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This is a single-center, placebo-controlled, randomized, ascending dose, double-blind study. This study will be evaluating ascending doses of 50, 100, 200, and 400 mg of E6007. This study consists of 5 steps, 1 to 5. In steps 1 to 4 (at ascending doses of 50, 100, 200, and 400 mg), subjects will be randomly assigned in a 6:2 ratio (E6007: placebo) to receive single dose of the study drug under fasted condition. Following 3 days of washout period, subject will receive the study drug once daily for 7 days starting on the fifth day from the single dose administration.
For step 3 (200 mg), subjects will subsequently have at least 17 days of washout period before being escalated to step 5 (200 mg) to receive single dose of E6007 under fed condition, to evaluate food effect of the study drug.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 50 mg E6007 fasted condition | Experimental | E6007 50mg or E6007 matching placebo x 1, orally once daily in the morning under fasted condition. Drug administration on 1 day for single dose period (Day 1) and 7 days (Day 5 to 11) for repeated dose period. |
|
| 100 mg E6007 fasted condition | Experimental | E6007 50mg or E6007 matching placebo x 2, orally once daily in the morning under fasted condition. Drug administration on 1 day for single dose period (Day 1) and 7 days (Day 5 to 11) for repeated dose period. |
|
| 200 mg E6007 fasted condition | Experimental | E6007 50mg or E6007 matching placebo x 4, orally once daily in the morning under fasted condition. Drug administration on 1 day for single dose period (Day 1) and 7 days (Day 5 to 11) for repeated dose period. |
|
| 400 mg E6007 fasted condition | Experimental | E6007 50mg or E6007 matching placebo x 8, orally once daily in the morning under fasted condition. Drug administration on 1 day for single dose period (Day 1) and 7 days (Day 5 to 11) for repeated dose period. |
|
| 200 mg E6007 fed condition |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| E6007 | Drug |
|
| Measure | Description | Time Frame |
|---|---|---|
| Safety and tolerability of E6007 as a measure of Adverse events | Screening and up to 17 days after last administration of drug | |
| Plasma E6007 concentration over time period - Cmax (maximum concentration) | Up to 15 days | |
| Plasma E6007 concentration over time period - tmax (Time to achieve maximum concentration (Cmax)) | Up to 15 days | |
| Plasma E6007 concentration over time period - AUC (0-t) (Area Under the Curve (AUC) from Time Zero to Last Quantifiable Concentration) | Up to 15 days | |
| Plasma E6007 concentration over time period - AUC (0-inf) (AUC extrapolated to infinity) | Up to 15 days | |
| Plasma E6007 concentration over time period - t1/2 (Terminal phase half-life) | Up to 15 days | |
| Plasma E6007 concentration over time period - CL/F (Apparent clearance) | Up to 15 days | |
| Plasma E6007 concentration over time period - Vz/F (Apparent volume of distribution) | Up to 15 days | |
| Plasma E6007 concentration over time period - Css,max (maximum steady state concentration) | Up to 15 days | |
| Plasma E6007 concentration over time period - AUC (0-tau) (AUC from time zero to time tau over a dosing interval at steady state) |
| Measure | Description | Time Frame |
|---|---|---|
| Dose proportionality under fasted conditions with Cmax, AUC (0-t), AUC(0-inf), Cssmax and AUC(0-t) | Up to 15 days | |
| Geometric mean proportion (fed:fasted) of Cmax, AUC(0-t) and AUC(0-inf) for 200mg E6007 dose | Up to 5 days |
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Inclusion criteria
Subjects must meet all of the following criteria to be included in this study:
Exclusion criteria
Subjects who meet any of the following criteria will be excluded from this study:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Sumida-ku | Tokyo | Japan |
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| Experimental |
E6007 50mg or E6007 matching placebo x 4, orally once daily in the morning under fed condition. Drug administration on 1 day (Day 1). |
|
| E6007 matching placebo | Drug |
|
| Up to 15 days |
| Evaluate relationship between E6007 plasma concentrations and electrocardiogram (ECG) parameter (QTcF) | Up to 15 days |