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Completed

NCT Number: NCT05110027

Enpatoran Human Mass Balance and Absolute Bioavailability Study

The purpose of Period 1 of this study is to provide a definitive quantitative characterization of the mass balance, and rates and routes of excretion of enpatoran, and to determine and quantify enpatoran and its metabolites in excreta (urine and feces) and plasma. The purpose of Period 2 of this study is to determine the absolute oral bioavailability of enpatoran. Total minimum duration of study participation for each participant is approximately 50 days.

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Key information

Conditions

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

PRA Health Sciences

Groningen, 9702, Netherlands

Who can participate

Healthy volunteers accepted: No

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

Inclusion criteria

  • Are overtly healthy as determined by medical evaluation, including medical history, physical examination, laboratory tests, and cardiac monitoring (blood pressure, heart rate and 12-lead electrocardiogram)
  • Have a body weight within 50 to 110 kilogram (kg) and Body mass index (BMI) within the range ≥ 18.0 and ≤ 30.0 kilogram per meter square (kg/m^2)
  • Other protocol defined inclusion criteria could apply

Exclusion criteria

  • History or presence of clinically relevant respiratory, gastrointestinal, renal, hepatic, hematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, connective tissue diseases or disorders
  • Prior history of cholecystectomy or splenectomy, and any clinically relevant surgery within 6 months prior to Screening
  • Any surgical or medical condition which might significantly alter the absorption, distribution, metabolism and excretion (ADME) of drugs, or which may jeopardize the participant in case of participation in the study
  • History of any malignancy
  • History or presence of epilepsy, neurological disorders with seizure propensity or undiagnosed loss of consciousness, severe head trauma within 6 months or severe depression within 12 months prior to Screening), or neuropsychiatric conditions
  • History of chronic or recurrent acute infection or any bacterial, viral, parasitic or fungal infections within 30 days prior to Screening and at any time between Screening and admission, or hospitalization due to infection within 6 months prior to Screening, or a history of herpes zoster within 12 months prior to Screening.
  • History of drug hypersensitivity ascertained or presumptive allergy/hypersensitivity to the active drug substance and/or formulation ingredients; history of serious allergic reactions leading to hospitalization or any other hypersensitivity reaction in general, which may affect the safety of the participant and/or outcome of the study per the Investigator's discretion
  • History of alcoholism or drug abuse within 1 year prior to Screening, or evidence of such abuse as indicated by the laboratory assays conducted during Screening
  • Any condition, including findings in the laboratory tests, medical history, or other Screening assessments, that in the opinion of the Investigator constitutes an inappropriate risk or a contraindication for participation in the study or that could interfere with the study's objectives, conduct, or evaluation
  • Other protocol defined exclusion criteria could apply

Treatment and study plan

Enpatoran

Drug

Participants will receive single oral dose of enpatoran tablet on Day 1

[14C]enpatoran microtracer

Drug

Participants will receive single oral dose of non-labeled enpatoran solution spiked with microtracer of [14C]enpatoran on Day 1 of Period 1.

[14C]enpatoran microdose

Drug

Participants will receive intravenous [14C]enpatoran microdose administered at 1.5 hours after the oral dose of enpatoran on Day 1 of Period 2.

Primary outcomes

  1. Period 1: Percent Urinary Recovery (feurine) of Total Radioactivity per Sampling Interval

    Time frame: -24-0 hours (pre-dose), 0-4, 4-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours after the initiation of the intravenous (IV) dose

  2. Period 1: Percent Fecal Recovery (fefeces) of Total Radioactivity per Sampling Interval

    Time frame: -24-0 hours (pre-dose), 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours after the initiation of the intravenous (IV) dose

  3. Period 1: Percent Total Recovery in Urine and Feces (fetotal) of Total Radioactivity per Sampling Interval

    Time frame: Urine: -24-0 hours (pre-dose), 0-4, 4-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours post-dose; Feces: -24-0 hours (pre-dose), 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, and 144-168 hours post-dose of IV injection

  4. Period 1: Pharmacokinetic Plasma and Blood Concentration of Total Radioactivity

    Time frame: Pre-dose (Day 1), 15, 30 minutes, 1, 1.5, 2.0, 4.0, 6.0, 8.0, 12, 24, 48, 72, 96, 120, 144, 168 hours post-dose

  5. Period 1: Pharmacokinetic Plasma Concentration of Enpatoran

    Time frame: Pre-dose (Day 1), 15, 30 minutes, 1, 1.5, 2.0, 4.0, 6.0, 8.0, 12, 24, 48, 72, 96, 120, 144, 168 hours post-dose

  6. Period 2: Pharmacokinetic Plasma and Blood Concentration of [14C]Enpatoran and Enpatoran

    Time frame: [14C]Enpatoran: Pre-dose, 5, 15, 30 minutes, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose; Enpatoran: Pre-dose, 30 minutes, 2, 4, 6, 8, 12, 24, 48, 72 hours post-dose

Secondary outcomes

  1. Period 1 and 2: Safety Profile as Assessed by Incidence of Treatment-Emergent Adverse Events (AEs), Serious Adverse Events (SAEs), Laboratory Variables, Vital Signs and Electrocardiogram (ECG) Measurements

    Time frame: Period 1: Baseline up to Day 14; Period 2: Baseline up to Day 4

Sponsors and collaborators

Lead sponsor

Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany

Industry

Registry information

Official study title

Phase I, Open-Label, 2-Period, Single-Sequence Study to Evaluate the Mass Balance and Absorption, Disposition, Metabolism and Excretion of [14C]Enpatoran, and the Absolute Bioavailability of Enpatoran in Healthy Male Participants

Important dates

Study start
2021
Primary completion
2021
Study completion
2021
First posted
Nov 5, 2021
Registry last updated
Apr 4, 2022

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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