First-in-Human Single and Multiple Dose of GLPG1972

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

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: GLPG1972 single ascending doses; Drug: Placebo single dose; Drug: GLPG1972 multiple ascending doses; Drug: Placebo multiple doses

• Study Type: Interventional
• Enrollment (Actual): 41
• 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: Male

Description

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

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

What is the study measuring?

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

Collaborators and Investigators

• Sponsor: Galapagos NV
• Investigators: Study Director: Ennis Lee, MD, Galapagos NV

Study record dates

Study Major Dates

• Study Start: November 1, 2015
• Primary Completion (Actual): April 1, 2016
• Study Completion (Actual): July 1, 2016

Study Registration Dates

• First Submitted: November 19, 2015
• First Submitted That Met QC Criteria: November 20, 2015
• First Posted (Estimate): November 23, 2015

Study Record Updates

• Last Update Posted (Estimate): July 29, 2016
• Last Update Submitted That Met QC Criteria: July 28, 2016
• Last Verified: March 1, 2016

More Information

Terms related to this study

• Other Study ID Numbers: GLPG1972-CL-101; 2015-004156-21 (EudraCT Number)