This is an open-label study to determine the pharmacokinetics of a new tablet formulation of GLPG1972 and to compare it with this of the liquid solution used during the First-in-Human study (GLPG1972-CL-101). The impact of food intake on the oral bioavailability of GLPG1972 administered as tablet will also be investigated in this study. A dose of 600 mg has been selected. The study is a phase I randomized open-label cross-over study with three single dose treatments: A) 600 mg GLPG1972 oral solution after overnight fast, B) 600 mg GLPG1972 oral tablet after overnight fast, C) 600 mg GLPG1972 oral tablet 30 minutes after high-fat high-calorie breakfast. A washout of at least 6 days between subsequent dosing days is respected so that no measurable plasma levels or biologically significant effects are remaining. There will be frequent assessment of adverse experiences post-dose. Twelve healthy male subjects will be selected according to the inclusion and exclusion criteria and 2 subjects each will be randomized to one of the 6 treatment sequences (ABC, ACB, BAC, BCA, CAB, CBA)
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
12
dosing after overnight fasting
dosing after overnight fasting
dosing after high-fat high-calorie breakfast
PRA-EDS
Zuidlaren, Netherlands
Maximum observed plasma concentration (Cmax) of GLPG1972
To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast
Time frame: From pre-dose (period 1) until 6 days after the last dose (period 3)
Plasma concentration of GLPG1972 24 hours after dosing
To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast
Time frame: 24 hours after each dose
The time of the occurrence of Cmax of GLPG1972
To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast
Time frame: From pre-dose (period 1) until 6 days after the last dose (period 3)
The area under the plasma concentration versus time curve
To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast
Time frame: From pre-dose until 6 days post-dose for each dosing period
The apparent terminal half-life of GLPG1972
To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast
Time frame: From pre-dose (period 1) until 6 days after the last dose (period 3)
The number of adverse events reported
To evaluate safety and tolerability of single oral doses of GLPG1972
Time frame: From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose
Changes in clinical laboratory evaluations
To evaluate safety and tolerability of single oral doses of GLPG1972
Time frame: From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose
Changes in vital signs
To evaluate safety and tolerability of single oral doses of GLPG1972
Time frame: From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose
Changes in physical examination parameters
To evaluate safety and tolerability of single oral doses of GLPG1972
Time frame: From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose
Changes in ECG parameters
To evaluate safety and tolerability of single oral doses of GLPG1972
Time frame: From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.