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This is a drug-drug interaction study to evaluate the effects of steady-state exposure of E5555 and its main metabolites on the pharmacokinetics (PK) of metformin, an organic cation transporter-2 (OCT2) substrate. In addition, the study will also investigate the effects of E5555 on several renal function parameters.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Arm 1 | Experimental |
| |
| Arm 2 | Experimental |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| E5555 | Drug | Drug: Oral E5555 400 mg/matching placebo, oral metformin 500 mg, iohexal 20 mL intravenous (IV), and para-aminohippuric acid (PAH) 7 mg/kg IV. |
|
| Measure | Description | Time Frame |
|---|---|---|
| To evaluate the effects of multiple doses of E5555 on single dose pharmacokinetics of metformin. | 15 days |
| Measure | Description | Time Frame |
|---|---|---|
| To assess the effects of multiple doses of E5555 on the glomerular filtration rate estimated using iohexol. | Days 7 and 14 | |
| To assess the effects of multiple doses of E5555 on the effective renal plasma flow estimated using para-aminohippuric acid (PAH). |
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Inclusion Criteria:
- Healthy male or female subjects aged greater than or equal to 18 years to 55 years
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Dr. Bhaskar Rege | Eisai Inc. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Quintiles Phase I Services | Overland Park | Kansas | 661200 | United States |
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| ID | Term |
|---|---|
| C540445 | E 5555 |
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| E5555 | Drug | Drug: Oral E5555 100 mg/matching placebo, oral metformin 500 mg, iohexal 20 mL intravenous (IV), and para-aminohippuric acid (PAH) 7 mg/kg IV bolus. |
|
| Days 7 and 14 |
| To assess the multiple dose pharmacokinetics of E5555 and its main 6 metabolites. | Days 12-18 |
| To assess the safety and tolerability of multiple doses of E5555 and a single dose of metformin either given alone or concomitantly | Day 1 - Day 18 |