TGRX-678 Pharmacokinetic Mass Balance

[14C]TGRX-678 Mass Balance Study in Chinese Healthy Male Adults

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.

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.

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