Absorption, Distribution, Metabolism and Excretion of [14C]-Labelled BIA 3-202 and Metabolites

NCT02772614 | Completed Phase 1

• 1 other identifier: BIA-3202-106
• Study Type: interventional
• Target: 4
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is: To determine the rate and routes of excretion of BIA 3-202 and the mass balance in urine and faeces To determine the kinetics of total radioactivity in blood To determine the kinetics of total radioactivity in plasma To determine the kinetics of BIA 3-202 and its metabolites in plasma

Conditions

Parkinson's Disease

Keywords

Nebicapone, Parkinson's disease

Outcome Measures

Primary Outcomes (4)

• maximum plasma concentration (Cmax)

  pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose

• time of occurrence of Cmax (tmax)

  pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose

• area under the plasma concentration-time curve from time zero to the last sampling time at which concentrations are at or above the limit of quantification, calculated by the linear trapezoidal rule (AUC0-t)

  pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose

• area under the plasma concentration versus time curve from time zero to infinity, calculated from AUC0-t + (C(t)/λz), where C(t) is the last quantifiable concentration and λz the apparent terminal rate constant (AUC0-∞)

  pre-dose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 120, 168, 216, and 264 hours post-dose

Study Arms (1)

Nebicapone (200 mg)

EXPERIMENTAL

Each subject was to receive one single dose of 2.5 MBq \[14C\]-labelled BIA 3-202 (200 mg) together with a total of 250 mL non-carbonated water. The study drug was given after an overnight fast of at least 10 hours after the in-house stay. During waking hours on Day 1, subjects had to have a fluid intake of at least 150 mL per hour starting 1 hour before study drug administration.

Drug: BIA 3-202 (200 mg)

Interventions

BIA 3-202 (200 mg) DRUG

200 mg powder for oral use of unlabelled BIA 3-202

Nebicapone (200 mg)

Eligibility Criteria

• Age: 40 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male subject, 40-55 years of age. Take only Caucasians.
• Clinically acceptable sitting blood pressure and pulse rate , i.e.: BP: 110-160 mmHg systolic, 65-95 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 weight must be between 50 and 95 kg and within -10% / +20% of normal for their height and frame size (according to Metropolitan Life Insurance Table, see Appendix 1\&2 of the Study Protocol). Frame size will be determined using elbow breadth measurement.
• 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.

You may not qualify if:

• 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) and CK values must be within the normal range.
• Positive results of the drug screening.
• Known hypersensitivity to BIA 3-202.
• Heavy smokers, i.e., more than 10 cigarettes per day.

Sponsors & Collaborators

• Bial - Portela C S.A.: lead

Study Sites (1)

Swiss Pharma Contract Ltd

Allschwil, Basel, CH-4123, Switzerland

Location

MeSH Terms

Conditions

Parkinson Disease

Interventions

nebicapone

Condition Hierarchy (Ancestors)

Parkinsonian Disorders; Basal Ganglia Diseases; Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Movement Disorders; Synucleinopathies; Neurodegenerative Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 12, 2016
• First Posted: May 13, 2016
• Study Start: January 1, 2006
• Primary Completion: February 1, 2006
• Study Completion: February 1, 2006
• Last Updated: May 13, 2016

Record last verified: 2016-05

Data Sharing

• IPD Sharing: Will not share

Locations

CH (1)