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

Phase 1

Completed

• Conditions: Healthy Volunteers
• Interventions: Drug: 14C-XEN1101

• Registration Number: NCT04952467
• Lead Sponsor: Xenon Pharmaceuticals Inc.

Brief Summary

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.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2021-06-27
• Study First Submitted QC: 2021-06-27
• Study First Posted: 2021-07-07
• Study Start: 2021-07-14
• Primary Completion: 2021-10-04
• Study Completion: 2021-10-04
• Status Verified: 2022-01
• Last Update Submitted: 2022-01-13
• Last Update Posted: 2022-01-14

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 6

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 & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
Drug: (14C)-XEN1101	14C-XEN1101	Subjects will receive oral 14C-XEN1101 under fed conditions.

Primary Outcome Measures

Name	Time	Method
Total radioactivity excreted in urine and faeces following oral administration of XEN1101	From Screening up to Day 57 post-dose	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

Secondary Outcome Measures

Name	Time	Method
Plasma whole blood concentration ratios for total radioactivity	From Screening up to Day 57 post-dose	Evaluation of whole blood:plasma concentration ratios for total radioactivity for corresponding time points
Pharmacokinetic (PK) data for 14C-XEN1101; Tmax	From Screening up to Day 57 post-dose	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
PK data for 14C-XEN1101; Cmax	From Screening up to Day 57 post-dose	Maximum observed concentration for XEN1101 and metabolites in plasma and for total radioactivity in plasma and whole blood following oral administration of 14C-XEN1101
14C Metabolite profiling in of plasma, urine and feces	From Screening up to Day 57 post-dose	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
PK data for 14C-XEN1101; T1/2	From Screening up to Day 57 post-dose	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
Mass balance data for 14C-XEN1101 in urine	From Screening up to Day 57 post-dose	CumAe(urine)expressed as a percentage of the radioactive dose administered (Cum%Ae(urine))
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
Mass balance data for 14C-XEN1101 in feces	From Screening up to Day 57 post-dose	CumAe(feces) expressed as a percentage of the radioactive dose administered Cum%Ae(feces)

Trial Locations

Locations (1)

Quotient Sciences; 🇬🇧 Ruddington, Nottingham, United Kingdom