Phase I Study in Healthy Male Subjects Comparing QGC001 to Placebo
Phase 1
Completed
- Conditions
- Essential Hypertension
- Interventions
- Drug: QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)]Drug: Placebo
- Registration Number
- NCT01900171
- Lead Sponsor
- Quantum Genomics SA
- Brief Summary
QGC001/1QG1 is a Phase I "first time in man" study aiming to determine the overall safety and tolerability of single ascending oral doses of QGC001 in healthy male subjects compared to placebo, as well as the pharmacokinetics of QGC001 and its metabolite EC33 and the pharmacodynamic properties of QGC001 (effects on the renin-angiotensin-aldosterone system, blood pressure and heart rate) in healthy male subjects.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 56
Inclusion Criteria
- Caucasian, male healthy subjects of 18 to 45 years of age.
- Body weight ≥50 kg, with a body mass index calculated as weight in kg/(height in m2) from 18 to 27 kg/m2 at screening.
- Subjects will sign and date an informed consent form before any study-specific screening procedure is performed.
- Healthy, as determined by the investigator on the basis of medical history, physical examination findings, clinical laboratory test results, vital sign measurements, and digital 12 lead ECG readings.
- Non-smoker or smoker of fewer than 5 cigarettes per day as determined by history. Must be able to abstain from smoking during the inpatient stay.
- Have a high probability for compliance with and completion of the study.
Exclusion Criteria
- Any significant cardiovascular, hepatic, renal, respiratory, gastrointestinal, endocrine, immunologic, dermatological, haematological, neurologic, psychiatric disease or history of any clinically important drug allergy.
- Acute disease state within 7 days before study day 1.
- History of drug abuse within 1 year before study day 1.
- History of alcoholism within 1 year before day 1. Consumption of more than 50 g of ethanol per day.
- Positive serologic findings for human immunodeficiency virus antibodies, hepatitis B surface antigen, and/or hepatitis C virus antibodies.
- Positive findings of urine drug screen (e.g., amphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine, methadone, opiates, MDMA)
- History of any clinically important drug allergy.
- Prohibited Treatments: use of any investigational drug within 90 days or prescription drug within 30 days before investigational medical product administration.
- Consumption of any caffeine-containing products in excess of 6 cups per day (or equivalent), of grapefruit, grapefruit-containing products, or alcoholic beverages within 24 hours before study day 1.
- Use of any over-the-counter drugs including herbal supplements (except for the occasional use of acetaminophen [paracetamol], aspirin and vitamins ≤100% recommended daily allowance) within 7 days before investigational medicinal product administration.
- Donation of blood (i.e. 450 ml) within 90 days before study day 1.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- PARALLEL
- Arm && Interventions
Group Intervention Description 10 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. 50 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. 125 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. 250 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. 500 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. 750 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. 1,000 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. 1,250 mg of QGC001 QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] Each dose of QGC001 was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1. Placebo Placebo The placebo was administered orally with 100 mL of sterile water for irrigation at 08:00 in the morning of Day 1.
- Primary Outcome Measures
Name Time Method Adverse events up to 11 days Blood pressure up to 11 days Heart rate up to 11 days Body temperature up to 11 days 12-lead ECG up to 11 days Red blood cell count up to 11 days Haemoglobin up to 11 days Haematocrit up to 11 days White blood cell count with differential up to 11 days Platelet count up to 11 days Plasma sodium up to 11 days Plasma potassium up to 11 days Plasma calcium up to 11 days Plasma total bilirubin up to 11 days Plasma conjugated bilirubin up to 11 days Plasma Aspartate Amino Transferase (ASAT) up to 11 days Plasma Alanine Amino Transferase (ALAT) up to 11 days Plasma Gamma Glutamyl Transferase (GGT) up to 11 days Plasma alkaline phosphatases up to 11 days Plasma total protein up to 11 days Plasma Creatine PhosphoKinase (CPK) up to 11 days Plasma creatinine up to 11 days Plasma glucose up to 11 days Plasma cholesterol up to 11 days Plasma triglycerides up to 11 days Urinary pH up to 11 days Urinary protein up to 11 days Urinary glucose up to 11 days Urinary leukocytes up to 11 days Urinary nitrites up to 11 days Urinary ketones up to 11 days Urinary blood up to 11 days
- Secondary Outcome Measures
Name Time Method Maximum observed plasma concentration (Cmax) of QGC001 H0, H 0.5, H1, H1.5, H2, H3, H4, H5, H6, H9, H12, H24 and H48 post-dose Time at which Cmax is observed (tmax) of QGC001 H0, H 0.5, H1, H1.5, H2, H3, H4, H5, H6, H9, H12, H24 and H48 post-dose Elimination rate constant (λz) of QGC001 H0, H 0.5, H1, H1.5, H2, H3, H4, H5, H6, H9, H12, H24 and H48 post-dose Terminal half-life (t1/2,z) of QGC001 H0, H 0.5, H1, H1.5, H2, H3, H4, H5, H6, H9, H12, H24 and H48 post-dose Area Under the Concentration-time curve (AUClast and AUC0-∞) of QGC001 H0, H 0.5, H1, H1.5, H2, H3, H4, H5, H6, H9, H12, H24 and H48 post-dose Maximum observed plasma concentration (MRCmax) of metabolic ratios H0, H 0.5, H1, H1.5, H2, H3, H4, H5, H6, H9, H12, H24 and H48 post-dose Area Under the Concentration-time curve (MRAUC) of metabolic ratios H0, H 0.5, H1, H1.5, H2, H3, H4, H5, H6, H9, H12, H24 and H48 post-dose Cumulative amount eliminated (Ae) H-12 to H0 pre-dose and H0- H6, H6-H12 and H12-H24 post-dose Fraction recovered (Fe) H-12 to H0 pre-dose and H0- H6, H6-H12 and H12-H24 post-dose Renal clearance (CLR) H-12 to H0 pre-dose and H0- H6, H6-H12 and H12-H24 post-dose Plasma renin H-1 pre-dose and H2, H4 and H9 post-dose Determination of renin in blood samples. In dose groups 1 and 2, no pharmacodynamic evaluations will be done.
Plasma aldosterone H-1 pre-dose and H2, H4 and H9 post-dose Determination of aldosterone in blood samples. In dose groups 1 and 2, no pharmacodynamic evaluations will be done.
Plasma cortisol H-1 pre-dose and H2, H4 and H9 post-dose Determination of cortisol in blood samples. In dose groups 1 and 2, no pharmacodynamic evaluations will be done.
Plasma copeptin H-1 pre-dose and H2, H4 and H9 post-dose Determination of copeptin in blood samples (if possible, will be determined later). In dose groups 1 and 2, no pharmacodynamic evaluations will be done.
Urinary aldosterone H-12 to H0 pre-dose, H0-H6, H6-H12 and H12-H24 post-dose Aldosterone analysis in urine samples. In dose groups 1 and 2, no pharmacodynamic evaluations will be done.
Urinary cortisol H-12 to H0 pre-dose, H0-H6, H6-H12 and H12-H24 post-dose Cortisol analysis in urine samples. In dose groups 1 and 2, no pharmacodynamic evaluations will be done.
Urinary creatinin H-12 to H0 pre-dose, H0-H6, H6-H12 and H12-H24 post-dose Creatinin analysis in urine samples. In dose groups 1 and 2, no pharmacodynamic evaluations will be done.
Trial Locations
- Locations (1)
Biotrial PARIS
🇫🇷Rueil-Malmaison, France