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.

Study Overview

• Status: Completed
• Conditions: Parkinson Disease
• Intervention / Treatment: Drug: BIA 9-1067

Detailed Description

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

• Study Type: Interventional
• Enrollment (Actual): 4
• Phase: Phase 1

Contacts and Locations

Study Locations

• Switzerland
  • Base
    • Allschwil, Base, Switzerland, CH-4123
      • Covance Basel Research Unit AG (formerly Swiss Pharma Contract Ltd)

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 40 years to 55 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
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 Names: Opicapone

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum Plasma Concentration (Cmax)	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	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

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Time to Reach Maximum Plasma Concentration (Tmax)	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	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
Area Under the Plasma-concentration Time Curve Until the Last Quantifiable Sampling Point (AUC0-t)	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	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
Area Under the Plasma-concentration Time Curve With Extrapolation to Infinity (AUC0-∞)	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	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

Collaborators and Investigators

• Sponsor: Bial - Portela C S.A.
• Investigators: Principal Investigator: Seiberling Michael, MD, Covance

Study record dates

Study Major Dates

• Study Start: May 1, 2009
• Primary Completion (Actual): June 1, 2009
• Study Completion (Actual): September 1, 2010

Study Registration Dates

• First Submitted: January 19, 2012
• First Submitted That Met QC Criteria: January 19, 2012
• First Posted (Estimate): January 24, 2012

Study Record Updates

• Last Update Posted (Estimate): January 9, 2015
• Last Update Submitted That Met QC Criteria: December 30, 2014
• Last Verified: December 1, 2014

More Information

Terms related to this study

• Keywords: Parkinson Disease; BIA 9-1067
• Additional Relevant MeSH Terms: Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Parkinsonian Disorders; Basal Ganglia Diseases; Movement Disorders; Synucleinopathies; Neurodegenerative Diseases; Parkinson Disease; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Antiparkinson Agents; Anti-Dyskinesia Agents; Catechol O-Methyltransferase Inhibitors; Opicapone
• Other Study ID Numbers: BIA-91067-103

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No