Healthy
Conditions
Brief summary
The purpose of this First-in-Human study is to evaluate the safety and tolerability after single ascending oral doses of GLPG1205 given to healthy male subjects, compared to placebo. Also, the safety and tolerability of multiple ascending oral doses of GLPG1205 given to healthy male subjects daily for 14 days compared to placebo, will be evaluated. Furthermore, during the course of the study after single and multiple oral dose administrations, the amount of GLPG1205 present in the blood and urine (pharmacokinetics) as well as the receptor occupancy by GLPG1205 in blood samples (pharmacodynamics) will be characterized compared to placebo. Also, the potential of cytochrome P450 (CYP)3A4 induction after repeated dosing with GLPG1205 will be explored.
Interventions
DRUGGLPG1205 single ascending doses, oral suspension
Single dose, oral suspension at 10 mg/mL or 50 mg/mL, starting dose of 10mg escalating up to 800mg
DRUGPlacebo single ascending doses, oral suspension
Single dose, oral suspension matching placebo
DRUGGLPG1205, multiple ascending doses, oral suspension
Multiple doses, daily for 14 days, oral suspension at 10 mg/mL or 50 mg/mL, anticipated doses: 100mg to 400mg
Multiple doses, daily for 14 days, oral suspension matching placebo
Sponsors
Galapagos NV
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)
Eligibility
Sex/Gender
MALE
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male, age 18-50 years * BMI between 18-30 kg/m2
Exclusion criteria
* Any condition that might interfere with the procedures or tests in this study * Drug or alcohol abuse * Smoking
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Safety and tolerability after single dose | Between screening and 7-10 days after the last dose | To evaluate the safety and tolerability of GLPG1205 in comparison with placebo after a single oral dose in healthy subjects in terms of adverse events, physical examinations, vital signs, ECG and lab assessments |
| Safety and tolerability after multiple doses | Between screening and 7-10 days after the last dose | To evaluate the safety and tolerability of GLPG1205 in comparison with placebo after multiple oral doses daily for 14 days in healthy subjects in terms of adverse events, physical examinations, vital signs, ECG and lab assessments |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Ratio of 6-b-hydroxycortisol/cortisol in urine | Twelve hours before dosing on Day 1 and Day 14 | To assess the potential of CYP3A4 induction after repeated dosing with GLPG1205 by means of the ratio of 6-b-hydroxycortisol/cortisol in urine |
| The amount of GLPG1205 in plasma and urine over time after a single oral dose | Between Day 1 predose and 48 hours post dose | To characterize the amount of GLPG1205 in plasma and urine over time - pharmacokinetics (PK) - after a single oral dose in healthy subjects |
| Receptor occupancy by GLPG1205 on blood cells after multiple doses | Day 1 and Day 14, predose up to 24 hours post dose | To characterize the pharmacodynamics (PD) of GLPG1205 by means of receptor occupancy by GLPG1205 on blood cells after multiple oral doses in healthy subjects |
| Receptor occupancy by GLPG1205 on blood cells after a single dose | Day 1 predose up to 24 hours post dose | To characterize the pharmacodynamics (PD) of GLPG1205 by means of receptor occupancy by GLPG1205 on blood cells after a single oral dose in healthy subjects |
| The amount of GLPG1205 in plasma and urine over time after multiple oral doses | Between Day 1 predose and Day 16 (48 hours after the last dose) | To characterize the amount of GLPG1205 in plasma and urine over time - pharmacokinetics (PK) - after multiple oral doses in healthy subjects |
Countries
Belgium
Outcome results
None listed