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Mass Balance Recovery and Metabolite Identification of Carbon-14 BIA 28-6156

Phase 1
Completed
Conditions
Parkinson Disease
Interventions
Drug: Carbon-14 BIA 28-6156
Registration Number
NCT05220072
Lead Sponsor
Bial R&D Investments, S.A.
Brief Summary

The study is designed to determine the absorption, distribution, metabolism and elimination (ADME) of BIA 28-6156 in humans, further explore the PK of BIA 28-6156, evaluate the extent of distribution of total radioactivity into blood cells, provide additional safety and tolerability information and collect samples for metabolite profiling and structural identification.

Detailed Description

This is an open-label, single-dose, single period study in healthy male subjects. It is planned to enroll 6 subjects. All subjects will receive a single oral dose Carbon-14 BIA 28-6156. Blood samples will be collected at regular intervals for PK analysis, mass balance and metabolite profiling and identification from pre-dose up to 240 h post-dose. Urine and faecal samples will be collected at regular intervals for mass balance and metabolite profiling and identification from pre-dose until the mass balance criteria have been met.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
6
Inclusion Criteria
  • Healthy males aged 30 to 65 years inclusive
  • Body mass index (BMI) of 18.0 to 35.0 kg/m2
  • Must be willing and able to communicate and participate in the whole study
  • Must have regular bowel movements
  • Must provide written informed consent
  • Must agree to adhere to contraception requirements
Exclusion Criteria
  • Subjects who have received any IMP in a clinical research study within the 90 days prior to Day 1
  • Subjects who are, or are immediate family members of, a study site or sponsor employee
  • Evidence of current SARS-CoV-2 infection from results of diagnostic tests or from symptoms reported at screening or admission
  • History of any drug or alcohol abuse in the past 2 years
  • Regular alcohol consumption
  • A confirmed positive alcohol breath test at screening or admission
  • Current smokers and those who have smoked within the last 12 months.
  • Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months
  • Subjects with pregnant or lactating partners
  • Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years.
  • Subjects who do not have suitable veins for multiple venepunctures/cannulation
  • Clinically significant abnormal clinical chemistry, haematology or urinalysis. Subjects with Gilbert's Syndrome are allowed.
  • Confirmed positive drugs of abuse test result
  • Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) antibody results
  • Evidence of renal impairment at screening, as indicated by an estimated creatinine clearance (CLcr) of <80 mL/min using the Cockcroft-Gault equation
  • History of clinically significant cardiovascular, renal, hepatic, dermatological, chronic respiratory or gastrointestinal disease, neurological or psychiatric disorder
  • Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients
  • Presence or history of clinically significant allergy requiring treatment. Hay fever is allowed unless it is active
  • Donation of blood or plasma within the previous 3 months or loss of greater than 400 mL of blood
  • Subjects who are taking, or have taken, any prescribed or over-the-counter drug or herbal remedies (other than up to 4 g of paracetamol per day) in the 14 days before IMP administration.
  • Failure to satisfy the investigator of fitness to participate for any other reason

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Carbon-14 BIA 28-6156Carbon-14 BIA 28-6156Healthy volunteers receive a single dose of Carbon-14 BIA 28-6156
Primary Outcome Measures
NameTimeMethod
Collection of plasma samples for metabolite profilingPre-dose until 240 hours post-dose

Collection of major metabolites for metabolite profiling of BIA28-6156

Collection of urine and faecal samples for total radioactivityUrine and Faeces: Pre-dose until 288 hours post-dose

Total radioactivity for total recovery of Carbon-14 BIA28-6156

Mass balance recovery of total radioactivity in all excreta (urine and faeces)Urine: Day 1 through Day 11, Faeces: Day -1 through Day 11

CumAe and Cum%Ae

Collection of plasma samples for structural identificationPre-dose until 240 hours post-dose

Identification of chemical structure of major metabolites of BIA28-6156

Collection of whole blood samples for total radioactivityPre-dose until 240 hours post-dose

Total radioactivity for total recovery of Carbon-14 BIA28-6156

Secondary Outcome Measures
NameTimeMethod
Determination of routes and rates of elimination of Carbon-14 BIA 28-6156Day 1 through Day 11
Identification of the chemical structure of each metabolite accounting for more than 10% by AUC of circulating plasma total radioactivity and more than 10% of total radioactive doseUrine and Faeces: Day 1 through Day 11, Plasma: Day 1 through Day 7
Measurement of BIA 28-6156 PK parametersDay 1 through Day 11
Evaluation of whole blood: plasma concentration ratios for total radioactivityDay 1 through Day 7
Adverse events (AEs)Screening through Day 11

Trial Locations

Locations (1)

Quotient Sciences

🇬🇧

Ruddington, Nottingham, United Kingdom

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