Multiple Ascending Dose Study of GLPG0974 in Healthy Subjects

Double-blind, Randomized, Placebo-controlled Study for the Assessment of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Ascending Oral Doses of GLPG0974 in Healthy Male Subjects

The purpose of this study is to evaluate the safety and tolerability after multiple ascending oral doses of GLPG0974 given to healthy male subjects for 14 days, compared to placebo.

Furthermore, during the course of the study, the amount of GLPG0974 present in the blood and urine (pharmacokinetics) as well as the effects of GLPG0974 on mechanism of action-related parameters in the blood and stool samples (pharmacodynamics) will be characterized compared to placebo.

Also, the effect of the compound on glucose tolerance will be explored as well as the potential of cytochrome P450 (CYP)3A4 induction by repeated dosing with GLPG0974.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo; Drug: GLPG0974

• Study Type: Interventional
• Enrollment (Actual): 32
• 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: Parallel Assignment
• Masking: Quadruple

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Other: 50 mg GLPG0974 or placebo; 50 mg GLPG0974 dose as oral capsule or placebo capsule, daily for 14 days	Drug: Placebo; Drug: GLPG0974
Other: 100 mg GLPG0974 or placebo; 100 mg GLPG0974 dose as oral capsule or placebo oral capsule, daily for 14 days	Drug: Placebo; Drug: GLPG0974
Other: 200 mg GLPG0974 or placebo; 200 mg GLPG0974 dose as oral capsule or placebo capsule, daily for 14 days	Drug: Placebo; Drug: GLPG0974
Other: 400 mg GLPG0974 or placebo; 400 mg GLPG0974 dose as oral capsule or placebo capsule, daily for 14 days	Drug: Placebo; Drug: GLPG0974

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Safety and tolerability	To evaluate the safety and tolerability of GLPG0974 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

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
The amount of GLPG0974 in plasma and urine over time after multiple oral dose	To characterize the amount of GLPG0974 in plasma and urine over time - pharmacokinetics (PK) - after multiple oral doses in healthy subjects	Between Day 1 predose and Day 14
Inhibition of CD11b on neutrophils in blood after multiple oral doses of GLPG0974	To characterize the pharmacodynamics (PD) of GLPG0974 by means of inhibition of expression of CD11b on neutrophils after multiple oral doses in healthy subjects	Day 1 and Day 13, predose until 24h post dose

Other Outcome Measures

Outcome Measure	Measure Description	Time Frame
Ratio of 6b-hydroxycortisol/cortisol in urine	Potential of CYP3A4 induction by repeated dosing with GLPG0974 will be assessed by means of the ratio of 6b-hydroxycortisol/cortisol in urine	Predose and postdose on Day 1 and Day 13 for 24h
Levels of faecal calprotectin in stool	Concentrations of faecal calprotectin will be measured as a pharmacodynamic marker in a single stool sample predose and postdose	Prior to first dosing and postdose (between Day 12 and 15)
Glucose and insulin concentrations after glucose loading	Oral glucose tolerance test by means of measuring concentrations of glucose and insulin after glucose loading, once predosing and once postdosing of GLPG0974	Day -1 (predose) and Day 14 (postdose)

Collaborators and Investigators

• Sponsor: Galapagos NV

Study record dates

Study Major Dates

• Study Start: October 1, 2012
• Primary Completion (Actual): February 1, 2013
• Study Completion (Actual): February 1, 2013

Study Registration Dates

• First Submitted: November 2, 2012
• First Submitted That Met QC Criteria: November 2, 2012
• First Posted (Estimate): November 6, 2012

Study Record Updates

• Last Update Posted (Estimate): February 12, 2013
• Last Update Submitted That Met QC Criteria: February 9, 2013
• Last Verified: February 1, 2013

More Information

Terms related to this study

• Other Study ID Numbers: GLPG0974-CL-102