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

January 19, 2012
June 20, 2012
May 2009
June 2009   (final data collection date for primary outcome measure)
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
To determine the rate and routes of excretion of BIA 9-1067 and the mass balance in urine and faeces [ Time Frame: 24 hours ] [ Designated as safety issue: Yes ]
To determine the kinetics of total radioactivity in blood To determine the kinetics of total radioactivity in plasma To determine the kinetics of BIA 9-1067 and its metabolites in plasma
Complete list of historical versions of study NCT01515891 on ClinicalTrials.gov Archive Site
  • 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
To identify and quantify the BIA 9-1067 metabolites in plasma, urine, and faeces [ Time Frame: 24 hours ] [ Designated as safety issue: Yes ]
To identify the biotransformation pathways of BIA 9-1067 in man To evaluate the absorption of BIA 9-1067.
Not Provided
Not Provided
 
Absorption, Distribution, Metabolism and Excretion of [14C]-Labeled BIA 9-1067 and Metabolites
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

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

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

Interventional
Phase 1
Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Treatment
Parkinson Disease
Drug: BIA 9-1067
90 µCi (3.33 MBq) [14C]-labeled of 100 mg BIA 9-1067 (single-dose).
Other Name: Entacapone
Experimental: BIA 9-1067
90 µCi (3.33 MBq) [14C]-labeled of 100 mg BIA 9-1067 (single-dose).
Intervention: Drug: BIA 9-1067
Not Provided

*   Includes publications given by the data provider as well as publications identified by ClinicalTrials.gov Identifier (NCT Number) in Medline.
 
Completed
4
September 2010
June 2009   (final data collection date for primary outcome measure)

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.
Male
40 Years to 55 Years
Yes
Contact information is only displayed when the study is recruiting subjects
Switzerland
 
NCT01515891
BIA-91067-103
No
Bial - Portela C S.A.
Bial - Portela C S.A.
Not Provided
Principal Investigator: Seiberling Michael, MD Covance
Bial - Portela C S.A.
June 2012

ICMJE     Data element required by the International Committee of Medical Journal Editors and the World Health Organization ICTRP