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This study is an open-label, randomized, single dose, four period, balanced crossover study to assess in eligible healthy male or female subjects.
This study is an open-label, randomized, single dose, four period, balanced crossover study to assess in eligible healthy male or female subjects:
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| GSK1322322 IV formulation | Experimental | Subjects will be randomized in a cross over fashion to receive the GSK1322322 administered via IV formulation |
|
| GSK1322322 Wet milled Tablet (Fasted) | Experimental | Subjects will be randomized in a cross over fashion to receive the GSK1322322 administered via Wet milled Tablet (Fasted) |
|
| GSK1322322 Oral mesylate salt solution | Experimental | Subjects will be randomized in a cross over fashion to receive the GSK1322322 administered via Oral mesylate salt solution |
|
| GSK1322322 Wet milled Tablet (Fed) | Experimental | Subjects will be randomized in a cross over fashion to receive the GSK1322322 administered via Wet milled Tablet (Fed) |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| GSK1322322 (mesylate salt) Powder for Injection | Drug | 1500 mg (mesylate salt) as free base, dissolved in sterile water for injection to a concentration of 100 mg/mL free base equivalent and sterilized via filtration. 15 mL of solution, equivalent to 1500 mg GSK 1322322, is the diluted into 0.9% Sodium Chloride Injection prior to infusion |
| Measure | Description | Time Frame |
|---|---|---|
| To estimate the relative bioavailability of wet milled tablet formulations of GSK1322322 with and without food as compared to an oral mesylate salt solution following single doses in healthy subjects. | GSK1322322 AUC(0-∞) and Cmax following wet milled tablet formulation administered with and without moderate fat/calorie meal. GSK1322322 AUC(0-∞) and Cmax following oral mesylate salt solution administration. | 72 Hours |
| To estimate the effect of body weight on the pharmacokinetics of GSK1322322 formulations (IV and oral) following single dose administration to healthy subjects. | GSK1322322 AUC(0-∞) and Cmax in each body weight group following IV or oral formulation administration to assess effect of body weight. | 72 Hours |
| Measure | Description | Time Frame |
|---|---|---|
| To evaluate the safety and tolerability of GSK1322322 after single doses of each formulation in healthy subjects. | Safety parameters including adverse events, clinical laboratory tests, concomitant medications, electrocardiograms, and vital signs. | 14 Days |
| To estimate the absolute bioavailability of the different oral formulations of GSK1322322 as compared to IV mesylate salt formulation following single doses in healthy subjects. |
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Inclusion Criteria:
Exclusion Criteria:
A positive pre-study Hepatitis B surface antigen or positive Hepatitis C antibody result within 3 months of screening
Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
A positive pre-study drug/alcohol screen.
A positive test for HIV antibody.
History of regular alcohol consumption within 6 months of the study defined as: An average weekly intake of >14 drinks for males or >7 drinks for females. One drink is equivalent to 12 g of alcohol: 12 ounces (360 ml) of beer, 5 ounces (150 ml) of wine or 1.5 ounces (45 ml) of 80 proof distilled spirits.
The subject has participated in a clinical trial and has received an investigational product within the following time period prior to the first dosing day in the current study: 30 days, 5 half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
Exposure to more than four new chemical entities within 12 months prior to the first dosing day.
Unable to refrain from the use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St John's Wort) within 7 days (or 14 days if the drug is a potential enzyme inducer) or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless in the opinion of the Investigator and GSK Medical Monitor the medication will not interfere with the study procedures or compromise subject safety due to potential drug interaction.
History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy that, in the opinion of the investigator or GSK Medical Monitor, contraindicates their participation.10. Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
Pregnant females as determined by positive [serum or urine] hCG test at screening or prior to dosing.
Lactating females.
Unwillingness or inability to follow the procedures outlined in the protocol.
Subject is mentally or legally incapacitated.
History of sensitivity to heparin or heparin-induced thrombocytopenia.
Urinary cotinine levels indicative of smoking or history or regular use of tobacco- or nicotine-containing products within 6 months prior to screening.
Unable to refrain from consumption of red wine, seville oranges, grapefruit or grapefruit juice [and/or pummelos, exotic citrus fruits, grapefruit hybrids or fruit juices] from 7 days prior to the first dose of study medication.
Exclusion criteria for screening ECG (a single repeat is allowed for eligibility determination): Males Females Heart rate <45 and >100 bpm <50 and >100 bpm PR Interval <120 and >220 msec QRS duration <70 and >120 msec QTc interval (Bazett) >450 msec
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| Name | Affiliation | Role |
|---|---|---|
| GSK Clinical Trials | GlaxoSmithKline | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| GSK Investigational Site | Minneapolis | Minnesota | 55404 | United States |
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| Label | URL |
|---|---|
| Results for study116595 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 |
|---|---|---|---|
| 116595 | Annotated Case Report Form | 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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|
| GSK1322322 (freebase) tablets | Drug | 500 mg tablets for a 1500 mg total single dose (3 tablets). Taken with 240 mL of water |
|
| GSK1322322 (mesylate salt) Powder for Oral Solution | Drug | 1500 mg as a free base, dissolved in purified water to a concentration of 100 mg/mL free base equivalent. 15 mL of solution, equivalent to1500 mg GSK1322322 is administered orally with 225 mL of water |
|
| GSK1322322 (freebase) tablets FED | Drug | Drug 500 mg tablets for a 1500 mg total single dose (3 tablets) (FED moderate fat meal) Taken with 240 mL of water |
|
GSK1322322 AUC(0-∞) following different oral formulations (oral mesylate salt solution and wet milled tablet) versus IV formulation to assess absolute bioavailability. GSK1322322 pharmacokinetic parameters will be computed with noncompartmental analysis |
| 72 Hours |
For additional information about this study please refer to the GSK Clinical Study Register |
| 116595 | Clinical Study Report | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 116595 | Informed Consent Form | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 116595 | Individual Participant Data Set | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 116595 | Study Protocol | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 116595 | Dataset Specification | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| 116595 | Statistical Analysis Plan | View IPD | For additional information about this study please refer to the GSK Clinical Study Register |
| ID | Term |
|---|---|
| D001424 | Bacterial Infections |
| ID | Term |
|---|---|
| D001423 | Bacterial Infections and Mycoses |
| D007239 | Infections |
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| ID | Term |
|---|---|
| C583947 | GSK1322322 |
| D011208 | Powders |
| D007267 | Injections |
| D013607 | Tablets |
| D012996 | Solutions |
| ID | Term |
|---|---|
| D004304 | Dosage Forms |
| D004364 | Pharmaceutical Preparations |
| D004333 | Drug Administration Routes |
| D004358 | Drug Therapy |
| D013812 | Therapeutics |
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