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The purpose of this study is to evaluate the safety and tolerability after multiple ascending oral doses of GLPG0974 given to healthy male subjects for 14 days, compared to placebo.
Furthermore, during the course of the study, the amount of GLPG0974 present in the blood and urine (pharmacokinetics) as well as the effects of GLPG0974 on mechanism of action-related parameters in the blood and stool samples (pharmacodynamics) will be characterized compared to placebo.
Also, the effect of the compound on glucose tolerance will be explored as well as the potential of cytochrome P450 (CYP)3A4 induction by repeated dosing with GLPG0974.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 50 mg GLPG0974 or placebo | Other | 50 mg GLPG0974 dose as oral capsule or placebo capsule, daily for 14 days |
|
| 100 mg GLPG0974 or placebo | Other | 100 mg GLPG0974 dose as oral capsule or placebo oral capsule, daily for 14 days |
|
| 200 mg GLPG0974 or placebo | Other | 200 mg GLPG0974 dose as oral capsule or placebo capsule, daily for 14 days |
|
| 400 mg GLPG0974 or placebo | Other | 400 mg GLPG0974 dose as oral capsule or placebo capsule, daily for 14 days |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GLPG0974 | Drug |
|
| Measure | Description | Time Frame |
|---|---|---|
| Safety and tolerability | To evaluate the safety and tolerability of GLPG0974 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 |
| Measure | Description | Time Frame |
|---|---|---|
| The amount of GLPG0974 in plasma and urine over time after multiple oral dose | To characterize the amount of GLPG0974 in plasma and urine over time - pharmacokinetics (PK) - after multiple oral doses in healthy subjects | Between Day 1 predose and Day 14 |
| Inhibition of CD11b on neutrophils in blood after multiple oral doses of GLPG0974 |
| Measure | Description | Time Frame |
|---|---|---|
| Ratio of 6b-hydroxycortisol/cortisol in urine | Potential of CYP3A4 induction by repeated dosing with GLPG0974 will be assessed by means of the ratio of 6b-hydroxycortisol/cortisol in urine | Predose and postdose on Day 1 and Day 13 for 24h |
| Levels of faecal calprotectin in stool |
Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Frédéric Vanhoutte, MD | Lakefront Biotherapeutics NV | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| SGS LSS Clinical Pharmacology Unit Antwerp | Antwerp | Antwerp | Belgium |
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| ID | Term |
|---|---|
| C000595478 | 4-(((R)-1-(benzo(b)thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl)-(3-chloro-benzyl)-amino)-butyric acid |
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| Placebo | Drug |
|
To characterize the pharmacodynamics (PD) of GLPG0974 by means of inhibition of expression of CD11b on neutrophils after multiple oral doses in healthy subjects |
| Day 1 and Day 13, predose until 24h post dose |
Concentrations of faecal calprotectin will be measured as a pharmacodynamic marker in a single stool sample predose and postdose |
| Prior to first dosing and postdose (between Day 12 and 15) |
| Glucose and insulin concentrations after glucose loading | Oral glucose tolerance test by means of measuring concentrations of glucose and insulin after glucose loading, once predosing and once postdosing of GLPG0974 | Day -1 (predose) and Day 14 (postdose) |