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This study is being conducted to measure the relative bioavailability of the original gelatin capsule formulation and a new formulation, immediate release (IR) tablet of Afuresertib (GSK2110183). The study will be composed of Screening, Treatment, and Follow-up Periods. A subject's total time involved in the study will be approximately 9 weeks. The study will enroll approximately 18 healthy volunteers.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Sequence 1 | Experimental | Participants will receive treatment in following sequence in each of the three study periods (one treatment per period): ABC |
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| Sequence 2 | Experimental | Participants will receive treatment in following sequence in each of the three study periods (one treatment per period): ACB |
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| Sequence 3 | Experimental | Participants will receive treatment in following sequence in each of the three study periods (one treatment per period): BAC |
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| Sequence 4 | Experimental | Participants will receive treatment in following sequence in each of the three study periods (one treatment per period): BCA |
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| Sequence 5 | Experimental | Participants will receive treatment in following sequence in each of the three study periods (one treatment per period): CAB |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GSK2110183 Gelatin Capsule | Drug | White opaque hard gelatin capsule with a unit dose strength of 25 milligrams (mg) for oral administration |
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| Measure | Description | Time Frame |
|---|---|---|
| Composite of pharmacokinetic (PK) parameters to determine relative bioavailability of afuresertib after administering it as a single dose in an original gelatin capsule in the fasted state and in a newly formulated IR tablet in the fed and fasted state. | PK parameters include: area under the plasma concentration-time curve from time zero to infinity (AUC [0-infinity]), area under the plasma concentration time curve from time zero to last time of quantifiable concentration (AUC [0-t]), maximum observed plasma concentration (Cmax), and time to Cmax (tmax). | PK Samples will be collected Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72, 120, and 168 hours post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| Number of subjects with adverse events (AEs). | AEs will be collected from the start of Study Treatment and until the Follow-up contact. | Up to 9 weeks |
| Clinical laboratory parameter assessment as a measure of safety and tolerability |
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Inclusion Criteria:
Exclusion Criteria:
An average weekly intake of >21 units for males or >14 units for females. One unit is equivalent to 10 grams (g) of alcohol: 270 mL of full strength beer (4.8%), 375 mL of mid strength beer (3.5%), 470 mL of light beer (2.7%), 250 mL pre-mix full strength spirit (5%), 100mL of wine (13.5%) and 30 mL of spirit (40%).
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| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | GlaxoSmithKline | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Randwick | New South Wales | 2031 | Australia |
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| Label | URL |
|---|---|
| Results for study 201039 can be found on the GSK Clinical Study Register. | View source |
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| ID | Term |
|---|---|
| D009369 | Neoplasms |
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| Sequence 6 | Experimental | Participants will receive treatment in following sequence in each of the three study periods (one treatment per period): CBA |
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| GSK2110183 IR Tablet | Drug | White round biconvex film coated IR tablet with a unit dose strength of 25 mg for oral administration |
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Laboratory parameters include: hematology, clinical chemistry and urinalysis.
| Up to 9 weeks |
| Concomitant medications review as a measure of safety and tolerability | Up to 9 weeks |
| Electrocardiogram (ECGs) measurement as a measure of safety and tolerability | Triplicate 12-lead ECGs will be collected at Screening; in each Dosing Period on Day 1 and Day 3 of Dosing Period; and at Follow-up. | Up to 9 weeks |
| Vital sign measurement as a measure of safety and tolerability | Vital sign measurements will include systolic and diastolic blood pressure and pulse rate. | Up to 9 weeks |
| Composite of PK parameter following single dose administration of IR tablet in fasted state | PK parameters include: AUC (0 - infinity), AUC (0 - t), Cmax, and tmax. | PK Samples will be collected Pre-dose and 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 72, 120, and 168 hours post-dose |