A Phase 1 interventional study of Riociguat (Adempas) and Macitentan (Opsumit) in Healthy Subjects, sponsored by Actelion. Completed at 1 site in Germany. Open to male participants aged 18 Years to 45 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2018-02-08.
Sponsored by Actelion · Phase 1, Interventional, and Other
Both macitentan and riociguat are indicated in the treatment of pulmonary arterial hypertension (PAH) and may be administered concomitantly. The primary objective of this study is to evaluate the effect of macitentan administered for 11 days on the pharmacokinetics (PK) (i.e., amount and time of presence in the blood of riociguat) of a single dose of riociguat in healthy male subjects.
Key Inclusion Criteria:
Key Exclusion Criteria:
Other protocol defined inclusion and exclusion criteria may apply.
All subjects will receive treatment A followed by treatment B. Treatment A consists of a single oral dose (1 mg) of riociguat (Adempas) on Day 1. Treatment B consists of a loading oral dose of 30 mg macitentan (Opsumit) (3 tablets of 10 mg) on Day 5, then 10 mg of macitentan once daily from Day 6 to Day 15, with a concomitant administration of riociguat (1 mg) on Day 10.
Drug: Riociguat (Adempas) · Drug: Macitentan (Opsumit)
Riociguat film-coated tablets for oral administration at a strength of 1 mg
Macitentan film-coated tablets for oral administration at a strength of 10 mg
Also known as: ACT-064992
Area under the plasma concentration-time curve (AUC) from zero to infinity [AUC(0-inf)] of riociguat
AUC(0-inf) of riociguat will be assessed following administration of riociguat alone or concomitantly with macitentan.
Time frame: Day 1 (pre-dose to 96 hours post-dose ), Day 10 (pre-dose to 144 hours post-dose)
Maximum plasma concentration (Cmax) of riociguat
The maximum observed plasma concentration of riociguat will be assessed following administration of riociguat alone or concomitantly with macitentan.
Time frame: Day 1 (pre-dose to 96 hours post-dose ), Day 10 (pre-dose to 144 hours post-dose)
Time to reach Cmax (tmax) of riociguat and its metabolite M1
The maximum observed time to reach Cmax of riociguat and M1 will be assessed following administration of riociguat alone or concomitantly with macitentan.
Time frame: Day 1 (pre-dose to 96 hours post-dose ), Day 10 (pre-dose to 144 hours post-dose)
Elimination half life (t1/2) of riociguat and its metabolite M1
t1/2 of riociguat and M1 will be assessed following administration of riociguat alone or concomitantly with macitentan.
Time frame: Day 1 (pre-dose to 96 hours post-dose ), Day 10 (pre-dose to 144 hours post-dose)
AUC(0-t) of riociguat and its metabolite M1
AUC(0-t) is the area under the plasma concentration-time curve from zero to time t of the last measured concentration above the limit of quantification. It will be determined for both riociguat and its metabolite M1 following administration of riociguat alone or concomitantly with macitentan.
Time frame: Day 1 (pre-dose to 96 hours post-dose ), Day 10 (pre-dose to 144 hours post-dose)
AUC(0-inf) of riociguat metabolite M1
AUC(0-inf) of M1 will be assessed following administration of riociguat alone or concomitantly with macitentan.
Time frame: Day 1 (pre-dose to 96 hours post-dose ), Day 10 (pre-dose to 144 hours post-dose)
Maximum plasma concentration (Cmax) of riociguat metabolite M1
The maximum observed plasma concentration of M1 will be assessed following administration of riociguat alone or concomitantly with macitentan.
Time frame: Day 1 (pre-dose to 96 hours post-dose ), Day 10 (pre-dose to 144 hours post-dose)
Trough concentration (Ctrough) of macitentan and its metabolite ACT-132577
Ctrough of macitentan and its metabolite ACT-132577 will be assessed during the treatment period with macitentan (Day 10 to Day 15)
Time frame: Day 10 to Day 15 (before macitentan administration) and in the morning of Day 16
This study is completed, as verified in Feb 2018. You cannot join it, but the record below documents what was studied.
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