A Study to Evaluate the Absorption, Metabolism, and Excretion and Absolute Bioavailability of Xevinapant in Healthy Male Participants

Debiopharm International SA12 enrolled

Overview

The purpose of the study is to determine absorption, metabolism, and excretion of a single oral dose of \[14C\]-xevinapant. This information will enable assessment of absorption and clearance mechanisms of \[14C\]-xevinapant as well as identify metabolites. In addition, the study will allow to determine absolute bioavailability of xevinapant and understand its intravenous pharmacokinetics.

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

NONE

Enrollment

Conditions

Healthy Volunteers

Interventions

Radiolabelled Xevinapant 200 mg (Oral Solution)DRUG

\[14C\]-Xevinapant 200 mg administered as an oral solution on Day 1 of Part 1, containing approximately 100 microcurie (μCi) \[3.7 megabecquerel (MBq)\] in fasted conditions.

Radiolabelled Xevinapant 100 μg (IV Solution)DRUG

100 μg \[14C\]-xevinapant single dose administered as an IV bolus on Day 1, containing approximately 0.2 μCi \[7.4 kilobecquerel (kBq)\].

Xevinapant 200 mg (Oral Solution)DRUG

Xevinapant 200 mg administered as an oral solution on Day 1 of Part 2 in fasted conditions

Eligibility

Sex: MALEMin age: 18 YearsMax age: 65 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Part 1: Males of any race, between 35 and 65 years of age, inclusive. Part 2: Males of any race, between 18 and 65 years of age, inclusive * Body mass index between 18.0 and 30.0 kilograms per meter square (kg/m\^2), inclusive * Weight between 50 kilograms (kg) and 110 kg, inclusive * History of a minimum of 1 bowel movement per day. * Willing to adhere to the prohibitions and restrictions specified in the study protocol Exclusion Criteria: * Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, endocrine, or psychiatric disorder, as determined by the Investigator (or designee) * History of alcohol consumption of \>21 units per week. One unit of alcohol equals 12 ounce (oz) \[360 millilitre (mL)\] beer, 1½ oz (45 mL) liquor, or 5 oz (150 mL) wine. * Participation in a clinical study involving administration of an investigational drug (new chemical entity) in the past 90 days prior to dosing, or less than 5 times the half-life, whichever is longer, prior to administration of study drug * Poor peripheral venous access * Have participated in any clinical study involving a radiolabeled investigational product within 12 months prior to check-in.

Locations (1)

Labcorp Clinical Research Unit

Leeds, United Kingdom

Outcomes

Primary Outcomes

Mass Balance Recovery Measured Through Total Radioactivity Excreted in Expired Air, Urine and Feces

Time frame: Up to Day 29

Area Under Concentration-Time Curve From Time Zero to Infinity (AUC0-infinity); Time 0 to 24 Hours (AUC0-24); Time 0 to Last Quantifiable Concentration (AUC0-last) of Total Radioactivity in Blood and Plasma, and of Xevinapant and Metabolite in Plasma

Time frame: Up to Day 29

Maximum Observed Concentration (Cmax) of Total Radioactivity in Blood and Plasma, and of Xevinapant and Metabolite in Plasma

Time frame: Up to Day 29

Time to Maximum Observed Concentration (Tmax) of Total Radioactivity in Blood and Plasma, and of Xevinapant and Metabolite in Plasma

Time frame: Up to Day 29

Apparent Terminal Elimination Half-life (T1/2) of Total Radioactivity in Blood and Plasma, and of Xevinapant and Metabolite in Plasma

Time frame: Up to Day 29

Apparent Volume of Distribution During Terminal Phase (Vz/F) of Total Radioactivity in Blood and Plasma, and of Xevinapant and Metabolite in Plasma

Time frame: Up to Day 29

Apparent Total Clearance (CL/F) of Total Radioactivity in Blood and Plasma and of Xevinapant and Metabolite in Plasma

Time frame: Up to Day 29

Renal Clearance (CLr) of Total Radioactivity, Xevinapant and Metabolite

Time frame: Up to Day 29

Xevinapant Metabolite Concentrations in Urine, Feces, Blood and Plasma

Time frame: Up to Day 8

Absolute Bioavailability (F) of Xevinapant in Plasma

Data from ClinicalTrials.gov

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Secondary Outcomes

Blood to Plasma Ratio of Xevinapant and Metabolite

Time frame: Up to Day 8

Plasma Protein Binding Expressed as Fraction unbound, fu of Xevinapant

Time frame: Up to Day 8

Safety and Tolerability as Measured by Number of Participants With Treatment-Emergent Adverse Events

Time frame: Up to Day 29

Safety and Tolerability as Measured by Number of Participants With Clinically significant Laboratory Abnormalities

Time frame: Up to Day 29

Safety and Tolerability as Measured by Number of Participants With Clinically significant 12-lead ECG Parameters Abnormalities

Time frame: Up to Day 29

Safety and Tolerability as Measured by Number of Participants With Clinically significant Vital Signs Abnormalities

Time frame: Up to Day 29

Safety and Tolerability as Measured by Number of Participants With Clinically significant Physical Examination Abnormalities

Time frame: Up to Day 29