TGRX-678 Pharmacokinetic Mass Balance

Phase 1

Not yet recruiting

• Conditions: Chronic Myeloid Leukemia
• Interventions: Drug: [14C]TGRX-678

• Registration Number: NCT06986772
• Lead Sponsor: Shenzhen TargetRx, Inc.

Brief Summary

This is a pharmacokinetic study for \[14C\]TGRX-678 on mass balance to evaluate distribution, metabolism and excretion of TGRX-678, a tyrosine kinase inhibitor indicated for treatment of chronic myeloid leukemia.

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-678 using the Carbon-14 labelled isotope of TGRX-678 compound. Safety and pharmacokinetic evaluation will also be conducted.

Study Timeline

• Status Verified: 2025-05
• Study First Submitted: 2025-05-15
• Study First Submitted QC: 2025-05-15
• Last Update Submitted: 2025-05-15
• Study First Posted: 2025-05-23
• Last Update Posted: 2025-05-23
• Study Start: 2025-06-01
• Primary Completion: 2025-09-01
• Study Completion: 2025-12-01

Recruitment & Eligibility

• Status: NOT_YET_RECRUITING
• Sex: Male
• Target Recruitment: 6

Inclusion Criteria

• Healthy adult males
• age between 18 and 45 (both included) years old
• body weight index between 19.0 and 26.0 kg/m2 (both included, and body weight not lower than 50 kg
• can volunteeringly consent
• can communicate well with investigators and complete study according to protocol requirements

Exclusion Criteria

• abnormal and of clinical significance results on physical exam, regular laboratory tests, thyroid function, anal check, chest x-ray, abdominal ultrasound check or 12-lead ECG
• positive test results on hepatitis B surface antigen/ E antigen, hepatitis C antibody, HIV antigen/antibody or syphylus antibody
• abnornal and of clinical significance results on eye exam
• usage of any inducers or inhibitors for drug metabolism enzymes (especially CYP3A4) within 30 days of screening
• usage of any prescriptional drug, OTC drug, herbal medicine, traditional Chinese medicine, or food supplements (i.e., vitamins, calcium) within 14 days of screening
• history of any clinically significant serious diseases or any conditions that at investigator's discretion may affect study results
• have condition that may affect drug absoption
• received major surgery or with un-healed surgical wounds within 6 months of screening
• have allergies to at least 2 substances or at investigator's discretion may be allergic to investigational drug or any excipients
• have hemorrhoids; have history of or is having conditions that cause bloody feces, irritable bowel syndrome, or inflammatory bowel disease
• habitutory constipation or diarrhea
• alcohol abuse, or frequent use of alcohol within 6 months of screening
• smoking of more than 5 cigarettes per day within 3 months of screening, or habitutory use of nicotine products and cannot quit during study
• drug abuse, or use of soft drug (marajuana) within 3 months of screening, or use of hard drug (phenylamine or PCP type drugs) within 1 year of screening, or tested positive in urine drug test during screening
• habitutory use of grape fruit juice, or overuse of tea, coffee or caffeinated drugs, and cannot quit during study
• long-term occupational exposure to radioactive conditions, or have history of significant radioactive substance exposure or participated in clinical study using radioactive-labeled drugs within 1 year of current study
• 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; received blood donation within 1 months of study, 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 & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
TGRX-678	[14C]TGRX-678	healthy male subjects will be given 240mg/250uCi\[14C\]TGRX-678 in suspension

Primary Outcome Measures

Name	Time	Method
Urine radioactivity	Day-1 (day before dosing), Day 1 to Day 54 after dosing	\[C14\]TGRX-678 radioactivity detected in urine
Fecal radioactivity	Day-1 (day before dosing), Day 1 to Day 54 after dosing	\[C14\]TGRX-678 radioactivity detected in feces
Urine %Dose	Day-1 (day before dosing), Day 1 to Day 54 after dosing	percentage of \[C14\]TGRX-678 radioactivity in urine
Plasma Cmax	Day-1 (day before dosing), Day 1 to Day 54 after dosing	Maximum concentration of \[C14\]TGRX-678 measured in plasma
Plasma AUC(0-t)	Day-1 (day before dosing), Day 1 to Day 54 after dosing	Area under curve for TGRX-678 plasma concentration from before dose to last measureable timepoint
Plasma AUC (Area under curve) percentage	Day-1 (day before dosing), Day 1 to Day 54 after dosing	percentage of \[C14\]TGRX-678 radioactivity in plasma
Fecal %Dose	Day-1 (day before dosing), Day 1 to Day 54 after dosing	percentage of \[C14\]TGRX-678 radioactivity in feces
Plasma Tmax	Day-1 (day before dosing), Day 1 to Day 54 after dosing	Time to maximum concentration of \[C14\]TGRX-678 measured in plasma

Secondary Outcome Measures

Name	Time	Method
Adverse events/serious adverse events	Day-1 (day before dosing), Day 1 to Day 54 after dosing or the day sample collection is completed	to record and analyse subjects with adverse events (AEs) and serious adverse events (SAEs)

Trial Locations

Locations (1)

The First Affiliated Hospital of Soochow University; 🇨🇳 Suzhou, Jiangsu, China