Open-label study to compare the bioavailability of an oral tablet of GLPG1972 relative to an oral solution after single-dose intake in healthy subjects and to evaluate the effect of food on the oral tablet.

GLPG1972 is a new investigational compound that may eventually be used for the
treatment of osteoarthritis.

GLPG1972 is a potent inhibitor of human ADAMTS-5. ADAMTS-5 is an enzyme
(protein) which is present in many tissues in the body, mainly in uterus,
placenta and cartilage. ADAMTS-5 is responsible for the destruction of the
cartilage which could lead to osteoarthritis. Blocking ADAMTS-5 could result in
an inhibition of the cartilage destruction which may be a treatment for
osteoarthritis.

GLPG1972 is not yet registered as a drug but has been given to humans before.

The purpose of the study is to investigate the absorption, distribution and
elimination of GLPG1972 administered as oral solution compared to GLPG1972
administered as oral tablets (this is called bioavailability). Furthermore, the
effect of food on the absorption, distribution and elimination of GLPG1972
administered as oral tablets will be investigated. It will also be investigated
how safe GLPG1972 is and how well GLPG1972 is tolerated.

The actual study will consist of 3 treatment periods during which the
volunteers will stay in the clinical research center in Groningen for 3 days (2
nights): from the afternoon of Day -1 (1 day before administration of the study
compound) to the morning of Day 2. On Day 3 they will visit the clinical
research center in Groningen for a short visit. The time interval between the
different treatments for each volunteer is at least 6 days.

The post-study visit will take place 7-10 days after administration of the
study compound in Period 3. The appointment for the post-study visit will be
made with you during the study.

The participation to the entire study, from pre-study screening until the post
study visit, will be approximately 7 weeks.

In one of the three treatment periods of the study, the volunteers will receive
GLPG1972 as oral solution (Treatment A). After intake of the study compound
they are also required to drink an additional amount of 240 milliliters water.
In the other two treatment periods, they will receive GLPG1972 as oral tablets
with 240 milliliters of tap water (Treatments B and C).

Treatments A and B will be given under fasted conditions. This means that the
volunteers are not allowed to eat for at least 10 hours before administration
of the study compound. During fasting they are allowed to drink water with the
exception of 2 hours prior to until 2 hours after administration of the study
compound. Fasting will continue until 4 hours after administration of the study
compound. Then they will receive a lunch. Before administration of Treatment C
they will receive a standardized, non-vegetarian, high fat and high calorie
breakfast. They are not allowed to eat for at least 10 hours before consumption
of this high fat and high calorie breakfast. During fasting the volunteers are
allowed to drink water. The breakfast will have to be finished within 20
minutes and the entire breakfast must be consumed. At 30 minutes after the
start of the high fat and high calorie breakfast they will receive Treatment C.
They are not allowed to eat for at least 4 hours after administration of the
study compound. Then the volunteers will receive a lunch.

Treatment A: 600 mg GLPG1972 as an oral solution after an overnight fast
Treatment B: 600 mg GLPG1972 as oral tablets (2 tablets) after an overnight
fast
Treatment C: 600 mg GLPG1972 as oral tablets (2 tablets) after a high fat and
high calorie breakfast

Pain, minor bleeding, bruising, possibly an infection due to blood sampling.