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

Hypertension Clinical Trial

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

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT03014375
• Other study ID #: BIA-5453-103
• Status: Completed
• Phase: Phase 1
• First received: January 5, 2017
• Last updated: January 6, 2017
• Start date: September 2008
• Est. completion date: October 2008

Study information

• Verified date: January 2017
• Source: Bial - Portela C S.A.
• Contact: n/a
• Is FDA regulated: No
• Health authority: Switzerland: Ethikkommission
• Study type: Interventional

Clinical Trial 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

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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 4
• Est. completion date: October 2008
• Est. primary completion date: October 2008
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Male
• Age group: 40 Years to 55 Years

Eligibility

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

Study Design

Endpoint Classification: Pharmacokinetics Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment

Related Conditions & MeSH terms

• Congestive Heart Failure
• Heart Failure
• Hypertension

Intervention

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).

Locations

Country	Name	City	State
Switzerland	Swiss Pharma Contract Ltd.	Allschwil

Sponsors (1)

Lead Sponsor	Collaborator
Bial - Portela C S.A.

Country where clinical trial is conducted

Switzerland, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	urinary excretion of BIA 5-453 associated radioactivity	following a single 600 mg oral dose labeled with 98 µCi of [14C]	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.	No
Primary	faecal excretion of BIA 5-453 associated radioactivity	baseline period. Following dose, each faeces sample was collected during the 264 hours post-dose period.	following a single 600 mg oral dose labeled with 98 µCi of [14C]	No
Primary	amount of BIA 5-453 associated radioactivity present in the expired air	following a single 600 mg oral dose labeled with 98 µCi of [14C]	baseline, 0.5h, 1h, 1.5h, 2h, 2.5h, 3h, 4h 6h, 8h, 12h and 24h post-dose	No