First-in-Human Single and Multiple Dose of GLPG1205

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: GLPG1205 single ascending doses, oral suspension; Drug: Placebo single ascending doses, oral suspension; Drug: GLPG1205, multiple ascending doses, oral suspension; Drug: Placebo, multiple ascending doses, oral suspension

• Registration Number: NCT01887106
• Lead Sponsor: Galapagos NV

Brief Summary

The purpose of this First-in-Human study is to evaluate the safety and tolerability after single ascending oral doses of GLPG1205 given to healthy male subjects, compared to placebo. Also, the safety and tolerability of multiple ascending oral doses of GLPG1205 given to healthy male 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 GLPG1205 present in the blood and urine (pharmacokinetics) as well as the receptor occupancy by GLPG1205 in blood samples (pharmacodynamics) will be characterized compared to placebo.

Also, the potential of cytochrome P450 (CYP)3A4 induction after repeated dosing with GLPG1205 will be explored.

Detailed Description

Not available

Study Timeline

• Study Start: 2013-06
• Study First Submitted: 2013-06-22
• Study First Submitted QC: 2013-06-22
• Study First Posted: 2013-06-26
• Primary Completion: 2013-09
• Status Verified: 2013-10
• Study Completion: 2013-10
• Last Update Submitted: 2013-10-13
• Last Update Posted: 2013-10-16

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 40

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 & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
GLPG1205 single dose	GLPG1205 single ascending doses, oral suspension	Single oral dose of GLPG1205 suspension - ascending doses
Placebo single dose	Placebo single ascending doses, oral suspension	Single oral dose of placebo suspension
GLPG1205 multiple doses	GLPG1205, multiple ascending doses, oral suspension	Multiple oral doses of GLPG1205 suspension - ascending doses
Placebo multiple doses	Placebo, multiple ascending doses, oral suspension	Multiple oral doses of placebo suspension

Primary Outcome Measures

Name	Time	Method
Safety and tolerability after single dose	Between screening and 7-10 days after the last dose	To evaluate the safety and tolerability of GLPG1205 in comparison with placebo after a single oral dose in healthy subjects in terms of adverse events, physical examinations, vital signs, ECG and lab assessments
Safety and tolerability after multiple doses	Between screening and 7-10 days after the last dose	To evaluate the safety and tolerability of GLPG1205 in comparison with placebo after multiple oral doses daily for 14 days in healthy subjects in terms of adverse events, physical examinations, vital signs, ECG and lab assessments

Secondary Outcome Measures

Name	Time	Method
Ratio of 6-b-hydroxycortisol/cortisol in urine	Twelve hours before dosing on Day 1 and Day 14	To assess the potential of CYP3A4 induction after repeated dosing with GLPG1205 by means of the ratio of 6-b-hydroxycortisol/cortisol in urine
The amount of GLPG1205 in plasma and urine over time after a single oral dose	Between Day 1 predose and 48 hours post dose	To characterize the amount of GLPG1205 in plasma and urine over time - pharmacokinetics (PK) - after a single oral dose in healthy subjects
The amount of GLPG1205 in plasma and urine over time after multiple oral doses	Between Day 1 predose and Day 16 (48 hours after the last dose)	To characterize the amount of GLPG1205 in plasma and urine over time - pharmacokinetics (PK) - after multiple oral doses in healthy subjects
Receptor occupancy by GLPG1205 on blood cells after multiple doses	Day 1 and Day 14, predose up to 24 hours post dose	To characterize the pharmacodynamics (PD) of GLPG1205 by means of receptor occupancy by GLPG1205 on blood cells after multiple oral doses in healthy subjects
Receptor occupancy by GLPG1205 on blood cells after a single dose	Day 1 predose up to 24 hours post dose	To characterize the pharmacodynamics (PD) of GLPG1205 by means of receptor occupancy by GLPG1205 on blood cells after a single oral dose in healthy subjects

Trial Locations

Locations (1)

SGS LSS Clinical Pharmacology Unit Antwerp; 🇧🇪 Antwerp, Belgium