Single-dose Pharmacokinetics and Relative Bioavailability of Two Different Formulations of Opicapone

Study Overview
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Brief Summary
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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
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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.

Official Title
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Single-dose Pharmacokinetics and Relative Bioavailability of Two Different Formulations of Opicapone in Healthy Volunteers

Conditions
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Parkinson Disease

Intervention / Treatment
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* Drug: BIA 9-1067 non-micronized
* Drug: BIA 9-1067 micronized


Participation Criteria
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Eligibility Criteria
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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,

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 45 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: BIA 9-1067 non-micronized - micronized<br>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 | Drug: BIA 9-1067 non-micronized<br> <br> * Other names: OPC, Opicapone;Drug: BIA 9-1067 micronized<br> <br> * Other names: OPC, Opicapone;|
| Experimental: BIA 9-1067 micronized - non-micronized<br>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 | Drug: BIA 9-1067 non-micronized<br> <br> * Other names: OPC, Opicapone;Drug: BIA 9-1067 micronized<br> <br> * Other names: OPC, Opicapone;|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Cmax - Maximum Observed Plasma Concentration | Maximum observed plasma concentration of BIA 9-1067 | before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose. | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| 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 | before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose. | 
| Tmax - Time of Occurrence of Cmax of BIA 9-1067 | tmax - time of occurrence of maximum observed plasma concentration of BIA 9-1067 | before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose. | 
| 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. | before OPC dosing, and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose. |