Single-dose Mass Balance Recovery and Metabolite Profile and Identification of 14C-XEN1101

An Open Label, Single-dose, Single-period Study to Assess the Pharmacokinetics, Mass Balance Recovery, Metabolite Profile and Metabolite Identification of 14C-XEN1101 in Healthy Male Subjects

This study will evaluate the mass balance recovery and metabolite profile, and will identify metabolite structures following a single oral dose of 14C-XEN1101 in healthy adult male subjects.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: 14C-XEN1101

• 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: 30 years to 65 years (ADULT, OLDER_ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Key Inclusion Criteria:

• Body mass index (BMI) of 18.0 to 32.0 kg/m2
• Must be willing and able to communicate and participate in the whole study
• Provide written informed consent
• Adhere to the specified contraception requirements

Key Exclusion Criteria:

• Subjects who have received any investigational medicinal product (IMP) in a clinical research study within 90 days
• Evidence of any current infection or an infection within 14 days before study drug administration
• History of any drug or alcohol abuse in the past 2 years
• 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 millisievert (mSv) in the last 12 months or 10 mSv in the last 5 years. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 2017, shall participate in the study
• Participation in a clinical trial involving administration of radiolabelled compound(s) within 180 days of the planned dosing date of this study
• Clinically significant abnormal clinical chemistry, haematology, coagulation or urinalysis. Subjects with Gilbert's Syndrome will be excluded.
• 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
• History of clinically significant cardiovascular, renal, hepatic, dermatological, chronic respiratory or gastrointestinal disease, neurological or psychiatric disorder
• Donation of blood or plasma within the previous 3 months or loss of greater than 400 mL of blood

Study Plan

How is the study designed?

Design Details

• Primary Purpose: BASIC_SCIENCE
• Allocation: NA
• Interventional Model: SINGLE_GROUP
• Masking: NONE

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Drug: (14C)-XEN1101; Subjects will receive oral 14C-XEN1101 under fed conditions.	Drug: 14C-XEN1101; Subjects will receive a single oral administration of a capsule containing 20 mg XEN1101

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Total radioactivity excreted in urine and faeces following oral administration of XEN1101	Cumulative amount of total radioactivity excreted in urine and feces combined (CumAe(total)) and expressed as a % of the radioactive dose administered (Cum%Ae(total)) following oral administration of 14C-XEN1101	From Screening up to Day 57 post-dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
14C Metabolite profiling in of plasma, urine and feces	Chemical structure of each metabolite classified as >10% (by AUC) of total radioactivity in plasma and >10% dose excreted in urine and faeces following oral administration of XEN1101	From Screening up to Day 57 post-dose
Pharmacokinetic (PK) data for 14C-XEN1101; Tmax	Time of maximum observed concentration for XEN1101 and metabolites in plasma and for total radioactivity in plasma and whole blood following oral administration of 14C-XEN1101	From Screening up to Day 57 post-dose
PK data for 14C-XEN1101; Cmax	Maximum observed concentration for XEN1101 and metabolites in plasma and for total radioactivity in plasma and whole blood following oral administration of 14C-XEN1101	From Screening up to Day 57 post-dose
PK data for 14C-XEN1101; T1/2	Terminal elimination half-life for XEN1101 and metabolites in plasma and for total radioactivity in plasma and whole blood following oral administration of 14C-XEN1101	From Screening up to Day 57 post-dose
Mass balance data for 14C-XEN1101 in urine	CumAe(urine)expressed as a percentage of the radioactive dose administered (Cum%Ae(urine))	From Screening up to Day 57 post-dose
Mass balance data for 14C-XEN1101 in feces	CumAe(feces) expressed as a percentage of the radioactive dose administered Cum%Ae(feces)	From Screening up to Day 57 post-dose
Plasma whole blood concentration ratios for total radioactivity	Evaluation of whole blood:plasma concentration ratios for total radioactivity for corresponding time points	From Screening up to Day 57 post-dose
Frequency and severity of treatment-emergent adverse events (TEAEs), treatment-emergent serious adverse events (SAEs), and TEAEs leading to treatment discontinuations		From Screening up to Day 57 post-dose

Collaborators and Investigators

• Sponsor: Xenon Pharmaceuticals Inc.

Study record dates

Study Major Dates

• Study Start (ACTUAL): July 14, 2021
• Primary Completion (ACTUAL): October 4, 2021
• Study Completion (ACTUAL): October 4, 2021

Study Registration Dates

• First Submitted: June 27, 2021
• First Submitted That Met QC Criteria: June 27, 2021
• First Posted (ACTUAL): July 7, 2021

Study Record Updates

• Last Update Posted (ACTUAL): January 14, 2022
• Last Update Submitted That Met QC Criteria: January 13, 2022
• Last Verified: January 1, 2022

More Information

Terms related to this study

• Keywords: Phase 1; Mass Balance; XEN1101
• Other Study ID Numbers: XPF-008-103; 2021-000735-32 (EUDRACT_NUMBER)

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
• product manufactured in and exported from the U.S.: Yes