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.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
40
Single dose, oral suspension at 10 mg/mL or 50 mg/mL, starting dose of 10mg escalating up to 800mg
Single dose, oral suspension matching placebo
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
SGS LSS Clinical Pharmacology Unit Antwerp
Antwerp, Antwerp, Belgium
Safety and tolerability after single 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
Time frame: Between screening and 7-10 days after the last dose
Safety and tolerability after multiple doses
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
Time frame: Between screening and 7-10 days after the last dose
The amount of GLPG1205 in plasma and urine over time after a single oral dose
To characterize the amount of GLPG1205 in plasma and urine over time - pharmacokinetics (PK) - after a single oral dose in healthy subjects
Time frame: Between Day 1 predose and 48 hours post dose
The amount of GLPG1205 in plasma and urine over time after multiple oral doses
To characterize the amount of GLPG1205 in plasma and urine over time - pharmacokinetics (PK) - after multiple oral doses in healthy subjects
Time frame: Between Day 1 predose and Day 16 (48 hours after the last dose)
Ratio of 6-b-hydroxycortisol/cortisol in urine
To assess the potential of CYP3A4 induction after repeated dosing with GLPG1205 by means of the ratio of 6-b-hydroxycortisol/cortisol in urine
Time frame: Twelve hours before dosing on Day 1 and Day 14
Receptor occupancy by GLPG1205 on blood cells after a single 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
Time frame: Day 1 predose up to 24 hours post dose
Receptor occupancy by GLPG1205 on blood cells after multiple doses
To characterize the pharmacodynamics (PD) of GLPG1205 by means of receptor occupancy by GLPG1205 on blood cells after multiple oral doses in healthy subjects
Time frame: Day 1 and Day 14, predose up to 24 hours post dose
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