The purpose of this study is to evaluate the single-dose (SD) pharmacokinetics (PK), pharmacodynamics (PD), safety and tolerability of 10, 40, and 80 mg E5501 followed by a selected dose for multiple dosing (MD) in healthy Japanese, Chinese, and Caucasian subjects.
This study will evaluate the single-dose (SD) pharmacokinetics (PK), pharmacodynamics (PD), safety, and tolerability of oral doses of 10, 40, and 80 mg E5501 administered to 36 healthy male and female Japanese, Chinese, and Caucasian subjects. For the SD Treatment Period, 12 subjects from each ethnic group will be randomized to receive single doses of 10, 40, or 80 mg E5501 or matching placebo each treatment period. Each subject will be allocated to a treatment sequence to be dosed with either placebo for the three periods or dosed with each of the three different doses in the three periods. For the Multiple-Dose (MD) Treatment Period the 12 subjects in each ethnic group will be further randomized as active (dose level to be determined from the SD Treatment Period or placebo in a 3:1 ratio.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
36
Treatment Group 1: 10mg E5501 as a single dose in Treatment Period 1, followed by a single dose of 40mg E5501 in Treatment Period 2, followed by a single dose of 80mg E5501 in Treatment Period 3, followed by a selected dose for the Multiple Dose reatment Period.
Treatment Group 2: 40 mg E5501 as a single dose in Treatment Period 1, followed by a single dose of 80mg E5501 in Treatment Period 2, followed by a single dose of 10mg E5501 in Treatment Period 3, followed by a selected dose for the Multiple Dose Treatment Period.
Treatment Group 3: 80mg E5501 as a single dose in Treatment Period 1, followed by a single dose of 10mg E5501 in Treatment Period 2, followed by a single dose of 40mg E5501 in Treatment Period 3, followed by a selected dose for the Multiple Dose Treatment Period.
Parexel International, Early Phase Clinical Unit
Los Angeles, California, United States
• To compare the single-dose pharmacokinetics (PK), as measured by AUCinf of three doses of E5501 (10, 40, and 80 mg) in healthy Japanese and Chinese subjects relative to healthy Caucasian subjects
Time frame: up to 96 hours post-dose
• To compare the multiple-dose steady-state PK, as measured by AUCss, of E5501 in healthy Japanese and Chinese subjects relative to Caucasian subjects
Time frame: up to 96 hours after dosing on Day 7 or up to 240 hours after the first drug dosing
• To compare the multiple-dose pharmacodynamic (PD) response as measured by platelet counts for E5501 in healthy Japanese and Chinese subjects relative to Caucasian subjects
Time frame: through Day 21 for each SD Treatment Period and through Day 30 for the MD Treatment Period
• To compare the single-dose pharmacokinetics (PK), as measured by Cmax of three doses of E5501 (10, 40, and 80 mg) in healthy Japanese and Chinese subjects relative to healthy Caucasian subjects
Time frame: up to 96 hours post-dose
To evaluate single-dose linearity of 10, 40 and 80mg E5501 in healthy Japanese, Chinese, and Caucasian subjects
Time frame: from Day 1 SD Treatment Period 1 through Day 30 MD Treatment Period 4
To characterize PK/PD relationships between E5501 exposure and platelet count response in healthy Japanese, Chinese, and Caucasian subjects
Time frame: from Day 1 SD Treatment Period 1through Day 30 MD Treatment Period 4
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Treatment Group 4: A single dose of matching placebo in each of the three Single Dose Treatment Periods and in the Multiple Dose Treatment Period