TGRX-326 Pharmacokinetic Mass Balance

Mass Balance Study of [14C]TGRX-326 in Healthy Adult Chinese Male Participants

This is a pharmacokinetic study for TGRX-326 on mass balance to evaluate distribution, metabolism and excretion of TGRX-326, an ALK inhibitor indicated for treatment of Non-small cell lung cancer.

Study Overview

• Status: Completed
• Conditions: Non Small Cell Lung Cancer
• Intervention / Treatment: Drug: [14C]TGRX-326

Detailed Description

This study is designed as a single-center, single-dose, non-randomized and open-label study. The study will be conducted in healthy male participants to evaluate distribution, metabolic pathways and route of excretion of TGRX-326 using the Carbon-14 labelled isotope of TGRX-326 compound. Safety evaluation will also be conducted.

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Jiangsu
    • Suzhou, Jiangsu, China, 215006
      • The First Affiliated Hospital of Soochow University

Participation Criteria

Eligibility Criteria

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

Description

Inclusion Criteria:

• Healthy adult males
• Age between 18 and 45 years old (both limits included)
• Body weight index between 19.0 and 26.0 kg/m2 (both limits included), and body weight not less than 50.0kg
• Willing to consent
• Able to communicate with investigator and complete study according to study protocol

Exclusion Criteria:

• Clinically significant results from comprehensive physical and clinical examinations
• Positive results on hepatitis, HIV or syphilis
• Clinically significant results from eye examination
• Usage of inducer or inhibitor drugs to drug metabolism with 30 days prior to screening
• Usage of any prescription or non-prescription drug, Chinese herbal medicine or dietary supplements
• Presence of any significant medical history or clinical conditions that could affect study results per investigators' judgement
• Presence of any condition that could affect drug absorption
• Reception of major surgery within 6 months before screening, or surgical wounds not completely healed
• Presence of allergic reactions or may be allergic to ingredients in the investigational drug
• Presence of hemorrhoids, or having history of or is having conditions that cause bloody feces
• Habitual congestion or diarrhea
• Alcohol abuse or excessive alcohol consumption within 6 months before screening
• Excessive smoking within 3 months before screening
• Substance abuse or positive results on urine substance test
• Habits of grapefruit juice consumption or excessive caffeinated drinks consumption
• History of long-term exposure under radiation; or significant radiation exposure 1 year before this study; or participation in other radioactive drug studies
• Having difficulties to receive venous needle puncture, or cannot tolerate venous needle puncture, or history of hematophobia or needle sickness
• Participation in any other clinical studies within 3 months before screening
• Reception of vaccine within 1 months before screening, or planning to be vaccinated during the study
• Planning to have children or donate sperms during the study and within 1 year after the study, or Not agreeing to take contraceptive measures during and within 1 year after study completion
• Blood donation or blood loss of > 400 ml within 3 months before screening; blood donation or blood loss of > 200 ml within 1 month before screening; reception of blood transfusion within 1 months before screening, or planning to donate blood within 3 months after study completion
• Having special dietary requirements and unable to follow the uniform dietary plan in the study
• Any conditions that the investigator deemed unfit for the study

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Experimental: TGRX-326; healthy subjects will be given 60mg/100uCi[14C]TGRX-326 in suspension	Drug: [14C]TGRX-326; Healthy subjects will be given TGRX-326 60 mg orally on day 1.; Other Names: TGRX-326

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Urine radioactivity	[C14]TGRX-326 radioactivity detected in urine	Day-1 (day before dosing), Day 1 to Day 18 after dosing
Fecal radioactivity	[C14]TGRX-326 radioactivity detected in feces	Day-1 (day before dosing), Day 1 to Day 18 after dosing
Plasma AUC (Area under curve) percentage	percentage of [C14]TGRX-326 radioactivity in plasma	Day-1 (day before dosing), Day 1 to Day 18 after dosing
Urine %Dose	percentage of [C14]TGRX-326 radioactivity in urine	Day-1 (day before dosing), Day 1 to Day 18 after dosing
Fecal %Dose	percentage of [C14]TGRX-326 radioactivity in feces	Day-1 (day before dosing), Day 1 to Day 18 after dosing
Plasma Cmax	Maximum concentration of [C14]TGRX-326 measured in plasma	Day-1 (day before dosing), Day 1 to Day 18 after dosing
Plasma Tmax	Time to maximum concentration of [C14]TGRX-326 measured in plasma	Day-1 (day before dosing), Day 1 to Day 18 after dosing

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse events/serious adverse events	to record and analyse subjects with adverse events (AEs) and serious adverse events (SAEs)	From screening through completion of study, an average of 1 to 1.5 months.

Collaborators and Investigators

• Sponsor: Shenzhen TargetRx, Inc.
• Collaborators: The First Affiliated Hospital of Soochow University
• Investigators: Principal Investigator: Liyan Miao, MD, The First Affiliated Hospital of Soochow University

Study record dates

Study Major Dates

• Study Start (Actual): June 26, 2024
• Primary Completion (Actual): July 8, 2024
• Study Completion (Actual): July 21, 2024

Study Registration Dates

• First Submitted: May 27, 2024
• First Submitted That Met QC Criteria: May 27, 2024
• First Posted (Actual): May 31, 2024

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: February 19, 2025
• Last Verified: February 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Neoplasms by Site; Neoplasms; Respiratory Tract Diseases; Lung Diseases; Respiratory Tract Neoplasms; Thoracic Neoplasms; Lung Neoplasms; Carcinoma, Bronchogenic; Bronchial Neoplasms; Carcinoma, Non-Small-Cell Lung
• Other Study ID Numbers: TGRX-326-1004

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