TGRX-678 Pharmacokinetic Mass Balance

NCT06986772 | Completed Phase 1

• 1 other identifier: TGRX-678-1003
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

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.

Conditions

Chronic Myeloid Leukemia

Outcome Measures

Primary Outcomes (8)

• Urine radioactivity

  \[C14\]TGRX-678 radioactivity detected in urine

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

• Fecal radioactivity

  \[C14\]TGRX-678 radioactivity detected in feces

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

• Plasma AUC (Area under curve) percentage

  percentage of \[C14\]TGRX-678 radioactivity in plasma

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

• Urine %Dose

  percentage of \[C14\]TGRX-678 radioactivity in urine

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

• Fecal %Dose

  percentage of \[C14\]TGRX-678 radioactivity in feces

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

• Plasma Cmax

  Maximum concentration of \[C14\]TGRX-678 measured in plasma

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

• Plasma Tmax

  Time to maximum concentration of \[C14\]TGRX-678 measured in plasma

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

• Plasma AUC(0-t)

  Area under curve for TGRX-678 plasma concentration from before dose to last measureable timepoint

  Day-1 (day before dosing), Day 1 to Day 54 after dosing

Secondary Outcomes (1)

• Adverse events/serious adverse events

  Day-1 (day before dosing), Day 1 to Day 54 after dosing or the day sample collection is completed

Study Arms (1)

TGRX-678

EXPERIMENTAL

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

Drug: [14C]TGRX-678

Interventions

[14C]TGRX-678 DRUG

Healthy subjects will be given TGRX-678 240 mg orally on day 1.

TGRX-678

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Shenzhen TargetRx, Inc.: lead
• The First Affiliated Hospital of Soochow University: collaborator

Study Sites (1)

The First Affiliated Hospital of Soochow University

Suzhou, Jiangsu, 215006, China

Location

MeSH Terms

Conditions

Leukemia, Myelogenous, Chronic, BCR-ABL Positive

Condition Hierarchy (Ancestors)

Leukemia, Myeloid; Leukemia; Neoplasms by Histologic Type; Neoplasms; Myeloproliferative Disorders; Bone Marrow Diseases; Hematologic Diseases; Hemic and Lymphatic Diseases; Chronic Disease; Disease Attributes; Pathologic Processes; Pathological Conditions, Signs and Symptoms

Study Officials

• Liyan Miao, MD

  The First Affiliated Hospital of Soochow University

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 15, 2025
• First Posted: May 23, 2025
• Study Start: July 7, 2025
• Primary Completion: August 17, 2025
• Study Completion: August 25, 2025
• Last Updated: September 4, 2025

Record last verified: 2025-09

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)