Chronic Obstructive Pulmonary Disease
Conditions
Keywords
Pharmacokinetic, Roflumilast
Brief summary
The primary objective is to assess the pharmacokinetics (PK) of roflumilast and its metabolite roflumilast N-oxide after single and repeated oral administrations of roflumilast 500 μg in healthy Chinese subjects.
Interventions
DRUGRoflumilast
Period I: single dose of roflumilast 500 μg orally in the morning. Period II: repeated dose of roflumilast 500 μg orally in the morning for 14 days.
Sponsors
AstraZeneca
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
40 Years to No maximum
Healthy volunteers
No
Inclusion criteria
Main Inclusion Criteria: * Healthy male and female (24 male and 8 female) subjects of Chinese ethnic origin, age 40 years and older. * Assessed as healthy based on a screening examination including medical history, physical examination, blood pressure, pulse rate, ECG assessment, and clinical laboratory results. * Body weight according to a Body Mass Index (BMI) between 19 and 28 kg/\[m²\], (both inclusive) and a body weight ≥ 50 kg. * Females with childbearing potential who are using medically acceptable and reliable method of contraception for the entire study duration, such as tubal ligation, hysterectomy, intrauterine device without hormones or post-menopausal females, the latter is defined as females who have had no menstrual period for at least 2 years. Main
Exclusion criteria
* History or current evidence of clinically relevant allergies or idiosyncrasy to drugs or food * History of allergic reactions to roflumilast or any inactive ingredients of the trial medication * History or current evidence of any clinically relevant cardiovascular, pulmonary, hepatic, renal, gastrointestinal, hematological, endocrinological, metabolic, neurological, psychiatric, or other disease (within the last 2 years) * History of malignancy within the past 5 years * Electrocardiogram (ECG) abnormalities of clinical relevance (e.g. QTc according to Bazett's formula: QTc \> 450 msec (male), QTc \> 470 msec (female), PQ ≥ 220 msec) * Blood pressure ≥ 140 mm HG systolic or ≥ 90 mm HG diastolic * Elevated transaminases \> 2 x upper Limit of normal range and or increased of the total bilirubin \> 1.5 upper Limit of normal range * Clinically relevant abnormalities in clinical chemical, hematological or any other laboratory variables * Chronic or clinically relevant acute infections * Proneness to orthostatic dysregulation, faintings, or blackouts * Positive results in any of the virology tests of acute or chronic infectious HIV and hepatitis A, B, and C virus infections * Positive drug screen * Abuse of alcohol or drugs * Positive β-HCG pregnancy test (female) * Pregnant or lactating females
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| To determine the pharmacokinetic profiles after single and repeated dose of roflumilast 500 µg administered to healthy Chinese subjects. | Period I: single dose, PK-Investigation over 8 days, Period II: repeated dose for 14 days, PK-Investigation on days 14 and 15 | PK samples at pre-dose, 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 16h and 24h, 36h, 48h, 72h, 96h, 120h, 144h and 168h post dose after single dose and at the time points pre-dose, 0.25h, 0.5h, 0.75h, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 16h and 24h after administration of a repeated dose |
Secondary
| Measure | Time frame |
|---|---|
| The safety and tolerability of single and repeated dose roflumilast 500 µg will be evaluated in terms of adverse event, ECG, blood pressure, pulse rate, and clinical laboratory tests. | During screening, clinical part and final check |
Countries
China
Outcome results
None listed