Part A Primary objective: • To evaluate the safety, tolerability, and pharmacokinetic profile of a single dose of YZJ-4729 tartrate injection. Secondary objectives: * To investigate the PK/PD profile of YZJ-4729 tartrate injection administered as a single dose; * To investigate the metabolic transformation characteristics of YZJ-4729 tartrate; * To assess the relationship between plasma concentrations and change in QT interval (C-QT) and the effect on QT interval in subjects after a single dose of YZJ-4729 tartrate injection. Part B Primary objective: • To evaluate the safety, tolerability and pharmacokinetic profile of YZJ-4729 tartrate injection administered at the same dose and at different infusion rates . Secondary objectives: • To investigate the PK/PD profile of YZJ-4729 tartrate injection administered at the same dose and at different infusion rates.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
66
Infusion, QD
Infusion, QD
Xiangya Third Hospital, Central South University
Changsha, China
Incidence of adverse events (AEs) and serious adverse events (SAEs)
Time frame: Part A: From Day 1 to Day 5 Part B: From Day 1 to Day 17
Incidence of participants with clinical laboratory abnormalities
Time frame: Part A: From Day 1 to Day 5 Part B: From Day 1 to Day 17
Incidence of participants with vital signs abnormalities
Time frame: Part A: From Day 1 to Day 5 Part B: From Day 1 to Day 17
Incidence of participants with physical exam abnormalities
Time frame: Part A: From Day 1 to Day 5 Part B: From Day 1 to Day 17
Cmax
Cmax is defined as the observed maximum plasma concentration.
Time frame: Pre-dose to 72 hours post-dose
AUCinf
AUCinf is defined as the area under the plasma concentration-time curve extrapolated to infinity from time zero.
Time frame: Pre-dose to 72 hours post-dose
AUC0-24h
AUC0-24h is defined as the area under the plasma concentration-time curve from time zero to 24h.
Time frame: Pre-dose to 72 hours post-dose
AUC0-t
AUC0-24h is defined as the area under the plasma concentration-time curve from time zero to the last observable concentration.
Time frame: Pre-dose to 72 hours post-dose
t1/2z
t1/2z is defined as the elimination half-life.
Time frame: Pre-dose to 72 hours post-dose
Tmax
Tmax is defined as the observed time to reach Cmax.
Time frame: Pre-dose to 72 hours post-dose
CL
CL is defined as the clearance.
Time frame: Pre-dose to 72 hours post-dose
Vz
V is defined as the apparent volume of distribution.
Time frame: Pre-dose to 72 hours post-dose
MRT
MRT is defined as the mean residence time.
Time frame: Pre-dose to 72 hours post-dose
Ae0-t
Ae0-t is defined as the cumulative amount of drug excreted in urine or fecal from time zero to the last observable concentration.
Time frame: Pre-dose to 72 hours post-dose
Cumulative excretion percentage of drug through urine and feces
Time frame: Pre-dose to 72 hours post-dose
Pupil diameter
Time frame: Pre-dose to 12 hours post-dose
Change from baseline of QTcF by timepoint
Time frame: Pre-dose to 24 hours post-dose
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