A Study to Assess the Safety and Tolerability of E6742 in Japanese Healthy Adult Participants

NCT04683185 | Completed Phase 1

• 2 other identifiers: E6742-J081-005jRCT2031200316
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

The primary purpose of the study is to evaluate the safety, tolerability and pharmacokinetics (PK) of multiple ascending oral doses of E6742 in Japanese healthy adult participants.

Conditions

Healthy Volunteers

Keywords

E6742; Healthy participants; Pharmacokinetics

Outcome Measures

Primary Outcomes (17)

• Incidence of Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

  Safety assessments will consist of monitoring and recording all adverse events (AEs) and SAEs; laboratory evaluation for hematology, blood chemistry, and urine values; periodic measurement of vital signs and electrocardiograms (ECGs); and the performance of physical examinations.

  Baseline up to 28 days after the last dose of study drug (approximately Day 35)

• Cmax: Maximum Observed Plasma Concentration for E6742 and its Metabolite (ER-001132963) on Day 1

  Day 1: 0-12 hours

• tmax: Time at Which the Highest Drug Plasma Concentration Occurs for E6742 and its Metabolite (ER-001132963) on Day 1

  Day 1: 0-12 hours

• AUC(0-12h): Area Under the Plasma Concentration-time Curve From Zero Time to 12 Hours Postdose for E6742 and its Metabolite (ER-001132963) on Day 1

  Day 1: 0-12 hours

• AUC Metabolite to E6742 Ratio Following Molecular Weight Correction to E6742 Equivalents on Day 1

  Day 1: 0-12 hours

• Css,max: Maximum Observed Plasma Concentration at Steady State for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-168 hours

• tss,max: Time at Which the Highest Drug Plasma Concentration Occurs at Steady State for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-168 hours

• Css,av: Average Steady State Plasma Concentration for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-168 hours

• AUC(0-t): Area Under the Plasma Concentration-time Curve From Zero Time to Time of Last Quantifiable Concentration for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-168 hours

• AUC(0-12hr): Area Under the Plasma Concentration-time Curve Within a Dosing Interval at Steady State for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-12 hours

• t1/2: Terminal Elimination Phase Half-life for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-168 hours

• CLss/F: Apparent Total Clearance at Steady State for E6742 on Day 7

  Day 7: 0-168 hours

• Vss/F: Apparent Volume of Distribution at Steady State for E6742 on Day 7

  Day 7: 0-168 hours

• PTF: Peak-trough Fluctuation for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-168 hours

• Accumulation Ratio for Cmax and AUC for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-168 hours

• Metabolite to E6742 AUC Ratio Following Molecular Weight Correction to E6742 Equivalents on Day 7

  Day 7: 0-168 hours

• AUC(0-12hr)ss: Area Under the Plasma Concentration-time Curve Within a Dosing Interval at Steady State for E6742 and its Metabolite (ER-001132963) on Day 7

  Day 7: 0-12 hours

Secondary Outcomes (1)

• Change From Baseline in Corrected QT Interval (QTc) for E6742

  Day 1 and 7: 0-12 hours

Study Arms (3)

Cohort 2: E6742 200 mg or Placebo

EXPERIMENTAL

Participants will receive E6742 200 mg or E6742-matched placebo, tablets, orally, twice daily for 6 days under fasted conditions and once on Day 7 in the morning.

Drug: E6742; Drug: Placebo

Cohort 3: E6742 400 mg or Placebo

EXPERIMENTAL

Participants will receive E6742 400 mg or E6742-matched placebo, tablets, orally, twice daily for 6 days under fasted conditions and once on Day 7 in the morning.

Drug: E6742; Drug: Placebo

Cohort 1: E6742 100 milligram (mg) or Placebo

EXPERIMENTAL

Participants will receive E6742 100 mg or E6742-matched placebo, tablets, orally, twice daily for 6 days under fasted conditions and once on Day 7 in the morning.

Drug: E6742; Drug: Placebo

Interventions

E6742 DRUG

E6742 tablets.

Cohort 1: E6742 100 milligram (mg) or Placebo; Cohort 2: E6742 200 mg or Placebo; Cohort 3: E6742 400 mg or Placebo

Placebo DRUG

E6742-matched placebo tablets.

Cohort 1: E6742 100 milligram (mg) or Placebo; Cohort 2: E6742 200 mg or Placebo; Cohort 3: E6742 400 mg or Placebo

Eligibility Criteria

• Age: 20 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Non-smoking, male or female Japanese, greater than or equal to (\>=) age 20 years and less than or equal to (\<=) 55 years old at the time of informed consent
• Body mass index (BMI) \>=18.5 and less than (\<) 25.0 kilogram per meter square (kg/m\^2) at Screening

You may not qualify if:

• Females who are breastfeeding or pregnant at Screening or Baseline
• Females of childbearing potential who:
• Within 28 days before study entry, did not use a highly effective method of contraception, which includes any of the following:
• Total abstinence
• An intrauterine device (IUD) or intrauterine hormone-releasing system (IUS)
• A contraceptive implant
• An oral contraceptive
• Have a vasectomized partner with confirmed azoospermia
• Do not agree to use a highly effective method of contraception (as described above) throughout the entire study period and for 28 days after study drug discontinuation
• Males who have not had a successful vasectomy (confirmed azoospermia) or they and their female partners do not meet the criteria above (that is, not of childbearing potential or practicing highly effective contraception throughout the study period and for 5 times the half-life of the study drug plus 90 days after study drug discontinuation)
• Clinically significant illness that requires medical treatment within 8 weeks or a clinically significant infection within 4 weeks before dosing
• Any history of gastrointestinal surgery that may affect PK profiles of E6742 at Screening
• Any clinically abnormal symptom or organ impairment found by medical history, ophthalmic examination or chest X ray test at Screening, or founded by physical examinations, vital signs, ECG finding, or laboratory test results at Screening or Baseline
• A prolonged QTc corrected using Fridericia's method (QTcF) interval (QTcF greater than \[\>\] 450 millisecond \[ms\]) demonstrated on ECG at Screening or Baseline. A history of risk factors for torsade de pointes or the use of concomitant medications that prolonged the QT/QTc interval
• Persistent systolic blood pressure \>130 millimeter of mercury (mmHg) or diastolic blood pressure \>85 mmHg diastolic at Screening or Baseline

Sponsors & Collaborators

• Eisai Co., Ltd.: lead

Study Sites (1)

Eisai Trial Site #1

Bunkyō-Ku, Tokyo, Japan

Location

Related Links

• Study results will be disclosed on the jRCT registry record.

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: OTHER
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 21, 2020
• First Posted: December 24, 2020
• Study Start: December 28, 2020
• Primary Completion: June 21, 2021
• Study Completion: June 21, 2021
• Last Updated: July 20, 2021

Record last verified: 2021-05

Data Sharing

• IPD Sharing: Will share

Locations

JP (1)