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| ID | Type | Description | Link |
|---|---|---|---|
| jRCT2031200316 | Registry Identifier | jRCT |
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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 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. |
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| 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. |
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| 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. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| E6742 | Drug | E6742 tablets. |
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| Measure | Description | Time Frame |
|---|---|---|
| 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 |
| Measure | Description | Time Frame |
|---|---|---|
| Change From Baseline in Corrected QT Interval (QTc) for E6742 | High precision method QT analysis (HPQT) will be performed using data extracted from the 12-hour holter recording obtained from the morning of day 1 (predose) through 12 hours after dosing, the morning of day 7 (predose) through 12 hours after dosing. | Day 1 and 7: 0-12 hours |
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Inclusion Criteria:
Exclusion Criteria:
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:
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
Heart rate less than 45 or more than 100 beats per min at Screening or Baseline
Any lifetime history of suicidal ideation or any lifetime history of suicidal behavior as indicated by the Suicidal Ideation section of the Columbia Suicide Severity Rating Scale (C-SSRS)
Any lifetime history of psychiatric disease
Any current psychiatric symptoms as indicated by a standard screening tool (Patient Health Questionnaire 9 [PHQ 9])
Any suicidal ideation with intent with or without a plan within Screening or 6 months before Screening (that is, answering "Yes" to questions 4 or 5 on the C-SSRS)
History of autoimmune disease or immunodeficiency
Known to be positive for tuberculosis test (T-spot. TB Test) at Screening
Received immunoglobulin or blood preparation within 6 months before the study treatment
Received inoculation within 4 weeks before the study treatment (8 weeks before in case of live or attenuated vaccine)
Family living together or cohabitant of a patient with an influenza virus infection
In contact with Coronavirus disease (COVID 19) patient within 4 weeks before study drug administration
Known to be other than negative for Severe acute respiratory syndrome coronavirus 2 (SARS Cov 2) antibody test at Screening
Known to be other than negative for SARS Cov 2 polymerase chain reaction (PCR) test at Screening or Baseline
History of retinopathy, maculopathy or macular degeneration
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Eisai Trial Site #1 | Bunkyō-Ku | Tokyo | Japan |
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| Label | URL |
|---|---|
| Study results will be disclosed on the jRCT registry record. | View source |
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Eisai's data sharing commitment and further information on how to request data can be found on our website http://eisaiclinicaltrials.com/.
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| Placebo | Drug | E6742-matched placebo tablets. |
|
| 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 |