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| Name | Class |
|---|---|
| Axis Clinicals Limited | INDUSTRY |
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In this open label, single-sequence study, subjects received one dose of XS004 Dasatinib Amorphous Solid Dispersion Film-Coated Tablet, 90 mg Test Formulation at the start of study on Day 1 and Day 6. Omeprazole 40 mg was administered on Day 2, 3, 4, 5 and 6. The study was conducted in two groups.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Dasatinib ASD alone | Experimental | At the clinic, participants were administered a single oral dose of 90 mg Dasatinib (Amorphous Solid Dispersion Film-Coated Tablet) on Day 1 after an overnight fast of at least 9 hours. Dasatinib was given with approximately 240 mL of room temperature water. Fasting continued for at least 4 hours following drug administration, after which a standardized lunch was served. |
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| Dasatinib ASD + Omeprazole | Other | At the clinic, on Day 2 to Day 6, participants were administered a single oral dose of Omeprazole 40 mg × 1 Delayed Release Capsule once before meals in the evening with approximately 150 mL of room temperature water. No food was allowed two hours before and one hour after administration of Omeprazole. In addition, participants were administered a single oral dose of 90 mg Dasatinib (Amorphous Solid Dispersion Film-Coated Tablet) on Day 6 after an overnight fast of at least 9 hours. Dasatinib was given with approximately 240 mL of room temperature water. Fasting continued for at least 4 hours following drug administration, after which a standardized lunch was served. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Dasatinib ASD | Drug | XS004 Dasatinib Amorphous Solid Dispersion Film-Coated Tablet, 90 mg Test Formulation |
|
| Measure | Description | Time Frame |
|---|---|---|
| Maximum Observed Plasma Concentration of Dasatinib (Cmax) | Pharmacokinetic parameters (Cmax) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods. | Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6. |
| Area Under the Plasma Concentration-Time Curve from Zero to 24h | Pharmacokinetic parameters (AUC 0-24) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods. | Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6. |
| Area Under the Plasma Concentration-Time Curve from Zero Extrapolated to Infinity | Pharmacokinetic parameters (AUC 0-INF) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods. | Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6. |
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Plasma Concentration-Time Curve (Percent Extrapolation) | Pharmacokinetic parameters (AUC %Extrapolation) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods. | Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Per Andersson, PhD | Xspray Pharma AB | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| AXIS Clinicals | Dilworth | Minnesota | 56529-1342 | United States |
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| Omeprazole 40 MG | Drug | Omeprazole Delayed Release Capsules, USP 40 mg |
|
| Time of Maximum Observed Plasma Concentration of Dasatinib (Tmax) | Pharmacokinetic parameters (Tmax) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods. | Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6. |
| Elimination Rate Constant (Kel) | Pharmacokinetic parameters (Kel) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods. Apparent first order elimination rate constant calculated from a semi-log plot of plasma concentration versus time point. | Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6. |
| Terminal Half-Life (T1/2) | Pharmacokinetic parameters (T1/2) for plasma dasatinib on Day 1 (Dasatinib alone) and on Day 6 (Dasatinib + Omeprazole) calculated for each subject using drug concentration-time data by non-compartmental methods. | Blood samples collected at 15 time points (including pre-dose) during the study period on Day 1 and Day 6. |
| ID | Term |
|---|---|
| D009853 | Omeprazole |
| ID | Term |
|---|---|
| D053799 | 2-Pyridinylmethylsulfinylbenzimidazoles |
| D013454 | Sulfoxides |
| D013457 | Sulfur Compounds |
| D009930 | Organic Chemicals |
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
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