NCT06829563

Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of RZ-629 in Healthy Subjects and T2D

A Phase Ia/Ib, Randomized, Double-blind, Placebo-controlled, Single Ascending Dose/Multiple Dose Study of RZ-629 to Evaluate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Food Effect in Healthy Subjects and T2D Patients.

• Status: Recruiting
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 134 (estimated)
• Sponsor: Rezubio Pharmaceuticals Co., Ltd. · Industry
• Sex: All
• Age: 18 Years – 65 Years
• Healthy volunteers: Accepted

Summary

The main purpose of this study is to evaluate the safety, tolerability, pharmacokinetic (PK), and pharmacodynamic (PD) biomarkers in single ascending doses (SAD), food effect, and multiple doses studies of RZ-629 in healthy participants and T2D.

Detailed description

This study comprises of 3 parts - Part 1, Part 2, and Part 3. Part 1 (SAD in healthy participants) - A total of 50 healthy subjects will be allocated to 5 groups in the SAD study. Each group includes 10 subjects (8 subjects will receive RZ-629 and 2 receive placebo). All subjects will check-in on the day before the administration (Day -1) and on Day 1. Each subject in fasted state will be randomly assigned to receive a single oral dose of RZ-629 or placebo. Subjects will remain in the clinical research unit (CRU) through the completion of the safety/tolerability evaluation. The safety review committee (SRC) will review all safety data and blinded summary of available PK data through the safety follow-up and decide to proceed to the next dose level. Part 2 (food effect in healthy participants) - A total of 12 healthy subjects will be enrolled to FE study. Subjects in the FE group will be divided into subgroup A and subgroup B equally. During period 1, subjects in subgroup A will receive a single oral dose of RZ-629 tablet with 240 mL of water following a fast of at least 10 hours. Water is not allowed 1 h predose until 1 h post dose. Food or drinks are not allowed until 4 h after the dosing. Subjects in subgroup B will received the dose of RZ-629 tablet with 240 mL of water following a standardized high-calorie meal consumed after an overnight fast of at least 10 h. The meal is approximately 500 kcal, composed of approximately 50% carbohydrates, 30% fat, and 20% protein.The high-fat meal should be consumed within 30 minutes. The 25 mg RZ-629 tablet should be administrated 30 minutes after starting the high-calorie meal. Water is not allowed 1 h predose until 1 h post dose. No food or drinks are allowed for 4 hours post-dose for all subjects in subgroup B. During period 2, administration will be performed in a crossover manner, i.e., subjects in subgroup A will receive the study drug after consuming a high-fat meal, and subjects in subgroup B will receive the study drug under fasting conditions. There is a washout period of 10 days between each dose. Relevant PK and PD sampling, and safety assessments will be completed during the study. Part 3 (multiple doses in healthy subjects and in T2D patients) - A total of 72 subjects will be recruited with each cohort including 8 subjects for multiple doses in healthy subjects (body mass index \[BMI\] between 19 and 32 kg/m2, 6 on RZ-629 and 2 on placebo) and 12 subjects for multiple doses in T2D patients (BMI between 25 and 40 kg/m2, 9 on RZ-629 and 3 on placebo). Subjects will check in on Day -2 to Day -1 for healthy subjects and Day -2 for T2DM patients after 28 days of screening. On Day 1, healthy subjects will be randomly assigned to orally receive the RZ-629 or placebo once daily for a consecutive 7 days. After being evaluated by the investigator, patients will leave the CRU on Day 2 and return to the CRU on Day 5, Day 6, Day 7 and stay until Day 10, for safety and tolerability assessments, and will be discharged with the consent of the investigator. All subjects will return to the CRU for safety follow-up on Day 15 + 2. T2D patients cohorts will be enrolled after safety assessment of multiple doses study in healthy subjects. T2D patients will be randomly assigned to orally receive RZ-629 or placebo once daily for a consecutive 28 days. After being evaluated by the investigator, patients will leave the CRU on Day 2 and return to the CRU on Day 8, Day 15, and Day 22 for biosample collection and safety examination. They will then return to the CRU on Day 27 and stay until the end of Day 29. All subjects will return to the CRU for safety follow-up on Day 35 + 2.

Conditions

• Diabetes

Interventions

Type	Name	Description
DRUG	RZ-629	Administered orally
DRUG	Placebo	Administered orally
OTHER	Fasted	Participants will be treated with RZ-629 in fasted or fed condition and then cross over after washout
OTHER	Fed	Participants will be treated with RZ-629 in fasted or fed condition and then cross over after washout

Timeline

• Start date: 2025-01-30
• Primary completion: 2025-12-20
• Completion: 2026-02-20
• First posted: 2025-02-17
• Last updated: 2025-08-21

Locations

1 site across 1 country: Australia

Regulatory

• FDA-regulated drug study