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This is a study to evaluate the relative bioavailability and tolerability of two different pimicotinib capsules in healthy subjects under fasting condition. 26 healthy subjects are planned to be enrolled and will be evenly randomized to either Study Sequence A or Study Sequence B . Subjects in Sequence A/Sequence B will receive a single 50 mg oral dose of test/reference pimicotinib in period 1 and cross over in period 2. Blood samples will be collected for PK analysis in totally 32 time-points.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| pimicotinib (test capsule-reference capsule) | Other | subjects in sequence A will receive a single oral dose of 50 mg test capsule administered as 2 x 25 mg (the capsule is commercial formulation to be marketed) in period 1 day 1 and receive a single oral dose of 50 mg reference capsule administered as 2 x 25 mg (the capsule was used in phase 3 study Part 1) in period 2 day 1. |
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| pimicotinib (reference capsule-test capsule) | Other | subjects in sequence B will receive a single oral dose of 50 mg reference capsule administered as 2 x 25 mg (the capsule was used in phase 3 study Part 1) in period 1 day 1 and receive a single oral dose of 50 mg test capsule administered as 2 x 25 mg (the capsule is commercial formulation to be marketed) in period 2 day 1 . |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| pimicotinib capsules | Drug | pimicotinib capsules |
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| Measure | Description | Time Frame |
|---|---|---|
| Cmax | Peak concentration, the maximum observed plasma concentration of pimicotinib | Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours. |
| AUC0-∞ | Area under the plasma concentration-time curve of pimicotinib from time 0 to infinity, calculated as: AUC0-∞=AUClast +Clast/λz; Clast refers to the last measurable (non-BQL) plasma concentration of pimicotinib. | Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours. |
| AUClast | Area under the plasma concentration-time curve of pimicotinib from time 0 to the time of last measurable (non-BQL) concentration (calculated using the Linear Up Log Down trapezoidal method) | Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours. |
| Measure | Description | Time Frame |
|---|---|---|
| AE | To evaluate the safety following a single oral dose of the two different pimicotinib capsules under fasting conditions in healthy subjects, including Adverse events (AEs), serious adverse events (SAEs), vital signs, physical examinations, electrocardiograms (ECGs), laboratory tests | through study completion, an average of 24 days |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Yanhua Ding, Doctor | The First Hospital of Jilin University | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| The First Hospital of Jilin University | Changchun | Jilin | China |
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| t1/2 |
Elimination half-life |
| Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours. |
| CL/F | Total apparent clearance after a single oral dose | Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours. |
| Vz/F | Apparent volume of distribution after a single oral dose | Period 1& Period 2: pre-dose, postdose 15 minutes, 0.5 hour, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 24 hours, 48 hours, 96 hours, 120 hours, 144 hours, 192 hours and 240 hours. |