Relative Bioavailability and Bioequivalence Of Different Formulations of Opicapone in Healthy Volunteers
Phase 1
Completed
- Conditions
- Parkinson
- Interventions
- Registration Number
- NCT02305277
- Lead Sponsor
- Bial - Portela C S.A.
- Brief Summary
Single-centre, open-label, randomised, three-part, two-way crossover study in 84 healthy volunteers. In each part, the study consisted of two consecutive single-dose treatment periods separated by a washout period of at least 14 days.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 85
Inclusion Criteria
- A signed and dated informed consent form before any study-specific screening procedure was performed;
- Male or female subjects aged 18 to 45 years, inclusive;
- Body mass index (BMI) between 18 and 30 kg/m2 inclusive;
- 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 antibodies (HCV Ab) and anti-human immunodeficiency virus antibodies (HIV-1 and HIV-2 Ab) at screening;
- Clinical laboratory test results clinically acceptable at screening and admission to each treatment period;
- Negative screen for alcohol and drugs of abuse at screening and admission to each treatment period;
- Non-smokers or ex-smokers for at least 3 months;
- Able to participate, and willing to give written informed consent and comply with the study restrictions.
- If female:
- She was not of childbearing potential by reason of surgery or, if of childbearing potential, she used 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 all the duration of the study;
- She had a negative serum pregnancy test at screening and a negative urine pregnancy test at admission to each treatment period.
Exclusion Criteria
- Subjects who had a 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;
- Had clinically relevant findings in laboratory tests, particularly any abnormality in the coagulation tests, or any abnormality in the liver function tests;
- Had a history of relevant atopy or drug hypersensitivity;
- Had a history of alcoholism and/or drug abuse;
- Consumed 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°)];
- Had a significant infection or known inflammatory process on screening or admission to each treatment period;
- Had acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period;
- Had used medicines within 2 weeks of admission to first period that could affect the safety or other study assessments, in the Investigator's opinion;
- Had previously received opicapone;
- Had used any investigational drug or participated in any clinical trial within 90 days prior to screening;
- Had participated in more than 2 clinical trials within the 12 months prior to screening;
- Had donated or received any blood or blood products within the 3 months prior to screening;
- Were vegetarians, vegans or had medical dietary restrictions;
- Could not communicate reliably with the Investigator;
- Were unlikely to co-operate with the requirements of the study;
- Were unwilling or unable to give written informed consent;
If female:
- She was pregnant or breast-feeding.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description BIA 9-1067 25 mg Sequence 2 BIA 9-1067 (to-be-marketed, TBM) volunteers received a single oral dose of 25 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 5 mg Sequence 1 BIA 9-1067 (clinical micronized, CM) volunteers received a single oral dose of 5 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 5 mg Sequence 1 BIA 9-1067 (to-be-marketed, TBM) volunteers received a single oral dose of 5 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 25 mg Sequence 1 BIA 9-1067 (to-be-marketed, TBM) volunteers received a single oral dose of 25 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 50 mg Sequence 1 BIA 9-1067 (to-be-marketed, TBM) volunteers received a single oral dose of 50 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 50 mg Sequence 2 BIA 9-1067 (to-be-marketed, TBM) volunteers received a single oral dose of 50 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 25 mg Sequence 1 BIA 9-1067 (clinical micronized, CM) volunteers received a single oral dose of 25 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 50 mg Sequence 1 BIA 9-1067 (clinical micronized, CM) volunteers received a single oral dose of 50 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 5 mg Sequence 2 BIA 9-1067 (clinical micronized, CM) volunteers received a single oral dose of 5 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 25 mg Sequence 2 BIA 9-1067 (clinical micronized, CM) volunteers received a single oral dose of 25 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 50 mg Sequence 2 BIA 9-1067 (clinical micronized, CM) volunteers received a single oral dose of 50 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed BIA 9-1067 5 mg Sequence 2 BIA 9-1067 (to-be-marketed, TBM) volunteers received a single oral dose of 5 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed
- Primary Outcome Measures
Name Time Method Cmax - Maximum Observed Plasma Concentration before OPC dosing, and ½, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose
- Secondary Outcome Measures
Name Time Method Tmax - Time of Occurrence of Cmax before OPC dosing, and ½, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose AUC0-t - Area Under the Plasma Concentration-time Curve for BIA 9-1067 before OPC dosing, and ½, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose Area Under the plasma concentration-time Curve from time 0 to the time of last quantifiable concentration