • Any obvious disease associated with immune deficiency

  • Febrile illness in the week before the LPS challenge

  • Hypersensitivity to ticagrelor or any excipients

  • Active pathological bleeding

  • History of intracranial haemorrhage

  • History of dyspepsia

  • quantitative bleeding assessment tool (BAT) score >3 (see Appendix 1)

  • Participation in another drug trial or donation of blood 3 months prior, until 3 months after the planned LPS challenge

  • Cardiac conduction abnormalities on the ECG consisting of a 2nd degree atrioventricular block, third degree atrioventricular block or a complex bundle branch block

  • Hypertension (defined as RR systolic > 160 or RR diastolic > 90)

  • Hypotension (defined as RR systolic < 100 or RR diastolic < 50)

  • Renal impairment (defined as MDRD < 60 ml/min)

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Ticagrelor and acetylsalicylic acidticagrelor7 day treatment with ticagrelor 2x90mg after a loading dose of 180 mg and acetylsalicyclic acid 1x80mg after a loading dose of 160 mg.
Ticagrelor and acetylsalicylic acidAcetylsalicylic acid lysinate7 day treatment with ticagrelor 2x90mg after a loading dose of 180 mg and acetylsalicyclic acid 1x80mg after a loading dose of 160 mg.
PlaceboPlacebo7 day treatment with 2 placebos
Placebo and acetylsalicylic acidPlacebo7 day treatment with placebo and acetylsalicyclic acid 1x80mg after a loading dose of 160 mg
Clopidogrel and acetylsalicylic acidAcetylsalicylic acid lysinate7 day treatment with clopidogrel x75 mg after a loading dose of 300 mg and acetylsalicyclic acid 1x80mg after a loading dose of 160 mg
Placebo and acetylsalicylic acidAcetylsalicylic acid lysinate7 day treatment with placebo and acetylsalicyclic acid 1x80mg after a loading dose of 160 mg
Clopidogrel and acetylsalicylic acidClopidogrel7 day treatment with clopidogrel x75 mg after a loading dose of 300 mg and acetylsalicyclic acid 1x80mg after a loading dose of 160 mg
Primary Outcome Measures
NameTimeMethod
concentration plasma TNFalpha (pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

Secondary Outcome Measures
NameTimeMethod
platelet von Willebrandfactor expressionmeasured after challenge with endotoxin at day 7 of medication

measured with flow cytometry

VASP-Pdifference between measurement prior to start of study drug after challenge with endotoxin at day 7 of medication

ELISA

blood pressuremeasured after challenge with endotoxin at day 7 of medication

mmHg

platelet monocyte complexesmeasured after challenge with endotoxin at day 7 of medication

flowcytometric determination of monocytic load with platelets

concentration plasma IL-10 (pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

concentration plasma IL-1RA (pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

concentration plasma MCP-1(pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

platelet reactivitymeasured after challenge with endotoxin at day 7 of medication

ex vivo stimulation of platelets with ADP and collagen, response measured as P-selectin and fibrinogen)

concentration plasma IFNgamma(pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

plasma adenosinemeasured after challenge with endotoxin at day 7 of medication
concentration plasma MIP-1b(pg/ml)measured after challenge with endotoxin at day 7 of medication
concentration plasma IL-6 (pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

concentration plasma IL-8 (pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

concentration plasma IL-1beta (pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

concentration plasma MIP-1a(pg/ml)measured after challenge with endotoxin at day 7 of medication

measured with Luminex assay

monocytic tissue factor expressionmeasured after challenge with endotoxin at day 7 of medication

tissue factor expression on monocytes as measured by flow cytometry

temperaturemeasured after challenge with endotoxin at day 7 of medication

tympanic temperature

platelet neutrophil complexesmeasured after challenge with endotoxin at day 7 of medication

flowcytometric determination of neutrophil load with platelets

monocytic HLA-DR expressionmeasured after challenge with endotoxin at day 7 of medication

as measured by flow cytometry

CD14/16 ratiomeasured after challenge with endotoxin at day 7 of medication

measured with flow cytometry

symptoms during endotoxin daymeasured after challenge with endotoxin at day 7 of medication

6 point likert scale

Trial Locations

Locations (1)

Intensive Care Medicine, Radboud University Nijmegen Medical Centre

🇳🇱

Nijmegen, Gelderland, Netherlands

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