Phase 1
Conditions
Brief summary
The study will be a comparative oral bioavailability study between GKT137831 capsules and tablets, together with an assessment of the impact of concomitant food intake on the relative bioavailability of GKT137831 tablets. This will be a randomized three-way open cross-over study.
Interventions
DRUGGKT137831
oral bioavailable small molecule that selectively inhibit NOX1 and NOX4
Sponsors
Eurofins Optimed
York Bioanalytical Solution
Calliditas Therapeutics AB
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
OTHER
Masking
NONE
Intervention model description
Subject will be randomly allocated with different formulations of treatment or conditions (Fasting or Fed) during three periods (P1, P2 and P3).
Eligibility
Sex/Gender
MALE
Age
18 Years to 60 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy male subject, aged 18 to 60 years inclusive; 2. Non-smoker subject or smoker of not more than 5 cigarettes a day ; 3. No history of alcohol or drug abuse 4. Body Mass Index (BMI) between 18 and 27 5 kg/m2 inclusive; 5. Considered as healthy after a comprehensive clinical assessment (detailed medical history and complete physical examination); 6. Signing a written informed consent prior to selection;
Exclusion criteria
1. Blood donation (including in the frame of a clinical study) within 2 months before administration; 2. General anaesthesia within 3 months before administration; 3. Presence or history of drug hypersensitivity, or allergic disease diagnosed and treated by a physician; 4. Inability to abstain from intensive muscular effort; 5. No possibility of contact in case of emergency; 6. Any drug intake (except paracetamol) during the last month prior to the first administration; 7. History or presence of drug or alcohol abuse (alcohol consumption \> 40 grams / day); 8. Excessive consumption of beverages with xanthine bases (\> 4 cups or glasses / day); 9. Positive Hepatitis B surface (HBs) antigen or anti Hepatitis C Virus (HCV) antibody, or positive results for Human Immunodeficiency Virus (HIV) 1 or 2 tests; 10. Positive results of screening for drugs of abuse; 11. Subject who, in the judgment of the Investigator, is likely to be non-compliant or uncooperative during the study, or unable to cooperate because of a language problem, poor mental development; 12. Exclusion period of a previous study; 13. Administrative or legal supervision;
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Oral bioavailability (Fz) | 72 hours | To compare the relative oral bioavailability GKT137831 formulated in capsules or in tablets in healthy male subjects. |
| Food effect on Oral bioavailability (Fz) | 72 hours | To assess the impact of concomitant food intake on the relative bioavailability of GKT137831 after single oral dose administration of a 400 mg GKT137831 tablet in healthy male subjects. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Number of participants with treatment-related adverse events as assessed by CTCAE v5.0 | 7 days | To compare the safety and tolerability of single oral dose administration of 400 mg GKT137831 formulated in capsules or in tablets, and to evaluate the potential impact of concomitant food intake on the safety and tolerability of single oral dose administration of 400 mg GKT137831 tablet in healthy adult male subjects. |
| Oral bioavailability of GKT138184 | 72 hours | To compare the relative oral bioavailability GKT138184 after oral administration of GKT137831 formulated in capsules or in tablets in healthy male subjects. |
| Food effect on oral bioavailability of GKT138184 | 72 hours | To assess the impact of concomitant food intake on the relative bioavailability of GKT138184 after single oral dose administration of a 400 mg GKT137831 tablet in healthy male subjects. |
Countries
France
Outcome results
None listed