TGRX-678 Phase I Oral Pharmacokinetic Study

Phase 1

Completed

• Conditions: Chronic Myeloid Leukemia
• Interventions: Drug: TGRX-678

• Registration Number: NCT06697899
• Lead Sponsor: Shenzhen TargetRx, Inc.

Brief Summary

A study evaluating the effects of food intake on the pharmacokinetic (PK) profiles of TGRX-678

Detailed Description

This study is designed as single-center, single-dose, randomized, open-label and parallel-comparison to evaluate food effect on PK profile of TGRX-678 in healthy subjects. Safety and tolerability of the drug is also evaluated during study.

Study Timeline

• Study First Submitted: 2024-11-18
• Study First Submitted QC: 2024-11-18
• Study First Posted: 2024-11-20
• Study Start: 2024-11-24
• Primary Completion: 2025-01-06
• Study Completion: 2025-02-20
• Status Verified: 2025-05
• Last Update Submitted: 2025-05-15
• Last Update Posted: 2025-05-16

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 76

Inclusion Criteria

• Healthy participants, male or female
• Age between 18 and 45 (both inclusive)
• Body Weight: male ≥ 50 kg, female ≥ 45 kg; Body Mass Index (BMI) between 19.0 and 26.0 kg/m^2 (both inclusive)
• Signing informed concent at own will
• Able to communicate with researcher and able to complete study per protocol instruction

Exclusion Criteria

• Clinically significant abnormal results in lab test, physical exam or 12-lead electrocardiogram (ECG) test
• Positive results for Hepatitis B, Hepatitis C, HIV or Syphilis
• QT interval elongation as indicated by 12-lead ECG test during screening period
• Use of any medication that could impact CYP3A4 enzyme activities within 30 days prior to Screening period
• Use of any medication within 14 days of first dose of the investigational drug
• Vaccinated within 30 days of first dose of the investigational drug, or planning to be vaccinated during study
• History of instrumental cardiovascular diseases
• Received major surgery within 6 months prior to Screening, or with surgical wounds not completely healed
• History of any severe disease or conditions that could affect study results per investigator's discretion
• History of allergic conditions or is allergic to components of the investigational drug
• Having conditions that could affect drug absorption or difficulties to swallow
• History of smoking of >5 cigarettes per day within 3 months prior to screening, or cannot stop tabacco using during study
• History of alcohol abuse, or alcohol consumption of >14 unit alcohol within 3 months prior to screening
• History of substance use, or tested positive for drug test during screening
• History of specific food (i.e., grapefruit, mango) consumption, or/and large tea/coffee/caffeinated drink/grapefruit product intake of > 8 cups per day, within 2 weeks prior to first dose
• Having special dietary requirement and cannot comply with food requirement of the study
• Pregnant or breastfeeding female, or tested positive in pregnancy test
• History of unprotected sexual activities within 1 month prior to screening
• Having plans for pregnancy during the study and within 6 months after study completion; or not agreeing to take strict contraceptive measures during study and within 6 months after study completion
• History of blood loss/ blood donation of ≥ 400 mL within 3 months prior to screening, or planning to donate blood within 1 month after study completion
• Any reasons that is deemed unsuitable for study participation as determined by investigator

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Fasting	TGRX-678	Participants take TGRX-678 under fasting state
Low-fat Diet	TGRX-678	Participants take TGRX-678 after low-fat meal intake
High-fat Diet	TGRX-678	Participants take TGRX-678 after high-fat meal intake

Primary Outcome Measures

Name	Time	Method
Plasma volume of distribution (Vz/F)	During Treatment period (Day 1 to Day 43)	Apparent volume of distribution of TGRX-678 in plasma
Plasma clearance (CL/F)	During Treatment period (Day 1 to Day 43)	Apparent clearance of TGRX-678 in plasma
Plasma Tmax	During Treatment period (Day 1 to Day 43)	Time to maximum concentration (Tmax) of TGRX-678 measured in plasma
Plasma Tlag	During Treatment period (Day 1 to Day 43)	Time between drug administration to drug absorption (Tlag) as indicated by TGRX-678 plasma concentration
Plasma Cmax	During Treatment period (Day 1 to Day 43)	Maximum concentration (Cmax) of TGRX-678 measured in plasma
Plasma AUC(0-t)	During Treatment period (Day 1 to Day 43)	Area Under drug concentration-time curve (AUC) from time 0 to last measureable timepoint for TGRX-678 as measured in plasma
Plasma AUC(0-inf)	During Treatment period (Day 1 to Day 43)	Area Under drug concentration-time curve from time 0 to infinity for TGRX-678 as measured in plasma
AUC(%Extrap)	During Treatment period (Day 1 to Day 43)	Calculated percentage of Area under curve for AUC(0-inf) that is from last measurable timepoint ot infinity, calculated based on TGRX-678 plasma concentration over time curve.
Half Life (T1/2)	During Treatment period (Day 1 to Day 43)	Time for TGRX-678 to decrease from maximum plasma concentration to half of maximum plasma concentration

Secondary Outcome Measures

Name	Time	Method
Adverse Events (AE)	Starting from consent signing and until end of Treatment period (Day 1 to Day 43)	To record adverse events to participants during study participation

Trial Locations

Locations (1)

Nanjing Drum Tower Hospital; 🇨🇳 Nanjing, Jiangsu, China