Absorption, Distribution, Metabolism and Excretion of [14C]-Labeled BIA 9-1067 and Metabolites

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
Bial - Portela C S.A.
ClinicalTrials.gov Identifier:
NCT01515891
First received: January 19, 2012
Last updated: June 20, 2012
Last verified: June 2012
  Purpose

To determine the absorption, metabolism and excretion of BIA 9-1067.


Condition Intervention Phase
Parkinson Disease
Drug: BIA 9-1067
Phase 1

Study Type: Interventional
Study Design: Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: 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 9-1067 and Metabolites Following a Single-dose Oral Administration

Resource links provided by NLM:


Further study details as provided by Bial - Portela C S.A.:

Primary Outcome Measures:
  • maximum plasma concentration (Cmax) [ Time Frame: 24 hours:pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose ] [ Designated as safety issue: No ]
    Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites


Secondary Outcome Measures:
  • time to reach maximum plasma concentration (tmax) [ Time Frame: 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose ] [ Designated as safety issue: No ]
    Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites

  • area under the plasma-concentration time curve until the last quantifiable sampling point (AUC0-t) [ Time Frame: 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose ] [ Designated as safety issue: No ]
    Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites

  • area under the plasma-concentration time curve with extrapolation to infinity (AUC0-∞) [ Time Frame: 24 hours at the following times: pre-dose and 1, 1.75, 2.25, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose ] [ Designated as safety issue: No ]
    Whole blood samples for total radioactivity analysis, plasma samples for total radioactivity analysis, and plasma samples for analysis of BIA 9-1067 and its metabolites

  • quantification of metabolites [ Time Frame: 4 hours at the following times:(pre-dose including the period 0-1.5 h), 1.5-5.5, 5.5-9, 9-24, 24-48, 48-72, 72-120, 120-168, 168-216, and 216-264 hours post-dose ] [ Designated as safety issue: No ]
    Metabolite profiles, identification and quantification of metabolites in urine and faeces

  • Identification of clearance mechanisms [ Time Frame: 24 hours ] [ Designated as safety issue: No ]
    Whole blood samples for total radioactivity analysis; plasma samples for total radioactivity analysis and for analysis of BIA 9-1067 and its metabolites; urine and faeces samples; Exhaled air samples will be collected


Enrollment: 4
Study Start Date: May 2009
Study Completion Date: September 2010
Primary Completion Date: June 2009 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: BIA 9-1067
90 µCi (3.33 MBq) [14C]-labeled of 100 mg BIA 9-1067 (single-dose).
Drug: BIA 9-1067
90 µCi (3.33 MBq) [14C]-labeled of 100 mg BIA 9-1067 (single-dose).
Other Name: Entacapone

Detailed Description:

Monocentre, open, non-placebo-controlled, single-group, single-dose study

  Eligibility

Ages Eligible for Study:   40 Years to 55 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

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 were to be measured after 3 minutes resting in a sitting position.
  • Subject body mass index was to 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 had 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 9-1067.
  • 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.
  Contacts and Locations
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, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT01515891

Locations
Switzerland
Covance Basel Research Unit AG (formerly Swiss Pharma Contract Ltd)
Allschwil, Base, Switzerland, CH-4123
Sponsors and Collaborators
Bial - Portela C S.A.
Investigators
Principal Investigator: Seiberling Michael, MD Covance
  More Information

No publications provided

Responsible Party: Bial - Portela C S.A.
ClinicalTrials.gov Identifier: NCT01515891     History of Changes
Other Study ID Numbers: BIA-91067-103
Study First Received: January 19, 2012
Last Updated: June 20, 2012
Health Authority: Switzerland: Swissmedic

Keywords provided by Bial - Portela C S.A.:
Parkinson Disease
BIA 9-1067

Additional relevant MeSH terms:
Parkinson Disease
Parkinsonian Disorders
Basal Ganglia Diseases
Brain Diseases
Central Nervous System Diseases
Nervous System Diseases
Movement Disorders
Neurodegenerative Diseases

ClinicalTrials.gov processed this record on October 19, 2014