A Study of Macitentan in Healthy Chinese Adult Male Participants
Study Details
Study Description
Brief Summary
The purpose of this study is to assess what macitentan and its active metabolite (aprocitentan) does to the body after single dose administration of macitentan in Chinese healthy adult male participants.
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
|
Phase 1 |
Study Design
Arms and Interventions
| Arm | Intervention/Treatment |
|---|---|
| Experimental: Macitentan 75 milligrams (mg) Healthy participants will receive a single-dose of macitentan 75 mg tablet on Day 1 under fed condition. |
Drug: Macitentan
Macitentan tablet will be administered orally.
Other Names:
|
| Experimental: Placebo Healthy participants will receive matching placebo tablet on Day 1 under fed condition. |
Drug: Placebo
Placebo will be administered orally.
|
Outcome Measures
Primary Outcome Measures
- Maximum Observed Plasma Concentration (Cmax) of Macitentan and Aprocitentan [Pre dose up to 336 hours post dose on Day 1]
Cmax is the maximum observed plasma concentration of macitentan and aprocitentan.
- Time to Maximum Observed Plasma Concentration (Tmax) of Macitentan and Aprocitentan [Pre dose up to 336 hours post dose on Day 1]
Tmax is the time to reach maximum observed plasma concentration of macitentan and aprocitentan.
- Area Under the Plasma Concentration Time Curve from Time Zero to Time of the Last Quantifiable Concentration (AUC [0-Last]) of Macitentan and Aprocitentan [Pre dose up to 336 hours post dose on Day 1]
AUC (0-Last) is the area under the plasma concentration time curve from time 0 to time of the last measurable concentration of macitentan and aprocitentan.
- Area Under the Plasma Concentration Time Curve from Time Zero to Infinite time (AUC [0-Infinity]) of Macitentan and Aprocitentan [Pre dose up to 336 hours post dose on Day 1]
AUC (0-Infinity) is the area under the plasma concentration time curve from time 0 to infinite time of macitentan and aprocitentan.
- Apparent Elimination Half-Life (t1/2) of Macitentan and Aprocitentan [Pre dose up to 336 hours post dose on Day 1]
t1/2 is the apparent elimination half-life associated with the terminal slope of the semilogarithmic drug concentration-time curve of macitentan and aprocitentan.
- Total Systemic Clearance (CL/F) of Macitentan and Aprocitentan [Pre dose up to 336 hours post dose on Day 1]
CL/F is the total systemic clearance following single-dose extravascular administration of macitentan and aprocitentan.
- Apparent Volume of Distribution (Vz/F) of Macitentan and Aprocitentan [Pre dose up to 336 hours post dose on Day 1]
Vz/F is the apparent volume of distribution based on terminal phase of macitentan and aprocitentan.
- Number of Participants with Adverse Events (AEs) [Up to 9 weeks]
An 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 causal relationship with the intervention.
- Number of Participants with Adverse Events of Special Interest (AESI) [Up to 9 weeks]
Number of participants with AESIs will be reported. AESIs includes hypotension, anemia, edema, and liver events.
- Number of Participants with Serious Adverse Events (SAEs) [Up to 9 weeks]
Number of participants with SAEs will be reported. A SAE is any AE that results in: death, persistent or significant disability/incapacity, requires inpatient hospitalization or prolongation of existing hospitalization, is life-threatening experience, is a congenital anomaly/birth defect, is suspected transmission of any infectious agent via a medicinal product, is medically important to prevent one of the outcomes listed above.
- Number of Participants with Clinical Laboratory Tests Abnormalities [Up to 9 weeks]
Number of participants with clinical laboratory tests (including serum chemistry, hematology, and urinalysis) abnormalities will be reported.
- Number of Participants with Vital Signs Abnormalities [Up to 9 weeks]
Number of participants with vital signs (blood pressure, pulse rate, respiratory rate, and temperature [ear or axillary]) abnormalities will be reported.
- Number of Participants with 12-lead Electrocardiogram (ECG) Abnormalities [Up to 9 weeks]
Number of participants with 12-lead ECG abnormalities will be reported.
- Number of Participants with Physical Examinations Abnormalities [Up to 9 weeks]
Number of participants with physical examinations abnormalities will be reported.
Eligibility Criteria
Criteria
Inclusion Criteria:
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Chinese Male
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Be health medically stable on the basis of physical examination, medical history, vital signs, 12-lead electrocardiograms (ECG) 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
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Be healthy on the basis of clinical laboratory tests performed at screening. If the results of the serum chemistry panel, hematology, or urinalysis are outside the normal reference ranges, the participant may be included only if the investigator judges the abnormalities or deviations from normal to be not clinically significant. This determination must be recorded in the participant's source documents and initialed by the investigator
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Body mass index (weight /height2) between 18.0 and 27.9 kilograms per meter square (kg/m2) (inclusive), and body weight not less than 50.0 kg
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Systolic blood pressure (BP) was between 100 and 140 millimeter of mercury (mmHg) and for diastolic BP - between 60 and 90 mmHg (after the participant is supine for 5 minutes and including boundary values)
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A 12-lead ECG consistent with normal cardiac conduction and function
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A participant must agree not to donate sperm for the purpose of reproduction during the study and for a minimum 90 days after receiving the last dose of study intervention
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Must sign an ICF indicating that he understands the purpose of, and procedures required for the study and is willing to participate in the study
Exclusion Criteria:
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History of or current clinically significant medical illness including (but not limited to) cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders (including any abnormal bleeding or blood dyscrasias), lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, hepatic or renal insufficiency (creatinine clearance below 80 milliliters per minute (mL/min) calculated using Cockcroft-Gault equation), thyroid disease, neurologic or psychiatric disease, infection, or any other illness that the investigator considers should exclude the participant or that could interfere with the interpretation of the study results
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Clinically significant abnormal physical examination, vital signs, or 12-lead ECG at screening or at admission to the study site as deemed appropriate by the investigator
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One or more of the following laboratory abnormalities at screening, defined as Grade 1 or more by the World Health Organisation (WHO )Toxicity Grading Scale for Determining the Severity of Adverse Events, February 2003: aspartate aminotransferase (AST) or alanine transaminase (ALT) greater than or equal to (>=)1.25x upper limit of normal (ULN); Total bilirubin >=1.25x ULN; Hemoglobin less than or equal to (<=)11 grams per deciliter (g/dL)
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History of malignancy within 5 years before screening (exceptions are squamous and basal cell carcinomas of the skin or malignancy, which is considered cured with minimal risk of recurrence)
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Known allergies, hypersensitivity, or intolerance to macitentan or its excipients
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Use of any prescription or nonprescription medication (including vitamins and herbal supplements), except for acetaminophen within 14 days before the first dose of the study intervention is scheduled until completion of the study
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | Peking University Third Hospital | Beijing | China | 100191 |
Sponsors and Collaborators
- Actelion
Investigators
- Study Director: Actelion Clinical Trial, Actelion
Study Documents (Full-Text)
None provided.More Information
Publications
None provided.- CR109324
- 67896062PAH1009