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Adrecizumab-LPS Study

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
Drug: Endotoxin
Drug: Placebo
Registration Number
NCT03083171
Lead Sponsor
Adrenomed AG
Brief Summary

In this randomized, double-blind, placebo-controlled study, either a single dose of Adrecizumab (0.5, 2.0 or 8.0 mg/kg) or placebo will be administrated to 24 healthy male volunteers during experimental endotoxemia.

Detailed Description

Adrenomedullin (ADM) is a natural occurring 52 amino acid peptide which is mainly expressed in endothelial and smooth muscle cells. ADM plasma levels are increased in patients with sepsis and related with severity of disease. ADM is a key regulator of vasotonus and of endothelial integrity in sepsis. Adrecizumab is an antibody against the N-terminus of ADM which only partially inhibits the bioactivity of ADM. Several septic animal studies have shown that administration of Adrecizumab leads to stabilization of hemodynamics in mice and pigs, improved renal function, reduced catecholamine demand, improved fluid balance and improved survival. The administration of Adrecizumab to rodents, non-human primates and recently humans, has been tolerated very well.

The experimental human endotoxemia model, in which healthy male volunteers receive a low dose of lipopolysaccharide (LPS) derived from Escherichia coli, is widely used to study the effects of systemic inflammation in humans in vivo and is considered a safe and highly reproducible method to activate the innate immune system. Furthermore, previous data has shown that experimental human endotoxemia results in increased plasma ADM levels. In this study, the investigators wish to assess the safety, tolerability and pharmacokinetics/-dynamics of Adrecizumab under inflammatory conditions in healthy volunteers.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
24
Inclusion Criteria
  1. Written informed consent to participate in this trial prior to any study-mandated procedure.
  2. Male subjects aged 18 to 35 years inclusive.
  3. Subjects have to agree to use a reliable way of contraception with their partners from study entry until 3 months after study drug administration.
  4. BMI between 18 and 30 kg/m², with a lower limit of body weight of 50 kg and a upper limit of 100 kg.
  5. Healthy as determined by medical history, physical examination, vital signs, 12-lead electrocardiogram, and clinical laboratory parameters.
Exclusion Criteria
  1. Unwillingness to abstain from any medication, including recreational drugs or vitamin supplements during the course of the study and within 7 days prior to the treatment day.

  2. Unwillingness to abstain from smoking, or alcohol, within 1 day prior to the treatment day and 1 day after the treatment day.

  3. Previous participation in a trial where LPS was administered.

  4. Surgery or trauma with significant blood loss or blood donation within 3 months prior to the treatment day.

  5. History, signs or symptoms of cardiovascular disease, in particular:

    • History of frequent vasovagal collapse or of orthostatic hypotension
    • Resting pulse rate ≤45 or ≥100 beats/min
    • Hypertension (RR systolic >160 or RR diastolic >90 mmHg)
    • Hypotension (RR systolic <100 or RR diastolic <50 mmHg)
    • Conduction abnormalities on the ECG consisting of a 1st degree atrioventricular block or a complex bundle branch block
    • Any chronic cardiac arrhythmias (except PAC's, PVC's)
  6. Renal impairment: plasma creatinine >120 μmol/L

  7. Liver function tests (alkaline phosphatase, AST, ALT and/or γ-GT) above 2x the upper limit of normal.

  8. History of asthma

  9. Atopic constitution

  10. CRP above 2x the upper limit of normal, or clinically significant acute illness, including infections, within 2 weeks prior to the treatment day.

  11. Treatment with investigational drugs or participation in any other clinical trial within 30 days prior to the treatment day.

  12. Known or suspected of not being able to comply with the trial protocol.

  13. Known hypersensitivity to any excipients of the drug formulations used.

  14. Inability to personally provide written informed consent (e.g. for linguistic or mental reasons) and/or take part in the study.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Adrecizumab 0.5 mg/kgEndotoxinA single intravenous dose of 0.5 mg/kg Adrecizumab given over a 1 hour period.
Adrecizumab 2.0 mg/kgEndotoxinA single intravenous dose of 2.0 mg/kg Adrecizumab given over a 1 hour period.
Adrecizumab 8.0 mg/kgEndotoxinA single intravenous dose of 8.0 mg/kg Adrecizumab given over a 1 hour period.
PlaceboPlacebo-
PlaceboEndotoxin-
Adrecizumab 2.0 mg/kgAdrecizumabA single intravenous dose of 2.0 mg/kg Adrecizumab given over a 1 hour period.
Adrecizumab 8.0 mg/kgAdrecizumabA single intravenous dose of 8.0 mg/kg Adrecizumab given over a 1 hour period.
Adrecizumab 0.5 mg/kgAdrecizumabA single intravenous dose of 0.5 mg/kg Adrecizumab given over a 1 hour period.
Primary Outcome Measures
NameTimeMethod
Safety and tolerability expressed in total number of treatment related (serious) adverse events.3 months follow-up period

Adverse events include: Clinically significant variation in vital signs compared to baseline (blood pressure and heart rate), local infusion reaction at site of i.v. IMP infusion, clinically significant changes in ECG compared to baseline and clinically significant deflections in laboratory parameters compared to baseline.

Secondary Outcome Measures
NameTimeMethod
CytokinesT=0 hours, T=1 hours, T=1.5 hours, T=2 hours, T=2.5 hours T=3 hours, T=4 hours, T=5 hours, T=6 hours, T=9 hours after LPS administration

Blood plasma levels of TNF-alfa, IL-6, IL-8, IL-10, MCP-1, IP-10 and G-CSF

Clearance of free Adrecizumab (pharmacokinetics)T=0 hours, T=0.25 hours, T=0.5 hours, T=1 hours, T=1.5 hours, T=2 hours, T=3 hours, T=4 hours, T=8 hours, T=24 hours, T=7 days, T=14 days, T=28 days, T=60 days, T=90 days after Adrecizumab administration
Peak plasma concentration (Cmax) of free Adrecizumab (pharmacokinetics)T=0 hours, T=0.25 hours, T=0.5 hours, T=1 hours, T=1.5 hours, T=2 hours, T=3 hours, T=4 hours, T=8 hours, T=24 hours, T=7 days, T=14 days, T=28 days, T=60 days, T=90 days after Adrecizumab administration
Terminal t1/2 of free Adrecizumab (pharmacokinetics)T=0 hours, T=0.25 hours, T=0.5 hours, T=1 hours, T=1.5 hours, T=2 hours, T=3 hours, T=4 hours, T=8 hours, T=24 hours, T=7 days, T=14 days, T=28 days, T=60 days, T=90 days after Adrecizumab administration
Volume of distribution of free Adrecizumab (pharmacokinetics)T=0 hours, T=0.25 hours, T=0.5 hours, T=1 hours, T=1.5 hours, T=2 hours, T=3 hours, T=4 hours, T=8 hours, T=24 hours, T=7 days, T=14 days, T=28 days, T=60 days, T=90 days after Adrecizumab administration
Area under the curve (AUC) of free Adrecizumab (pharmacokinetics)T=0 hours, T=0.25 hours, T=0.5 hours, T=1 hours, T=1.5 hours, T=2 hours, T=3 hours, T=4 hours, T=8 hours, T=24 hours, T=7 days, T=14 days, T=28 days, T=60 days, T=90 days after Adrecizumab administration
Plasma levels of adrenomedullin and MR-proadrenomedullinT=0 hours, T=1 hours, T=1.25 hours, T=1.5 hours, T=2 hours, T=2.5 hours T=3 hours, T=4 hours, T=5 hours, T=9 hours, T=24 hours, T=7 days, T=14 days, T=28 days, T=60 days, T=90 days after LPS administration
Kidney damage markersBaseline, T=0 to T=3 hours, T=3 to T=6 hours, T=6 to T=9 hours, T=9 to T=12 hours, T=12 to T=24 hours after LPS administration

In urine and plasma, including, but not limited to pro-enkephalin, creatinine clearance, NGAL and KIM-1

Trial Locations

Locations (1)

Dept. of Intensive Care Medicine, Research-unit, Radboud university medical center

🇳🇱

Nijmegen, Gelderland, Netherlands

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