The purpose of this study is to investigate how safe 2 different formulations (immediate-release (IR) and modified-release (MR) tablets) of the new compound GLPG3312 are and how well they are tolerated when they are administered to healthy volunteers. Immediate-release and modified-release tablets contain the same active ingredient, but the modified-release tablet is covered with a protective layer, so it will dissolve in the intestines and not in the stomach. GLPG3312 has not been administered to humans before. Next to assessing the safety and tolerability, the purpose of this study is to investigate how food affects how quickly and to what extent GLPG3312 in a modified release formulation is absorbed and eliminated from the body. In addition, the effect of GLPG3312 on the body will be investigated by evaluating the effect of GLPG3312 on markers of the immune response.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
QUADRUPLE
Enrollment
95
GLPG3312 IR tablets, up to 4 single ascending oral doses (A, B, C, D).
Placebo tablets
GLPG3312 MR film-coated tablets, up to 4 single ascending oral doses (H, I, J, K).
GLPG3312 MR film-coated tablets, single oral dose (N) on 2 occasions, i.e. in fed state after a high-fat high-calorie breakfast, and in fasted state.
GLPG3312 MR film-coated tablets, up to 2 multiple ascending oral doses (O, P).
GLPG3312 MR optimized film-coated tablets, up to 3 multiple ascending oral doses (Q, R, S).
Placebo optimized tablets
PRA Health Sciences
Groningen, Netherlands
Frequency and severity of treatment emergent adverse events (TEAEs), treatment-emergent serious adverse events, and TEAEs leading to treatment discontinuations
To evaluate the safety and tolerability of oral single and multiple ascending doses of GLPG3312, in adult, healthy, subjects, when given as Immediate Release (IR) formulation (in fasted conditions) or as Modified Release (MR) formulation (in fasted and fed conditions)
Time frame: From screening through study completion, an average of 9 months.
Maximum observed plasma concentration (Cmax) of GLPG3312 (μg/mL) (Part 1)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy subjects, when given as IR formulation
Time frame: Between Day 1 pre-dose and Day 4
Maximum observed plasma concentration (Cmax) of GLPG3312 (μg/mL) (Part 2)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 7
Maximum observed plasma concentration (Cmax) of GLPG3312 (μg/mL) under fed conditions (high-fat high calorie) versus fasted conditions (Part 3)
To evaluate the food effect on the PK of a single oral dose of GLPG3312 in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 7
Maximum observed plasma concentration (Cmax) of GLPG3312 (μg/mL) (Part 4)
To evaluate the pharmacokinetics (PK) of oral MAD of GLPG3312, in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 21
Area under curve (AUC) of GLPG3312 (μg.h/mL) (Part 1)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy, subjects, when given as IR formulation
Time frame: Between Day 1 pre-dose and Day 4
Area under curve (AUC) of GLPG3312 (μg.h/mL) (Part 2)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 7
Area under curve (AUC) of GLPG3312 (μg.h/mL) under fed conditions (high-fat high calorie) versus fasted conditions (Part 3)
To evaluate the food effect on the PK of a single oral dose of GLPG3312 in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 7
Area under curve (AUC) of GLPG3312 (μg.h/mL) (Part 4)
To evaluate the pharmacokinetics (PK) of oral MAD of GLPG3312, in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 21
Terminal elimination half-life (t1/2) of GLPG3312 (h) (Part 1)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy, subjects, when given as IR formulation
Time frame: Between Day 1 pre-dose and Day 4
Terminal elimination half-life (t1/2) of GLPG3312 (h) (Part 2)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 7
Terminal elimination half-life (t1/2) of GLPG3312 (h) (Part 4)
To evaluate the pharmacokinetics (PK) of oral MAD of GLPG3312, in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 21
Cumulative amount of GLPG3312 excreted in urine (Aeurine)(mg) (Part 1)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy subjects, when given as IR formulation
Time frame: Between Day 1 pre-dose and Day 4
Cumulative amount of GLPG3312 excreted in urine (Aeurine)(mg) (Part 2)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 7
Cumulative amount of GLPG3312 excreted in urine (Aeurine)(mg) (Part 4)
To evaluate the PK of single and multiple ascending oral doses of GLPG3312, in adult, healthy subjects, when given as MR formulation.
Time frame: Between Day 1 pre-dose and Day 21
Cumulative amount of GLPG3312 excreted in feces (Aefeces)(mg) (Part 4)
To evaluate the PK of single and multiple ascending oral doses of GLPG3312, in adult, healthy subjects, when given as MR formulation.
Time frame: Between Day 1 pre-dose and Day 21
Ratio in extent and exposure following dosing of GLPG3312 as MR formulation compared to following dosing as IR formulation, under fasted conditions (Part 1 versus Part 2)
To evaluate the pharmacokinetics (PK) of oral SAD of GLPG3312, in adult, healthy, subjects, when given as IR or as MR formulation
Time frame: Between Day 1 pre-dose and Day 4
Ratio in extent and exposure following dosing of GLPG3312 as MR tablets under fed conditions (high-fat high calorie) versus fasted conditions (Part 3)
To evaluate the food effect on the PK of a single oral dose of GLPG3312 in adult, healthy, subjects, when given as MR formulation
Time frame: Between Day 1 pre-dose and Day 7
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