Parkinson
Conditions
Keywords
Opicapone,, Parkinson,, Bial,, BIA 9-1067
Brief summary
The objectives of this study were to characterize the effects of food on the pharmacokinetics (PK) and tolerability of BIA 9-1067 in healthy male subjects.
Detailed description
Methodology: Single center, randomized, single dose, open-label, 2-period, 2-sequence, crossover study.
Interventions
DRUGBIA 9-1067
A single oral dose of 50 mg (2 x 25 mg capsules) was administered in the morning of each study period under fasting or fed conditions. The two single dose administrations were separated by a wash-out of 7 days.
Sponsors
Bial - Portela C S.A.
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Availability for the entire study period and willingness to adhere to the protocol requirements as evidenced by the informed consent form (ICF) duly read, signed and dated by the volunteer * Male volunteer * Volunteer aged of at least 18 years but not older than 45 years * Volunteer with a body mass index (BMI) greater than or equal to 18.5 and below 30 kg/m2 * Clinical laboratory values within the laboratory's stated normal range; if not within this range, they must be without any clinical significance * Healthy according to the medical history, laboratory results and physical examination * Light-, non- or ex-smokers. A light smoker is defined as someone smoking 10 cigarettes or less per day for at least 3 months before day 1 of this study. An ex-smoker is defined as someone who completely stopped smoking for at least 12 months before day 1 of this study * The informed consent form must be signed by all volunteers, prior to their participation in the study.
Exclusion criteria
* Volunteers presenting any of the following will not be included in the study:Significant history of hypersensitivity to any catechol-structured drugs (e.g. rimiterole, isoprenaline, adrenaline, noradrenaline, dopamine, dopexamine or dobutamide) or any related products (including excipients of the formulations) as well as severe hypersensitivity reactions (like angioedema) to any drugs * Presence of significant gastrointestinal, liver or kidney disease, or any other conditions known to interfere with the absorption, distribution, metabolism or excretion of drugs or known to potentiate or predispose to undesired effects * History of significant gastrointestinal, liver or kidney disease that may affect drug bioavailability * Presence or history of significant cardiovascular, pulmonary, hematologic, neurologic, psychiatric, endocrine, immunologic, dermatologic or connective tissue disease * Suicidal tendency, history of or disposition to seizures, state of confusion, clinically relevant psychiatric diseases * Presence of significant heart disease or disorder according to ECG * Previous history of Neuroleptic Malignant Syndrome (NMS) and/or nontraumatic rhabdomyolysis * Pheochromocytoma due to the increased risk of hypertensive crisis * Use of MAO inhibitors within 14 days of day 1 of the study * Maintenance therapy with any drug, or significant history of drug dependency or alcohol abuse (\> 3 units of alcohol per day, intake of excessive alcohol, acute or chronic) * Any clinically significant illness in the previous 28 days before day 1 of this study * Use of any enzyme-modifying drugs, including strong inhibitors of cytochrome P450 (CYP) enzymes (such as cimetidine, fluoxetine, quinidine, erythromycin, ciprofloxacin, fluconazole, ketoconazole, diltiazem and HIV antivirals) and strong inducers of CYP enzymes (such as barbiturates, carbamazepine, glucocorticoids, phenytoin and rifampin), in the previous 28 days before day 1 of this study * Volunteers who took an Investigational Product (in another clinical trial) or donated 50 mL or more of blood in the previous 28 days before day 1 of this study * Poor motivation, intellectual problems likely to limit the validity of consent to participate in the study or limit the ability to comply with the protocol requirements or inability to cooperate adequately, inability to understand and to observe the instructions of the physician * Donation of 500 mL or more of blood (Canadian Blood Services, Hema-Quebec, clinical studies, etc.) in the previous 56 days before day 1 of this study * Positive urine screening of drugs of abuse * Any history of tuberculosis and/or prophylaxis for tuberculosis * Positive results to HIV, HBsAg or anti-HCV tests
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Cmax - Maximum Observed Plasma Concentration | Day 1 | Cmax - Maximum observed plasma concentration of BIA 9-1067 |
| AUCt - Cumulative Area Under the Plasma Concentration Time Curve | Day 1 | AUCt - Cumulative Area Under the plasma concentration time Curve for BIA 9-1067 |
| Area Under the Concentration-time Curve Extrapolated to Infinity (AUC∞) | Day 1 | Area Under the Concentration-time Curve Extrapolated to Infinity (AUC∞) for BIA 9-1067 |
Countries
Canada
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Group A Fed/Fasted A single 50 mg dose of BIA 9-1067 (2 x 25 mg capsules) was to be administered on:
Period 1: Fed Washout Period (7days) Period 2: Fasted
BIA 9-1067: A single oral dose of 50 mg (2 x 25 mg capsules) was administered in the morning of each study period under fasting or fed conditions. The two single dose administrations were separated by a wash-out of 7 days. | 6 |
| Group B Fasted/Fed A single 50 mg dose of BIA 9-1067 (2 x 25 mg capsules) was to be administered on:
Period 1: Fasted Washout Period (7days) Period 2: Fed
BIA 9-1067: A single oral dose of 50 mg (2 x 25 mg capsules) was administered in the morning of each study period under fasting or fed conditions. The two single dose administrations were separated by a wash-out of 7 days. | 6 |
| Total | 12 |
Baseline characteristics
| Characteristic | Group A Fed/Fasted | Group B Fasted/Fed | Total |
|---|---|---|---|
| Age, Categorical <=18 years | 0 Participants | 0 Participants | 0 Participants |
| Age, Categorical >=65 years | 0 Participants | 0 Participants | 0 Participants |
| Age, Categorical Between 18 and 65 years | 6 Participants | 6 Participants | 12 Participants |
| Sex: Female, Male Female | 0 Participants | 0 Participants | 0 Participants |
| Sex: Female, Male Male | 6 Participants | 6 Participants | 12 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — |
| other Total, other adverse events | 3 / 11 | 4 / 12 |
| serious Total, serious adverse events | 0 / 11 | 0 / 12 |
Outcome results
Primary
Area Under the Concentration-time Curve Extrapolated to Infinity (AUC∞)
Area Under the Concentration-time Curve Extrapolated to Infinity (AUC∞) for BIA 9-1067
Time frame: Day 1
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Fasted Conditions | Area Under the Concentration-time Curve Extrapolated to Infinity (AUC∞) | 2113.6 ng·h/mL | Standard Deviation 915.2 |
| Fed Condition | Area Under the Concentration-time Curve Extrapolated to Infinity (AUC∞) | 1027.2 ng·h/mL | Standard Deviation 545.4 |
Primary
AUCt - Cumulative Area Under the Plasma Concentration Time Curve
AUCt - Cumulative Area Under the plasma concentration time Curve for BIA 9-1067
Time frame: Day 1
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Fasted Conditions | AUCt - Cumulative Area Under the Plasma Concentration Time Curve | 879.2 ng·h/mL | Standard Deviation 286.6 |
| Fed Condition | AUCt - Cumulative Area Under the Plasma Concentration Time Curve | 1989.5 ng·h/mL | Standard Deviation 984.8 |
Primary
Cmax - Maximum Observed Plasma Concentration
Cmax - Maximum observed plasma concentration of BIA 9-1067
Time frame: Day 1
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Fasted Conditions | Cmax - Maximum Observed Plasma Concentration | 635.0 ng/mL | Standard Deviation 250.8 |
| Fed Condition | Cmax - Maximum Observed Plasma Concentration | 238.2 ng/mL | Standard Deviation 168.4 |