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Sufficient subjects with a confirmed diagnosis of MS (EDSS score of 6.5 or below), will be recruited to ensure that 30 subjects (approx. equal numbers of each gender) complete the study. Subjects will undergo a screening visit, then four study days, each separated by a washout period of at least 7 days, when the different firategrast batches of drug substance will be administered, and a follow-up visit.
An open-label, randomised, four period crossover study to investigate the relative pharmacokinetic profiles of tablets from three batches of firategrast with different surface areas and two different tablet formulations containing the same batch of firategrast, given as single 900mg doses to male and female subjects with a diagnosis of Multiple Sclerosis
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Sequence ADBC | Experimental | Subjects will be administered formulation A, formulation D, formulation B and formulation C across four study days each separated by a washout period of at least seven days. Subjects will fast overnight prior to dosing. Blood samples will be collected at intervals over a period of 24 hours post-dose. |
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| Sequence BACD | Experimental | Subjects will be administered formulation B, formulation A, formulation C and formulation D across four study days each separated by a washout period of at least seven days. Subjects will fast overnight prior to dosing. Blood samples will be collected at intervals over a period of 24 hours post-dose. |
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| Sequence CBDA | Experimental | Subjects will be administered formulation C, formulation B, formulation D and formulation A across four study days each separated by a washout period of at least seven days. Subjects will fast overnight prior to dosing. Blood samples will be collected at intervals over a period of 24 hours post-dose. |
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| Sequence DCAB | Experimental | Subjects will be administered formulation D, formulation C, formulation A and formulation B across four study days each separated by a washout period of at least seven days. Subjects will fast overnight prior to dosing. Blood samples will be collected at intervals over a period of 24 hours post-dose. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Formulation A | Drug | Formulation A will contain firategrast drug substance from native drug batch Irvine. Subjects will be administered three tablets of 300 milligrams with drug substance surface area of 2.1 square meter per gram. The tablets will be administered with 240 milliliters of water. |
| Measure | Description | Time Frame |
|---|---|---|
| The AUC(0-24) for firategrast following administration of tablets made from three different batches of drug with different surface areas. | Pre-dose. 0.5 hours, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12 hours, 16 hours, 24 hours post dose |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax and Tmax. The AUC(0-24) Cmax and Tmax of of SB683699 metabolite GW786375X. | Pre-dose. 0.5 hours, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12 hours, 16 hours, 24 hours post dose | |
| AEs, vital signs and clinical laboratory data during the course of the study. |
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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 | Prague | 150 18 | Czechia | |||
| GSK Investigational Site |
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| Label | URL |
|---|---|
| Results for study 109079 can be found on the GSK Clinical Study Register. | View source |
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| ID | Term |
|---|---|
| D009103 | Multiple Sclerosis |
| ID | Term |
|---|---|
| D020278 | Demyelinating Autoimmune Diseases, CNS |
| D020274 | Autoimmune Diseases of the Nervous System |
| D009422 | Nervous System Diseases |
| D003711 | Demyelinating Diseases |
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| ID | Term |
|---|---|
| C585685 | Firategrast |
| C000605651 | D-Worm |
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| Formulation B | Drug | Formulation B will contain firategrast drug substance from native drug batch Tonbridge. Subjects will be administered three tablets of 300 milligrams with drug substance surface area of 2.6 square meter per gram. The tablets will be administered with 240 milliliters of water. |
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| Formulation C | Drug | Formulation C will contain firategrast drug substance from Tonbridge single pass micronized drug. Subjects will be administered three tablets of 300 milligrams with drug substance surface area of 3-4 square meter per gram. The tablets will be administered with 240 milliliters of water. |
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| Formulation D | Drug | Formulation D will contain firategrast drug substance from Tonbridge with reduced tablet size. Subjects will be administered three tablets of 300 milligrams with drug substance surface area of 2.6 square meter per gram. The tablets will be administered with 240 milliliters of water. |
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| Throughout the course of the study |
| SB-683699 and GW786375X plasma concentration to derive pharmacokinetic parameters. | Pre-dose. 0.5 hours, 1 hour, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 12 hours, 16 hours, 24 hours post dose |
| Berlin |
| 10117 |
| Germany |
| GSK Investigational Site | Grodzisk Mazowiecki | 05-825 | Poland |
| GSK Investigational Site | Poznan | 60-479 | Poland |
| D001327 | Autoimmune Diseases |
| D007154 | Immune System Diseases |