COVID-19 is an emerging, rapidly evolving situation.
Get the latest public health information from CDC:

Get the latest research information from NIH: Menu

Absorption, Distribution, Metabolism and Excretion of [14C]- Labeled BIA 5-453 and Metabolites

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT03014375
Recruitment Status : Completed
First Posted : January 9, 2017
Last Update Posted : January 9, 2017
Information provided by (Responsible Party):
Bial - Portela C S.A.

Brief Summary:

The purpose of this study is to:

To determine the rate and routes of excretion of BIA 5-453 and the mass balance in urine and faeces

Condition or disease Intervention/treatment Phase
Hypertension Congestive Heart Failure Drug: BIA-5-453 Phase 1

Detailed Description:

Monocentre, open, non-placebo-controlled, single-group, single-dose study Safety measurements (12-lead ECG, vital signs, blood chemistry and haematology) will be conducted before and after the study, adverse events will be monitored throughout the study.

Subjects should be hospitalized the day before the administration until 264 hours thereafter.

Layout table for study information
Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 4 participants
Allocation: N/A
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: An Open-label Study in Healthy Male Subjects to Assess the Absorption, Distribution, Metabolism and Excretion of [14C]-Labeled BIA 5-453 and Metabolites Following a Single-dose Oral Administration
Study Start Date : September 2008
Actual Primary Completion Date : October 2008
Actual Study Completion Date : October 2008

Resource links provided by the National Library of Medicine

Arm Intervention/treatment
Experimental: Etamicastat
Single administration. 100 μCi/ 3.7 MBq 14C labeled BIA 5-453 50 mg, hard gelatina capsules
Drug: BIA-5-453
Each subject will receive a single oral dose of 100 μCi/ 3.7 MBq 14C labeled BIA 5-453 (600 mg).

Primary Outcome Measures :
  1. urinary excretion of BIA 5-453 associated radioactivity [ Time Frame: pre-dose, then it was collected from 0-4, 4-8, 8-24, 24-48, 48-72, 72-120, 120-168, 168-216, and 216-264 hours post-dose. ]
    following a single 600 mg oral dose labeled with 98 μCi of [14C]

  2. faecal excretion of BIA 5-453 associated radioactivity [ Time Frame: following a single 600 mg oral dose labeled with 98 μCi of [14C] ]
    baseline period. Following dose, each faeces sample was collected during the 264 hours post-dose period.

  3. amount of BIA 5-453 associated radioactivity present in the expired air [ Time Frame: baseline, 0.5h, 1h, 1.5h, 2h, 2.5h, 3h, 4h 6h, 8h, 12h and 24h post-dose ]
    following a single 600 mg oral dose labeled with 98 μCi of [14C]

Information from the National Library of Medicine

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies.

Layout table for eligibility information
Ages Eligible for Study:   40 Years to 55 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Healthy Caucasian male subjects, 40-55 years of age.
  • Sitting blood pressure and pulse rate within a clinically acceptable range for the purposes of the study, i.e.: BP: 100 160 mmHg systolic, 50 95 mmHg diastolic and pulse rate: 50 100 bpm. Blood pressure and pulse will be measured after 3 minutes resting in a sitting position.
  • Subject body mass index must be between 18 and 28 kg/m2
  • Normal 12-lead ECG
  • Ability to communicate well with the investigator and comply with the requirements of the entire study.
  • The subject has given his written informed consent to participate in the study.

Exclusion Criteria:

  • History of serious adverse reactions or hypersensitivity to any drug.
  • Presence or history of allergies requiring acute or chronic treatment (except seasonal allergic rhinitis).
  • History of alcohol or drug abuse in the last 5 years.
  • Abnormal physical findings of clinical significance at the screening examination or baseline which would interfere with the objectives of the study.
  • Need of any prescription medication within 14 days prior to the administration of the drug and/or nonprescription medication within 7 days prior to the administration of the drug.
  • Participation in other clinical trials during the previous month in which an investigational drug or a commercially available drug was tested.
  • Loss of 500 mL blood or more during the 3 month period before the study, e.g., as a donor.
  • Existence of any surgical or medical condition which might interfere with the absorption, distribution, metabolism or excretion of the drug, i.e., impaired renal or hepatic function, diabetes mellitus, cardiovascular abnormalities, chronic symptoms of pronounced constipation or diarrhoea or conditions associated with total or partial obstruction of the urinary tract.
  • Symptoms of a significant somatic or mental illness in the 4 week period preceding drug administration.
  • History of hepatitis B and / or C and / or positive serology results which indicate the presence of hepatitis B and / or C.
  • Positive results from the HIV serology.
  • Clinically significant abnormal laboratory values (as determined by the Principal Investigator) at the screening evaluation, however, liver parameters (SGPT, SGOT) values must be within the normal range.
  • Positive results of the drug screening.
  • Known hypersensitivity to BIA 5-453.
  • Heavy smokers, i.e., more than 10 cigarettes per day
  • Exposure to artificial ionizing radiation in the last 12 months (e.g., x-ray investigation)
  • Subject who had more than 4 flights (with more than 2 hours flight time) within the last year prior to the administration of the drug

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT03014375

Layout table for location information
Swiss Pharma Contract Ltd.
Allschwil, Switzerland, CH-4123
Sponsors and Collaborators
Bial - Portela C S.A.
Layout table for additonal information
Responsible Party: Bial - Portela C S.A. Identifier: NCT03014375    
Other Study ID Numbers: BIA-5453-103
First Posted: January 9, 2017    Key Record Dates
Last Update Posted: January 9, 2017
Last Verified: January 2017
Individual Participant Data (IPD) Sharing Statement:
Plan to Share IPD: Undecided
Additional relevant MeSH terms:
Layout table for MeSH terms
Heart Failure
Cardiovascular Diseases
Heart Diseases