TGRX-326 Pharmacokinetic Food Effect Bioavailability Study

Phase 1

Completed

• Conditions: Non Small Cell Lung Cancer

• Registration Number: NCT06304805
• Lead Sponsor: Shenzhen TargetRx, Inc.

Brief Summary

A study evaluating the effects of food intake on the pharmacokinetic (PK) profiles of TGRX-326 and the effect of different drug specifications on human bioavailability for TGRX-326, a drug indicated for non-small cell lung cancer treatment

Detailed Description

This study is designed as single-center, randomized, open-label, 3-cycle, 6-sequence and crossover design to evaluate 1) food effect on PK profile of TGRX-326; 2) effect of different specifications of TGRX-326 on human bioavailability. Safety for food effect on TGRX-326 and safety for different TGRX-326 specifications were also evaluated.

Study Timeline

• Study Start: 2023-12-13
• Primary Completion: 2024-01-12
• Study Completion: 2024-01-19
• Study First Submitted: 2024-03-05
• Study First Submitted QC: 2024-03-05
• Study First Posted: 2024-03-12
• Status Verified: 2025-05
• Last Update Submitted: 2025-05-16
• Last Update Posted: 2025-05-18

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 24

Inclusion Criteria

• able to understand the purpose, methods and possible adverse events of the study and agree to volunteering consent before the start of study
• healthy subject; male or female
• Age between 18 and 55 (inclusive)
• body mass index (BMI) between 19.0 and 26.0 (inclusive), male weight <=50 kg, female weight <=45 kg
• normal/ clinically insignificant test results (including physical exam, laboratory tests, 12-lead ECG, chest x-ray, etc.)
• participant/partner of the participant does not have plans for child bearing from screening until 6 months after study, and is willing to take contraceptive measures during study period and for 6 months, and does not have plans to donate sperm/egg during the said period

Exclusion Criteria

• history of allergic reactions, or allergic to any components to the study drugs that by investigator's judgement unsuitable for the study
• any clinically significant conditions that could affect study outcomes, safety or compliance
• history of major surgery within 3 months before first dose, or have plans to receive surgery during the study, or history of any surgery that could affect drug absorption, distribution, metabolism and excretion
• have difficulties to receive venous needle puncture, or cannot tolerate venous needle puncture, or history of hematophobia or needle sickness
• history of substance abuse
• have special food requirement or cannot follow food requirement of the study, or lactose intolerant
• use of any investigational drug or participation of any clinical study (for drug or medical device) within 3 months before first dose, or cannot participate the study in person/on site
• history of blood donation, blood loss (>= 400 mL, excluding normal blood loss during female menstrual period), or reception of blood transfusion within 3 months before screening
• history of daily cigarette consumption of more than 5 within 3 months before screening, or cannot avoid using cigarette/tabacco products during the study
• history of alcohol abuse (more than 14 units of alcohol per week) within 3 months before screening, or cannot avoid alcohol consumption during study
• history of large tea/coffee/caffeinated drink intake (more than 8 cups per day) within 3 months before first dose
• history of irregular dietary schedule within 1 months of first dose (including, dieting, overeating, low sodium intake, etc.)
• use of any prescription / over-the-counter drug, or Chinese herbal medication, or health supplementary products within 14 days of test article administration
• vaccination within 14 days before first test article administration, or have plans to receive vaccination during the study period
• any one positive result for hepatitis-B surface antigen, Hepatitis C antibody, HIV antibody or syphilis antibody
• alcohol breathing test results of > 0.0 mg/100mL for blood alcohol concentration
• positive test results on substance use (including, morphine, methylamphetamine, ketamine, tetrahydrocannabinol, methylene-dioxy-methyl-amphetamine)
• female in pregnancy or breastfeeding period, or positive pregnancy test result
• history of unprotected sexual activities within 14 days before first dose
• consumption of food or drink rich in caffeine/xanthine (such as chocolate, coffee, tea, coke) or food/food product of grapefruit, dragon fruit, mango, tangerine, or any food that could affect drug absorption, distribution, metabolism and excretion
• any reasons that is deemed unsuitable for study participation as determined by investigator

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Primary Outcome Measures

Name	Time	Method
Plasma AUC(0-inf)	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Area Under drug concentration-time curve from time 0 to infinity for TGRX-326 as measured in plasma
Plasma AUC(0-t)	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Area Under drug concentration-time curve (AUC) from time 0 to last measureable timepoint for TGRX-326 as measured in plasma
Plasma Cmax	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Maximum concentration of TGRX-326 measured in plasma

Secondary Outcome Measures

Name	Time	Method
Plasma Tmax	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Time to maximum concentration of TGRX-326 measured in plasma
Plasma clearance (CL/F)	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Apparent clearance of TGRX-326 in plasma
AUC(%Extrap)	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Calculated percentage of Area under curve for AUC(0-inf) that is from last measurable timepoint ot infinity, calculated based on TGRX-326 plasma concentration over time curve.
Plasma volume of distribution (Vz/F)	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Apparent volume of distribution of TGRX-326 in plasma
terminal elimination rate constant (lambda-z)	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	terminal elimination rate constant calculated from plasma TGRX-326 concentrations
Elimination half-life (T1/2-Z)	During treatment period on Day 1 of each of three cycles (each cycle is one day, and there is a 10-day washout period between two cycles)	Time for TGRX-326 to decrease from maximum plasma concentration to half of maximum plasma concentration
Adverse events/serious adverse events	through completion of the study, a total duration of 37 days	to record and analyse subjects with adverse events (AEs) and serious adverse events (SAEs)

Trial Locations

Locations (1)

First Affiliated Hospital Bengbu Medical College; 🇨🇳 Bengbu, Anhui, China