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A Study to Assess Safety, Tolerability, and Pharmacokinetics of E2307 in Healthy Young and Elderly Japanese Subjects

Phase 1
Completed
Conditions
Healthy Subjects
Interventions
Drug: E2307 Matching Placebo
Registration Number
NCT02289599
Lead Sponsor
Eisai Co., Ltd.
Brief Summary

This study will be a single-center, single dose, randomized, double-blind, placebo-controlled study in healthy Japanese male subjects. The study will consist of 2 parts: Part A (young subjects) and Part B (elderly subjects). In Part A sequential cohorts of subjects will be treated with single ascending doses of E2307. The maximum tolerated dose (MTD) will be determined in Part A. Part B will be initiated after Part A is completed. In Part B one cohort of healthy elderly subjects will be treated with a single dose of E2307 at one dose level below the MTD. In part A, a total of 56 subjects will be enrolled into 7 cohorts sequentially and randomized 3:1 to receive either E2307 (1 mg, 3 mg, 10 mg, 30 mg, 100 mg, 200 mg, or 300 mg) or placebo. In part B, a total of 8 subjects will be randomized, 6 subjects to a single dose of E2307 and 2 subjects to placebo.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
24
Inclusion Criteria

Parts A and B

  1. Provide written informed consent

  2. Willing and able to comply with all aspects of the protocol

    Part A: Young cohort

  3. Non-smoking, male subjects age >=20 years and less than 55 years old at the time of informed consent

    Part B: Elderly Cohort

  4. Non-smoking, male subjects age >=65 years and less than 85 years old at the time of informed consent

Exclusion Criteria

Subjects who meet any of the following criteria will be excluded from this study:

  1. Clinically significant illness that requires medical treatment within 8 weeks or a clinically significant infection that requires medical treatment within 4 weeks of dosing
  2. Any history of abdominal surgery that may affect PK profiles of E2307 (eg. hepatectomy, nephrectomy, digestive organ resection)
  3. Known history of clinically significant drug allergy (at Screening)

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Part A: 10 mg E2307 (young cohort)E2307E2307 (1 x 10 mg E2307 capsule) or placebo (1 x 1 E2307 matching placebo capsule)
Part A: 10 mg E2307 (young cohort)E2307 Matching PlaceboE2307 (1 x 10 mg E2307 capsule) or placebo (1 x 1 E2307 matching placebo capsule)
Part A: 1 mg E2307 (young cohort)E2307E2307 (1 x 1 mg E2307 capsule) or placebo (1 x 1 E2307 matching placebo capsule)
Part A: 1 mg E2307 (young cohort)E2307 Matching PlaceboE2307 (1 x 1 mg E2307 capsule) or placebo (1 x 1 E2307 matching placebo capsule)
Part A: 3 mg E2307 (young cohort)E2307E2307 (3 x 1 mg E2307 capsules) or placebo (3 x 1 E2307 matching placebo capsules)
Part A: 3 mg E2307 (young cohort)E2307 Matching PlaceboE2307 (3 x 1 mg E2307 capsules) or placebo (3 x 1 E2307 matching placebo capsules)
Part A: 30 mg E2307 (young cohort)E2307E2307 (3 x 10 mg E2307 capsules) or placebo (3 x 1 E2307 matching placebo capsules)
Part A: 30 mg E2307 (young cohort)E2307 Matching PlaceboE2307 (3 x 10 mg E2307 capsules) or placebo (3 x 1 E2307 matching placebo capsules)
Part A: 100 mg E2307 (young cohort)E2307E2307 (1 x 100 mg E2307 capsule) or placebo (1 x 1 E2307 matching placebo capsule)
Part A: 100 mg E2307 (young cohort)E2307 Matching PlaceboE2307 (1 x 100 mg E2307 capsule) or placebo (1 x 1 E2307 matching placebo capsule)
Part A: 200 mg E2307 (young cohort)E2307E2307 (2 x 100 mg E2307 capsules) or placebo (2 x 1 E2307 matching placebo capsules)
Part A: 200 mg E2307 (young cohort)E2307 Matching PlaceboE2307 (2 x 100 mg E2307 capsules) or placebo (2 x 1 E2307 matching placebo capsules)
Part A: 300 mg E2307 (young cohort)E2307E2307 (3 x 100 mg E2307 capsules) or placebo (3 x 1 E2307 matching placebo capsules)
Part A: 300 mg E2307 (young cohort)E2307 Matching PlaceboE2307 (3 x 100 mg E2307 capsules) or placebo (3 x 1 E2307 matching placebo capsules)
Part B: Elderly cohortE2307One dose level below MTD from Part A
Primary Outcome Measures
NameTimeMethod
Plasma PK of E2307: Vz/F (apparent volume of distribution at terminal phase)Up to 12 days

Vz/F are calculated for E2307 only

Plasma PK of E2307: AUC ratio (AUC ratio of metabolite to parent)Up to 12 days
Urine PK of E2307: Ae (cumulative amount of drug excreted in urine up to 264 hours postdose)Up to 12 days
Urine PK of E2307: CLR (renal clearance)Up to 12 days
Plasma PK of E2307: t1/2 (terminal elimination phase half-life)Up to 12 days
Number of adverse events/serious adverse eventsUp to 30 days
Plasma pharmacokinetics (PK) of E2307: Cmax (maximum observed concentration)Up to 12 days
Plasma PK of E2307: tmax (time at which the highest drug concentration occurs)Up to 12 days
Plasma PK of E2307: AUC(0-t) [area under the concentration (AUC)-time curve from zero time to time of last quantifiable concentration]Up to 12 days
Plasma PK of E2307: AUC(0-inf) [area under the concentration-time curve from zero time extrapolated to infinite time]Up to 12 days
Plasma PK of E2307: CL/F (apparent total clearance following oral administration)Up to 12 days

CL/F are calculated for E2307 only

Secondary Outcome Measures
NameTimeMethod
Mean difference in change of mean blood pressure (BP) between E2307 and placebo24 hours predose and continue until 24 hours postdose (Day 2)
QT interval assessment using Holter monitoring24 hours predose through Day 2 (at 24 hours postdose)
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