A Clinical Study of MK-4482 in Chinese Healthy Male Participants (MK-4482-009)

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: MK-4482

• Registration Number: NCT06816030
• Lead Sponsor: Merck Sharp & Dohme LLC

Brief Summary

The goal of the study is to learn what happens to MK-4482 after single and multiple doses in healthy Chinese participants over time. Researchers also want to learn about the safety of MK-4482, including how well people tolerate it.

Detailed Description

Not available

Study Timeline

• Study Start: 2023-06-28
• Primary Completion: 2023-08-05
• Study Completion: 2023-08-05
• Status Verified: 2025-02
• Study First Submitted: 2025-02-04
• Study First Submitted QC: 2025-02-04
• Last Update Submitted: 2025-02-04
• Study First Posted: 2025-02-10
• Last Update Posted: 2025-02-10

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 16

Inclusion Criteria

The main inclusion criteria include but are not limited to the following:

• Has a Body Mass Index (BMI) of 19 to 24 weight (kg)/height (m)2, inclusive, and body weight of ≥ 50 kg at the screening visit.

Exclusion Criteria

The main exclusion criteria include but are not limited to the following:

• Has a history of clinically significant abnormalities or diseases.
• Has history of cancer.
• Has a history of significant multiple and/or severe allergies.
• Had any major surgery.
• Has participated in another investigational study within 3 months prior to the screening visit.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
MK-4482	MK-4482	Participants in period 1 received, MK-4482 800 mg single oral dose in the morning on Day 1. Participants in period 2 received, MK-4482 800mg oral dose administered every 12 hours (Q12H) on Day 1 through Day 6 for11 doses.

Primary Outcome Measures

Name	Time	Method
Elimination Half Life (T1/2) After Single Oral Dose of MK-4482 in Period 1	At designated time points up to 72 hours post-dose	T1/2 is defined as the time required for the concentration or amount of NHC in the body to be reduced by one-half after a single oral dose of MK-4482 in period 1.
Time to Reach Maximum Observed Plasma Concentration (Tmax ) After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	Tmax of NHC following multiple oral doses of MK-4482 in period 2.
The Minimum Concentration (Ctrough) After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	Ctrough of NHC that occurred following multiple doses of MK-4482 in period 2.
Apparent Total Clearance (CL/F) After Single Oral Dose of MK-4482 in Period 1	At designated time points up to 72 hours post-dose	CL/F of NHC from plasma after single oral dose of MK-4482 in period 1.
The Maximum Observed Plasma Concentration (Cmax) After Single Oral Dose of MK-4482 in Period 1	At designated time points up to 72 hours post-dose	Cmax of N-hydroxycytidine (NHC) after a single oral dose of MK-4482 in period 1.
Time to Reach Maximum Observed Plasma Concentration (Tmax ) After Single Oral Dose of MK-4482 in Period 1.	At designated time points up to 72 hours post-dose	Tmax of NHC following single oral dose of MK-4482 in period 1.
Apparent Volume of Distribution (Vz/F) After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	Vz/F of NHC during terminal phase after multiple doses of MK-4482 in period 2.
Area Under the Plasma Concentration-time Curve From Time 0 to 12 Hours Post-dose (AUC0-12hr) After Single Oral Dose of MK-4482 in Period 1	At designated time points up to 72 hours post-dose	This is a measure of the average amount of NHC in the plasma over a period of 12 hours after single oral dose of MK-4482 in period 1.
Elimination Half Life (T1/2) After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	T1/2 is defined as the time required for the concentration or amount of NHC in the body to be reduced by one-half after multiple oral doses of MK-4482 in period 2.
Apparent Volume of Distribution (Vz/F) After Single Oral Dose of MK-4482 in Period 1	At designated time points up to 72 hours post-dose	Vz/F of NHC during terminal phase after single oral dose of MK-4482 in period 1.
Area Under the Plasma Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) After Single Oral Dose of MK-4482 in Period 1	At designated time points up to 72 hours post-dose	AUC0-last of NHC following a single oral dose of MK-4482 in period 1.
Area Under The Plasma Concentration Versus Time Curve From Time Zero (pre-dose) to Extrapolated Infinite Time (AUC0-inf) After Single Oral Dose of MK-4482 in Period 1	At designated time points up to 72 hours post-dose	AUC0-inf of NHC after single oral dose of MK-4482 in period 1.
The Maximum Observed Plasma Concentration (Cmax) After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	Cmax of NHC after multiple oral doses of MK-4482 in period 2.
Clearance at Steady State (CLss/F) After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	CLss/F of plasma NHC following multiple doses of MK-4482 in period 2.
Area Under the Plasma Concentration-time Curve From Time 0 to 12 Hours Post-dose (AUC0-12hr) After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	This is a measure of the average amount of NHC in the plasma over a period of 12 hours after multiple oral doses of MK-4482 in period 2.
Accumulation Ratio on Cmax After Multiple Oral Doses of MK-4482 in Period 2	At designated time points up to 72 hours post-dose	The maximum concentration at steady state following multiple doses of MK-4482 in period 2 divided by the maximum concentration following the initial dosing in Period 1.
Accumulation Ratio on AUC0-12hr After Multiple Oral Doses of MK-4482	At designated time points up to 72 hours post-dose	The AUC0-12hr at steady state following multiple doses of MK-4482 in period 2 divided by the AUC0-12hr following the initial dosing in Period 1.

Secondary Outcome Measures

Name	Time	Method
Number of Participants Who Discontinue Study Treatment Due to an AE	Up to ~ 5.5 weeks	An AE is any untoward medical occurrence in a participant, temporally associated with the use of study treatment, whether or not considered related to the study treatment. The number of participants who discontinue study treatment due to an AE will be reported.
Number of Participants Who Experience an Adverse Event (AE)	Up to ~ 5.5 weeks	An AE is any untoward medical occurrence in a participant, temporally associated with the use of study treatment, whether or not considered related to the study treatment. The number of participants who experience an AE will be reported.

Trial Locations

Locations (1)

Peking University Third Hospital (Site 0001); 🇨🇳 Beijing, Beijing, China