Study of the Product QGC001 as a Single Dose and Multiple Doses Administered Orally to Healthy Adult Subjects

NCT01900184 | Completed Phase 1 DMC

• 1 other identifier: QGC001/1QG2
• Study Type: interventional
• Target: 69
• Locations: 1 country
• Sites: 1

Brief Summary

1QG2 is a Phase 1 study aiming to assess the safety and tolerability of ascending single/multiple oral doses (SAD \& MAD) in healthy young subjects, the preliminary food interaction and the effect of QGC001 on blood pressure and heart rate, but also to determine pharmacokinetic preliminary profiles of QGC001 and its metabolite EC33 and pharmacodynamic preliminary profiles of QGC001 and its metabolite EC33 especially effects on the renin-angiotensin-aldosterone and copeptin systems.

Conditions

Essential Hypertension

Outcome Measures

Primary Outcomes (33)

• Adverse events

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Red blood cell count

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Haemoglobin

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Haematocrit

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• White blood cell count with differential

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Platelet count

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma sodium

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma potassium

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma calcium

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma total bilirubin

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma conjugated bilirubin

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma Aspartate Amino Transferase (ASAT)

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma Alanine Amino Transferase (ALAT)

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma Gamma Glutamyl Transferase (GGT)

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma alkaline phosphatases

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma total protein

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma Creatine PhosphoKinase (CPK)

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma creatinine

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma glucose

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma cholesterol

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Plasma triglycerides

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Urinary pH

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Urinary protein

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Urinary glucose

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Urinary leukocytes

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Urinary nitrites

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Urinary ketones

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Urinary blood

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Weight assessment (kg)

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Body temperature (°C)

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Supine and orthostatic (systolic and diastolic) blood pressure

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• Heart rate

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

• 12-lead ECG

  up to 4 weeks for SAD, 5 weeks for FI and 6 weeks for MAD

Secondary Outcomes (21)

• Maximum observed plasma concentration (Cmax) of QGC001

  up to 3 days for SAD and FI, up to 9 days for MAD

• Time at which Cmax is observed (tmax) of QGC001

  up to 3 days for SAD and FI, up to 9 days for MAD

• Elimination rate constant (λz) of QGC001

  up to 3 days for SAD and FI, up to 9 days for MAD

• Terminal half-life (t1/2,z) of QGC001

  up to 3 days for SAD and FI, up to 9 days for MAD

• Area Under the Concentration-time curve (AUClast and AUC0-∞) of QGC001

  up to 3 days for SAD and FI, up to 9 days for MAD

Study Arms (4)

500 mg bid of QGC001

EXPERIMENTAL

Each dose of QGC001 will be administered in solution with 200 mL of purified water.

Drug: QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)]

750 mg bid of QGC001

EXPERIMENTAL

Each dose of QGC001 will be administered in solution with 200 mL of purified water.

Drug: QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)]

1,000 mg bid of QGC001

EXPERIMENTAL

Each dose of QGC001 will be administered in solution with 200 mL of purified water.

Drug: QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)]

Placebo

PLACEBO COMPARATOR

The placebo will be administered in solution with 200 mL of purified water.

Drug: Placebo

Interventions

QGC001 [(3S,3'S)-4,4'-dithiobis (3-aminobutane-1-sulfonic acid)] DRUG

1,000 mg bid of QGC001; 500 mg bid of QGC001; 750 mg bid of QGC001

Placebo DRUG

Contains magnesium stearate, silica dental type, anhydrous lactose

Placebo

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Caucasian, male healthy subjects of 18 to 45 years of age (inclusive).
• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Quantum Genomics SA: lead

Study Sites (1)

Biotrial PARIS

Rueil-Malmaison, 92502, France

Location

Related Publications (1)

• Khosla J, Aronow WS, Frishman WH. Firibastat: An Oral First-in-Class Brain Aminopeptidase A Inhibitor for Systemic Hypertension. Cardiol Rev. 2022 Jan-Feb 01;30(1):50-55. doi: 10.1097/CRD.0000000000000360.

  PMID: 33027067 DERIVED

MeSH Terms

Conditions

Essential Hypertension

Condition Hierarchy (Ancestors)

Hypertension; Vascular Diseases; Cardiovascular Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: TRIPLE
• Who Masked: PARTICIPANT, INVESTIGATOR, OUTCOMES ASSESSOR
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 27, 2013
• First Posted: July 16, 2013
• Study Start: December 1, 2012
• Primary Completion: March 1, 2013
• Study Completion: March 1, 2013
• Last Updated: July 16, 2013

Record last verified: 2013-07

Locations

FR (1)