PK Study of Xevinapant (Debio 1143) in Healthy East Asian Participants

NCT05519540 | Completed Phase 1 Results

• 2 other identifiers: MS202359_00042022-002182-15
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study was to evaluate the pharmacokinetics (PK) of Xevinapant (Debio 1143) and its metabolite D-1143-MET1 as well as safety and tolerability of Xevinapant (Debio 1143) in healthy East Asian participants.

Conditions

Healthy

Keywords

East Asian; Japanese; Pharmacokinetic; Ethnic sensitivity

Outcome Measures

Primary Outcomes (3)

• Area Under the Plasma Concentration-Time Curve From Time Zero to Last Sample Time (AUC0-tlast) of Xevinapant (Debio 1143)

  The area under the concentration-time curve (AUC) from time zero (= dosing time) to the last sampling time (tlast) at which the concentration is at or above the lower limit of quantification. Calculated using the mixed log-linear trapezoidal rule (linear up, log down).

  Predose, 0.25, 0.5, 1.0, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 , 36, 48 and 72 hours postdose

• Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC0-inf) of Xevinapant (Debio 1143)

  The AUC from time zero (dosing time) extrapolated to infinity, based on the predicted value for the concentration at t last , as estimated using the linear regression from Terminal first order (elimination) rate constant (Lambda z) determination. AUC0-inf = AUC0-t plus Clast pred/lambda z. Lambda Z was terminal elimination rate constant determined from the terminal slope of the log-transformed plasma concentration curve using linear regression on terminal data points of the curve.

  Predose, 0.25, 0.5, 1.0, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 , 36, 48 and 72 hours postdose

• Maximum Observed Plasma Concentration (Cmax) of Xevinapant (Debio 1143)

  Cmax was obtained directly from concentration versus time curve.

  Predose, 0.25, 0.5, 1.0, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24 , 36, 48 and 72 hours postdose

Secondary Outcomes (19)

• Number of Participants With Treatment-Emergent Adverse Events (TEAEs), Serious TEAEs, and Related TEAE's

  Up to Day 8

• Number of Participants With Treatment Emergent Adverse Events (TEAEs) by Severity

  Baseline (Day 1) up to Day 8

• Number of Participants With Clinically Significant Changes From Baseline in Laboratory Values

  Baseline (Day 1) up to Day 8

• Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings

  Baseline (Day 1) up to Day 8

• Number of Participants With Clinically Significant Change From Baseline in Vital Signs

  Baseline (Day 1) up to Day 8

Study Arms (2)

Group 1: Japanese Participants: Xevinapant (Debio 1143)

EXPERIMENTAL

Xevinapant (Debio 1143) was administered in Healthy Japnaese participants at a dose of 200 milligrams (mg), orally under fasted conditions.

Drug: Xevinapant (Debio 1143)

Group 2: Non-Japanese East Asian Participants: Xevinapant (Debio 1143)

EXPERIMENTAL

Xevinapant (Debio 1143) was administered in Healthy Non- Japanese participants at a dose of 200 mg, orally under fasted conditions.

Drug: Xevinapant (Debio 1143)

Interventions

Xevinapant (Debio 1143) DRUG

All participants (Japanese and non-Japanese) received a single oral dose of 200mg xevinapant (Debio 1143) on Day 1 under fasted condition.

Group 1: Japanese Participants: Xevinapant (Debio 1143); Group 2: Non-Japanese East Asian Participants: Xevinapant (Debio 1143)

Eligibility Criteria

• Age: 18 Years - 60 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy participant of Japanese or other East Asian origin. Group 1: Japanese participants must be first generation (born in Japan) with both biological parents and all 4 biological grandparents being Japanese native born, lived for less than (\<)10 years outside of Japan, and have no significant change in lifestyle since leaving Japan. Group 2: Other non-Japanese East Asian participants must have both biological parents and 4 biological grandparents of East Asian descent, lived for \<10 years outside of their countries, and have no significant change in lifestyle since leaving from there. East Asia includes Korea or Greater China
• 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)
• Have a body weight within 50 and 110 kilograms \[kg\] (inclusive) and Body Mass Index (BMI) within the range 18.0 to 32.0 kilograms per meter square \[Kg/m\^2\] (inclusive)

You may not qualify if:

• 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
• History of relevant 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 allergy reaction in general, which the Investigator considers may affect the safety of the participant and/or outcome of the study
• History of splenectomy
• History of any malignancy (hematologic or solid tumor) before the Screening Visit, except for adequately treated superficial basal cell carcinoma of the skin (no more than 3 lesions requiring treatment in lifetime) or carcinoma in situ/cervical intraepithelial neoplasia of the uterine cervix
• History of or a positive screening test for hepatitis B, hepatitis C, or human immunodeficiency virus type I and II
• Use of any investigational drug in any clinical study within 5 half-lives from last administration

Sponsors & Collaborators

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

Study Sites (1)

Labcorp Clinical Research Unit Limited

Leeds, United Kingdom

Location

Related Links

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

MeSH Terms

Interventions

N-benzhydryl-5-(2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo(1,2-a)(1,5)diazocine-8-carboxamide

Results Point of Contact

• Title: Communication Center
• Organization: Merck Healthcare KGaA, Darmstadt Germany, an affiliate of Merck KGaA, Darmstadt, Germany

service@emdgroup.com

+49-6151-72-5200

Study Officials

• Medical Responsible

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

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restrictive Agreement: Yes

Study Design

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

Study Record Dates

• First Submitted: August 25, 2022
• First Posted: August 29, 2022
• Study Start: September 26, 2022
• Primary Completion: April 21, 2023
• Study Completion: April 21, 2023
• Last Updated: August 20, 2025
• Results First Posted: August 20, 2025

Record last verified: 2024-07

Data Sharing

• IPD Sharing: Will not share

Locations

GB (1)