Human Absorption, Distribution, Metabolism and Excretion (ADME) of [14C]-Evobrutinib

NCT03725072 | Completed Phase 1

• 2 other identifiers: MS200527_00752018-003371-35
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of the study is to determine the absorption, metabolism, and excretion of \[14C\]-evobrutinib in healthy participants

Conditions

Healthy

Keywords

[14C]-evobrutinib; Healthy; Pharmacokinetics; Metabolism; Excretion

Outcome Measures

Primary Outcomes (13)

• Total Radioactivity Recovery Rate of Evobrutinib, Total Radioactivity and its Metabolites

  Pre-dose up to Day 35 post-dose

• Percentage Excretion of Evobrutinib, Total Radioactivity and its Metabolites in Urine and Feces

  Pre-dose up to Day 35 post-dose

• Renal Clearance of Evobrutinib, Total Radioactivity and its Metabolites

  Pre-dose up to Day 35 post-dose

• Maximum Observed Plasma Concentration (Cmax) of Total [14C] Radioactivity (Evobrutinib and Metabolites)

  Pre-dose up to Day 35 post-dose

• Time to Reach Maximum Plasma Concentration (Tmax) of Total [14C] Radioactivity (Evobrutinib and Metabolites)

  Pre-dose up to Day 35 post-dose

• Terminal Elimination Half-Life (t1/2) of Total [14C] Radioactivity (Evobrutinib and Metabolites)

  Pre-dose up to Day 35 post-dose

• Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Total [14C] Radioactivity (Evobrutinib and Metabolites)

  Pre-dose up to Day 35 post-dose

• Maximum Observed Plasma Concentration (Cmax) of Evobrutinib

  Pre-dose up to Day 35 post-dose

• Time to Reach Maximum Plasma Concentration (Tmax) of Evobrutinib

  Pre-dose up to Day 35 post-dose

• Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Evobrutinib

  Pre-dose up to Day 35 post-dose

• Terminal Elimination Half-Life (t1/2) of Evobrutinib

  Pre-dose up to Day 35 post-dose

• Apparent Volume of Distribution During Terminal Phase (Vz/f) of Evobrutinib

  Pre-dose up to Day 35 post-dose

• Apparent Clearance (CL/f) of Evobrutinib

  Pre-dose up to Day 35 post-dose

Secondary Outcomes (3)

• Number of Participants with Clinically Significant Change From Baseline in Vital Signs, Laboratory Parameters and Electrocardiogram Findings

  From time of first dose to end of study participation approximately at Day 37

• Occurrence of Treatment -emergent Adverse Events (TEAEs) and Serious TEAEs

  From time of first dose to end of study participation approximately at Day 37

• Occurrence of Treatment -emergent Adverse Events (TEAEs) and Serious TEAEs by Severity

  From time of first dose to end of study participation approximately at Day 37

Study Arms (1)

Evobrutinib

EXPERIMENTAL

Drug: Evobrutinib

Interventions

Evobrutinib DRUG

Participants will receive a single, oral dose of evobrutinib under fasting conditions as a solution, which will contain \[14C\]-evobrutinib.

Also known as: M2951

Evobrutinib

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants are overtly healthy as determined by medical evaluation, including medical history, physical examination, laboratory tests, and cardiac monitoring
• Have a body weight within 50.0 to 120.0 kilogram (kg) (inclusive) and body mass index within the range 19.0 - 30.0 kilogram per meter square (kg/m\^2) (inclusive)
• Male participants agree to be consistent with local regulations on contraception methods
• Can give signed informed consent

You may not qualify if:

• 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
• Any surgical or medical condition which might significantly alter the ADME of drugs
• History of any malignancy, chronic or recurrent acute infection
• History of shingles
• History of drug hypersensitivity ascertained or presumptive allergy/hypersensitivity to the active drug substance and/or formulation ingredients
• History of alcoholism or drug abuse
• History of residential exposure to tuberculosis, or a positive QuantiFERON test at screening
• Administration of live vaccines or live-attenuated virus vaccines
• 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
• Prior/concomitant therapy
• Relevant radiation exposure
• Clinically relevant findings (excluding minor deviations) in biochemistry, hematology, coagulation and urinalysis
• Vital signs (pulse rate and blood pressure) outside the normal range
• Estimated Glomerular Filtration rate according to the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI)

Sponsors & Collaborators

• Merck KGaA, Darmstadt, Germany: lead

Study Sites (1)

PRA Health Sciences

Groningen, 9728 NZ, Netherlands

Location

Related Links

• Trial Awareness and Transparency website
• Medical Information Location Map - Med Info Contacts

MeSH Terms

Interventions

evobrutinib

Study Officials

• Medical Responsible

  Merck KGaA, Darmstadt, Germany

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 29, 2018
• First Posted: October 30, 2018
• Study Start: October 30, 2018
• Primary Completion: December 5, 2018
• Study Completion: December 5, 2018
• Last Updated: July 7, 2020

Record last verified: 2020-07

Locations

NL (1)