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Study to Assess the Pharmacokinetics of R406 in Healthy Subjects when Fostamatinib 150 mg is Administered Alone in Fed and Fasted state and in Combination with Ranitidine in Fasted State, and to Assess the Relative Bioavailability of Process Variants of Tablets
An Open-label, Single-center, 2-Part, Randomized Study to Assess the Pharmacokinetics of R406 in Healthy Subjects when Fostamatinib 150 mg is Administered Alone in Fed and Fasted state and in Combination with Ranitidine in Fasted State, and to Assess the Relative Bioavailability of Process Variants of Tablets
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part A1 | Active Comparator | 1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference), fed 3 x 50mg microcrystalline cellulose-based 13% drug loaded tablets,(blue) fed |
|
| Part A2 | Active Comparator | 1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference) 3 x 50mg microcrystalline cellulose-based 13% drug loaded tablets,(blue) fed 150 mg ranitidine |
|
| Part B1 | Active Comparator | 1 x 150mg mannitol based 38% drug-loaded tablet (batch variant A) |
|
| Part B2 | Active Comparator | 1 x 150mg mannitol based 38% drug loaded tablet (batch variant B) |
|
| Part B3 | Active Comparator |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Fostamatinib - 1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference) | Drug | 1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference) |
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics profile of R406 in terms of maximum observed plasma concentration (Cmax) and area under the plasma concentration-time curve from time zero extrapolated to infinity (AUC). | Day 1 (predose) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, and 96 hours postdose |
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetic profile of R406 in terms of area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration [AUC(0-t)], time to Cmax (tmax), terminal half-life (t1/2λz), terminal rate constant (λz). | Day 1 (predose) and at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72, and 96 hours postdose | |
| Description of the safety profile in terms of frequency of adverse events. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Eleanor Lisbon, MD | Quintiles Phase I unit 6700 w 115th st Overland Park, Ks 66211 | Principal Investigator |
| Christopher D O'Brien, MD PHD | AstraZeneca | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Overland Park | Kansas | United States |
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1 x 150mg mannitol-based 38% drug-loaded tablet(orange reference) |
|
| Fostamatinib - 3 x 50mg microcrystalline cellulose-based 13% drug loaded tablets,(blue) fed | Drug | 3 x 50mg microcrystalline cellulose-based 13% drug loaded tablets,(blue) fed |
|
| Fostamatinib - 1 x 150mg mannitol based 38% drug-loaded tablet (batch variant A) | Drug | 1 x 150mg mannitol based 38% drug-loaded tablet (batch variant A) |
|
| Fostamatinib - 1 x 150mg mannitol based 38% drug loaded tablet (batch variant B) | Drug | 1 x 150mg mannitol based 38% drug loaded tablet(batch variant B) |
|
| Ranitidine | Drug | 150 mg ranitidine |
|
| up to 3 - 5 days after discharge |
| Description of the safety profile in terms of severity of adverse events. | up to 3 - 5 days after discharge |
| ID | Term |
|---|---|
| D011899 | Ranitidine |
| ID | Term |
|---|---|
| D005663 | Furans |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
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