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The purpose of this study is to determine the absolute oral bioavailability and intravenous pharmacokinetics of GSK962040. The oral dose of 50 mg has been selected because it was well tolerated following single oral administration and it is considered to be within therapeutic dose range. The need to characterize the intravenous disposition of GSK962040 is in anticipation of drug use in special populations such as critically.
GSK962040 is a selective non-peptide motilin receptor agonist which is being developed for the treatment of conditions associated with slow rates of gastric emptying. The purpose of this study is to determine the absolute bioavailability and the metabolic profile of GSK962040. Subjects will be administered a single oral dose of 50 mg followed by a single intravenous dose of 10 mL containing 100 microgram (not more than 270 nCi, 10 kBq) 14C GSK962040, administered by infusion over 15 minutes, beginning at 90 min after administration of the oral dose (approximate Cmax). The oral dose of 50 mg was well tolerated following single oral administration and is predicted to be a therapeutic dose. There is need to characterize GSK962040 disposition in anticipation of drug use in special populations such as critically ill patients. The intravenous (infused) microdose (100 microgram) is 500-fold lower than the oral dose, therefore exposure to GSK962040 originating from the infused microdose is considered negligible.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| A | Experimental | GSK962040 (50 mg, SD, oral) |
|
| B | Experimental | 14C GSK962040 (100 μg, SD, iv) |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| A | Drug | GSK962040 (50 mg, SD, oral) |
| |
| B |
| Measure | Description | Time Frame |
|---|---|---|
| PK parameters for GSK962040 following i.v. dose: AUC(0-inf), Cmax, tmax, t½, systemic clearance (CL), renal clearance (CLr), metabolic clearance (CLm), volume of distribution (Vss), and mean residence time (MRT). | 14 days | |
| PK parameters following oral dose: AUC(0-inf), AUC(0-t), Cmax, tmax, t½, tlag, CLoral and absolute bioavailability (F). | 14 days |
| Measure | Description | Time Frame |
|---|---|---|
| Adverse Events | 14 days | |
| Urine and fecal recovery of GSK962040 following a single oral and i.v. dose of [14C] GSK962040. | 14 days | |
| Urine, fecal recovery and total recovery of radiocarbon (as a percentage of total radioactive dose in each interval and cumulative) |
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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 | Nottingham | NG11 6JS | United Kingdom |
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| Label | URL |
|---|---|
| Results for study 114136 can be found on the GSK Clinical Study Register. | View source |
| Researchers can use this site to request access to anonymised patient level data and/or supporting documents from clinical studies to conduct further research. | View source |
| ID | Type | URL | Comment |
|---|---|---|---|
| 114136 | Individual Participant Data Set | View IPD |
Patient-level data for this study will be made available through www.clinicalstudydatarequest.com following the timelines and process described on this site.
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| Drug |
14C GSK962040 (100 μg, SD, iv) |
|
| 14 days |
| Characterization and semi-quantitation of GSK962040-related metabolites in plasma, urine, and fecal homogenates following a single oral and i.v. dose of [14C] GSK962040. | 14 days |
| Vital signs | 14 days |
| ECGs | 14 days |
| Clinical lab assessments | 14 days |
For additional information about this study please refer to the GSK Clinical Study Register |
| 114136 | Statistical Analysis Plan | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 114136 | Dataset Specification | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 114136 | Study Protocol | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 114136 | Informed Consent Form | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 114136 | Annotated Case Report Form | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 114136 | Clinical Study Report | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| ID | Term |
|---|---|
| D018589 | Gastroparesis |
| ID | Term |
|---|---|
| D013272 | Stomach Diseases |
| D005767 | Gastrointestinal Diseases |
| D004066 | Digestive System Diseases |
| D010243 | Paralysis |
| D009461 | Neurologic Manifestations |
| D012816 | Signs and Symptoms |
| D013568 | Pathological Conditions, Signs and Symptoms |
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