First-in-Human Single and Multiple Dose of GLPG1205

Study Overview
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Brief Summary
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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.

Official Title
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Randomized, Double-blind, Placebo-controlled, Dose-ranging Study for the Assessment of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Ascending Oral Doses of GLPG1205 in Healthy Male Subjects

Conditions
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Healthy

Intervention / Treatment
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* Drug: GLPG1205 single ascending doses, oral suspension
* Drug: Placebo single ascending doses, oral suspension
* Drug: GLPG1205, multiple ascending doses, oral suspension
* Drug: Placebo, multiple ascending doses, oral suspension


Participation Criteria
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Eligibility Criteria
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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

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 50 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Quadruple


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: GLPG1205 single dose<br>Single oral dose of GLPG1205 suspension - ascending doses | Drug: GLPG1205 single ascending doses, oral suspension<br>* Single dose, oral suspension at 10 mg/mL or 50 mg/mL, starting dose of 10mg escalating up to 800mg<br>|
| Placebo Comparator: Placebo single dose<br>Single oral dose of placebo suspension | Drug: Placebo single ascending doses, oral suspension<br>* Single dose, oral suspension matching placebo<br>|
| Experimental: GLPG1205 multiple doses<br>Multiple oral doses of GLPG1205 suspension - ascending doses | Drug: GLPG1205, multiple ascending doses, oral suspension<br>* Multiple doses, daily for 14 days, oral suspension at 10 mg/mL or 50 mg/mL, anticipated doses: 100mg to 400mg<br>|
| Placebo Comparator: Placebo multiple doses<br>Multiple oral doses of placebo suspension | Drug: Placebo, multiple ascending doses, oral suspension<br>* Multiple doses, daily for 14 days, oral suspension matching placebo<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| 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 | 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 | Between screening and 7-10 days after the last dose | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| 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 | 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 | 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 | 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 | 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 | Day 1 and Day 14, predose up to 24 hours post dose |