Clinical trial NCT06986772: TGRX-678 Pharmacokinetic Mass Balance
Official title: [14C]TGRX-678 Mass Balance Study in Chinese Healthy Male Adults
Study type: INTERVENTIONAL
Overall status: NOT_YET_RECRUITING
Phase: PHASE1
Conditions: Chronic Myeloid Leukemia
Lead sponsor: Shenzhen TargetRx, Inc.
Sponsor class: INDUSTRY
Collaborators: name: The First Affiliated Hospital of Soochow University
First posted: 2025-05-23
Enrollment: 6
Sex: MALE
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

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.

Eligibility criteria: 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

Primary outcomes:
measure: Urine radioactivity
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
measure: Fecal radioactivity
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
measure: Plasma AUC (Area under curve) percentage
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
measure: Urine %Dose
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
measure: Fecal %Dose
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
measure: Plasma Cmax
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
measure: Plasma Tmax
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
measure: Plasma AUC(0-t)
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing
Secondary outcomes:
measure: Adverse events/serious adverse events
timeFrame: Day-1 (day before dosing), Day 1 to Day 54 after dosing or the day sample collection is completed
Other outcomes:
Locations:
city: Suzhou
country: China
facility: The First Affiliated Hospital of Soochow University
state: Jiangsu
Study officials:
affiliation: The First Affiliated Hospital of Soochow University
name: Liyan Miao, MD
role: PRINCIPAL_INVESTIGATOR
References: