A Phase 1 interventional study of Macitentan 10 mg and Tadalafil 20 mg in Healthy, sponsored by Actelion. Completed at 1 site in United States. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2025-03-30.
Sponsored by Actelion · Phase 1, Interventional, and Basic science
The purpose of this study is to demonstrate bioequivalence on the primary pharmacokinetic (PK) parameters between macitentan and tadalafil administered as a fixed dose combination (FDC) (test) of macitentan/tadalafil and the co- administered free combination (reference) of macitentan (Opsumit) and tadalafil (Adcirca) in fasted conditions in healthy adult participants; and to evaluate the effect of food on the primary PK parameters of macitentan and tadalafil administered as an FDC of macitentan/tadalafil in fed versus fasted conditions in healthy adult participants.
Actelion is the lead sponsor of 140 studies on the registry; 1 is open to participants now.
Of its 27 completed or terminated interventional studies of FDA-regulated products, 24 (89%) have results posted.
Counted across the registry records on this site, refreshed daily.
Exclusion Criteria:
Participants will receive single oral dose of fixed dose combination (FDC) of macitentan/tadalafil under fasting conditions in (test) (Treatment A) Treatment Period 1 followed by single oral dose of FDC of macitentan/tadalafil under fed conditions (test) (Treatment B) in Treatment Period 2 and then single oral dose of macitentan/tadalafil under fasting conditions (reference) (Treatment C) in Treatment Period 3 on Day 1 of each Treatment Period. There will be a wash-out period of at least 12 days between Day 1 of subsequent treatment period.
Drug: Macitentan 10 mg · Drug: Tadalafil 20 mg · Drug: Macitentan 10 mg/Tadalafil 20mg FDC
Participants will receive Treatment B in Treatment Period 1 followed by Treatment C in Treatment Period 2 and Treatment A in Treatment Period 3. There will be a wash-out period of at least 12 days between Day 1 of subsequent treatment period.
Drug: Macitentan 10 mg · Drug: Tadalafil 20 mg · Drug: Macitentan 10 mg/Tadalafil 20mg FDC
Participants will receive Treatment C in Treatment Period 1 followed by Treatment A in Treatment Period 2 and Treatment B in Treatment Period 3. There will be a wash-out period of at least 12 days between Day 1 of subsequent treatment period.
Drug: Macitentan 10 mg · Drug: Tadalafil 20 mg · Drug: Macitentan 10 mg/Tadalafil 20mg FDC
Participants will receive Treatment A in Treatment Period 1 followed by Treatment C in Treatment Period 2 and Treatment B in Treatment Period 3. There will be a wash-out period of at least 12 days between Day 1 of subsequent treatment period.
Drug: Macitentan 10 mg · Drug: Tadalafil 20 mg · Drug: Macitentan 10 mg/Tadalafil 20mg FDC
Participants will receive Treatment C in Treatment Period 1 followed by Treatment B in Treatment Period 2 and Treatment A in Treatment Period 3. There will be a wash-out period of at least 12 days between Day 1 of subsequent treatment period.
Drug: Macitentan 10 mg · Drug: Tadalafil 20 mg · Drug: Macitentan 10 mg/Tadalafil 20mg FDC
Participants will receive Treatment B in Treatment Period 1 followed by Treatment A in Treatment Period 2 and Treatment C in Treatment Period 3. There will be a wash-out period of at least 12 days between Day 1 of subsequent treatment period.
Drug: Macitentan 10 mg · Drug: Tadalafil 20 mg · Drug: Macitentan 10 mg/Tadalafil 20mg FDC
Macitentan 10mg tablet will be administered orally as per assigned treatment sequence.
Also known as: Opsumit, JNJ-67896062
Tadalafil 20mg tablet will be administered orally as per assigned treatment sequence.
Also known as: Adcirca, JNJ-10291697
FDC of Macitentan 10 mg/Tadalafil 20 mg will be administered orally as single dose tablets.
Also known as: ACT-064992D
Maximum Observed Plasma Analyte Concentration (Cmax) of Macitentan and its Metabolite JNJ-68212820, and Tadalafil.
Cmax is defined as the maximum observed plasma analyte concentration.
Time frame: Predose up to 216 hours (up to Day 10)
Area Under the Plasma Analyte Concentration Time Curve of Macitentan, its Metabolite JNJ-68212820, and Tadalafil from Time Zero to Time of the Last Quantifiable Concentration (AUC [0-Last])
AUC (0-last) is defined as area under the plasma analyte concentration time curve of macitentan, its metabolite JNJ-68212820 and tadalafil from time 0 to the time of the last quantifiable (non-below quantification limit \[non-BQL\]) concentrations.
Time frame: Predose up to 216 hours (up to Day 10)
Area Under the Plasma Concentration Time Curve of Macitentan and its Metabolite JNJ-68212820, and Tadalafil from Time Zero to Infinite time (AUC [0-Infinity])
AUC (0-infinity) is defined as area under the plasma concentration-time curve of macitentan and its metabolite JNJ-68212820, and tadalafil from time 0 to infinite time, calculated as the sum of AUC (0-last) and C(last)/lambda(z) where C(last) is the last observed measurable (non-BQL) plasma analyte concentration.
Time frame: Predose up to 216 hours (up to Day 10)
Time to Reach Maximum Observed Plasma Analyte Concentration (Tmax) of Macitentan and its Metabolite JNJ-68212820, Tadalafil
Tmax is defined as actual sampling time to reach the maximum observed plasma analyte concentration.
Time frame: Predose up to 216 hours (up to Day 10)
Area Under the Plasma Concentration Versus Time Curve of Macitentan and its Metabolite JNJ-68212820, Tadalafil From Time Zero up to 72 Hours Post Dosing (AUC72h)
(AUC 0-72h) is defined as the area under the plasma concentration-time curve of macitentan and its metabolite JNJ-68212820, tadalafil from time 0 to 72 hours postdose, calculated by linear-linear trapezoidal summation.
Time frame: Predose up to 216 hours (up to Day 10)
Apparent Elimination Half-Life (t1/2) of Macitentan and its Metabolite JNJ-68212820, Tadalafil
t1/2 is defined as apparent elimination half-life calculated as 0.693/lambda(z).
Time frame: Predose up to 216 hours (up to Day 10)
Apparent Terminal Elimination Rate Constant (lambda z) of Macitentan and its Metabolite JNJ-68212820, Tadalafil
Apparent terminal elimination rate constant is estimated by linear regression using the terminal log-linear phase of the log-transformed concentration versus time curve.
Time frame: Predose up to 216 hours (up to Day 10)
Total Apparent Oral Clearance (CL/F) of Macitentan and its Metabolite JNJ-68212820, Tadalafil
CL/F is defined as total apparent oral clearance calculated as dose/AUC(0-infinity).
Time frame: Predose up to 216 hours (up to Day 10)
Apparent Volume of Distribution (Vd/F) of Macitentan and its Metabolite JNJ-68212820, Tadalafil
Vd/F is defined as apparent volume of distribution calculated as dose/(lambda(z) \*AUC (0 to infinity).
Time frame: Predose up to 216 hours (up to Day 10)
Last Observed Measurable Plasma Concentration (Clast) of Macitentan and its Metabolite JNJ-68212820, Tadalafil
Clast is defined as the last observed measurable (non-BQL) plasma concentration of macitentan and its metabolite JNJ-68212820, Tadalafil.
Time frame: Predose up to 216 hours (up to Day 10)
Plan to share: Yes — The data sharing policy of the Janssen Pharmaceutical Companies of Johnson \& Johnson is available at www.janssen.com/clinical-trials/transparency. As noted on this site, requests for access to the study data can be submitted through Yale Open Data Access (YODA) Project site at yoda.yale.edu
No publications or documents are linked to this record.
This study is completed, as verified in Mar 2025. You cannot join it, but the record below documents what was studied.
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