The purpose of this study is to estimate the effect of rifampicin or itraconazole on the single dose PK of ensartinib.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
36
225 mg oral dose on day 1 in period 1 and on day 18 in period 2
600 mg QD from day 9 to day 22 in period 2
200 mg QD from day 9 to day 19 in period 2
The Second Affiliated hospital of Zhejiang University School of Medicine
Hangzhou, Zhejiang, China
Plasma AUC0-t for Ensartinib Given Alone and With Rifampicin
AUC0-t is the plasma area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration (Clast).
Time frame: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours post-dose on Day 1 after Ensartinib 225 mg administration in Period 1, and at the same time points on Day 18 after Ensartinib 225 mg with rifampin administration in Period 2.
Plasma AUC0-t for Ensartinib Given Alone and With Itraconazole
AUC0-t is the plasma area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration (Clast).
Time frame: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post-dose on Day 1 after Ensartinib 100 mg administration in Period 1, and at the same time points on Day 12 after Ensartinib 100 mg with Itraconazole administration in Period 2.
Plasma AUC0-∞ for Ensartinib Given Alone and With Rifampicin
AUC0-∞ is the plasma area under the plasma concentration-time profile from time 0 extrapolated to infinite time.
Time frame: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours post-dose on Day 1 after Ensartinib 225 mg administration in Period 1, and at the same time points on Day 18 after Ensartinib 225 mg with rifampin administration in Period 2.
Plasma AUC0-∞ for Ensartinib Given Alone and With Itraconazole
AUC0-∞ is the plasma area under the plasma concentration-time profile from time 0 extrapolated to infinite time.
Time frame: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post-dose on Day 1 after Ensartinib 100 mg administration in Period 1, and at the same time points on Day 12 after Ensartinib 100 mg with Itraconazole administration in Period 2.
Plasma Cmax for Ensartinib Given Alone and With Rifampicin
Maximum plasma concentration
Time frame: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120 hours post-dose on Day 1 after Ensartinib 225 mg administration in Period 1, and at the same time points on Day 18 after Ensartinib 225 mg with rifampin administration in Period 2.
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100 mg oral dose on day 1 in period 1 and on day 12 in period 2
Plasma Cmax for Ensartinib Given Alone and With Itraconazole
Maximum plasma concentration
Time frame: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post-dose on Day 1 after Ensartinib 100 mg administration in Period 1, and at the same time points on Day 12 after Ensartinib 100 mg with Itraconazole administration in Period 2.