Oral Bioavailability of Solid Formulation of GLPG1837 With and Without Food

• ClinicalTrials.gov Identifier: NCT02562859
• Recruitment Status: Completed
• First Posted: September 29, 2015
• Last Update Posted: October 23, 2015
• Sponsor: Galapagos NV
• Information provided by (Responsible Party): Galapagos NV

Study Description

Brief Summary:

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.

Condition or disease	Intervention/treatment	Phase
Healthy	Drug: 500 mg GLPG1837 as oral suspension; Drug: 500 mg GLPG1837 as oral tablet	Phase 1

Study Design

• Study Type: Interventional (Clinical Trial)
• Actual Enrollment: 12 participants
• Allocation: Randomized
• Intervention Model: Crossover Assignment
• Masking: None (Open Label)
• Primary Purpose: Treatment
• Official Title: 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
• Study Start Date: September 2015
• Actual Primary Completion Date: October 2015
• Actual Study Completion Date: October 2015

Arms and Interventions

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

Outcome Measures

Primary Outcome Measures :

1. The maximum observed concentration (Cmax) of GLPG1837 (metabolite) in plasma [ Time Frame: Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837) ]
   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
2. The concentration observed at 24 hours post dose (C24h) of GLPG1837 (metabolite) in plasma [ Time Frame: Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 2 (24h post dose) in period 3 (last dose of GLPG1837) ]
   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
3. The time of occurrence of Cmax (tmax) of GLPG1837 (metabolite) in plasma [ Time Frame: Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837) ]
   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
4. The area under the plasma concentration versus time curve (AUC) of GLPG1837 (metabolite) in plasma [ Time Frame: Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837) ]
   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
5. The apparent terminal half-life (t1/2) of GLPG1837 (metabolite) in plasma [ Time Frame: Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837) ]
   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
6. The metabolite over GLPG1837 ratios in plasma [ Time Frame: Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837) ]
   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

Secondary Outcome Measures :

1. Number of adverse events [ Time Frame: Between Screening and 7 to 10 days after the last dose of GLPG1837 ]
   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
2. Changes in vital signs as measured by heart rate, blood pressure and oral body temperature [ Time Frame: Between Screening and 7 to 10 days after the last dose of GLPG1837 ]
   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
3. Changes in 12-lead ECG measures [ Time Frame: Between Screening and 7 to 10 days after the last dose of GLPG1837 ]
   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
4. Changes in physical exam measures [ Time Frame: Between Screening and 7 to 10 days after the last dose of GLPG1837 ]
   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
5. Changes in blood safety lab parameters [ Time Frame: Between Screening and 7 to 10 days after the last dose of GLPG1837 ]
   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
6. Changes in urine safety lab parameters [ Time Frame: Between Screening and 7 to 10 days after the last dose of GLPG1837 ]
   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

Eligibility Criteria

• Ages Eligible for Study: 18 Years to 50 Years (Adult)
• Sexes Eligible for Study: Male
• Accepts Healthy Volunteers: Yes

Criteria

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

Contacts and Locations

Locations

Belgium

SGS LSS Clinical Pharmacology Unit Antwerp

Antwerp, Belgium

Sponsors and Collaborators

Galapagos NV

Investigators

• Study Director: Frédéric Vanhoutte, MD; Galapagos NV

More Information

• Responsible Party: Galapagos NV
• ClinicalTrials.gov Identifier: NCT02562859
• Other Study ID Numbers: GLPG1837-CL-103; 2015-002518-55 ( EudraCT Number )
• First Posted: September 29, 2015
• Last Update Posted: October 23, 2015
• Last Verified: October 2015