TGRX-678 Phase I Oral Pharmacokinetic Study

Food Effect on Pharmacokinetic Profile for TGRX-678 Tablet in Chinese Healthy Subject With Single Oral Administration

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

Study Overview

• Status: Completed
• Conditions: Chronic Myeloid Leukemia
• Intervention / Treatment: Drug: 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 Type: Interventional
• Enrollment (Actual): 76
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Jiangsu
    • Nanjing, Jiangsu, China, 210008
      • Nanjing Drum Tower Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult
• Accepts Healthy Volunteers: Yes

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Fasting; Participants take TGRX-678 under fasting state	Drug: TGRX-678; All participants are given TGRX-678 orally at 240 mg
Experimental: Low-fat Diet; Participants take TGRX-678 after low-fat meal intake	Drug: TGRX-678; All participants are given TGRX-678 orally at 240 mg
Experimental: High-fat Diet; Participants take TGRX-678 after high-fat meal intake	Drug: TGRX-678; All participants are given TGRX-678 orally at 240 mg

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Plasma Tmax	Time to maximum concentration (Tmax) of TGRX-678 measured in plasma	During Treatment period (Day 1 to Day 43)
Plasma Tlag	Time between drug administration to drug absorption (Tlag) as indicated by TGRX-678 plasma concentration	During Treatment period (Day 1 to Day 43)
Plasma Cmax	Maximum concentration (Cmax) of TGRX-678 measured in plasma	During Treatment period (Day 1 to Day 43)
Plasma AUC(0-t)	Area Under drug concentration-time curve (AUC) from time 0 to last measureable timepoint for TGRX-678 as measured in plasma	During Treatment period (Day 1 to Day 43)
Plasma AUC(0-inf)	Area Under drug concentration-time curve from time 0 to infinity for TGRX-678 as measured in plasma	During Treatment period (Day 1 to Day 43)
AUC(%Extrap)	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.	During Treatment period (Day 1 to Day 43)
Half Life (T1/2)	Time for TGRX-678 to decrease from maximum plasma concentration to half of maximum plasma concentration	During Treatment period (Day 1 to Day 43)
Plasma volume of distribution (Vz/F)	Apparent volume of distribution of TGRX-678 in plasma	During Treatment period (Day 1 to Day 43)
Plasma clearance (CL/F)	Apparent clearance of TGRX-678 in plasma	During Treatment period (Day 1 to Day 43)

Secondary Outcome Measures

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

Collaborators and Investigators

• Sponsor: Shenzhen TargetRx, Inc.
• Collaborators: The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School
• Investigators: Principal Investigator: Juan Li, MD, Nanjing Drug Tower Hospital

Study record dates

Study Major Dates

• Study Start (Actual): November 24, 2024
• Primary Completion (Actual): January 6, 2025
• Study Completion (Actual): February 20, 2025

Study Registration Dates

• First Submitted: November 18, 2024
• First Submitted That Met QC Criteria: November 18, 2024
• First Posted (Actual): November 20, 2024

Study Record Updates

• Last Update Posted (Actual): May 16, 2025
• Last Update Submitted That Met QC Criteria: May 15, 2025
• Last Verified: May 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Pathologic Processes; Neoplasms; Chronic Disease; Disease Attributes; Neoplasms by Histologic Type; Hematologic Diseases; Leukemia, Myeloid; Bone Marrow Diseases; Leukemia; Myeloproliferative Disorders; Leukemia, Myelogenous, Chronic, BCR-ABL Positive
• Other Study ID Numbers: TGRX-678-1002

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No