First-in-Human Single and Multiple Dose of GLPG1837

Randomized, Double-blind, Placebo-controlled, Dose-escalation Study for the Assessment of Safety, Tolerability and Pharmacokinetics of Single and Multiple Ascending Oral Doses of GLPG1837 in Healthy Subjects

The purpose of this First-in-Human study is to evaluate the safety and tolerability after single ascending oral doses of GLPG1837 given to healthy subjects, compared to placebo. Also, the safety and tolerability of multiple ascending oral doses of GLPG1837 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 GLPG1837 and its metabolite present in the blood and urine (pharmacokinetics) will be characterized.

The effect of food on the pharmacokinetics of GLPG1837 and its metabolite will also be evaluated.

The potential of cytochrome P450 (CYP)3A4 induction after repeated dosing with GLPG1837 will be explored as well.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: GLPG1837 single ascending doses; Drug: Placebo single dose; Drug: GLPG1837 multiple ascending doses; Drug: Placebo multiple doses

• Study Type: Interventional
• Enrollment (Actual): 64
• Phase: Phase 1

Contacts and Locations

Study Locations

• Belgium
  • Antwerp, Belgium
    • SGS LSS Clinical Pharmacology Unit Antwerp

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Males or females of non-child bearing potential between 18-50 years of age (included)
• Subjects must have a body mass index between 18-30 kg/m² (included)
• 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 findings

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 or biologic investigational research study or participation within 15 weeks prior to initial study drug administration in an investigational research study with antibody administration
• 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
• Pregnant or lactating women or women of childbearing potential

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Quadruple

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo single dose; Single oral dose of placebo suspension	Drug: Placebo single dose; Single dose, oral suspension matching placebo
Placebo Comparator: Placebo multiple doses; Multiple oral doses of placebo suspension	Drug: Placebo multiple doses; Multiple doses, daily for 14 days, oral suspension, matching placebo
Experimental: GLPG1837 single dose; Single oral dose of GLPG1837 suspension - ascending doses	Drug: GLPG1837 single ascending doses; Single dose, oral suspension
Experimental: GLPG1837 muliple doses; Multiple oral doses of GLPG1837 suspension - ascending doses	Drug: GLPG1837 multiple ascending doses; Multiple doses, daily for 14 days, oral suspension

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of subjects with adverse events	To evaluate the safety and tolerability of GLPG1837 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
Number of subjects with abnormal laboratory parameters	To evaluate the safety and tolerability of GLPG1837 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
Number of subjects with abnormal vital signs	To evaluate the safety and tolerability of GLPG1837 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
Number of subjects with abnormal electrocardiogram	To evaluate the safety and tolerability of GLPG1837 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
Number of subjects with abnormal physical examination	To evaluate the safety and tolerability of GLPG1837 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 GLPG1837 and its metabolite in plasma	To characterize the amount of GLPG1837 and its metabolite 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 GLPG1837 and its metabolite in urine	To characterize the amount of GLPG1837 and its metabolite 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 induction after repeated oral dosing with GLPG1837 by means of the ratio of 6-b-hydroxycortisol/cortisol in urine	Twelve hours before dosing on Day 1 and Day 14

Collaborators and Investigators

• Sponsor: Galapagos NV

Study record dates

Study Major Dates

• Study Start: December 1, 2014
• Primary Completion (Actual): September 1, 2015
• Study Completion (Actual): September 1, 2015

Study Registration Dates

• First Submitted: December 19, 2014
• First Submitted That Met QC Criteria: December 19, 2014
• First Posted (Estimate): December 24, 2014

Study Record Updates

• Last Update Posted (Estimate): September 9, 2015
• Last Update Submitted That Met QC Criteria: September 7, 2015
• Last Verified: September 1, 2015

More Information

Terms related to this study

• Other Study ID Numbers: GLPG1837-CL-101; 2014-003853-32 (EudraCT Number)