Oral Bioavailability of Solid Formulation of GLPG1837 With and Without Food

An Open-label Study to Compare the Oral Bioavailability of an Oral Tablet of GLPG1837 Relative to an Oral Suspension After Single-dose Intake in Healthy Subjects and to Evaluate the Effect of Food on the Oral Tablet

The purpose of the study is to evaluate the amount of GLPG1837 and metabolite present in the blood (relative bioavailability) after a single oral administration of 500 mg GLPG1837 given as an oral suspension under fasted conditions as well as a tablet formulation under fasted and fed conditions, in male healthy subjects.

Also, the safety and tolerability of a single oral dose of 500 mg GLPG1837 given as an oral suspension under fasted conditions as well as a tablet formulation under fasted and fed conditions, will be assessed.

Twelve subjects will receive GLPG1837 on 3 occasions as single dose administrations: as an oral suspension fasted, as an oral tablet, fed and fasted. Treatment administrations will be separated by a wash-out period of at least 6 days.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: 500 mg GLPG1837 as oral suspension; Drug: 500 mg GLPG1837 as oral tablet

• Study Type: Interventional
• Enrollment (Actual): 12
• 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:

• Healthy male, age 18-50 years
• BMI between 18-30 kg/m2

Exclusion Criteria:

• Any condition that might interfere with the procedures or tests in this study
• Drug or alcohol abuse
• Smoking

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: GLPG1837 as oral suspension fasted; Single dose of 500 mg GLPG1837 as oral suspension after an overnight fast	Drug: 500 mg GLPG1837 as oral suspension; A single dose of 500 mg GLPG1837 administered as oral suspension
Experimental: GLPG1837 as oral tablet fasted; Single dose of 500 mg GLPG1837 as oral tablet after an overnight fast	Drug: 500 mg GLPG1837 as oral tablet; A single dose of 500 mg GLPG1837 administered as oral tablet
Experimental: GLPG1837 as oral tablet fed; Single dose of 500 mg GLPG1837 as oral tablet after a high-fat high-calorie breakfast	Drug: 500 mg GLPG1837 as oral tablet; A single dose of 500 mg GLPG1837 administered as oral tablet

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
The maximum observed concentration (Cmax) of GLPG1837 (metabolite) in plasma	To characterize and compare the maximum observed concentration (Cmax) of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition	Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)
The concentration observed at 24 hours post dose (C24h) of GLPG1837 (metabolite) in plasma	To characterize and compare the concentration observed at 24 hours post dose (C24h) of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition	Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 2 (24h post dose) in period 3 (last dose of GLPG1837)
The time of occurrence of Cmax (tmax) of GLPG1837 (metabolite) in plasma	To characterize and compare the time of occurrence of Cmax (tmax) of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition	Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)
The area under the plasma concentration versus time curve (AUC) of GLPG1837 (metabolite) in plasma	To characterize and compare the area under the plasma concentration versus time curve of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition	Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)
The apparent terminal half-life (t1/2) of GLPG1837 (metabolite) in plasma	To characterize and compare the apparent terminal half-life of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition	Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)
The metabolite over GLPG1837 ratios in plasma	To characterize and compare the metabolite over GLPG1837 ratios in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition	Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of adverse events	To evaluate the safety and tolerability of a single dose of GLPG1837 administered as oral suspension fasted, oral tablet fasted versus fed in male healthy subjects in terms of number of adverse events (AEs) reported	Between Screening and 7 to 10 days after the last dose of GLPG1837
Changes in vital signs as measured by heart rate, blood pressure and oral body temperature	To evaluate the safety and tolerability of a single dose of GLPG1837 administered as oral suspension fasted, oral tablet fasted versus fed in male healthy subjects in terms of changes in vital signs as measured by heart rate, blood pressure and oral body temperature reported	Between Screening and 7 to 10 days after the last dose of GLPG1837
Changes in 12-lead ECG measures	To evaluate the safety and tolerability of a single dose of GLPG1837 administered as oral suspension fasted, oral tablet fasted versus fed in male healthy subjects in terms of changes in 12-ECG measures reported	Between Screening and 7 to 10 days after the last dose of GLPG1837
Changes in physical exam measures	To evaluate the safety and tolerability of a single dose of GLPG1837 administered as oral suspension fasted, oral tablet fasted versus fed in male healthy subjects in terms of changes in physical examination reported	Between Screening and 7 to 10 days after the last dose of GLPG1837
Changes in blood safety lab parameters	To evaluate the safety and tolerability of a single dose of GLPG1837 administered as oral suspension fasted, oral tablet fasted versus fed in male healthy subjects in terms of changes in blood safety lab parameters reported	Between Screening and 7 to 10 days after the last dose of GLPG1837
Changes in urine safety lab parameters	To evaluate the safety and tolerability of a single dose of GLPG1837 administered as oral suspension fasted, oral tablet fasted versus fed in male healthy subjects in terms of changes in urine safety lab parameters reported	Between Screening and 7 to 10 days after the last dose of GLPG1837

Collaborators and Investigators

• Sponsor: Galapagos NV

Study record dates

Study Major Dates

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

Study Registration Dates

• First Submitted: September 23, 2015
• First Submitted That Met QC Criteria: September 27, 2015
• First Posted (Estimate): September 29, 2015

Study Record Updates

• Last Update Posted (Estimate): October 23, 2015
• Last Update Submitted That Met QC Criteria: October 21, 2015
• Last Verified: October 1, 2015

More Information

Terms related to this study

• Other Study ID Numbers: GLPG1837-CL-103; 2015-002518-55 (EudraCT Number)