HealthyPhase 1NCT04963439
A Study of Two Macitentan Pediatric Formulations in Healthy Adult Participants
A Phase 1 study testing Macitentan in people with Healthy, run by Actelion at 1 site in Belgium.
Trial summary
The purpose of this study is to assess the rate and extent of absorption of macitentan following administration of a single oral dose of macitentan formulated as final market image (FMI) (test), compared to macitentan as the clinical service formulation (CSF) under fasted conditions in healthy adult participants. Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy
- What is being tested?
- Macitentan
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 16 participants
- Where
- 1 siteBelgium
- Study dates
- 8 Jul 2021to 5 Oct 2021
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Healthy on the basis of physical examination, medical and surgical history collected at screening. If there are abnormalities, the participant may be included only if the investigator judges the abnormalities to be not clinically significant. This determination must be recorded in the participant's source documents and initialed by the investigator
- Systolic blood pressure (SBP) between 100 and 145 millimeters of mercury (mmHg) (inclusive) and diastolic blood pressure (DBP) between 50 and 90 mmHg (inclusive) at screening, preferably measured on the right arm, supine after 5 minutes of rest and standing after 3 minutes
- Twelve-lead electrocardiogram (ECG) with heart rate between 45 and 90 beats per minute (bpm) and without clinically relevant abnormalities, at the discretion of the investigator, measured after the participant is supine for at least 5 minutes, at screening
- Body weight not less than 50.0 kilograms (kg) and body mass index (BMI) between 18.5 and 30.0 kilograms per meter square (kg/m^2) (inclusive)
- All women must have a negative highly sensitive serum (beta-human chorionic gonadotropin [beta- hCG]) pregnancy test at screening and must have a negative urine pregnancy test on Day -1 of each intervention period
Who cannot join
- Known allergies, hypersensitivity, or intolerance to macitentan or drugs of the same class, or any excipients of the drug formulations
- Taken any disallowed therapies, concomitant therapy within 14 days (or longer, based on elimination half-life) before administration of study intervention in the first intervention period
- Received an investigational intervention (including investigational vaccines) or used an invasive investigational medical device within 30 days or 10 half-lives (whichever is longer) before study intervention intake in the first intervention period, or received a biological product within 3 months or 10 half-lives (whichever is longer) before study intervention intake in the first intervention period, or is currently enrolled in an investigational study
- Values of hepatic aminotransferase (alanine aminotransferase and/or aspartate aminotransferase) greater than (>) 1.5 * upper limit of normal at screening
- Positive results from the human immunodeficiency virus (HIV) (type 1 and 2) serology at screening
Trial locations and contacts
1 site in 1 country.
About this study
Official title: A Single-center, Open-label, Single-dose, Randomized, 2-way Crossover Phase 1 Study in Healthy Adult Participants to Assess the Relative Oral Bioavailability of Two Macitentan Pediatric Formulations
The purpose of this study is to assess the rate and extent of absorption of macitentan following administration of a single oral dose of macitentan formulated as final market image (FMI) (test), compared to macitentan as the clinical service formulation (CSF) under fasted conditions in healthy adult participants.
- Conditions
- Healthy
- Being tested
- Macitentan
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
MacitentanDrug
Also called Opsumit, ACT-064992
Macitentan dispersible tablets will be administered orally as per assigned treatment sequence.
| Study group | Role | What they receive |
|---|---|---|
| Treatment Sequence AB | Experimental | Participants will receive single oral dose of macitentan formulated as final market image (FMI) in fasted conditions (test) (Treatment A) in treatment period 1 followed by a single oral dose of macitentan as the clinical service formulation (CSF) in fasted conditions (reference) (Treatment B) in treatment period 2 on Day 1. Study intervention intake in subsequent intervention periods in an individual participant will be separated by a washout period of at least 10 days. Receives: Drug: Macitentan |
| Treatment Sequence BA | Experimental | Participants will receive Treatment B in treatment period 1 followed by Treatment A in treatment period 2 on Day 1. Study intervention intake in subsequent intervention periods in an individual participant will be separated by a washout period of at least 10 days. Receives: Drug: Macitentan |
What is being measured
The primary outcome is the main question the study is designed to answer.
Maximum Observed Plasma Analyte Concentration (Cmax) of Macitentan
Cmax is defined as maximum observed plasma analyte concentration of Macitentan.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-time Curve of Macitentan 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 from time zero to time of the last quantifiable (non-below quantification limit [BQL]) concentration, calculated by linear-linear trapezoidal summation.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-time Curve of Macitentan from Time Zero to Infinity (AUC [0-infinity])
AUC (0-infinity) is defined as area under the plasma analyte concentration-time curve of macitentan from time zero to infinite time, calculated as the sum of AUC (0-last) and C(last)/lambda(z), where AUC (0-last) is area under the plasma analyte concentration-time curve from time zero to last measurable concentration, C(last) is the last observed measurable (non-BQL) plasma analyte concentration and lambda(z) is apparent terminal elimination rate constant.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Secondary outcomes (15)
Actual Sampling Time to Reach the Maximum Observed Plasma Analyte Concentration (Tmax) of Macitentan and its Metabolite ACT-132577
Tmax is defined as actual sampling time to reach the maximum observed plasma analyte concentration of macitentan and its metabolite ACT-132577.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Last Observed Measurable Plasma Analyte Concentration (Clast) of Macitentan and its Metabolite ACT-132577
Clast is defined as last observed measurable BQL plasma analyte concentration of macitentan and its metabolite ACT-132577.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-time Curve of Macitentan and its Metabolite ACT-132577 from Time Zero to 72 Hours (AUC [0-72 Hours]) Postdose
AUC (0-72 hours) is defined as area under the plasma analyte concentration-time curve of macitentan and its metabolite ACT-132577 from time zero to 72 hours postdose, calculated by linear-linear trapezoidal summation.
Measured: Predose up to 72 hours post dose
Apparent Terminal Elimination Half-life (t1/2) of Macitentan and its Metabolite ACT-132577
t1/2 of macitentan and its metabolite ACT-132577 is time measured for the plasma analyte concentration to decrease by 1 half to its original concentration. It is associated with the terminal slope of the semi logarithmic drug concentration-time curve, and is calculated as 0.693/lambda(z).
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Apparent Terminal Elimination Rate Constant (Lambda[z]) of Macitentan and its Metabolite ACT-132577
Lambda(z) of macitentan and its metabolite ACT-132577 is defined as apparent terminal elimination rate constant, estimated by linear regression using the terminal log-linear phase of the log transformed concentration versus time curve.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Total Apparent Oral Clearance (CL/F) of Macitentan and its Metabolite ACT-132577
CL/F of macitentan and its metabolite ACT-132577 is defined as total apparent oral clearance, calculated as dose/AUC (0-infinity).
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Apparent Volume of Distribution (Vdz/F) of Macitentan and its Metabolite
Vdz/F of macitentan and its metabolite ACT-132577 is defined as apparent volume of distribution, calculated as dose/(Lambda[z]*AUC [0-infinity]).
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Maximum Observed Plasma Analyte Concentration (Cmax) of Metabolite ACT-132577
Cmax is defined as maximum observed plasma analyte concentration of metabolite ACT-132577.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-Time Curve of Metabolite ACT-132577 from Time Zero to Time of the Last Quantifiable Concentration (AUC [0-last])
AUC (0-last) of metabolite ACT-132577 is defined as area under the plasma analyte concentration-time curve from time zero to time of the last quantifiable (BQL) concentration, calculated by linear-linear trapezoidal summation.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-Time Curve of Metabolite ACT-132577 from Time Zero to Infinity (AUC [0-infinity])
AUC (0-infinity) is defined as area under the plasma analyte concentration-time curve of metabolite ACT-132577 from time zero to infinite time, calculated as the sum of AUC (0-last) and C(last)/lambda(z), where AUC (0-last) is area under the plasma analyte concentration-time curve from time zero to last measurable concentration, C(last) is the last observed measurable (non-BQL) plasma analyte concentration and lambda(z) is apparent terminal elimination rate constant.
Measured: Predose and up to 216 hours post dose (Up to Day 10)
Number of Participants with Adverse Events (AEs) and Serious Adverse Events (SAEs)
AE is any untoward medical occurrence in a clinical study participant administered a pharmaceutical (investigational or non investigational) product. An AE does not necessarily have a causal relationship with the pharmaceutical/biological agent under study. SAE is any untoward medical occurrence that at any dose may results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, is a suspected transmission of any infectious agent via a medicinal product.
Measured: Up to Week 10
Number of Participants with Abnormalities in Physical Examination
Number of participants with abnormalities in physical examination (including general appearance, respiratory, neurological, eyes, ear/nose/throat, thyroid, cardiovascular, abdominal/gastrointestinal, hepatic, musculoskeletal, and dermatologic) will be reported.
Measured: Up to Day 10 of each treatment period (Up to 7 weeks)
Number of Participants with Abnormalities in Vital Signs
Number of participants with abnormalities in vital signs (including temperature [tympanic], pulse rate, and blood pressure) will be reported.
Measured: Up to Day 10 of each treatment period (Up to 7 weeks)
Number of Participants with Abnormalities in Electrocardiograms (ECGs)
Number of participants with abnormalities in ECGs will be reported.
Measured: Up to Day 10 of each treatment period (Up to 7 weeks)
Number of Participants with Abnormalities in Clinical Laboratory Tests
Number of participants with abnormalities in clinical laboratory tests (such as serum chemistry, hematology, and urinalysis) will be reported.
Measured: Up to Day 10 of each treatment period (Up to 7 weeks)
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted15 Jul 2021
- Study start8 Jul 2021
- Primary completion12 Sep 2021
- Study completion5 Oct 2021
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for HealthyStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 16 participants (actual)
Sponsor and investigators
- Lead sponsor
- Actelion
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Actelion Clinical Trial, Study director, Actelion
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT04963439
- Sponsor's protocol ID
- CR109027
- Other IDs
- 2021-001258-67, 67896062PAH1008
- Status last verified
- Mar 2025
- First submitted
- 6 Jul 2021
- Last updated
- 30 Mar 2025
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
- Individual data sharing
- 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
Study at a glance
From the registry record, last updated by the sponsor on 30 Mar 2025. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Single-center, Open-label, Single-dose, Randomized, 2-way Crossover Phase 1 Study in Healthy Adult Participants to Assess the Relative Oral Bioavailability of Two Macitentan Pediatric Formulations
- ClinicalTrials.gov ID
- NCT04963439
- Acronym / sponsor ID
- CR109027
- Conditions
- Healthy
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 16 participants (actual)
- Lead sponsor
- ActelionIndustry (pharma, biotech, devices)
- Study start
- 8 Jul 2021 (actual)
- Primary completion
- 12 Sep 2021 (actual)
- Study completion
- 5 Oct 2021 (actual)
- First posted
- 15 Jul 2021 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The purpose of this study is to assess the rate and extent of absorption of macitentan following administration of a single oral dose of macitentan formulated as final market image (FMI) (test), compared to macitentan as the clinical service formulation (CSF) under fasted conditions in healthy adult participants.
Study design
- Primary purpose
- Other
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| Treatment Sequence AB | Experimental | Drug: MacitentanParticipants will receive single oral dose of macitentan formulated as final market image (FMI) in fasted conditions (test) (Treatment A) in treatment period 1 followed by a single oral dose of macitentan as the clinical service formulation (CSF) in fasted conditions (reference) (Treatment B) in treatment period 2 on Day 1. Study intervention intake in subsequent intervention periods in an individual participant will be separated by a washout period of at least 10 days. |
| Treatment Sequence BA | Experimental | Drug: MacitentanParticipants will receive Treatment B in treatment period 1 followed by Treatment A in treatment period 2 on Day 1. Study intervention intake in subsequent intervention periods in an individual participant will be separated by a washout period of at least 10 days. |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (5 listed)
- Healthy on the basis of physical examination, medical and surgical history collected at screening. If there are abnormalities, the participant may be included only if the investigator judges the abnormalities to be not clinically significant. This determination must be recorded in the participant's source documents and initialed by the investigator
- Systolic blood pressure (SBP) between 100 and 145 millimeters of mercury (mmHg) (inclusive) and diastolic blood pressure (DBP) between 50 and 90 mmHg (inclusive) at screening, preferably measured on the right arm, supine after 5 minutes of rest and standing after 3 minutes
- Twelve-lead electrocardiogram (ECG) with heart rate between 45 and 90 beats per minute (bpm) and without clinically relevant abnormalities, at the discretion of the investigator, measured after the participant is supine for at least 5 minutes, at screening
- Body weight not less than 50.0 kilograms (kg) and body mass index (BMI) between 18.5 and 30.0 kilograms per meter square (kg/m^2) (inclusive)
- All women must have a negative highly sensitive serum (beta-human chorionic gonadotropin [beta- hCG]) pregnancy test at screening and must have a negative urine pregnancy test on Day -1 of each intervention period
Key exclusion criteria (5 listed)
- Known allergies, hypersensitivity, or intolerance to macitentan or drugs of the same class, or any excipients of the drug formulations
- Taken any disallowed therapies, concomitant therapy within 14 days (or longer, based on elimination half-life) before administration of study intervention in the first intervention period
- Received an investigational intervention (including investigational vaccines) or used an invasive investigational medical device within 30 days or 10 half-lives (whichever is longer) before study intervention intake in the first intervention period, or received a biological product within 3 months or 10 half-lives (whichever is longer) before study intervention intake in the first intervention period, or is currently enrolled in an investigational study
- Values of hepatic aminotransferase (alanine aminotransferase and/or aspartate aminotransferase) greater than (>) 1.5 * upper limit of normal at screening
- Positive results from the human immunodeficiency virus (HIV) (type 1 and 2) serology at screening
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| MacitentanAlso: Opsumit, ACT-064992Macitentan dispersible tablets will be administered orally as per assigned treatment sequence. | Drug | Treatment Sequence AB, Treatment Sequence BA |
Primary outcome
Maximum Observed Plasma Analyte Concentration (Cmax) of Macitentan
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Cmax is defined as maximum observed plasma analyte concentration of Macitentan.
Area Under the Plasma Analyte Concentration-time Curve of Macitentan from Time Zero to Time of the Last Quantifiable Concentration (AUC [0-last])
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
AUC (0-last) is defined as area under the plasma analyte concentration-time curve of macitentan from time zero to time of the last quantifiable (non-below quantification limit [BQL]) concentration, calculated by linear-linear trapezoidal summation.
Area Under the Plasma Analyte Concentration-time Curve of Macitentan from Time Zero to Infinity (AUC [0-infinity])
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
AUC (0-infinity) is defined as area under the plasma analyte concentration-time curve of macitentan from time zero to infinite time, calculated as the sum of AUC (0-last) and C(last)/lambda(z), where AUC (0-last) is area under the plasma analyte concentration-time curve from time zero to last measurable concentration, C(last) is the last observed measurable (non-BQL) plasma analyte concentration and lambda(z) is apparent terminal elimination rate constant.
15 secondary outcomes
Actual Sampling Time to Reach the Maximum Observed Plasma Analyte Concentration (Tmax) of Macitentan and its Metabolite ACT-132577
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Last Observed Measurable Plasma Analyte Concentration (Clast) of Macitentan and its Metabolite ACT-132577
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-time Curve of Macitentan and its Metabolite ACT-132577 from Time Zero to 72 Hours (AUC [0-72 Hours]) Postdose
Time frame: Predose up to 72 hours post dose
Apparent Terminal Elimination Half-life (t1/2) of Macitentan and its Metabolite ACT-132577
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Apparent Terminal Elimination Rate Constant (Lambda[z]) of Macitentan and its Metabolite ACT-132577
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Total Apparent Oral Clearance (CL/F) of Macitentan and its Metabolite ACT-132577
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Apparent Volume of Distribution (Vdz/F) of Macitentan and its Metabolite
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Maximum Observed Plasma Analyte Concentration (Cmax) of Metabolite ACT-132577
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-Time Curve of Metabolite ACT-132577 from Time Zero to Time of the Last Quantifiable Concentration (AUC [0-last])
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Area Under the Plasma Analyte Concentration-Time Curve of Metabolite ACT-132577 from Time Zero to Infinity (AUC [0-infinity])
Time frame: Predose and up to 216 hours post dose (Up to Day 10)
Number of Participants with Adverse Events (AEs) and Serious Adverse Events (SAEs)
Time frame: Up to Week 10
Number of Participants with Abnormalities in Physical Examination
Time frame: Up to Day 10 of each treatment period (Up to 7 weeks)
Number of Participants with Abnormalities in Vital Signs
Time frame: Up to Day 10 of each treatment period (Up to 7 weeks)
Number of Participants with Abnormalities in Electrocardiograms (ECGs)
Time frame: Up to Day 10 of each treatment period (Up to 7 weeks)
Number of Participants with Abnormalities in Clinical Laboratory Tests
Time frame: Up to Day 10 of each treatment period (Up to 7 weeks)
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 30 Mar 2025.
- Individual participant dataSharing planned: 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
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Actelion Clinical Trial study director
Actelion
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Macitentan in people with Healthy, run by Actelion at 1 site in Belgium.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 5 inclusion and 5 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 30 Mar 2025. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in Belgium. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Maximum Observed Plasma Analyte Concentration (Cmax) of Macitentan (time frame: Predose and up to 216 hours post dose (Up to Day 10)). The study lists 3 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 30 Mar 2025.