Phase 1
Completed N=24
PK Study of Xevinapant (Debio 1143) in Healthy East Asian Participants
Healthy
Source: ClinicalTrials.gov NCT05519540 ↗
Enrolled (actual)
24
Serious AEs
0.0%
Results posted
Aug 2025
Primary outcomePrimary: Area Under the Plasma Concentration-Time Curve From Time Zero to Last Sample Time (AUC0-tlast) of Xevinapant (Debio 1143) — 9780; 10200 hours*nanogram per milliliter (h*ng/mL)
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero to Last Sample Time (AUC0-tlast) of Xevinapant (Debio 1143) |
9780; 10200 | — |
| PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC0-inf) of Xevinapant (Debio 1143) |
9860; 10200 | — |
| PRIMARY Maximum Observed Plasma Concentration (Cmax) of Xevinapant (Debio 1143) |
2070; 2160 | — |
| SECONDARY Number of Participants With Treatment-Emergent Adverse Events (TEAEs), Serious TEAEs, and Related TEAE's |
3; 5; 0; 0; 2; 1 | — |
| SECONDARY Number of Participants With Treatment Emergent Adverse Events (TEAEs) by Severity |
3; 4; 0; 1; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Changes From Baseline in Laboratory Values |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings |
0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Change From Baseline in Vital Signs |
0; 0 | — |
| SECONDARY Area Under Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24) of Xevinapant (Debio 1143) |
9160; 9460 | — |
| SECONDARY Time to Reach Maximum Observed Plasma Concentration (Tmax) of Xevinapant (Debio 1143) |
0.750; 1.00 | — |
| SECONDARY Apparent Terminal Half-Life (t1/2) of Xevinapant (Debio 1143) |
9.38; 10.5 | — |
| SECONDARY Apparent Clearance (CL/f) of Xevinapant (Debio 1143) |
20.3; 19.6 | — |
| SECONDARY Apparent Volume of Distribution During Terminal Phase (Vz/f) of Xevinapant (Debio 1143) |
274; 296 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t Last) of Metabolite D-1143-MET1 |
13800; 14400 | — |
| SECONDARY Area Under Plasma Concentration-Time Curve From Time Zero to 24 Hours (AUC0-24) of Metabolite D-1143-MET1 |
13000; 13400 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC0-inf) of Metabolite D-1143-MET1 |
13800; 14500 | — |
| SECONDARY Maximum Observed Plasma Concentration (Cmax) of Metabolite D-1143-MET1 |
1240; 1240 | — |
| SECONDARY Time to Reach Maximum Observed Plasma Concentration (Tmax) of Metabolite D-1143-MET1 |
3.00; 3.00 | — |
| SECONDARY Apparent Terminal Half-Life (t1/2) of Metabolite D-1143-MET1 |
5.23; 7.30 | — |
| SECONDARY Metabolite-to-parent Molar Ratio for AUC0-t (MR_AUC0-t) of Xevinapant and D-1143-MET1 |
1.66; 1.68 | — |
| SECONDARY Metabolite-to-parent Molar Ratio for AUC0-inf (MR_AUC0-inf) of Xevinapant and D-1143-MET1 |
1.65; 1.67 | — |
| SECONDARY Metabolite-to-parent Molar Ratio for Cmax (MR_Cmax) of Xevinapant and D-1143-MET1 |
0.704; 0.679 | — |
Eligibility Criteria
Inclusion Criteria
- 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)
- Other protocol defined inclusion criteria could apply
Exclusion Criteria
- 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
- Ongoing or active clinically significant viral (including Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)), bacterial or fungal infection, or any major episode of infection requiring hospitalization or treatment with parenteral anti-infectives less than or equal to (<=) 4 weeks prior to or during Screening Period, or completion of oral anti-infectives <= 2 weeks prior to Screening Visit. Vaginal candidiasis, onychomycosis, and genital or oral herpes simplex virus considered to be sufficiently controlled will not be exclusionary
- 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
- Other protocol defined exclusion criteria could apply
Data sourced from ClinicalTrials.gov (NCT05519540). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.