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

An Open Label, Single-dose, Single-period Study Designed to Assess the Mass Balance Recovery, Metabolite Profile and Metabolite Identification of Carbon-14 BIA 28-6156 in Healthy Male Subjects

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.

Study Overview

• Status: Completed
• Conditions: Parkinson Disease
• Intervention / Treatment: Drug: Carbon-14 BIA 28-6156

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.

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Nottingham
    • Ruddington, Nottingham, United Kingdom, NG11 6JS
      • Quotient Sciences

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 26 years to 61 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes

Description

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 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: Carbon-14 BIA 28-6156; Healthy volunteers receive a single dose of Carbon-14 BIA 28-6156	Drug: Carbon-14 BIA 28-6156; Carbon-14 BIA 28-6156 60 mg, containing NMT 3.7 MBq Carbon-14

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Mass balance recovery of total radioactivity in all excreta (urine and faeces)	CumAe and Cum%Ae	Urine: Day 1 through Day 11, Faeces: Day -1 through Day 11
Collection of urine and faecal samples for total radioactivity	Total radioactivity for total recovery of Carbon-14 BIA28-6156	Urine and Faeces: Pre-dose until 288 hours post-dose
Collection of plasma samples for metabolite profiling	Collection of major metabolites for metabolite profiling of BIA28-6156	Pre-dose until 240 hours post-dose
Collection of plasma samples for structural identification	Identification of chemical structure of major metabolites of BIA28-6156	Pre-dose until 240 hours post-dose
Collection of whole blood samples for total radioactivity	Total radioactivity for total recovery of Carbon-14 BIA28-6156	Pre-dose until 240 hours post-dose

Secondary Outcome Measures

Outcome Measure	Time Frame
Determination of routes and rates of elimination of Carbon-14 BIA 28-6156	Day 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 dose	Urine and Faeces: Day 1 through Day 11, Plasma: Day 1 through Day 7
Measurement of BIA 28-6156 PK parameters	Day 1 through Day 11
Evaluation of whole blood: plasma concentration ratios for total radioactivity	Day 1 through Day 7
Adverse events (AEs)	Screening through Day 11

Collaborators and Investigators

• Sponsor: Bial R&D Investments, S.A.
• Investigators: Principal Investigator: Somasekhara Menakuru, MBBS,MS,MRCS,DPM,MFPM, Quotient Sciences

Study record dates

Study Major Dates

• Study Start (Actual): August 28, 2021
• Primary Completion (Actual): October 16, 2021
• Study Completion (Actual): October 16, 2021

Study Registration Dates

• First Submitted: November 18, 2021
• First Submitted That Met QC Criteria: January 25, 2022
• First Posted (Actual): February 2, 2022

Study Record Updates

• Last Update Posted (Actual): May 28, 2025
• Last Update Submitted That Met QC Criteria: May 22, 2025
• Last Verified: May 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Synucleinopathies; Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Neurodegenerative Diseases; Movement Disorders; Parkinsonian Disorders; Basal Ganglia Diseases; Parkinson Disease
• Other Study ID Numbers: BIA 28-6156-106

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No