An Open-label Study in Healthy Male Subjects to Assess the Absorption, Distribution, Metabolism and Excretion of [14C]-Labelled BIA 9-1067 and Metabolites

July 22, 2015 updated by: Bial - Portela C S.A.

An Open-label Study in Healthy Male Subjects to Assess the Absorption, Distribution, Metabolism and Excretion of [14C]-Labelled BIA 9-1067 and Metabolites Following a Single Dose Oral Administration

The purpose of this study is to determine the rate and routes of excretion of OPC and the mass balance in urine, faeces and expired air.

Study Overview

Status

Completed

Intervention / Treatment

Detailed Description

This was a single-centre, open-label ADME study in 6 healthy male subjects. Subjects received a single dose of 100 mg OPC, containing 3.39 MBq of [14C] OPC as oral capsules.

The study consisted of an eligibility screening period within 3 weeks prior to drug administration, admission on Day -1, a treatment period involving drug administration on Day 1 followed by matrix collections for PK purposes and safety evaluations up to Day 11, discharge on Day 11, six 24-hour hospitalizations on Days 14/15, 21/22 (+/ 1 day), 28/29 (+/- 1 day), 42/43 (+/- 2 days), 56/57 (+/- 2 days) and 77/78 (+/ 3 days) for PK sample collections, and a follow up visit performed at least 14 days after discharge from the last 24-hour hospitalization or at early discontinuation.

Study Type

Interventional

Enrollment (Actual)

6

Phase

  • Phase 1

Contacts and Locations

This section provides the contact details for those conducting the study, and information on where this study is being conducted.

Study Locations

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Ages Eligible for Study

18 years to 55 years (Adult)

Accepts Healthy Volunteers

No

Genders Eligible for Study

Male

Description

Inclusion Criteria:

  1. Gender: male
  2. Age: 18 - 55 years, inclusive
  3. Body Mass Index (BMI): 18.0 - 30.0 kg/m2, inclusive Body weight (kg)and height2 (m2)
  4. Ability and willingness to abstain from alcohol, methylxanthine-containing beverages or food (coffee, tea, cola, chocolate, "powerdrinks") and grapefruit (juice) from 48 hours prior to entry in the clinical research centre until discharge
  5. Medical history without major pathology
  6. Resting supine blood pressure and a resting pulse rate showing no clinically relevant deviations as judged by the MI
  7. Computerised (12-lead) electrocardiogram (ECG) recording without signs of clinically relevant pathology or showing no clinically relevant deviations as judged by the MI
  8. Willingness to use adequate contraception from the time of dosing until 3 months after the follow-up visit
  9. All values for haematology and for clinical chemistry tests of blood and urine within the normal range or showing no clinically relevant deviations as judged by the MI
  10. Willingness to sign the written ICF

Exclusion Criteria:

  1. Evidence of clinically relevant pathology
  2. Mental handicap
  3. History of relevant drug and/or food allergies
  4. Regular/routine treatment with non-topical medications within 30 days prior to entrance into the clinical research centre
  5. Smoking (less than 60 days prior to drug administration)
  6. History of alcohol abuse or drug addiction (including soft drugs like cannabis products)
  7. Use of concomitant medication, except for acetaminophen (paracetamol), which was allowed up to 3 days before entrance into the clinical research centre. Multivitamins and vitamin C were allowed up to 7 days before entrance into the clinical research centre. All other medication (including over the counter medication, health supplements, and herbal remedies such as St. John's wort extract) was to be stopped at least 14 days prior to entrance into the clinical research centre
  8. Participation in a drug study within 60 days prior to drug administration. Participation in more than 3 other drug studies in the 10 months preceding administration of study drug
  9. Donation of more than 50 mL of blood within 60 days prior to drug administration. Donation of more than 1.5 litres of blood in the 10 months preceding administration of study drug
  10. Participation in another ADME study with a radiation burden -0.1 mSv in the period of 1 year before the start of the study
  11. Exposure to radiation for diagnostic reasons (except dental X-rays and plain X rays of thorax and bony skeleton - excluding spinal column), during work or during participation in a medical study in the previous year
  12. Irregular defecation pattern (less than once per 2 days)
  13. Positive screen on drugs of abuse (opiates, methadone, cocaine, amphetamines, cannabinoids, barbiturates, benzodiazepines, tricyclic antidepressants and alcohol)
  14. Intake of more than 24 units of alcohol per week (1 unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 mL of spirits)
  15. Positive screen on hepatitis B surface antigen (HBsAg)
  16. Positive screen on anti-hepatitis C virus (HCV)
  17. Positive screen on anti- human immunodeficiency virus (HIV) 1/2
  18. Illness within 5 days prior to drug administration

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

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

Arms and Interventions

Participant Group / Arm
Intervention / Treatment
Experimental: Opicapone (OPC)
100 mg OPC
The drug substance of 100 mg OPC was administered as 1 capsule.
Other Names:
  • BIA 9-1067

What is the study measuring?

Primary Outcome Measures

Outcome Measure
Measure Description
Time Frame
Cumulative Recovery of [14C]-Radioactivity
Time Frame: pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29

AEurine: Cumulative Recovery of [14C]-Radioactivity in urine AEfaeces: Cumulative Recovery of [14C]-Radioactivity in urine AEair: Cumulative Recovery of [14C]-Radioactivity in urine AEtotal: Cumulative Recovery of [14C]-Radioactivity in urine

Recovery % of dose has been derived from area under the excretion rate (to infinity) from 240h onwards

pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29

Secondary Outcome Measures

Outcome Measure
Measure Description
Time Frame
Cmax - Maximum Concentration
Time Frame: pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29
BIA 9-1103 is a Opicapone (OPC, BIA 9-1067) metabolite
pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29
Tmax - Time to Attain Maximum Concentration
Time Frame: pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29
BIA 9-1103 is a Opicapone (OPC, BIA 9-1067) metabolite
pre-dose and 0-6, 6-12, 12-24, 24-48, 48 72, 72-96, 96 120, 120-144, 144-168, 168-192, 192-216 and 216-240 hours post-dose; 24-hour collections on Days 14/15, 21/22, 28/29

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start

March 1, 2011

Primary Completion (Actual)

July 1, 2011

Study Completion (Actual)

July 1, 2011

Study Registration Dates

First Submitted

January 24, 2012

First Submitted That Met QC Criteria

June 19, 2014

First Posted (Estimate)

June 23, 2014

Study Record Updates

Last Update Posted (Estimate)

August 21, 2015

Last Update Submitted That Met QC Criteria

July 22, 2015

Last Verified

July 1, 2015

More Information

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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