Absorption, Distribution, Metabolism and Excretion of [14C] Labelled BIA 5-1058
Condition: Cardiovascular Diseases
MeSH terms: Cardiovascular Diseases
Study type: Interventional
Phase: Phase 1

Summary: 
      The purpose of the study is to determine the mass balance recovery in expired air, urine and
      faeces after a single oral dose of 400 mg 14C-labeled BIA 5-1058; to provide plasma, urine
      and faecal samples for metabolite profiling and structural identification; and determine the
      routes and rates of elimination of [14C]-BIA 5-1058
    

Detailed description: 
      This is a Phase 1, single-dose, single-centre, single period, open-label, absorption,
      distribution, metabolism and excretion study in 8 healthy adult male subjects. Subjects will
      receive a single oral dose of 400 mg [14C]-BIA 5-1058, containing not more than (NMT) 4.6 MBq
      (124 µCi) 14C, as an oral capsule. Subjects will be screened for eligibility to participate
      in the study between 28 and 2 days before dosing. Eligible subjects will be admitted to the
      clinical unit on the morning of Day -1 prior to investigational medicinal product (IMP)
      administration. Subjects will be dosed on the morning of Day 1 after an overnight fast of at
      least 10 hours and will remain resident in the clinic until up to 336 h after dosing (up to
      Day 15). Blood, urine, faeces and expired air will be collected at predefined time points for
      mass balance and PK analysis. It is planned that subjects will be released as a group when
      all subjects have achieved a mass balance cumulative recovery of >90% or if <1% of the dose
      administered has been collected in urine, faeces and expired air within 2 separate,
      consecutive 24 h periods. This may result in the subjects being discharged as a group prior
      to completion of the planned residency period. Once the discharge criteria or the planned
      residency period has been achieved, collection of all samples (blood, urine, faeces, and
      expired air) will be stopped and the subjects will undergo discharge assessments. Subjects
      who have not met the mass balance discharge criteria on Day 15 will return to the clinical
      unit for up to five further 24-hour residency periods (Days 21-22 [±1 day], 28-29 [±1 day],
      42-43 [±2 days], 56-57 [±2 days] and 77-78 [±3 days]) to collect blood samples for PK
      analysis and urine and faeces samples for analysis of total radioactivity. If the parent and
      metabolite are below the limit of quantification at any of these visits, subsequent return
      visits may be cancelled. If by Day 78, levels are not below the limit of quantification or if
      the additional 24 h residency periods are not considered appropriate or necessary, then home
      collections of urine and/or faeces may be requested at the discretion of the investigator for
      individual subjects.
    

Intervention name(s): 400 mg of BIA 5-1058
Intervention type(s): Drug
Intervention description(s): 1 x 400 mg capsule Oral, Fasted
Intervention model: Single Group Assignment
Masking: None (Open Label)
Primary purpose: Treatment