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Completed

NCT Number: NCT05433675

A Study of Two Macitentan Formulations in Healthy Adult Participants

The purpose of this study is to evaluate the bioequivalence of macitentan on the primary pharmacokinetics (PK) parameters between the dispersible final market image (FMI) macitentan tablet and the opsumit tablet in healthy adult participants in fasted conditions.

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Key information

Conditions

Healthy

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

SGS Belgium NV

Edegem, 2650, Belgium

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Healthy on the basis of physical examination, medical and surgical history performed at screening. If there are any abnormalities, they must be considered not clinically relevant and this determination must be recorded in the participant's source documents and initialed by the investigator
  • Body weight not less than 50 kilograms (kg) and body mass index (BMI) within the range 18.5 - 30.0 kilogram per meter square (kg/m^2)(inclusive), at screening
  • 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
  • A woman must agree not to donate eggs (ova, oocytes) for the purposes of assisted reproduction during the study and for a period of 30 days after the last study intervention intake
  • Must sign an ICF indicating that the participant understands the purpose of, and procedures required for, the study and is willing to participate in the study, before starting any screening activities

Exclusion criteria

  • Known allergies, hypersensitivity, or intolerance to macitentan, fructose or drugs of the same class, or any excipients of the drug formulations
  • History or clinical evidence of any disease or existence of any surgical or medical condition which might interfere with the absorption, distribution, metabolism, or excretion of the study intervention (appendectomy and herniotomy allowed, cholecystectomy not allowed)
  • A history of repeated fainting due to cardiac cause, collapse, syncope, orthostatic hypotension, or vasovagal reactions
  • Veins unsuitable for intravenous puncture on either arm (example, veins that are difficult to locate, access, or puncture, and veins with a tendency to rupture during or after puncture)
  • Woman who is breastfeeding/pregnant at screening or plans to breastfeed/become pregnant throughout the study until 30 days after last study intervention intake

Treatment and study plan

Macitentan

Drug

Macitentan dispersible and film-coated tablets will be administered orally as per assigned treatment sequence.

Other names: Opsumit, ACT-064992, JNJ-67896062

Primary outcomes

  1. Maximum Observed Plasma Analyte Concentration (Cmax) of Macitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    Cmax is defined as maximum observed plasma analyte concentration of macitentan.

  2. Area Under the Plasma Analyte Concentration Versus Time Curve From Time Zero To Time of the Last Quantifiable (Non-below Quantification Limit [Non-BQL]) Concentration (AUC [0-last]) of Macitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    AUC (0-last) is defined as area under the plasma analyte concentration versus time curve from time 0 to time of the last quantifiable (non-BQL) concentration of macitentan.

  3. Area Under the Plasma Analyte Concentration-time Curve From Time Zero to Infinite Time (AUC[0-infinity]) of Macitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    AUC (0-infinity) is defined as the area under the plasma analyte concentration-time curve from time 0 to infinite time of macitentan, calculated as the summation of AUC(0-last) and C(last)/lambda(z); where AUC(0-last) is area under the analyte concentration-time curve from time zero to last quantifiable time, Clast is the last observed measurable (non-BQL) plasma analyte concentration, and lambda(z) is apparent terminal elimination rate constant.

Secondary outcomes

  1. Actual Sampling Time to Reach the Maximum Observed Plasma Analyte Concentration (Tmax) of Macitentan and Aprocitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    Tmax is defined as actual sampling time to reach the maximum observed plasma analyte concentration of macitentan and aprocitentan.

  2. Last Observed Measurable (Non-BQL) Plasma Analyte Concentration (Clast) of Macitentan and Aprocitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    Clast is defined as last observed measurable (non-BQL) plasma analyte concentration of macitentan and aprocitentan.

  3. Area Under the Plasma Analyte Concentration-time Curve from Time Zero to 72 Hours Postdose (AUC [0-72 Hours]) of Macitentan and Aprocitentan

    Time frame: Predose up to 0 to 72 hours postdose (up to Day 4)

    AUC (0-72 hours) is defined as area under the plasma analyte concentration-time curve from time 0 to 72 hours postdose of macitentan and aprocitentan calculated by linear-linear trapezoidal summation.

  4. Apparent Terminal Elimination Half-life (t1/2) of Macitentan and Aprocitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    t1/2 is defined as apparent terminal elimination half-life of macitentan and aprocitentan, calculated as 0.693/lambda(z); where lambda(z) is apparent terminal elimination rate constant.

  5. Apparent Terminal Elimination Rate Constant (Lambda[z]) of Macitentan and Aprocitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    Lambda(z) is defined as apparent terminal elimination rate constant of macitentan and aprocitentan, estimated by linear regression using the terminal log-linear phase of the log transformed concentration versus time curve.

  6. Total Apparent Oral Clearance (CL/F) of Macitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    CL/F is defined as total apparent oral clearance of macitentan, calculated as dose/AUC (0-infinity).

  7. Apparent Volume of Distribution (Vdz/F) of Macitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    Vdz/F of macitentan is defined as apparent volume of distribution of macitentan, calculated as dose/(Lambda[z]*AUC [0-infinity]).

  8. Maximum Observed Plasma Analyte Concentration (Cmax) of Aprocitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    Cmax is defined as maximum observed plasma analyte concentration of aprocitentan.

  9. Area Under the Plasma Analyte Concentration Versus Time Curve From Time Zero To Time of the Last Quantifiable (Non-BQL) Concentration (AUC [0-last]) of Aprocitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    AUC (0-last) is defined as area under the plasma analyte concentration versus time curve from time 0 to time of the last quantifiable (non-BQL) concentration of aprocitentan.

  10. Area Under the Plasma Analyte Concentration-time Curve From Time Zero to Infinite Time (AUC [0-infinity]) of Aprocitentan

    Time frame: Predose up to 216 hours postdose (up to Day 10)

    AUC (0-infinity) is defined as the area under the plasma analyte concentration-time curve from time 0 to infinite time of aprocitentan, calculated as the summation of AUC(0-last) and C(last)/lambda(z); where AUC(0-last) is area under the analyte concentration-time curve from time zero to last quantifiable time, Clast is the last observed measurable (non-BQL) plasma analyte concentration, and lambda(z) is apparent terminal elimination rate constant.

  11. Number of Participants with Serious Adverse Events (SAEs)

    Time frame: From screening to the last follow-up visit (up to 10 weeks)

    An SAE is defined as any untoward medical occurrence that results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, leads to a congenital anomaly/birth defect in the offspring of a participant, or is an important medical event. An adverse event (AE) is any untoward medical occurrence in a clinical study participant administered a pharmaceutical (investigational or non investigational) product.

  12. Number of Participants with Abnormalities in Physical Examination

    Time frame: Up to Day 10

    Number of participants with abnormalities in physical examination (including height and body weight) will be reported.

  13. Number of Participants with Abnormalities in Vital Signs

    Time frame: Up to Day 10

    Number of participants with abnormalities in vital signs (including blood pressure, pulse/heart rate and oral temperature) will be reported.

  14. Number of Participants with Abnormalities in Electrocardiogram (ECG)

    Time frame: Up to Day 10

    Number of participants with abnormalities in ECG will be reported.

  15. Number of Participants with Abnormalities in Clinical Laboratory Tests

    Time frame: Up to Day 10

    Number of participants with abnormalities in clinical laboratory tests (including hematology, serum chemistry, coagulation, serology and urinalysis) will be reported.

Sponsors and collaborators

Lead sponsor

Actelion

Industry

Registry information

Official study title

A Single-center, Open-label, Single-dose, Randomized, 2-way Crossover Phase 1 Study in Healthy Adult Participants to Assess the Bioequivalence of the Dispersible Final Market Image (FMI) Macitentan Tablet (4 x 2.5 mg) and the Opsumit Tablet (10 mg) in Fasted Conditions

Important dates

Study start
2022
Primary completion
2022
Study completion
2022
First posted
Jun 27, 2022
Registry last updated
Mar 30, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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