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| ID | Type | Description | Link |
|---|---|---|---|
| 2016-003626-17 | EudraCT Number |
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This study is a first-in-human (FIH), Phase I, single center, randomized, double-blind, placebo-controlled, sequential group study in healthy male subjects to assess the safety, tolerability and PK of single ascending oral doses of GLPG2737 and multiple ascending oral doses of GLPG2737 administered for 14 days.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| GLPG2737 single dose | Experimental | Single doses of GLPG2737 oral suspension at up to 5 dose levels in ascending order |
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| Placebo single dose | Placebo Comparator | Single doses of Placebo oral suspension |
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| GLP2737 multiple dose | Experimental | Multiple doses of GLPG2737 oral suspension at up to 3 dose levels in ascending order |
|
| GLPG2737 multiple dose | Placebo Comparator | Multiple doses of Placebo oral suspension |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GLPG2737 single dose | Drug | GLPG2737 oral suspension, single ascending doses |
| |
| Measure | Description | Time Frame |
|---|---|---|
| Change versus placebo in the proportion of subjects with adverse events | To assess safety and tolerability of single and multiple ascending doses with GLPG2737 versus placebo in healthy subjects. | Between screening and 14 days (SAD part) and 15 days (MAD part) after the last dose |
| Measure | Description | Time Frame |
|---|---|---|
| Maximum observed plasma concentration (Cmax) of GLPG2737 | To characterize pharmacokinetics of GLPG2737 and its metabolites after single and multiple oral doses in healthy subjects | Between Day 1 predose and 5 days after the last dose |
| Time of occurrence of Cmax for GLPG2737 (tmax) |
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Inclusion Criteria:
Male between 18-50 years of age, inclusive, on the date of signing the Informed Consent Form (ICF).
Judged by the investigator to be in good health based upon the results of a medical history, physical examination, vital signs, 12-lead ECG, and clinical safety laboratory tests prior to the initial study drug administration.
Clinical safety laboratory test results must be within the laboratory reference ranges for males or test results that are outside the reference ranges for males need to be considered non clinically significant in the opinion of the investigator. One retest is allowed if deemed appropriate by the investigator.
Liver function tests must meet the following criteria:
Subject's screening ECG is considered normal or abnormal but clinically non-significant. QTcF must not exceed 450 msec. First degree heart block will not be considered as a significant abnormality.
Forced expiratory volume in 1 second (FEV1) ≥ 80% of predicted normal for age, gender and height at screening.
Discontinuation of all medications (including over-the-counter and/or prescription medication, dietary supplements, nutraceuticals, vitamins and/or herbal supplements) except occasional paracetamol (maximum dose of 2 g/day and maximum of 10 g/2 weeks) at least 2 weeks prior to the first study drug administration.
Negative drug and alcohol screen (opiates, methadone, cocaine, amphetamines [including ecstasy], cannabinoids, barbiturates, benzodiazepines, tricyclic antidepressants, and alcohol) prior to dosing.
Able and willing to comply with the prohibitions and restrictions as described in the protocol and with the contraceptive requirements as described in the protocol.
Able and willing to sign the ICF as approved by the IEC, prior to any screening evaluations.
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Chris Brearley, BM, MRCP, MFPM | Lakefront Biotherapeutics NV | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| PRA-EDS | Groningen | Netherlands |
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| Placebo single dose |
| Drug |
Placebo, oral suspension. |
|
| GLPG2737 multiple dose | Drug | GLPG2737 oral suspension, multiple ascending doses, daily for 14 days. |
|
| GLPG2737 multiple dose | Drug | Placebo, oral suspension, daily for 14 days |
|
To characterize pharmacokinetics of GLPG2737 and its metabolites after single and multiple oral doses in healthy subjects |
| Between Day 1 predose and 5 days after the last dose |
| Area under the plasma concentration-time curve (AUC0-t) of GLPG2737 | To characterize pharmacokinetics of GLPG2737 and its metabolites after single and multiple oral doses in healthy subjects | Between Day 1 predose and 5 days after the last dose |
| Ratio of 4-beta-hydroxycholesterol/cholesterol in plasma after multiple oral doses in healthy subjects | To explore the potential of CYP3A4 interaction with GLPG2737 | Day 1 predose and Day 14 |