An Open-label Study in Healthy Male Subjects to Assess the Absorption, Distribution, Metabolism and Excretion of [14C]-Labelled BIA 9-1067 and Metabolites
Primary Purpose
Parkinson's Disease (PD)
Status
Completed
Phase
Phase 1
Locations
Netherlands
Study Type
Interventional
Intervention
OPC
Sponsored by
About this trial
This is an interventional treatment trial for Parkinson's Disease (PD) focused on measuring Parkinson's disease (PD), BIA 9-1067, Opicapone
Eligibility Criteria
Inclusion Criteria:
- Gender: male
- Age: 18 - 55 years, inclusive
- Body Mass Index (BMI): 18.0 - 30.0 kg/m2, inclusive Body weight (kg)and height2 (m2)
- Ability and willingness to abstain from alcohol, methylxanthine-containing beverages or food (coffee, tea, cola, chocolate, "powerdrinks") and grapefruit (juice) from 48 hours prior to entry in the clinical research centre until discharge
- Medical history without major pathology
- Resting supine blood pressure and a resting pulse rate showing no clinically relevant deviations as judged by the MI
- Computerised (12-lead) electrocardiogram (ECG) recording without signs of clinically relevant pathology or showing no clinically relevant deviations as judged by the MI
- Willingness to use adequate contraception from the time of dosing until 3 months after the follow-up visit
- All values for haematology and for clinical chemistry tests of blood and urine within the normal range or showing no clinically relevant deviations as judged by the MI
- Willingness to sign the written ICF
Exclusion Criteria:
- Evidence of clinically relevant pathology
- Mental handicap
- History of relevant drug and/or food allergies
- Regular/routine treatment with non-topical medications within 30 days prior to entrance into the clinical research centre
- Smoking (less than 60 days prior to drug administration)
- History of alcohol abuse or drug addiction (including soft drugs like cannabis products)
- Use of concomitant medication, except for acetaminophen (paracetamol), which was allowed up to 3 days before entrance into the clinical research centre. Multivitamins and vitamin C were allowed up to 7 days before entrance into the clinical research centre. All other medication (including over the counter medication, health supplements, and herbal remedies such as St. John's wort extract) was to be stopped at least 14 days prior to entrance into the clinical research centre
- Participation in a drug study within 60 days prior to drug administration. Participation in more than 3 other drug studies in the 10 months preceding administration of study drug
- Donation of more than 50 mL of blood within 60 days prior to drug administration. Donation of more than 1.5 litres of blood in the 10 months preceding administration of study drug
- Participation in another ADME study with a radiation burden -0.1 mSv in the period of 1 year before the start of the study
- Exposure to radiation for diagnostic reasons (except dental X-rays and plain X rays of thorax and bony skeleton - excluding spinal column), during work or during participation in a medical study in the previous year
- Irregular defecation pattern (less than once per 2 days)
- Positive screen on drugs of abuse (opiates, methadone, cocaine, amphetamines, cannabinoids, barbiturates, benzodiazepines, tricyclic antidepressants and alcohol)
- Intake of more than 24 units of alcohol per week (1 unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 mL of spirits)
- Positive screen on hepatitis B surface antigen (HBsAg)
- Positive screen on anti-hepatitis C virus (HCV)
- Positive screen on anti- human immunodeficiency virus (HIV) 1/2
- Illness within 5 days prior to drug administration
Sites / Locations
- PRA
Arms of the Study
Arm 1
Arm Type
Experimental
Arm Label
Opicapone (OPC)
Arm Description
100 mg OPC
Outcomes
Primary Outcome Measures
Cumulative Recovery of [14C]-Radioactivity
AEurine: Cumulative Recovery of [14C]-Radioactivity in urine AEfaeces: Cumulative Recovery of [14C]-Radioactivity in urine AEair: Cumulative Recovery of [14C]-Radioactivity in urine AEtotal: Cumulative Recovery of [14C]-Radioactivity in urine
Recovery % of dose has been derived from area under the excretion rate (to infinity) from 240h onwards
Secondary Outcome Measures
Cmax - Maximum Concentration
BIA 9-1103 is a Opicapone (OPC, BIA 9-1067) metabolite
Tmax - Time to Attain Maximum Concentration
BIA 9-1103 is a Opicapone (OPC, BIA 9-1067) metabolite
Full Information
1. Study Identification
Unique Protocol Identification Number
NCT02169427
Brief Title
An Open-label Study in Healthy Male Subjects to Assess the Absorption, Distribution, Metabolism and Excretion of [14C]-Labelled BIA 9-1067 and Metabolites
Official Title
An Open-label Study in Healthy Male Subjects to Assess the Absorption, Distribution, Metabolism and Excretion of [14C]-Labelled BIA 9-1067 and Metabolites Following a Single Dose Oral Administration
Study Type
Interventional
2. Study Status
Record Verification Date
July 2015
Overall Recruitment Status
Completed
Study Start Date
March 2011 (undefined)
Primary Completion Date
July 2011 (Actual)
Study Completion Date
July 2011 (Actual)
3. Sponsor/Collaborators
Responsible Party, by Official Title
Sponsor
Name of the Sponsor
Bial - Portela C S.A.
4. Oversight
Data Monitoring Committee
No
5. Study Description
Brief Summary
The purpose of this study is to determine the rate and routes of excretion of OPC and the mass balance in urine, faeces and expired air.
Detailed Description
This was a single-centre, open-label ADME study in 6 healthy male subjects. Subjects received a single dose of 100 mg OPC, containing 3.39 MBq of [14C] OPC as oral capsules.
The study consisted of an eligibility screening period within 3 weeks prior to drug administration, admission on Day -1, a treatment period involving drug administration on Day 1 followed by matrix collections for PK purposes and safety evaluations up to Day 11, discharge on Day 11, six 24-hour hospitalizations on Days 14/15, 21/22 (+/ 1 day), 28/29 (+/- 1 day), 42/43 (+/- 2 days), 56/57 (+/- 2 days) and 77/78 (+/ 3 days) for PK sample collections, and a follow up visit performed at least 14 days after discharge from the last 24-hour hospitalization or at early discontinuation.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
Parkinson's Disease (PD)
Keywords
Parkinson's disease (PD), BIA 9-1067, Opicapone
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 1
Interventional Study Model
Single Group Assignment
Masking
None (Open Label)
Allocation
N/A
Enrollment
6 (Actual)
8. Arms, Groups, and Interventions
Arm Title
Opicapone (OPC)
Arm Type
Experimental
Arm Description
100 mg OPC
Intervention Type
Drug
Intervention Name(s)
OPC
Other Intervention Name(s)
BIA 9-1067
Intervention Description
The drug substance of 100 mg OPC was administered as 1 capsule.
Primary Outcome Measure Information:
Title
Cumulative Recovery of [14C]-Radioactivity
Description
AEurine: Cumulative Recovery of [14C]-Radioactivity in urine AEfaeces: Cumulative Recovery of [14C]-Radioactivity in urine AEair: Cumulative Recovery of [14C]-Radioactivity in urine AEtotal: Cumulative Recovery of [14C]-Radioactivity in urine
Recovery % of dose has been derived from area under the excretion rate (to infinity) from 240h onwards
Time Frame
pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29
Secondary Outcome Measure Information:
Title
Cmax - Maximum Concentration
Description
BIA 9-1103 is a Opicapone (OPC, BIA 9-1067) metabolite
Time Frame
pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29
Title
Tmax - Time to Attain Maximum Concentration
Description
BIA 9-1103 is a Opicapone (OPC, BIA 9-1067) metabolite
Time Frame
pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29
10. Eligibility
Sex
Male
Minimum Age & Unit of Time
18 Years
Maximum Age & Unit of Time
55 Years
Accepts Healthy Volunteers
Accepts Healthy Volunteers
Eligibility Criteria
Inclusion Criteria:
Gender: male
Age: 18 - 55 years, inclusive
Body Mass Index (BMI): 18.0 - 30.0 kg/m2, inclusive Body weight (kg)and height2 (m2)
Ability and willingness to abstain from alcohol, methylxanthine-containing beverages or food (coffee, tea, cola, chocolate, "powerdrinks") and grapefruit (juice) from 48 hours prior to entry in the clinical research centre until discharge
Medical history without major pathology
Resting supine blood pressure and a resting pulse rate showing no clinically relevant deviations as judged by the MI
Computerised (12-lead) electrocardiogram (ECG) recording without signs of clinically relevant pathology or showing no clinically relevant deviations as judged by the MI
Willingness to use adequate contraception from the time of dosing until 3 months after the follow-up visit
All values for haematology and for clinical chemistry tests of blood and urine within the normal range or showing no clinically relevant deviations as judged by the MI
Willingness to sign the written ICF
Exclusion Criteria:
Evidence of clinically relevant pathology
Mental handicap
History of relevant drug and/or food allergies
Regular/routine treatment with non-topical medications within 30 days prior to entrance into the clinical research centre
Smoking (less than 60 days prior to drug administration)
History of alcohol abuse or drug addiction (including soft drugs like cannabis products)
Use of concomitant medication, except for acetaminophen (paracetamol), which was allowed up to 3 days before entrance into the clinical research centre. Multivitamins and vitamin C were allowed up to 7 days before entrance into the clinical research centre. All other medication (including over the counter medication, health supplements, and herbal remedies such as St. John's wort extract) was to be stopped at least 14 days prior to entrance into the clinical research centre
Participation in a drug study within 60 days prior to drug administration. Participation in more than 3 other drug studies in the 10 months preceding administration of study drug
Donation of more than 50 mL of blood within 60 days prior to drug administration. Donation of more than 1.5 litres of blood in the 10 months preceding administration of study drug
Participation in another ADME study with a radiation burden -0.1 mSv in the period of 1 year before the start of the study
Exposure to radiation for diagnostic reasons (except dental X-rays and plain X rays of thorax and bony skeleton - excluding spinal column), during work or during participation in a medical study in the previous year
Irregular defecation pattern (less than once per 2 days)
Positive screen on drugs of abuse (opiates, methadone, cocaine, amphetamines, cannabinoids, barbiturates, benzodiazepines, tricyclic antidepressants and alcohol)
Intake of more than 24 units of alcohol per week (1 unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 mL of spirits)
Positive screen on hepatitis B surface antigen (HBsAg)
Positive screen on anti-hepatitis C virus (HCV)
Positive screen on anti- human immunodeficiency virus (HIV) 1/2
Illness within 5 days prior to drug administration
Facility Information:
Facility Name
PRA
City
Zuidlaren
ZIP/Postal Code
9471 GP
Country
Netherlands
12. IPD Sharing Statement
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An Open-label Study in Healthy Male Subjects to Assess the Absorption, Distribution, Metabolism and Excretion of [14C]-Labelled BIA 9-1067 and Metabolites
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