The study consists of 5 dose groups, starting at 25 mg, 6 subjects in 25 mg group, and 8 subjects in each other group (male or female), randomly assigned to study drug or placebo group to evaluate the safety, tolerability and PK characteristics. The subject number of single dose group may increase or decrease depending on the safety and PK data obtained. The dose levels are planned at 25 mg, 200 mg, 400 mg, 800 mg and 1200 mg. Based on observed tolerability and safety data or obtained PK data, adjustments are allowed at all dose levels in the clinical trial.
4 subjects in the 25 mg dose group will receive VV116 tablets and the other 2 subjects will receive placebo. In other dose groups, 6 subjects in each group will receive VV116 tablets and 2 subjects will receive placebo. 25mg,800mg and 1200 mg dose group will be given by sentinel administration (i.e. 1 study drug, 1 placebo). Subjects who receive sentinel administration will be observed for 48 hours and investigator will evaluate the safety parameters (including symptoms, vital signs, physical examination, etc.).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
TRIPLE
Enrollment
38
4 subjects will receive VV116 25mg,orally; 2 subjects will receive placebo,orally.
6 subjects will receive VV116 200mg,orally; 2 subjects will receive placebo,orally.
6 subjects will receive VV116 400mg,orally; 2 subjects will receive placebo,orally.
Shanghai Xuhui Central Hospital
Shanghai, Shanghai Municipality, China
Incidence of Treatment-Emergent Adverse Events
Incidence of Treatment-Emergent Adverse Events
Time frame: 7 days after treatment
Tmax
time at which Cmax occurs
Time frame: From time zero up to 48 hours post-dose following oral administration of VV116
Cmax
maximum observed plasma concentration
Time frame: From time zero up to 48 hours post-dose following oral administration of VV116
AUC0~t
area under the plasma concentration time curve from time zero to the last measurable concentration
Time frame: From time zero up to 48 hours post-dose following oral administration of VV116
AUC0-∞
area under the plasma concentration-time curve from time zero to infinity
Time frame: From time zero up to 48 hours post-dose following oral administration of VV116
structural of metabolites
Structure of main metabolites of VV116 in plasma, feces and urin. The main metabolites may include 116-N1 and M2.
Time frame: From time zero up to 72 hours post-dose following oral administration of VV116
Ae(total excretion of kidney)
Ae(total excretion of kidney)
Time frame: From time zero up to 72 hours post-dose following oral administration of VV116
Ae%(proportion of excretion of kidney)
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6 subjects will receive VV116 800mg,orally; 2 subjects will receive placebo,orally.
6 subjects will receive VV116 1200mg,orally; 2 subjects will receive placebo,orally.
Ae%(proportion of excretion of kidney)
Time frame: From time zero up to 72 hours post-dose following oral administration of VV116
CLr(renal clearance rate)
CLr(renal clearance rate)
Time frame: From time zero up to 72 hours post-dose following oral administration of VV116
Cumulative excretion and percentage of VV116 and major metabolites in feces.
Cumulative excretion and percentage of VV116 and major metabolites in feces.
Time frame: From time zero up to 72 hours post-dose following oral administration of VV116