First-in-Human Single and Multiple Dose of GLPG1205

Randomized, Double-blind, Placebo-controlled, Dose-ranging Study for the Assessment of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Ascending Oral Doses of GLPG1205 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 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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: 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

• Study Type: Interventional
• Enrollment (Actual): 40
• 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: No
• 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: Parallel Assignment
• Masking: Quadruple

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: GLPG1205 single dose; Single oral dose of GLPG1205 suspension - ascending doses	Drug: GLPG1205 single ascending doses, oral suspension; Single dose, oral suspension at 10 mg/mL or 50 mg/mL, starting dose of 10mg escalating up to 800mg
Placebo Comparator: Placebo single dose; Single oral dose of placebo suspension	Drug: Placebo single ascending doses, oral suspension; Single dose, oral suspension matching placebo
Experimental: GLPG1205 multiple doses; Multiple oral doses of GLPG1205 suspension - ascending doses	Drug: GLPG1205, multiple ascending doses, oral suspension; Multiple doses, daily for 14 days, oral suspension at 10 mg/mL or 50 mg/mL, anticipated doses: 100mg to 400mg
Placebo Comparator: Placebo multiple doses; Multiple oral doses of placebo suspension	Drug: Placebo, multiple ascending doses, oral suspension; Multiple doses, daily for 14 days, oral suspension matching placebo

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Safety and tolerability after single 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	Between screening and 7-10 days after the last dose
Safety and tolerability after multiple doses	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	Between screening and 7-10 days after the last dose

Secondary Outcome Measures

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

Collaborators and Investigators

• Sponsor: Galapagos NV

Study record dates

Study Major Dates

• Study Start: June 1, 2013
• Primary Completion (Actual): September 1, 2013
• Study Completion (Actual): October 1, 2013

Study Registration Dates

• First Submitted: June 22, 2013
• First Submitted That Met QC Criteria: June 22, 2013
• First Posted (Estimate): June 26, 2013

Study Record Updates

• Last Update Posted (Estimate): October 16, 2013
• Last Update Submitted That Met QC Criteria: October 13, 2013
• Last Verified: October 1, 2013

More Information

Terms related to this study

• Other Study ID Numbers: GLPG1205-CL-101