Study to Assess the Safety, Tolerability, Pharmacokinetic... | NCT03082235

NCT03082235

Protocol Section

Identification Module

Results Section

No data available

No data is available for this block.

Annotation Section

No data available

No data is available for this block.

Document Section

No data available

No data is available for this block.

Derived Section

Miscellaneous Info Module

Status Module

Arms/Interventions Module

Arm Groups

Label	Type	Description	Intervention Names
Cohort 1: 10 mg E6742	Experimental	Participants will receive 10 milligrams (mg) E6742 as a single oral dose in the fasted state.	Drug: E6742
Cohort 1: Matching placebo	Placebo Comparator	Participants will receive a single oral dose of placebo matching E6742 in the fasted state.	Drug: Placebo
Cohort 2: 25 mg E6742	Experimental	Participants will receive 25 mg E6742 as a single oral dose in the fasted state.	Drug: E6742
Cohort 2: Matching placebo	Placebo Comparator	Participants will receive a single oral dose of placebo matching E6742 in the fasted state.	Drug: Placebo
Cohort 3: 50 mg E6742	Experimental	Participants will receive 50 mg E6742 as a single oral dose in the fasted state.	Drug: E6742
Cohort 3: Matching placebo	Placebo Comparator

Name	Type	Description	Arm Group Labels	Other Names
E6742	Drug	gelatin capsules	Cohort 1: 10 mg E6742 Cohort 2: 25 mg E6742 Cohort 3: 50 mg E6742 Cohort 4: 100 mg E6742 Cohort 5: 200 mg E6742

Outcomes Module

Primary Outcomes

Measure	Description	Time Frame
Number of participants with any serious adverse event and number of participants with any non-serious adverse event	The number of participants with any serious adverse event and the number of participants with any non-serious adverse event will be reported.	from Screening up to Day 7
Mean maximum observed concentration (Cmax) of E6742 and the metabolite ER-1132963 in plasma	Cohorts 1, 2, 3, 5, and 6: Day 1 at predose and 0.5 (30 minutes), 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose; Day 2 (24 and 36 hours postdose); Day 3 (48 hours postdose); Day 4 (72 hours postdose); Day 5 (96 hours postdose); Day 6 (120 hours postdose); Day 7 (144 hours postdose). Cohort 4: In both periods (Treatment Periods 1 [7 days] and 2 [6 days]), Day 1 at predose and 0.5 (30 minutes), 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose; Day 2 (24 and 36 hours postdose); Day 3 (48 hours postdose); Day 4 (72 hours postdose); Day 5 (96 hours postdose); Day 6 (120 hours postdose); Day 7 (144 hours postdose).	Days 1 to 7
Time at which the highest drug concentration occurs (tmax) for E6742 and the metabolite ER-1132963 in plasma	Cohorts 1, 2, 3, 5, and 6: Day 1 at predose and 0.5 (30 minutes), 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose; Day 2 (24 and 36 hours postdose); Day 3 (48 hours postdose); Day 4 (72 hours postdose); Day 5 (96 hours postdose); Day 6 (120 hours postdose); Day 7 (144 hours postdose). Cohort 4: In both periods (Treatment Periods 1 [7 days] and 2 [6 days]), Day 1 at predose and 0.5 (30 minutes), 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose; Day 2 (24 and 36 hours postdose); Day 3 (48 hours postdose); Day 4 (72 hours postdose); Day 5 (96 hours postdose); Day 6 (120 hours postdose); Day 7 (144 hours postdose).	Days 1 to 7
Area under the concentration-time curve from zero time to 24 hours postdose (AUC[0-24h]) E6742 and the metabolite ER-1132963 in plasma	Cohorts 1, 2, 3, 5, and 6: Day 1 at predose and 0.5 (30 minutes), 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose; Day 2 (24 and 36 hours postdose); Day 3 (48 hours postdose); Day 4 (72 hours postdose); Day 5 (96 hours postdose); Day 6 (120 hours postdose); Day 7 (144 hours postdose). Cohort 4: In both periods (Treatment Periods 1 [7 days] and 2 [6 days]), Day 1 at predose and 0.5 (30 minutes), 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose; Day 2 (24 and 36 hours postdose); Day 3 (48 hours postdose); Day 4 (72 hours postdose); Day 5 (96 hours postdose); Day 6 (120 hours postdose); Day 7 (144 hours postdose).

Eligibility Module

Eligibility Criteria

Inclusion Criteria:

Nonsmoking, male or female, age ≥18 years and ≤45 years old at the time of informed consent
Body mass index (BMI) ≥18 and <32 kilograms per meters squared (kg/m2) at Screening

Exclusion Criteria:

Females who are breastfeeding or pregnant at Screening or Baseline (as documented by a positive beta-human chorionic gonadotropin [β-hCG] or human chorionic gonadotropin [hCG] test with a minimum sensitivity of 25 International Units per Liter [IU/L] or equivalent units of β-hCG [or hCG]). A separate baseline assessment is required if a negative screening pregnancy test was obtained more than 72 hours before the first dose of study drug.
Males who have not had a successful vasectomy (confirmed azoospermia) or they and their female partners do not meet the criteria above (ie, 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). No sperm donation is allowed during the study period and for 5 times the half-life of the study drug plus 90 days after study drug discontinuation.
Any history of gastrointestinal surgery that may affect pharmacokinetic (PK) profiles of E6742 (eg, hepatectomy, nephrectomy, digestive organ resection) at Screening
A prolonged QTcF interval (QTcF >450 ms) demonstrated on ECG at Screening or Baseline
Persistent systolic blood pressure >130 mmHg or diastolic blood pressure >85 mmHg diastolic at Screening or Baseline Heart rate less than 50 or more than 100 beats/min at Screening or Baseline
Known history of prolonged QT/QTc interval
Left bundle branch block
Known history of myocardial infarction or active ischemic heart disease
Known history of clinically significant arrhythmia or uncontrolled arrhythmia
Known history of clinically significant drug allergy at Screening
Known history of food allergies or presently experiencing significant seasonal or perennial allergy at Screening
Known to be human immunodeficiency virus (HIV) positive at Screening
Active viral hepatitis (A, B, or C) as demonstrated by positive serology at Screening
History of drug or alcohol dependency or abuse within the 2 years prior to Screening, or those who have a positive urine drug and alcohol test at Screening or Baseline
Intake of herbal preparations containing St. John's Wort within 4 weeks before dosing
Use of prescription drugs within 4 weeks before dosing
Intake of over-the-counter (OTC) medications within 2 weeks before dosing
Currently enrolled in another clinical study or used any investigational drug or device within 30 days (or 5 half-lives, whichever is longer) before informed consent
Receipt of blood products within 4 weeks, or donation of blood within 8 weeks, or donation of plasma within 1 week before dosing