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The purpose of the current Phase I, open-label, three-period, single sequence, crossover study, TPL116010, is to evaluate the potential drug-drug interaction between eltrombopag (ELT) and bocrprevir (BCP) and between ELT and telaprevir (TLP) in healthy subjects. In this study there will be a screening visit, three treatment periods, and a follow-up visit. In Period 1, subjects will receive a single dose of ELT on Day 1, and pharmacokinetic (PK) sampling will occur for 72 hours. In Period 2, subjects will receive BCP/TLP for 10 days with PK sampling for 8 hours. In Period 3, subjects will receive a single dose of ELT with BCP/TLP on Day 1 only with PK sampling for 72 hours. Subjects will return for a follow-up visit within 10 to 14 days of the last dose of study drugs. The total duration of the study from Screening to Follow-up will be approximately 9 weeks.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Eltrombopag | Experimental | Subjects will receive single oral dose of eltrombopag 200 mg in Period 1 with moderate-fat, low-calcium meal. |
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| Boceprevir | Experimental | Subjects will receive boceprevir 800 mg orally every 8 hours (hrs) for 10 days in Period 2 with moderate-fat meals. |
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| Telaprevir | Experimental | Subjects will receive telaprevir 750 mg orally every 8 hours hrs for 10 days in Period 2 with moderate-fat meals. |
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| Eltrombopag and Broceprevir | Experimental | Subjects will receive eltrombopag 200 mg as single oral dose and boceprevir 800 mg orally every 8 hrs for a day in Period 3 with moderate-fat meals. |
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| Eltrombopag and Telaprevir | Experimental | Subjects will receive eltrombopag 200 mg as single oral dose and telaprevir 750 mg orally every 8 hrs for a day in Period 3 with moderate-fat meals. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Eltrombopag | Drug | Each tablet contains 100 mg of Eltrombopag (Dose 200 mg) |
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| Measure | Description | Time Frame |
|---|---|---|
| Composite pharmacokinetic (PK) parameters of eltrombopag following administration of boceprevir for 10 days with a single dose of eltrombopag | Plasma eltrombopag PK Parameters: area under the concentration time-curves from time zero to infinity AUC(0-infinity) and maximum concentration (Cmax). | For 17 days |
| Composite PK parameters of boceprevir following administration of boceprevir for 10 days with a single dose of eltrombopag | Plasma boceprevir PK Parameters: AUC from time zero to the dosing interval AUC(0-Ï„), Cmax, and Concentraction at end of the dosing interval (CÏ„) | For 17 days |
| Composite PK parameters of eltrombopag following administration of telaprevir for 10 days with a single dose of eltrombopag | Plasma eltrombopag PK Parameters: AUC(0-infinity) and Cmax | For 17 days |
| Composite PK parameters of telaprevir following administration of telaprevir for 10 days with a single dose of eltrombopag | Plasma telaprevir PK Parameters: AUC(0-Ï„), Cmax, and CÏ„. | For 17 days |
| Measure | Description | Time Frame |
|---|---|---|
| Composite PK parameters of eltrombopag following administration of boceprevir for 10 days with a single dose of eltrombopag | Plasma eltrombopag PK Parameters: AUC from time zero to the last measurable concentration (AUC(0-t)), AUC obtained by extrapolation (%) (%AUCex), time from administration to first quantifiable concentration (tlag), time from administration to Cmax (tmax), elimination half life (t1/2), and apparent clearance (CL/F). |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | GlaxoSmithKline | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Baltimore | Maryland | 21225 | United States |
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| Label | URL |
|---|---|
| Results for study 116010 can be found on the GSK Clinical Study Register. | View source |
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| ID | Term |
|---|---|
| D013921 | Thrombocytopenia |
| ID | Term |
|---|---|
| D001791 | Blood Platelet Disorders |
| D006402 | Hematologic Diseases |
| D006425 | Hemic and Lymphatic Diseases |
| D000095542 | Cytopenia |
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| ID | Term |
|---|---|
| C520809 | eltrombopag |
| C512204 | N-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide |
| C486464 | telaprevir |
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| Boceprevir | Drug | Each capsule contains 200 mg of Boceprevir (Dose 800 mg) |
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| Telaprevir | Drug | Each tablet contains 375 mg of Telaprevir (Dose 750 mg) |
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| For 17 days |
| Composite PK parameters of boceprevir following administration of boceprevir for 10 days with a single dose of eltrombopag | Plasma boceprevir PK Parameter: tmax. | For 17 days |
| Composite PK parameters of eltrombopag following administration of telaprevir for 10 days with a single dose of eltrombopag | Plasma eltrombopag PK Parameters: AUC(0-t), %AUCex, tlag, tmax, t1/2, and CL/F. | For 17 days |
| Composite PK parameters of telaprevir following administration of telaprevir for 10 days with a single dose of eltrombopag | Plasma telaprevir PK Parameter: tmax. | For 17 days |
| Safety and tolerability as assessed by the collection of adverse events | For 28 days |
| Safety and tolerability as assessed by change from baseline in clinical laboratory tests | Clinical laboratory tests include hematology, clinical chemistry, urinalysis tests. | For 28 days |
| Safety and tolerability as assessed by change from baseline in vital sign | Vital sign measurements will include systolic and diastolic blood pressure and pulse rate. | For 28 days |