The study will be a single center, double-blind, randomized, placebo-controlled study to evaluate the safety, tolerability, PK and PD of AP303 following 2-week oral administration to Diabetic Kidney Disease patients.
Eligible patients will be enrolled into one of the two dose cohorts, each cohort will include 9 participants randomized to AP303 and placebo at a 2:1 ratio (6 on AP303 and 3 on placebo).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
18
AP303 Tablet 150μg QD
Placebo Tablet 150μg QD
Peking University First Hospital
Beijing, Beijing Municipality, China
RECRUITINGCmax
Maximum observed plasma concentration
Time frame: Day 1, Day 14
Tmax
Time to maximum observed plasma concentration
Time frame: Day 1, Day 14
AUC0-24h
Area under the plasma concentration versus time curve up to 24 hours
Time frame: Day 1
AUC0-last
Area under the plasma concentration versus time curve up to the last measurable concentration
Time frame: Day 1
AUC0-inf
Area under the plasma concentration versus time curve extrapolated to infinity
Time frame: Day 1
AUC0-t
Area under the plasma concentration-time curve for a dosing interval
Time frame: Day 14
t1/2
Apparent terminal half-life, computed as ln(2)/λz
Time frame: Day 1, Day 14
CL/F
Apparent oral clearance calculated from Dose/ AUC0-inf
Time frame: Day 1
V/F
Apparent volume of distribution of oral drug
Time frame: Day 1, Day 14
Cav
Average plasma concentration
Time frame: Day 14
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Ctrough
Trough plasma concentration
Time frame: Day 3-14
Rac
Ratio of accumulation
Time frame: Day 3-14
Incidence and severity of adverse events
Incidence and severity of adverse events
Time frame: Day 1-28
Incidence of laboratory abnormalities, based on hematology, clinical chemistry, coagulation and urinalysis test results
Incidence of laboratory abnormalities, based on hematology, clinical chemistry, coagulation and urinalysis test results
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Change of Heart rate in beats/min
Time frame: Day 1-28
Effect of AP303 on ECG parameters
change of QT in ms
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Change of PR in ms
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Change of QRS in ms
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Change of QTcF in ms
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Change of QTcB in ms
Time frame: Day 1-28
Vital signs(Systolic blood pressure)
Change of systolic blood pressure
Time frame: Day 1-28
Effect of AP303 on physical examination result
Number of pariticipants with abnormal physical examination findings by nature and severity
Time frame: Day 1-28
Body weight
Change of body weight
Time frame: Day 1-28
Vital signs (Diastolic blood pressure)
Change of diastolic blood pressure
Time frame: Day1-28
Vitlal signs (Body temperature)
Change of body temperature
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Number of participants with abnormal QTcB.
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Number of participants with abnormal QTcF
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Number of participants with abnormal QRS
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Number of participants with abnormal PR
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Number of participants with abnormal QT
Time frame: Day 1-28
Effect of AP303 on ECG parameters
Number of participants with abnormal heart rate
Time frame: Day 1-28
Fasting glucose
Change of fasting glucose
Time frame: Baseline, Days 6, 10, 14 and 28
Fasting lipid profile
Change of Triglyceride, HDL-C, LDL-C, Total cholesterol
Time frame: Baseline, Days 6, 10, 14 and 28
Serum creatinine
Change of serum creatinine
Time frame: Baseline, Days 6, 10, 14 and 28
eGFR
Change of estimated glomerular filtration rate
Time frame: Baseline, Days 6, 10, 14 and 28