The purpose of this study is to evaluate the safety, tolerability, and pharmacokinetics profiles of TG-1000 in healthy volunteers, and to evaluate the food effect on pharmacokinetics of single oral dose of TG-1000 in healthy volunteers.
This is a phase 1, single-center, randomized, double-blind, placebo-controlled, single-dose escalation study to evaluate the safety, tolerability, and pharmacokinetics profiles of TG-1000 in healthy volunteers, and to evaluate the food effect on pharmacokinetics of single oral dose of TG-1000 in healthy volunteers. The study will be divided into two parts. Part A is designed as randomized, double-blind, placebo-controlled, sequential, single ascending oral dose to evaluate the safety, tolerability, and PK profiles of TG-1000 in healthy volunteers. Part B is designed as randomized, open-label, two treatment (fasted vs. fed), two-period, two-sequence crossover to compare the effects of food on the Pharmacokinetic (PK) of single oral dose of TG-1000 in healthy subjects.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
QUADRUPLE
Enrollment
66
Xiangya Hospital of Central South University
Changsha, Hunan, China
Number of subjects of treatment-emergent adverse events
Any significant findings after dosing will be considered as adverse events.
Time frame: 8 days
Number of subjects of Significant Abnormal Vital Signs Findings
The systolic and diastolic blood pressure (mmHg), pulse/heart rate (beats/min), respiratory rate (breaths/min), and body temperature (oC) will be measured.
Time frame: 8 days
Number of subjects With Significant Abnormal Physical Examination Findings
A full general physical examination of the major body systems (General Appearance; Dermatological including skin and nails; Head and Neck; Chest region including Heart and Lung; Abdominal region including Gastrointestinal and Gastroenterology; Back region; Extremities; Psychiatric or Neurological; Lymph nodes; Other) will be performed by investigator.
Time frame: 8 days.
Number of subjects With Significant Abnormal 12-lead Electrocardiography (ECG) Findings
12-lead ECG will be performed after a rest in a supine position. The following ECG parameters will be listed: heart rate, the time between QRS complexes (RR Interval) (ms), the beginning of the P wave to the first deflection of the QRS complex (PR Interval) (ms), first deflection of QRS complex to end of QRS complex at isoelectric line (QRS duration) (ms), first deflection of QRS complex to end of T wave at isoelectric line (QT interval) (ms), Corrected QT interval by Bazett (QTcB) (ms), and Corrected QT interval by - Fridericia (QTcF) (ms).
Time frame: 8 days
Number of subjects With Significant Abnormal Holter Electrocardiography (ECG) Findings
Holter ECG will be monitor continue from 12 hr pre-dose until 24 hr post-dose. The Investigator will determine whether the results of the Holter monitoring are normal or abnormal.
Time frame: 12 hr pre-dose until 24 hr post-dose
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Number of Participants With Significant Abnormal Laboratory Values
Chemistry, Hematology, Coagulation, Urinalysis, Human Immunodeficiency Virus (HIV) test, Hepatitis A virus(HAV) test, Hepatitis B virus (HBV) test, Hepatitis C virus (HCV) test, syphilis, serum pregnancy tests and Breath Alcohol Test
Time frame: 8 days
Peak Plasma Concentration (Cmax)
Blood sample will be collected to evaluate PK profile and food effect of TG-1000.
Time frame: 15 days
time to Cmax (Tmax)
Blood sample will be collected to evaluate PK profile of TG-1000.
Time frame: 15 days
area under the curve from time zero to the time (AUC0-t)
Blood sample will be collected to evaluate PK profile and food effect of TG-1000.
Time frame: 15 days
area under the concentration-time curve from time zero to the last quantifiable concentration (AUC0-last)
Blood sample will be collected to evaluate PK profile of TG-1000.
Time frame: 15 days
area under the concentration-time curve from time zero to infinity (AUC0-inf)
Blood sample will be collected to evaluate PK profile and food Effect of TG-1000.
Time frame: 15 days
terminal elimination half-life (T1/2, z)
Blood sample will be collected to evaluate PK profile of TG-1000.
Time frame: 15 days
apparent total body clearance (CL/F)
Blood sample will be collected to evaluate PK profile of TG-1000.
Time frame: 15 days
apparent total volume distribution (V/F)
Blood sample will be collected to evaluate PK profile of TG-1000.
Time frame: 15 days
plasma concentration 24 h after dosing (C24)
Blood sample will be collected to evaluate PK profile of TG-1000.
Time frame: 15 days
urinary excretion ratio relative to dose from time zero to the time (Feu0-t)
Urine sample will be collected to evaluate PK profile of TG-1000.
Time frame: 15 days