Study of M5049 in Healthy Japanese and Caucasian Participants

NCT04880213 | Completed Phase 1

• 2 other identifiers: MS200569_00052020-005408-20
• Study Type: interventional
• Target: 36
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to evaluate and determine the safety, tolerability and pharmacokinetics of single-doses of M5049 up to 3 dose levels administered as film-coated tablet under fasted conditions in healthy Japanese and Caucasian participants.

Conditions

Healthy

Keywords

Healthy; M5049; Japanese; Caucasian

Outcome Measures

Primary Outcomes (7)

• Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Sampling Time (tlast) (AUC0-tlast) of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

• Area Under Plasma Concentration-Time Curve from Time Zero Extrapolated to Infinity (AUC0-inf) of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

• Maximum Observed Plasma Concentration (Cmax) of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

• Number of Participants with Treatment-Emergent Adverse Events (TEAEs), Serious TEAEs and TEAEs Leading to Death

  Baseline up to Day 8

• Number of Participants with Clinically Significant Changes from Baseline in Laboratory Parameters

  Baseline up to Day 3

• Number of Participants with Clinically Significant Changes from Baseline in Vital Signs

  Baseline up to Day 3

• Number of Participants with Clinically Significant Changes from Baseline in 12-lead Electrocardiogram (ECGs) Findings

  Baseline up to Day 3

Secondary Outcomes (5)

• Area Under the Plasma Concentration-Time Curve From Time Zero to 48 Hours Post-dose (AUC0-48) of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

• Time to Reach Maximum Plasma Concentration (tmax) of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

• Terminal Half-life (t1/2) of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

• Apparent Total Body Clearance (CL/f) of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

• Apparent Volume of Distribution (Vz/f) During Terminal Phase of M5049

  Pre-dose, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, 6, 8, 12, 24, 36 and 48 hours post-dose

Study Arms (6)

Japanese: M5049 Dose A (low dose)

EXPERIMENTAL

Drug: M5049

Japanese: M5049 Dose B (medium dose)

EXPERIMENTAL

Drug: M5049

Japanese: M5049 Dose C (high dose)

EXPERIMENTAL

Drug: M5049

Caucasian: M5049 Dose A (low dose)

EXPERIMENTAL

Drug: M5049

Caucasian: M5049 Dose B (medium dose)

EXPERIMENTAL

Drug: M5049

Caucasian: M5049 Dose C (high dose)

EXPERIMENTAL

Drug: M5049

Interventions

M5049 DRUG

Participants will receive single oral dose of film-coated tablet M5049 at low dose on Day 1 under fasted condition.

Caucasian: M5049 Dose A (low dose); Japanese: M5049 Dose A (low dose)

Eligibility Criteria

• Age: 20 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Japanese participants must be first generation (born in Japan) with both biological parents and all 4 biological grandparents being Japanese native born. Caucasian participants must have both biological parents and 4 biological grandparents of Caucasian descent
• Overtly healthy participants as determined by medical evaluation, including medical history, physical examination, laboratory tests, and cardiac monitoring (blood pressure, heart rate and 12-Lead resting ECG)
• Participants with body weight within 45 to 90 kilograms (kg) (female) and 55 to 90 kg (male) and body mass index (BMI) between 18.5 and 29.9 kilograms per meter square (kg/m\^2)
• A Caucasian participant will be matched by body weight (± 20% body weight \[kg\]), height (± 15% height \[centimeter (cm) \]) and sex to each Japanese participant

You may not qualify if:

• Participants with history of clinically relevant disease of any organ system that may interfere with the objectives of the study or provide a risk to the health of the participant
• Participants with history of relevant drug hypersensitivity
• Participants with history of splenectomy, epilepsy, other neurological disorders or neuropsychiatric conditions
• Participants with history of a tuberculosis and positive Screening test for hepatitis B surface antigen
• Participants with history of alcoholism or drug abuse

Sponsors & Collaborators

• Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany: lead

Study Sites (1)

Covance Clinical Research Unit Ltd.

Leeds, United Kingdom

Location

Related Publications (1)

• Klopp-Schulze L, Gopalakrishnan S, Yalkinoglu O, Kuroki Y, Lu H, Goteti K, Krebs-Brown A, Nogueira Filho M, Gradhand U, Fluck M, Shaw J, Dong J, Venkatakrishnan K. Asia-Inclusive Global Development of Enpatoran: Results of an Ethno-Bridging Study, Intrinsic/Extrinsic Factor Assessments and Disease Trajectory Modeling to Inform Design of a Phase II Multiregional Clinical Trial. Clin Pharmacol Ther. 2024 Jun;115(6):1346-1357. doi: 10.1002/cpt.3216. Epub 2024 Feb 28.

  PMID: 38415785 DERIVED

Related Links

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

Study Officials

• Medical Responsible

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

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 5, 2021
• First Posted: May 10, 2021
• Study Start: May 6, 2021
• Primary Completion: November 23, 2021
• Study Completion: November 23, 2021
• Last Updated: April 6, 2022

Record last verified: 2022-03

Data Sharing

• IPD Sharing: Will not share

Locations

GB (1)