Single-dose Pharmacokinetics and Relative Bioavailability of Two Different Formulations of Opicapone
Primary Purpose
Parkinson Disease
Status
Completed
Phase
Phase 1
Locations
Study Type
Interventional
Intervention
BIA 9-1067 non-micronized
BIA 9-1067 micronized
Sponsored by
About this trial
This is an interventional treatment trial for Parkinson Disease
Eligibility Criteria
Inclusion Criteria:
- A signed and dated informed consent form (ICF) before any study-specific screening procedure was performed,
- Male or female subjects aged 18 to 45 years, inclusive,
- Body mass index (BMI) between 19 and 30 kg/m2,
- Healthy as determined by pre-study medical history, physical examination, vital signs, complete neurological examination and 12-lead electrocardiogram (ECG),
- Negative tests for hepatitis B surface antigen (HBsAg), anti-hepatitis C virus (HCV) antibodies and anti-human immunodeficiency virus (HIV) antibodies at screening,
- Clinical laboratory test results clinically acceptable at screening and on D-1 of each treatment period,
- Negative screen for alcohol and drugs of abuse at screening and on D-1 of each treatment period,
- Non-smokers or ex-smokers for at least 3 months,
- Volunteer able to participate, and willing to give written informed consent and comply with the study restrictions,
If female:
- Was not of childbearing potential by reason of surgery or, if of childbearing potential, uses an effective non-hormonal method of contraception (intrauterine device or intrauterine system; condom or occlusive cap [diaphragm or cervical or vault caps] with spermicidal foam or gel or film or cream or suppository; true abstinence; or vasectomized male partner, provided that he was the sole partner of that subject) for the entire duration of the study,
- Negative serum pregnancy test at screening and a negative urine pregnancy test on D-1 of each treatment period.
Exclusion Criteria:
- Any clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, endocrine, connective tissue diseases or disorders, or had a clinically relevant surgical history,
- Any clinically relevant abnormality in the coagulation tests,
- Any clinically relevant abnormality in the liver function tests,
- History of relevant atopy or drug hypersensitivity,
- History of alcoholism and/or drug abuse,
- Current consumption of more than 14 units of alcohol per week [1 unit of alcohol = 280 mL beer (3-4°) = 100 mL wine (10-12°) = 30 mL spirits (40°)],
- Any significant infection or known inflammatory process on screening or admission to each treatment period,
- Any acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period,
- Use of medicines within 2 weeks of admission to first period that could affect the subject's safety or other study assessments, in the investigator's opinion,
- Previously received opicapone,
- Involvement in other clinical trials of any type within 90 days prior to screening,
- Participation in more than 2 clinical trials within the 12 months prior to screening,
- Blood donation or received any blood transfusion or any blood products within the 3 months prior to screening,
- Vegetarian, vegan or had medical dietary restrictions,
- Subject not able to communicate reliably with the investigator,
- Subjects who were unlikely to co-operate with the requirements of the study,
- Subjects who were unwilling or unable to give written informed consent,
If female:
- Pregnant or breast-feeding,
- If of childbearing potential, a positive serum pregnancy test,
- Volunteer who did not use an accepted effective contraceptive method or used oral contraceptives,
Sites / Locations
Arms of the Study
Arm 1
Arm 2
Arm Type
Experimental
Experimental
Arm Label
BIA 9-1067 non-micronized - micronized
BIA 9-1067 micronized - non-micronized
Arm Description
Each subject was orally administered with 50 mg OPC non-micronized followed by a washout period of 14 days. After washout period each subject was orally administered with 50 mg OPC micronized
Each subject was orally administered 50 mg OPC micronized followed by a washout period of 14 days. After washout period each subject was orally administered with 50 mg OPC non-micronized
Outcomes
Primary Outcome Measures
Cmax - Maximum Observed Plasma Concentration
Maximum observed plasma concentration of BIA 9-1067
Secondary Outcome Measures
AUC0-t - Area Under the Plasma Concentration-time Curve From Time 0 to the Time of Last Quantifiable Concentration
AUC0-t - Area under the plasma concentration-time curve from time 0 to the time of last quantifiable concentration of BIA 9-1067
Tmax - Time of Occurrence of Cmax of BIA 9-1067
tmax - time of occurrence of maximum observed plasma concentration of BIA 9-1067
AUC0-inf - Area Under the Plasma Concentration-time Curve From Time 0 to the Infinity
AUC0-inf - Area under the plasma concentration-time curve from time 0 to the infinity.
Full Information
1. Study Identification
Unique Protocol Identification Number
NCT02305316
Brief Title
Single-dose Pharmacokinetics and Relative Bioavailability of Two Different Formulations of Opicapone
Official Title
Single-dose Pharmacokinetics and Relative Bioavailability of Two Different Formulations of Opicapone in Healthy Volunteers
Study Type
Interventional
2. Study Status
Record Verification Date
July 2015
Overall Recruitment Status
Completed
Study Start Date
February 2014 (undefined)
Primary Completion Date
March 2014 (Actual)
Study Completion Date
March 2014 (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
Single-centre, open-label, randomised, two-way crossover study in 28 healthy volunteers. The study consisted of two consecutive single-dose treatment periods separated by a washout period of 14 days or more.
Detailed Description
Single-centre, open-label, randomised, two-way crossover study in 28 healthy volunteers. The study consisted of two consecutive single-dose treatment periods separated by a washout period of 14 days or more. A total of twenty-eight (28) healthy volunteers received a single dose of 50 mg OPC, orally.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
Parkinson Disease
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 1
Interventional Study Model
Crossover Assignment
Masking
None (Open Label)
Allocation
Randomized
Enrollment
28 (Actual)
8. Arms, Groups, and Interventions
Arm Title
BIA 9-1067 non-micronized - micronized
Arm Type
Experimental
Arm Description
Each subject was orally administered with 50 mg OPC non-micronized followed by a washout period of 14 days. After washout period each subject was orally administered with 50 mg OPC micronized
Arm Title
BIA 9-1067 micronized - non-micronized
Arm Type
Experimental
Arm Description
Each subject was orally administered 50 mg OPC micronized followed by a washout period of 14 days. After washout period each subject was orally administered with 50 mg OPC non-micronized
Intervention Type
Drug
Intervention Name(s)
BIA 9-1067 non-micronized
Other Intervention Name(s)
OPC, Opicapone
Intervention Type
Drug
Intervention Name(s)
BIA 9-1067 micronized
Other Intervention Name(s)
OPC, Opicapone
Primary Outcome Measure Information:
Title
Cmax - Maximum Observed Plasma Concentration
Description
Maximum observed plasma concentration of BIA 9-1067
Time Frame
before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose.
Secondary Outcome Measure Information:
Title
AUC0-t - Area Under the Plasma Concentration-time Curve From Time 0 to the Time of Last Quantifiable Concentration
Description
AUC0-t - Area under the plasma concentration-time curve from time 0 to the time of last quantifiable concentration of BIA 9-1067
Time Frame
before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose.
Title
Tmax - Time of Occurrence of Cmax of BIA 9-1067
Description
tmax - time of occurrence of maximum observed plasma concentration of BIA 9-1067
Time Frame
before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose.
Title
AUC0-inf - Area Under the Plasma Concentration-time Curve From Time 0 to the Infinity
Description
AUC0-inf - Area under the plasma concentration-time curve from time 0 to the infinity.
Time Frame
before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose.
10. Eligibility
Sex
All
Minimum Age & Unit of Time
18 Years
Maximum Age & Unit of Time
45 Years
Accepts Healthy Volunteers
Accepts Healthy Volunteers
Eligibility Criteria
Inclusion Criteria:
A signed and dated informed consent form (ICF) before any study-specific screening procedure was performed,
Male or female subjects aged 18 to 45 years, inclusive,
Body mass index (BMI) between 19 and 30 kg/m2,
Healthy as determined by pre-study medical history, physical examination, vital signs, complete neurological examination and 12-lead electrocardiogram (ECG),
Negative tests for hepatitis B surface antigen (HBsAg), anti-hepatitis C virus (HCV) antibodies and anti-human immunodeficiency virus (HIV) antibodies at screening,
Clinical laboratory test results clinically acceptable at screening and on D-1 of each treatment period,
Negative screen for alcohol and drugs of abuse at screening and on D-1 of each treatment period,
Non-smokers or ex-smokers for at least 3 months,
Volunteer able to participate, and willing to give written informed consent and comply with the study restrictions,
If female:
Was not of childbearing potential by reason of surgery or, if of childbearing potential, uses an effective non-hormonal method of contraception (intrauterine device or intrauterine system; condom or occlusive cap [diaphragm or cervical or vault caps] with spermicidal foam or gel or film or cream or suppository; true abstinence; or vasectomized male partner, provided that he was the sole partner of that subject) for the entire duration of the study,
Negative serum pregnancy test at screening and a negative urine pregnancy test on D-1 of each treatment period.
Exclusion Criteria:
Any clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, endocrine, connective tissue diseases or disorders, or had a clinically relevant surgical history,
Any clinically relevant abnormality in the coagulation tests,
Any clinically relevant abnormality in the liver function tests,
History of relevant atopy or drug hypersensitivity,
History of alcoholism and/or drug abuse,
Current consumption of more than 14 units of alcohol per week [1 unit of alcohol = 280 mL beer (3-4°) = 100 mL wine (10-12°) = 30 mL spirits (40°)],
Any significant infection or known inflammatory process on screening or admission to each treatment period,
Any acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period,
Use of medicines within 2 weeks of admission to first period that could affect the subject's safety or other study assessments, in the investigator's opinion,
Previously received opicapone,
Involvement in other clinical trials of any type within 90 days prior to screening,
Participation in more than 2 clinical trials within the 12 months prior to screening,
Blood donation or received any blood transfusion or any blood products within the 3 months prior to screening,
Vegetarian, vegan or had medical dietary restrictions,
Subject not able to communicate reliably with the investigator,
Subjects who were unlikely to co-operate with the requirements of the study,
Subjects who were unwilling or unable to give written informed consent,
If female:
Pregnant or breast-feeding,
If of childbearing potential, a positive serum pregnancy test,
Volunteer who did not use an accepted effective contraceptive method or used oral contraceptives,
12. IPD Sharing Statement
Learn more about this trial
Single-dose Pharmacokinetics and Relative Bioavailability of Two Different Formulations of Opicapone
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