Parkinson Disease
Conditions
Keywords
Parkinson Disease, BIA 9-1067
Brief summary
To determine the absorption, metabolism and excretion of BIA 9-1067.
Detailed description
Monocentre, open, non-placebo-controlled, single-group, single-dose study
Interventions
DRUGBIA 9-1067
90 µCi (3.33 MBq) \[14C\]-labeled of 100 mg BIA 9-1067 (single-dose).
Sponsors
Bial - Portela C S.A.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
40 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy Caucasian male subjects, 40-55 years of age. * Sitting blood pressure and pulse rate within a clinically acceptable range for the purposes of the study, i.e.: BP: 100 - 160 mmHg systolic, 50 - 95 mmHg diastolic and pulse rate: 50 - 100 bpm. Blood pressure and pulse were to be measured after 3 minutes resting in a sitting position. * Subject body mass index was to be between 18 and 28 kg/m2 * Normal 12-lead ECG * Ability to communicate well with the investigator and comply with the requirements of the entire study. * The subject had given his written informed consent to participate in the study.
Exclusion criteria
* History of serious adverse reactions or hypersensitivity to any drug. * Presence or history of allergies requiring acute or chronic treatment (except seasonal allergic rhinitis). * History of alcohol or drug abuse in the last 5 years. * Abnormal physical findings of clinical significance at the screening examination or baseline which would interfere with the objectives of the study. * Need of any prescription medication within 14 days prior to the administration of the drug and/or nonprescription medication within 7 days prior to the administration of the drug. * Participation in other clinical trials during the previous month in which an investigational drug or a commercially available drug was tested. * Loss of 500 mL blood or more during the 3 month period before the study, e.g., as a donor. * Existence of any surgical or medical condition which might interfere with the absorption, distribution, metabolism or excretion of the drug, i.e., impaired renal or hepatic function, diabetes mellitus, cardiovascular abnormalities, chronic symptoms of pronounced constipation or diarrhoea or conditions associated with total or partial obstruction of the urinary tract. * Symptoms of a significant somatic or mental illness in the 4 week period preceding drug administration. * History of hepatitis B and / or C and / or positive serology results which indicate the presence of hepatitis B and / or C. * Positive results from the HIV serology. * Clinically significant abnormal laboratory values (as determined by the Principal Investigator) at the screening evaluation, however, liver parameters (SGPT, SGOT) values must be within the normal range. * Positive results of the drug screening. * Known hypersensitivity to BIA 9-1067. * Heavy smokers, i.e., more than 10 cigarettes per day * Exposure to artificial ionizing radiation in the last 12 months (e.g., x-ray investigation) * Subject who had more than 4 flights (with more than 2 hours flight time) within the last year prior to the administration of the drug.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Plasma Concentration (Cmax) | 24 hours:pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose | Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Time to Reach Maximum Plasma Concentration (Tmax) | 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose | Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites |
| Area Under the Plasma-concentration Time Curve Until the Last Quantifiable Sampling Point (AUC0-t) | 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose | Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites |
| Area Under the Plasma-concentration Time Curve With Extrapolation to Infinity (AUC0-∞) | 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose | Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites |
Countries
Switzerland
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| BIA 9-1067 90 µCi (3.33 MBq) \[14C\]-labeled of 100 mg BIA 9-1067 (single-dose).
BIA 9-1067: 90 µCi (3.33 MBq) \[14C\]-labeled of 100 mg BIA 9-1067 (single-dose). | 4 |
| Total | 4 |
Baseline characteristics
| Characteristic | BIA 9-1067 |
|---|---|
| Age, Categorical <=18 years | 0 Participants |
| Age, Categorical >=65 years | 0 Participants |
| Age, Categorical Between 18 and 65 years | 4 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 4 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | — / — |
| other Total, other adverse events | 3 / 4 |
| serious Total, serious adverse events | 0 / 4 |
Outcome results
Primary
Maximum Plasma Concentration (Cmax)
Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites
Time frame: 24 hours:pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| BIA 9-1067 | Maximum Plasma Concentration (Cmax) | 482.98 ng-eq/mL | Standard Deviation 265.26 |
Secondary
Area Under the Plasma-concentration Time Curve Until the Last Quantifiable Sampling Point (AUC0-t)
Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites
Time frame: 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| BIA 9-1067 | Area Under the Plasma-concentration Time Curve Until the Last Quantifiable Sampling Point (AUC0-t) | 14038.27 h⋅ng-eq/mL | Standard Deviation 4823.78 |
Secondary
Area Under the Plasma-concentration Time Curve With Extrapolation to Infinity (AUC0-∞)
Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites
Time frame: 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| BIA 9-1067 | Area Under the Plasma-concentration Time Curve With Extrapolation to Infinity (AUC0-∞) | 33441.69 h⋅ng-eq/mL | Standard Deviation 14069.06 |
Secondary
Time to Reach Maximum Plasma Concentration (Tmax)
Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites
Time frame: 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| BIA 9-1067 | Time to Reach Maximum Plasma Concentration (Tmax) | 1.69 hours | Standard Deviation 0.75 |