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| ID | Type | Description | Link |
|---|---|---|---|
| 2019-004001-27 | EudraCT Number | ||
| 67896062PAH1003 | Other Identifier | Actelion |
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The purpose of this study is to evaluate the effect of macitentan at steady state on the pharmacokinetic (PK) of a single dose of riociguat and sildenafil (Part A); and rosuvastatin (Part B) when co-administered to healthy male participants under fasted conditions.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part A: Macitentan + Substrate Drug (Sildenafil/Riociguat) | Experimental | Participants will receive a single dose of film-coated tablet of sildenafil under fasted condition (Treatment A1), then riociguat under fasted condition (Treatment A2) followed by macitentan under fed condition (Treatment B1), then riociguat along with macitentan under fasted conditions followed by macitentan under fed conditions (Treatment B2) and then sildenafil along with macitentan under fasted condition (Treatment B3). Macitentan will be administered in an up-titration regimen. |
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| Part B: Macitentan + Substrate Drug (Rosuvastatin) | Experimental | Participants will receive a single dose of film-coated tablet of rosuvastatin under fasted condition (Treatment A1), then macitentan under fed condition (Treatment B1) followed by rosuvastatin along with macitentan under fasted condition followed by macitentan under fed condition (Treatment B2). Macitentan will be administered in an up-titration regimen. Part B of the study will be conducted depending on the results of Part A and feedback from Health Authorities. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Macitentan | Drug | Macitentan will be administrated as film-coated tablet in Part A and Part B. |
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| Measure | Description | Time Frame |
|---|---|---|
| Part A and Part B: Area Under the Plasma Analyte Concentration-time Curve from Time Zero to Infinite Time (AUC[0-infinity]) of Sildenafil, Riociguat, Rosuvastatin | AUC(0-infinity) is defined as area under the plasma analyte concentration-time curve from time 0 to infinite time. | Up to 25 days |
| Part A and Part B: Maximum Observed Plasma Analyte Concentration (Cmax) of Sildenafil, Riociguat, Rosuvastatin | Cmax is defined as the maximum observed plasma analyte concentration. | Up to 25 days |
| Measure | Description | Time Frame |
|---|---|---|
| Part A: Area Under the Plasma Analyte Concentration-time Curve from Time Zero to Infinite Time (AUC[0-infinity]) of Desmethyl-sildenafil, M1 (Metabolite of Riociguat) and ACT-132577 (Metabolite of Macitentan) | AUC(0-infinity) is defined as area under the plasma analyte concentration-time curve from time 0 to infinite time. | Up to 25 days |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Actelion Clinical Trial | Actelion | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Clinical Pharmacology Unit | Merksem | 2170 | Belgium |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 42023995 | Derived | Csonka D, Gargano C, Goyal N, De Meulder M, Yartsev V, Ruixo JJP. Effect of Once-Daily Macitentan 75 mg on the Pharmacokinetics of Sildenafil, Riociguat, or Rosuvastatin in Healthy Male Participants. J Clin Pharmacol. 2026 Apr;66(4):e70185. doi: 10.1002/jcph.70185. |
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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
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| ID | Term |
|---|---|
| C533860 | macitentan |
| D000068677 | Sildenafil Citrate |
| C542595 | riociguat |
| D000068718 | Rosuvastatin Calcium |
| ID | Term |
|---|---|
| D013449 | Sulfonamides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D013450 | Sulfones |
| D013457 |
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| Sildenafil | Drug | Sildenafil will be administrated as film-coated tablet in Part A. |
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| Riociguat | Drug | Riociguat will be administrated as film-coated tablet in Part A. |
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| Rosuvastatin | Drug | Rosuvastatin will be administrated as film-coated tablet in Part B. |
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| Part A: Maximum Observed Plasma Analyte Concentration (Cmax) of Desmethyl-sildenafil, M1 and ACT-132577 |
Cmax is defined as the maximum observed plasma analyte concentration. |
| Up to 25 days |
| Part A and Part B: Area Under the Plasma Analyte Concentration-time Curve from 0 to Time t of the Last Measured Concentration (AUC[0-t]) of Sildenafil, Desmethyl-sildenafil, Riociguat, M1, Macitentan, ACT-132577, Rosuvastatin | AUC(0-t) is defined as area under the plasma analyte concentration-time curve from time 0 to time t of the last measured concentration above the lower limit of quantification (LLOQ), calculated according to the linear trapezoidal rule, using the measured concentration-time values above the LLOQ. | Up to 25 days |
| Part A and Part B: Time to Reach Maximum Observed Plasma Analyte Concentration (Tmax) of Sildenafil, Desmethyl-sildenafil, Riociguat, M1, Macitentan, ACT-132577, Rosuvastatin | Tmax is defined as actual sampling time to reach maximum observed plasma analyte concentration. | Up to 25 days |
| Part A and Part B: Apparent Elimination Half-life (t1/2) of Sildenafil, Desmethyl-sildenafil, Riociguat, M1, Macitentan, ACT-132577, Rosuvastatin | t1/2 is defined as the time measured for the plasma concentration to decrease by 1 half of its original concentration. It is associated with the terminal slope of the semilogarithmic drug concentration-time curve, calculated as t1/2=0.693/ lambda(z). | Up to 25 days |
| Part A and Part B: Trough Plasma Concentration (Ctrough) of Macitentan and ACT-132577 | Ctrough is defined as the observed plasma concentration before dosing or at the end of the dosing interval. | Up to 25 days |
| Part B: Number of Participants with Adverse Event as a Measure of Safety and Tolerability | An adverse event is any untoward medical event that occurs in a participant administered an investigational product, and it does not necessarily indicate only events with clear causal relationship with the relevant investigational product. | Up to Day 45 |
| Sulfur Compounds |
| D010879 | Piperazines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D011687 | Purines |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D005464 | Fluorobenzenes |
| D006845 | Hydrocarbons, Fluorinated |
| D006846 | Hydrocarbons, Halogenated |
| D006838 | Hydrocarbons |
| D011743 | Pyrimidines |