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This study will investigate how 3 new types of drug formulations are absorbed by the body. This study is termed 'open-label', which means volunteers will be aware of which treatment they are receiving. The study involves all volunteers receiving all 3 different formulations, as a single dose, and there is no placebo (dummy-drug; no active ingredient) in this study. Volunteers will also receive a single dose of a formulation used in previous trials (reference formulation), so as a proper comparison with the new formulations can be made. One of the new formulations will also be administered along with food, to assess if the drug performs or is absorbed differently.
The present study will investigate the tolerability and pharmacokinetics of single oral doses of firategrast administered as the existing immediate release tablet formulation and as three modified release tablet formulations designed to release drug over differing relase rates. The range of release rates is expected to give preliminary information on the performance of a matrix modified release formulation for use in future efficacy studies.
Subjects will receive each formulation in the fasted state in a randomised 4-part single dose crossover fashion. Based on the review of pharmacokinetic data from at least the first two study sessions, subjects may also receive a fifth dose of firategrast, administered after a high fat meal. The formulation administered with food will be chosen based upon pharmacokinetic data from previous dose sessions. Doses administered will be different with respect to gender; the doses are expected to result in similar exposures across the genders.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Firategrast XRA | Experimental | Low extended release tablet |
|
| Firategrast XRB | Experimental | Medium extended releast tablet |
|
| Firategrast XRC | Experimental | High extended release tablet |
|
| Firategrast IR | Experimental | Immediate Release reference tablet |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| A | Drug | Single dose treatment IR formulation |
| |
| B |
| Measure | Description | Time Frame |
|---|---|---|
| Systemic concentration & AUC of study drug | pre-dose, up to 120 hours after each single dose |
| Measure | Description | Time Frame |
|---|---|---|
| Adverse events | from screening, through study day, and up to follow-up visit. Spontaneous reporting | |
| Systemic concentration & AUC of study drug metabolite | pre-dose, up to 120 hours after each single dose |
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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 | Randwick | New South Wales | 2031 | Australia |
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| Label | URL |
|---|---|
| Results for study 114107 can be found on the GSK Clinical Study Register. | View source |
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| Drug |
Low Extended release single dose |
|
| C | Drug | Medium extended release formulation |
|
| D | Drug | High extended release rate single dose |
|
| Vital signs | screening, pre-dose, up-to 15 hours post does, follow-up visit |
| 12-lead Electrocardiogram | screening, pre-dose and up to 8 hours post dose, then at follow-up |
| Heamatology, clinical chemistry and Uninalysis | Blood samples for standard clinical safety monitoring, and unine samples | screening, predose, up-to 8 hours post dose, follow-up |
| ID | Term |
|---|---|
| D020529 | Multiple Sclerosis, Relapsing-Remitting |
| ID | Term |
|---|---|
| D009103 | Multiple Sclerosis |
| D020278 | Demyelinating Autoimmune Diseases, CNS |
| D020274 | Autoimmune Diseases of the Nervous System |
| D009422 | Nervous System Diseases |
| D003711 | Demyelinating Diseases |
| D001327 | Autoimmune Diseases |
| D007154 | Immune System Diseases |
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| ID | Term |
|---|---|
| C007792 | Fumigant 93 |
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