First-in-Human Single and Multiple Dose of GLPG1972

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 GLPG1972 given to healthy subjects, compared to placebo. Also, the safety and tolerability of multiple ascending oral doses of GLPG1972 given to healthy 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 GLPG1972 present in the blood and urine (pharmacokinetics) will be characterized. The effect of food on the pharmacokinetics of GLPG1972 will also be evaluated. The potential of cytochrome P450 (CYP)3A4 interaction after repeated dosing with GLPG1972 will be explored as well. During the course of the study after multiple oral dose administrations, the effect of GLPG1972 on biomarkers present in the blood (pharmacodynamics) will be characterized.

Official Title
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Randomized, Double-blind, Placebo-controlled, Dose-escalation Study for the Assessment of the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Ascending Oral Doses of GLPG1972 in Healthy Male Subjects

Conditions
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Healthy

Intervention / Treatment
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* Drug: GLPG1972 single ascending doses
* Drug: Placebo single dose
* Drug: GLPG1972 multiple ascending doses
* Drug: Placebo multiple doses


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Males between 18-50 years of age Subjects must have a body mass index between 18-30 kg/m² Subjects must be judged to be in good health based upon the results of a medical history, physical examination, vital signs, 12-lead electrocardiogram and laboratory profile Exclusion Criteria: A subject with a known hypersensitivity to study drug ingredients or a significant allergic reaction to any drug Concurrent participation or participation within 8 weeks prior to the initial study drug administration in a drug/device investigational research study A subject with active drug or alcohol abuse within 2 years prior to the initial study drug administration Current sexually active (and/or child wish) male; a contraception method should be used

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: GLPG1972 single dose<br>Single oral dose of GLPG1972 solution - ascending doses | Drug: GLPG1972 single ascending doses<br>* single dose, oral solution<br>|
| Placebo Comparator: Placebo single dose<br>Single oral dose of placebo solution | Drug: Placebo single dose<br>* single dose, oral solution, matching placebo<br>|
| Experimental: GLPG1972 multiple doses<br>Multiple oral doses of GLPG1972 solution - ascending doses | Drug: GLPG1972 multiple ascending doses<br>* multiple doses, daily for 14 days, oral solution<br>|
| Placebo Comparator: Placebo multiple doses<br>Multiple oral doses of placebo solution | Drug: Placebo multiple doses<br>* multiple doses, daily for 14 days, oral solution<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Change versus placebo in number of subjects with adverse events | To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of adverse events | Between screening and 7-10 days after the last dose | 
| Change versus placebo in number of subjects with abnormal laboratory parameters | To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal laboratory parameters | Between screening and 7-10 days after the last dose | 
| Change versus placebo in number of subjects with abnormal vital signs | To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal vital signs | Between screening and 7-10 days after the last dose | 
| Change versus placebo in number of subjects with abnormal electrocardiogram | To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal electrocardiograms | Between screening and 7-10 days after the last dose | 
| Change versus placebo in number of subjects with abnormal physical examination | To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal physical examination | Between screening and 7-10 days after the last dose | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| The amount of GLPG1972 in plasma | To characterize the amount of GLPG1972 in plasma over time - pharmacokinetics (PK) - after a single oral dose and multiple oral doses in healthy subjects, fasted or fed | Between Day 1 predose and 48 hours after the (last) dose | 
| The amount of GLPG1972 in urine | To characterize the amount of GLPG1972 in urine over time - pharmacokinetics (PK) - after a single oral dose and multiple oral doses in healthy subjects, fasted or fed | Between Day 1 predose and 24 hours after the (last) dose | 
| Ratio of 6-b-hydroxycortisol/cortisol in urine | To assess the potential of CYP3A4 interaction after repeated oral dosing with GLPG1972 by means of the ratio of 6-b-hydroxycortisol/cortisol in urine | Twelve hours before dosing on Day 1 and Day 14 | 
| Levels of GLPG1972 biomarker in blood | To assess the pharmacodynamics (PD) of GLPG1972 by means of reduction of levels of biomarker in blood by GLPG1972 compared to placebo after repeated oral dosing | Between Day 1 predose and 48 hours after the last dose |