Trial Outcomes & Findings for A Phase 1,Open -Label Study to Assess the Absorption, Metabolism and Excretion of 14C-OPS-2071 Following a Single Oral Dose to Healthy Male Japanese Subjects (NCT NCT02440633)

Results Overview

A single dose of 14C-OPS-2071was administered as an oral suspension under fasting conditions on the morning of Day 1. We evaluated the cumulative excretion of total radioactivity (%) in feces and urine, up to 168 hours postdose.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

8 participants

Primary outcome timeframe

up to144-168h postdose.

Results posted on

2016-10-21

Participant Flow

Participant milestones

Participant milestones
Measure	14C-OPS-2071 Suspension containing 50 mg of 14C-OPS-2071 14C-OPS-2071: Subjects will swallow Single 25 mL of suspension containing 50 mg of 14C-OPS-2071 directly.
Overall Study STARTED	8
Overall Study COMPLETED	8
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

A Phase 1,Open -Label Study to Assess the Absorption, Metabolism and Excretion of 14C-OPS-2071 Following a Single Oral Dose to Healthy Male Japanese Subjects

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	14C-OPS-2071 n=8 Participants Suspension containing 50 mg of 14C-OPS-2071 14C-OPS-2071: Subjects will swallow Single 25 mL of suspension containing 50 mg of 14C-OPS-2071 directly.
Age, Categorical <=18 years	0 Participants n=5 Participants
Age, Categorical Between 18 and 65 years	8 Participants n=5 Participants
Age, Categorical >=65 years	0 Participants n=5 Participants
Age, Continuous	42.0 years STANDARD_DEVIATION 4.8 • n=5 Participants
Sex: Female, Male Female	0 Participants n=5 Participants
Sex: Female, Male Male	8 Participants n=5 Participants
Region of Enrollment United Kingdom	8 participants n=5 Participants

PRIMARY outcome

Timeframe: up to144-168h postdose.

A single dose of 14C-OPS-2071was administered as an oral suspension under fasting conditions on the morning of Day 1. We evaluated the cumulative excretion of total radioactivity (%) in feces and urine, up to 168 hours postdose.

Outcome measures

Outcome measures
Measure	Feces n=8 Participants	Urine n=8 Participants	Total n=8 Participants
The Amounts of Radioactivity Excreted in Urine and Faeces	78.0 percentage of administered dose Standard Deviation 13.1	6.08 percentage of administered dose Standard Deviation 1.71	84.1 percentage of administered dose Standard Deviation 12.7

PRIMARY outcome

Timeframe: predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 h postdose.

A single dose of 14C-OPS-2071was administered as an oral suspension under fasting conditions on the morning of Day 1. We measured total radioactivity in plasma and whole blood each. We evaluated AUC 0-168h of total radioactivity in plasma and whole blood each. The AUCs in plasma and whole blood are of total radioactivity including the parent and metabolites.

Outcome measures

Outcome measures
Measure	Feces n=8 Participants	Urine n=8 Participants	Total
Area Under Curve (AUC) of Total Radioactivity in Plasma and Whole Blood	649.0 μg eq.·h/L Standard Deviation 486.0	411.0 μg eq.·h/L Standard Deviation 73.9	—

PRIMARY outcome

Timeframe: predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 h postdose.

A single dose of 14C-OPS-2071was administered as an oral suspension under fasting conditions on the morning of Day 1. We measured OPS-2071 concentration in plasma and evaluated AUC 0-168h of OPS-2071 in plasma.

Outcome measures

Outcome measures
Measure	Feces n=8 Participants	Urine	Total
AUC of OPS-2071 in Plasma	392.0 μg·h/L Standard Deviation 95.8	—	—

Adverse Events

14C-OPS-2071

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	14C-OPS-2071 n=8 participants at risk Suspension containing 50 mg of 14C-OPS-2071 14C-OPS-2071: Subjects will swallow Single 25 mL of suspension containing 50 mg of 14C-OPS-2071 directly.
Gastrointestinal disorders Diarrhoea	25.0% 2/8 • Number of events 2 • From informed Consent up to 22 days post dose
Gastrointestinal disorders Dyspepsia	12.5% 1/8 • Number of events 1 • From informed Consent up to 22 days post dose
Infections and infestations Gastroenteritis	12.5% 1/8 • Number of events 1 • From informed Consent up to 22 days post dose
Infections and infestations Nasopharyngitis	12.5% 1/8 • Number of events 1 • From informed Consent up to 22 days post dose
Investigations Alanine aminotransferase increase	12.5% 1/8 • Number of events 1 • From informed Consent up to 22 days post dose
Nervous system disorders Headache	12.5% 1/8 • Number of events 1 • From informed Consent up to 22 days post dose
Injury, poisoning and procedural complications Arthropod bite	12.5% 1/8 • Number of events 1 • From informed Consent up to 22 days post dose

Additional Information

Study Director, Yoshitaka Kotobuki, Mr

Otsuka Pharmaceutical Co., Ltd.

Phone: +81-3-6361-7366

Results disclosure agreements

Principal investigator is a sponsor employee
Publication restrictions are in place