A Study in Healthy Male Volunteers Investigating the Safety, Absorption and Elimination of Single Doses of GLPG4059

Study Overview
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Brief Summary
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The main purpose of this study is to evaluate the safety, tolerability and pharmacokinetics of GLPG4059 in healthy volunteers after single oral administrations of GLPG4059 (SAD), compared to placebo (part 1). The effect of food (FE) (high-fat, high calorie) on the pharmacokinetics and relative bioavailability (rBA) of GLPG4059 will be assessed (part 2).

Official Title
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A First-in-human, Randomized, Double-blind, Placebo-controlled, Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Ascending Oral Doses of GLPG4059 in Adult, Healthy, Male Subjects

Conditions
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Healthy

Intervention / Treatment
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* Drug: GLPG4059 oral suspension
* Drug: Placebo
* Drug: GLPG4059 tablet


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Male between 18-54 years of age (extremes included), on the date of signing the informed consent form (ICF). A body mass index (BMI) between 18-30 kg/m2, inclusive. Judged to be in good health by the investigator based upon the results of a medical history, physical examination, vital signs, 12-lead ECG, and fasting clinical laboratory safety tests, available at screening and prior to randomization. ECG and vital signs parameters must be within the normal ranges. Bilirubin, aspartate aminotransferase (AST), and alanine aminotransferase (ALT) must be no greater than 1.5x upper limit of normal (ULN). Fasting plasma glucose must be <6.99 mmol/L, fasting defined as no caloric intake for at least 8 hours and hemoglobin A1c (HbA1c) <6.5% (48 mmol/mol). The test should be performed in a laboratory using a method that is national glycohemoglobin standardization program (NGSP) certified and standardized to the diabetes control and complications trial (DCCT) assay. Other clinical laboratory safety test results must be within the reference ranges or test results that are outside the reference ranges need to be considered not clinically significant in the opinion of the investigator. This list only contains the key inclusion criteria. Exclusion Criteria: Known hypersensitivity to Investigational Medicinal Product (IMP) ingredients or history of a significant allergic reaction to IMP ingredients as determined by the investigator. Positive serology for hepatitis B virus surface antigen (HBsAg) or hepatitis C virus (HCV) or history of hepatitis from any cause with the exception of hepatitis A that was resolved at least 3 months prior to first dosing of the IMP. This list only contains the key exclusion criteria.

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 54 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: Basic Science
Allocation: Randomized
Intervention Model: Sequential Assignment
Interventional Model Description: Part 1 (SAD) is randomized, double-blind, placebo-controlled; Part 2 (FE and rBA) is randomized, open-label.
Masking: Quadruple


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: GLPG4059 SAD<br>Single doses of GLPG4059 at up to 6 dose levels in ascending order | Drug: GLPG4059 oral suspension<br>* GLPG4059 for oral administration<br>|
| Placebo Comparator: Placebo SAD<br>Single doses of placebo | Drug: Placebo<br>* Placebo oral suspension<br>|
| Experimental: GLPG4059 rBA/FE oral suspension fasted<br>Single dose of GLPG4059 in fasted state | Drug: GLPG4059 oral suspension<br>* GLPG4059 for oral administration<br>|
| Experimental: GLPG4059 rBA/FE tablet fed<br>Single dose of GLPG4059 in fed state | Drug: GLPG4059 tablet<br>* GLPG4059 for oral administration<br>|
| Experimental: GLPG4059 rBA/FE tablet fasted<br>Single dose of GLPG4059 in fasted state | Drug: GLPG4059 tablet<br>* GLPG4059 for oral administration<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Frequency and severity of treatment-emergent adverse events (TEAEs), treatment-emergent serious adverse events, and TEAEs leading to treatment discontinuations | To evaluate the safety and tolerability of single ascending oral doses of GLPG4059, in adult, healthy, male subjects compared with placebo. | From screening through study completion, an average of 7 months | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Maximum observed plasma concentration (Cmax) of GLPG4059 | To evaluate the pharmacokinetics (PK) of single ascending oral doses of GLPG4059, in adult, healthy, male subjects. | Between Day 1 pre-dose and Day 4 | 
| Area under curve (AUC) of GLPG4059 | To evaluate the PK of single ascending oral doses of GLPG4059, in adult, healthy, male subjects | Between Day 1 pre-dose and Day 4 | 
| Terminal elimination half-life (t1/2) of GLPG4059 | To evaluate the PK of single ascending oral doses of GLPG4059, in adult, healthy, male subjects | Between Day 1 pre-dose and Day 4 |