Healthy Males
Conditions
Brief summary
This is a single-centre, open-label, non-randomised, period fixed sequence study designed to investigate the PK and safety of Firibastat (QGC001) modified release (MR) prototype tablet formulations and compare this to a reference Firibastat (QGC001) immediate release (IR) capsule formulation in healthy male subjects. It is planned to enrol 12 subjects to receive single oral doses of investigational medicinal product (IMP).
Detailed description
Subjects will be screened for eligibility to participate in the study up to 28 days before dosing and for each treatment period they will be admitted to the clinical unit on the evening prior to IMP administration (Day -1). On the morning of Day 1, subjects will receive IMP in the fasted state (or following a FDA standard high-fat breakfast, if applicable) and will remain on site until 48 h post-dose. Between the periods, an interim analysis and review of safety and PK data from dosed regimens will be performed in order to determine which Firibastat (QGC001) MR prototype tablet formulation and dose to administer in subsequent periods. A follow-up phone call will take place 7 to 10 days post-final dose to ensure the ongoing wellbeing of the subjects.
Interventions
DRUGFiribastat
Firibastat (QGC001) 500 mg
Sponsors
Quotient Sciences
Quantum Genomics SA
Study design
Intervention model
SEQUENTIAL
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Body mass index of 18.0 to 32.0 kg/m2 * Must adhere to the contraception requirements
Exclusion criteria
* Subjects who have received any IMP in a clinical research study within the previous 3 months * Subjects with pregnant partners * History of any drug or alcohol abuse in the past 2 years * Clinically significant abnormal biochemistry, haematology or urinalysis * Subjects with BP \<90/50 mmHg at screening
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetic (PK) profiles of Firibastat (QGC001) and active métabolites of modified release prototype tablet formulations. Assessment of the Maximum Plasma Concentration. | 3 months | \[Cmax\] |
| Pharmacokinetic (PK) profiles of Firibastat (QGC001) and active métabolites of modified release prototype tablet formulations. Assessment of the time at which the Cmax is observed. | 3 months | \[Tmax\] |
| Pharmacokinetic (PK) profiles of Firibastat (QGC001) and active métabolites of modified release prototype tablet formulations. Assessment of the Areas Under the Curve. | 3 months | \[AUC0-24, AUC0-last and AUC0-inf\] |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Safety and tolerability of single doses of Firibastat (QGC001) by assessing urinalysis aggregated as number of patients outside normal ranges. | 3 months | Bilirubin, Blood, Glucose, Ketones, Leukocytes, Nitrites, pH, Protein, Specific gravity, Urobilinogen |
| Safety and tolerability of single doses of Firibastat (QGC001) by assessing vital signs | 3 months | Blood pressure (mmHg) |
| Relative bioavailability of Firibastat (QGC001) modified release prototype tablet formulations compared to the immediate release capsule formulation | 3 months | \[AUC0-24 MR / AUC0-24 IR\] |
| Safety and tolerability of single doses of Firibastat (QGC001) by assessing Twelve-lead ECGs | 3 months | P wave, T wave, QRS complex, QT interval, RR interval, PR segment, ST segment, |
| Safety and tolerability of single doses of Firibastat (QGC001) by assessing AEs | 3 months | Adverse events will be recorded from the time of providing written informed consent until discharge from the study at the follow-up visit. During each study visit the subject will be questioned directly regarding the occurrence of any adverse medical event according to the source schedule. |
| Safety and tolerability of single doses of Firibastat (QGC001) by assessing safety haematology and chemistry laboratory tests aggregated as number of patients outside normal ranges. | 3 months | Basophils, Eosinophils, Haematocrit, Haemoglobin, Lymphocytes, Mean Cell, Haemoglobin, Mean Cell Haemoglobin Concentration, Mean Cell Volume, Monocytes, Neutrophils, Platelet Count, Red Blood Cell Count, White Blood Cell Count |
| Safety and tolerability of single doses of Firibastat (QGC001) by assessing chemistry laboratory tests aggregated as number of patients outside normal ranges. | 3 months | Alanine Aminotransferase, Albumin, Alkaline Phosphatase, Aspartate Aminotransferase, Bicarbonate, Bilirubin (Total), Calcium, Chloride, Creatine Kinase, Gamma Glutamyl Transferase, Glucose (Fasting), Potassium, Phosphate (Inorganic), Protein (Total), Sodium, Urea |
Countries
United Kingdom
Outcome results
None listed