Bioavailability Study of BIA 5-453

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

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

Study Overview

• Status: Completed
• Conditions: Hypertension; Congestive Heart Failure
• Intervention / Treatment: Drug: BIA 5-453

Detailed Description

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.

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• France
  • Rennes, France, F-35000
    • Biotrial's Human Pharmacology Unit

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

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.

Study Plan

How is the study designed?

Design Details

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

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: BIA 5-453 Fasting; BIA 5-453 200 mg in fasting conditions	Drug: BIA 5-453; 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; Other Names: Etamicastat
Experimental: BIA 5-453 Fed; BIA 5-453 200 mg in fed conditions	Drug: BIA 5-453; 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; Other Names: Etamicastat

What is the study measuring?

Primary Outcome Measures

Outcome Measure	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

Collaborators and Investigators

• Sponsor: Bial - Portela C S.A.

Study record dates

Study Major Dates

• Study Start (Actual): July 15, 2008
• Primary Completion (Actual): August 14, 2008
• Study Completion (Actual): August 14, 2008

Study Registration Dates

• First Submitted: March 20, 2017
• First Submitted That Met QC Criteria: March 20, 2017
• First Posted (Actual): March 27, 2017

Study Record Updates

• Last Update Posted (Actual): March 27, 2017
• Last Update Submitted That Met QC Criteria: March 20, 2017
• Last Verified: March 1, 2017

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Heart Diseases; Cardiovascular Diseases; Heart Failure
• Other Study ID Numbers: BIA-5453-104

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: UNDECIDED

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No