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OpenTrials
Completed

NCT Number: NCT04962724

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

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.

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Key information

Conditions

Age range

18 year–65 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

Labcorp Clinical Research Unit

Leeds, LS2 9LH, United Kingdom

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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.

Treatment and study plan

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

Primary outcomes

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

    Time frame: Up to Day 29

  2. 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

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

    Time frame: Up to Day 29

  4. 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

  5. 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

  6. 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

  7. 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

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

    Time frame: Up to Day 29

  9. Xevinapant Metabolite Concentrations in Urine, Feces, Blood and Plasma

    Time frame: Up to Day 8

  10. Absolute Bioavailability (F) of Xevinapant in Plasma

    Time frame: Up to Day 5

    Absolute Bioavailability (F) = (AUC0-infinity [oral]/ dose [oral]) /(AUC0-infinity [IV]/ dose [IV])

Secondary outcomes

  1. Blood to Plasma Ratio of Xevinapant and Metabolite

    Time frame: Up to Day 8

  2. Plasma Protein Binding Expressed as Fraction unbound, fu of Xevinapant

    Time frame: Up to Day 8

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

    Time frame: Up to Day 29

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

    Time frame: Up to Day 29

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

    Time frame: Up to Day 29

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

    Time frame: Up to Day 29

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

    Time frame: Up to Day 29

Sponsors and collaborators

Lead sponsor

Debiopharm International SA

Industry

Registry information

Official study title

A Phase 1, Open-label, 2-part, Single-dose Study of the Absorption, Metabolism, and Excretion of Oral [14C]-Xevinapant, and Absolute Oral Bioavailability of Xevinapant in Healthy Male Subjects

Important dates

Study start
2021
Primary completion
2021
Study completion
2021
First posted
Jul 15, 2021
Registry last updated
Dec 27, 2021

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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