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The purpose of this study is to estimate the effect of rifampicin or itraconazole on the single dose PK of ensartinib.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Cohort 1 | Experimental | All subjects in this cohort will receive the same dose of Ensartinib in both periods. Subjects will receive Ensartinib Alone in Period 1 followed by Ensartinib with Rifampicin in Period 2. |
|
| Cohort 2 | Experimental | All subjects in this cohort will receive the same dose of Ensartinib in both periods. Subjects will receive Ensartinib Alone in Period 1 followed by Ensartinib with Itraconazole in Period 2. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Ensartinib | Drug | 225 mg oral dose on day 1 in period 1 and on day 18 in period 2 |
| |
| Measure | Description | Time Frame |
|---|---|---|
| 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). | 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). | 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. | 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. | 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 |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Role | Phone | Extension | |
|---|---|---|---|---|
| Bo Jiang, Ph.D | Contact | 0571-87783759 | jiangbo@zju.edu.cn |
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| The Second Affiliated hospital of Zhejiang University School of Medicine | Hangzhou | Zhejiang | 310009 | China |
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| ID | Term |
|---|---|
| C000629294 | ensartinib |
| D012293 | Rifampin |
| D017964 | Itraconazole |
| ID | Term |
|---|---|
| D012294 | Rifamycins |
| D006576 | Heterocyclic Compounds, 4 or More Rings |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D006571 | Heterocyclic Compounds |
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| Rifampicin |
| Drug |
600 mg QD from day 9 to day 22 in period 2 |
|
| Itraconazole | Drug | 200 mg QD from day 9 to day 19 in period 2 |
|
| Ensartinib | Drug | 100 mg oral dose on day 1 in period 1 and on day 12 in period 2 |
|
Maximum plasma concentration |
| 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 Cmax for Ensartinib Given Alone and With Itraconazole | Maximum plasma concentration | 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. |
| D047029 | Lactams, Macrocyclic |
| D047028 | Macrocyclic Compounds |
| D011083 | Polycyclic Compounds |
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D010879 | Piperazines |