Bioavailability Study of BIA 5-453

Study Overview
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Brief Summary
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The purpose of this study was to compare the bioavailability and tolerability of BIA 5-453 under fasted and fed conditions.

Detailed Description
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This was a Single-centre, two-way crossover, randomised, open-label study in 12 healthy male volunteers. Subjects received a single oral 200 mg dose of BIA 5-453 following a standard meal in one period, and following at least 10 hours of fasting in another period. Treatment periods were separated by a washout interval of 2 weeks or more.

Official Title
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Comparative Bioavailability Study of BIA 5-453 Under Fasted and Fed Conditions

Conditions
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Hypertension, Congestive Heart Failure

Intervention / Treatment
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* Drug: BIA 5-453


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: aged between 18 and 45 years, inclusive. had a body mass index (BMI) between 19 and 30 kg/m2, inclusive. were healthy as determined by pre-study medical history, physical examination, vital signs, complete neurological examination and 12-lead ECG. had negative tests for HBsAg, anti-HCVAb and HIV-1 and HIV-2 Ab at screening had clinical laboratory test results clinically acceptable at screening and admission to the first treatment period. had negative screen for alcohol and drugs of abuse at screening and admission to the first treatment period. were non-smokers or smoked ≤ 10 cigarettes or equivalent per day. was able and willing to give written informed consent. Exclusion Criteria: 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. had a clinically relevant surgical history. had a clinically relevant family history. had a history of relevant atopy or drug hypersensitivity. had a history of alcoholism or drug abuse. consumed more than 14 units of alcohol a week. had a significant infection or known inflammatory process at screening or admission to the first treatment period. had acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to the first treatment period. used medicines within 2 weeks of admission to first period that affected the safety or other study assessments, in the investigator's opinion. used any investigational drug or participated in any clinical trial within 3 months prior to screening. participated in more than 2 clinical trials within the 12 months prior to screening. donated or received any blood or blood products within the 3 months prior to screening. was a vegetarian, vegan or with medical dietary restrictions. could not communicate reliably with the investigator. was unlikely to co-operate with the requirements of the study. was unwilling or unable to give written informed consent.

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

Sexes Eligible for Study
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Male

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 5-453 Fasting<br>BIA 5-453 200 mg in fasting conditions | Drug: BIA 5-453<br>* BIA 5-453 capsules 50 mg. Route of administration: Oral. In one period subjects received 4 capsules of 50 mg of BIA 5-453 after a fasting of at least 10 hours, and in the other period subjects were dosed with 4 capsules of 50 mg of BIA 5-453 after a standard high-fat and high-calorie meal<br>* Other names: Etamicastat;|
| Experimental: BIA 5-453 Fed<br>BIA 5-453 200 mg in fed conditions | Drug: BIA 5-453<br>* BIA 5-453 capsules 50 mg. Route of administration: Oral. In one period subjects received 4 capsules of 50 mg of BIA 5-453 after a fasting of at least 10 hours, and in the other period subjects were dosed with 4 capsules of 50 mg of BIA 5-453 after a standard high-fat and high-calorie meal<br>* Other names: Etamicastat;|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Cmax - the maximum plasma concentration |  | pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 and 72 hours post-dose | 
| Tmax - the time of occurrence of Cmax |  | pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 and 72 hours post-dose | 
| AUC0-t - the area under the plasma concentration-time curve from time zero to the last sampling time |  | pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 and 72 hours post-dose | 
| AUC0-∞ - the area under the plasma concentration versus time curve from time zero to infinity |  | pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48 and 72 hours post-dose |