Healthy
Conditions
Brief summary
This will be a Phase I, randomized, double-blind, placebo-controlled, 2 period cross-over, drug-drug interaction study to evaluate the effect of multiple oral doses of GLPG1205 or placebo (daily from Day 1 to Day 12) on a single dose pharmacokinetic profile of a cocktail of CYP450 substrates administered to healthy male subjects. The cocktail of CYP450 substrates will consist of 10 mg warfarin (CYP2C9 substrate), 20 mg omeprazole (CYP2C19 substrate) and 100 mg caffeine (CYP1A2 substrate). Fourteen healthy male subjects will receive during two treatment periods from Day 1 to Day 12 a daily dose of GLPG1205 or placebo. On Day 13, a single dose of the cocktail of CYP450 substrates will be co-administered either with GLPG1205 or with placebo. The two treatment periods will be separated by a wash-out period of at least 28 days. Also, the safety and tolerability of multiple oral doses of GLPG1205 administered with or without a cocktail of CYP450 substrates in healthy male subjects will be evaluated.
Interventions
DRUGGLPG1205
Once daily administration of 2 GLPG1205 capsules from Day 1 to Day 13
DRUGPlacebo
Once daily administration of 2 matching placebo capsules from Day 1 to Day 13
Single administration on Day 13 of cocktail of CYP450 substrates: warfarin tablet, omeprazole capsule and caffeine oral solution
Sponsors
Galapagos NV
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)
Eligibility
Sex/Gender
MALE
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
* healthy male, age 18-50 years * BMI between 18-30 kg/m2
Exclusion criteria
* Poor or moderate metabolizer for CYP2C9 or CYP2C19 as determined by genotyping * Having a contraindication as indicated in the respective Summary of Product Characteristics (or Package Leaflets) for warfarin, omeprazole or caffeine * Intake of nutraceuticals within 3 weeks prior to dosing or within 6 times the elimination half life * Intake of enzyme inducing or enzyme inhibiting drugs within 3 months prior to dosing * Intake of vitamin K within 3 weeks prior to dosing * Any condition that might interfere with the procedures or tests in this study * Drug or alcohol abuse * Smoking
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| The maximum observed concentration (Cmax) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo | Between Day 13 and 7 days after the last dose | To characterize the maximum observed concentration (Cmax) of CYP450 substrates in plasma over time after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects |
| The time of occurrence of Cmax (tmax) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo | Between Day 13 and 7 days after the last dose | To characterize the time of occurrence of Cmax (tmax) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects |
| The area under the plasma concentration versus time curve (AUC) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo | Between Day 13 and 7 days after the last dose | To characterize the area under the plasma concentration versus time curve (AUC) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects |
| The apparent terminal half-life (t1/2) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo | Between Day 13 and 7 days after the last dose | To characterize the apparent terminal half-life (t1/2) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects |
| The metabolite over parent AUC ratio (R) of CYP450 substrates in plasma after multiple oral doses of GLPG1205 or placebo | Between Day 13 and 7 days after the last dose | To characterize the metabolite over parent AUC ratio (R) of CYP450 substrates in plasma after a single dose of a cocktail of CYP450 substrates and multiple doses of GLPG1205 or placebo in healthy male subjects |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Number of adverse events | Between Screening and 7 days after the last dosing | To evaluate the safety and tolerability of GLPG1205 after multiple oral doses in healthy male subjects with or without coadministration of a cocktail of CYP450 substrates in terms of the number of adverse events reported |
| Changes in urine safety lab parameters | Between Screening and 7 days after the last dosing | To evaluate the safety and tolerability of GLPG1205 after multiple oral doses in healthy male subjects with or without coadministration of a cocktail of CYP450 substrates in terms of changes in urine safety parameters reported |
| Changes in vital signs as measured by heart rate, blood pressure, respiratory rate and oral body temperature | Between Screening and 7 days after the last dosing | To evaluate the safety and tolerability of GLPG1205 after multiple oral doses in healthy male subjects with or without coadministration of a cocktail of CYP450 substrates in terms of changes in vital signs as measured by heart rate, blood pressure, respiratory rate and oral body temperature reported |
| Changes in 12-lead ECG measures | Between Screening and 7 days after the last dosing | To evaluate the safety and tolerability of GLPG1205 after multiple oral doses in healthy male subjects with or without coadministration of a cocktail of CYP450 substrates in terms of changes in 12-ECG measures reported |
| Changes in physical examination measures | Between Screening and 7 days after the last dosing | To evaluate the safety and tolerability of GLPG1205 after multiple oral doses in healthy male subjects with or without coadministration of a cocktail of CYP450 substrates in terms of changes in physical examination measures reported |
| Changes in blood safety lab parameters | Between Screening and 7 days after the last dosing | To evaluate the safety and tolerability of GLPG1205 after multiple oral doses in healthy male subjects with or without coadministration of a cocktail of CYP450 substrates in terms of changes in blood safety parameters reported |
Countries
Belgium
Outcome results
None listed