A single-center, randomized, open-label, crossover study to evaluate the pharmacokinetic drug-drug interaction and safety of the quadruple therapy with Anaprazole 20mg/Amoxicilin 1000mg/Clarithromycin 500mg/Bismuth Potassium Citrate 0.6g in healthy Chinese male subjects.
The study composed of 2 cohorts, using a 4\*4 or 2\*2 crossover design in cohort 1 and 2, respectively. 4 rotating treatment sequences in cohort 1, each treatment sequence comprised 4 treatment periods, separated by a washout period of 9 days; 2 rotating treatment sequences in cohort 2, each treatment sequence comprised 2 treatment periods, separated by a washout period of 9 days
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
32
Cohort 1: Css,max of anaprazole (parent drug, KBP-3571) and its enantiomer(KBP-3570)and its major metabolites (KBP-1123 and KBP-1144), Unchanged amoxicillin, Unchanged clarithromycin and its metabolite (14-hydroxyclarithromycin)
Css,max is the peak plasma concentration at steady state
Time frame: Hour 0.5 pre-dose and 0.5,1,1.5,2,2.5,3,3.5,4,4.5,5,6,7,8,10,12,24 hours post-dose of Day 5,Day 19,Day 33,Day 47
Cohort 1: AUC of anaprazole (parent drug, KBP-3571) and its enantiomer(KBP-3570)and its major metabolites (KBP-1123 and KBP-1144), Unchanged amoxicillin, Unchanged clarithromycin and its metabolite (14-hydroxyclarithromycin)
AUC is area under the plasma concentration-time curve
Time frame: Hour 0.5 pre-dose and 0.5,1,1.5,2,2.5,3,3.5,4,4.5,5,6,7,8,10,12,24 hours post-dose of Day 5,Day 19,Day 33,Day 47
Cohort 2: Cmax of anaprazole (parent drug, KBP-3571) and its enantiomer(KBP-3570)and its major metabolites (KBP-1123 and KBP-1144), Unchanged amoxicillin, Unchanged clarithromycin and its metabolite (14-hydroxyclarithromycin)
Cmax is the peak plasma concentration
Time frame: Hour 0.5 pre-dose and 0.5,1,1.5,2,2.5,3,3.5,4,4.5,5,6,7,8,10,12,24 hours post-dose of Day 1,Day 11
Cohort 2: AUC of anaprazole (parent drug, KBP-3571) and its enantiomer(KBP-3570)and its major metabolites (KBP-1123 and KBP-1144), Unchanged amoxicillin, Unchanged clarithromycin and its metabolite (14-hydroxyclarithromycin)
AUC is area under the plasma concentration-time curve
Time frame: Hour 0.5 pre-dose and 0.5,1,1.5,2,2.5,3,3.5,4,4.5,5,6,7,8,10,12,24 hours post-dose of Day 1,Day 11
Number of subjects with adverse events and serious adverse events as assessed by CTCAE v5.0
All adverse events will be monitored in each subject
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Bismuth is to protect the gastric mucosa
Time frame: From signing informed consent to study completion. 56 days minimum, 68 days maximum(Cohort 1); 30 days minimum, 32 days maximum(Cohort 2)