The primary objective of this study is to demonstrate that macitentan and tadalafil administered as a fixed combination is bioequivalent to both compounds given as separate tablets given at the same doses as in the fixed combination (i.e. whether the amounts of macitentan and tadalfil which reach the blood are comparable).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
38
Tablets for oral administration containing 10 mg of macitentan and 40 mg of tadalafil
Film-coated tablets for oral administration formulated at a strength of 10 mg
Film-coated tablets for oral administration formulated at a strength of 20 mg
CRS Clinical Research Services Mannheim
Mannheim, Germany
Maximum plasma concentration (Cmax) of macitentan and tadalafil
The measured individual plasma concentrations of macitentan and tadalafil are used to directly obtain Cmax
Time frame: Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period
Area under the plasma concentration-time curve from 0 to time t [AUC(0-t)] of macitentan and tadalafil
AUC(0-t) is the area calculated from the concentration-time profile of macitentan and tadalafil, from time 0 to to time t of the last measured concentration above the limit of quantification
Time frame: Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period
Area under the plasma concentration-time curve to infinitiy [AUC(0-inf)] of macitentan and tadalafil
AUC(0-inf) is the area calculated from the concentration-time profile of macitentan and tadalafil, from time 0 to extrapolated infinite time
Time frame: Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period
maximal plasma concentration (Cmax) of ACT-132577
Cmax of the active metabolite of macitentan, ACT-132577, is measured directly from the plasma concentrations of ACT-132577
Time frame: Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period
Area under the plasma concentration-time curve from 0 to time t [AUC(0-t)] of ACT-132577
AUC(0-t) of the active metabolite of macitentan, ACT-132577, is calculated from the concentration-time profile of ACT-132577 from time 0 to time t of the last measured concentration above the limit of quantification
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Time frame: Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period
Area under the plasma concentration-time curve to infinity [AUC(0-inf)] of ACT-132577
AUC(0-inf) of the active metabolite of macitentan, ACT-132577, is calculated from the concentration-time profile of ACT-132577 from time 0 to extrapolated infinite time
Time frame: Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period