A Relative Bioavailability and Food Effect Trial of OPC-131461 in Healthy Adult Male Subjects

JRCT ID: jRCT2071210093

Registered date:12/11/2021

Basic Information

• Recruitment status: Complete
• Health condition(s) or Problem(s) studied: Volume overload in heart failure
• Date of first enrollment: 22/01/2022
• Target sample size: 16
• Study type: Interventional

Intervention(s)

[Relative bioavailability (BA) arm]
Subjects will receive single oral administration of OPC-131461 at 20 mg (suspension or 5-mg tablet x 4) in a fasting state.

[Food effect arm]
Subjects will receive single oral administration of OPC-131461 at 20 mg (5-mg tablet x 4) in a fasting state or within 10 minutes after completion of a high-fat meal.

Outcome(s)

Primary Outcome

Primary Pharmacokinetic Endpoints:
1) Relative BA arm:
Differences in the mean natural-log-transformed values and two-sided 90% confidence intervals (CIs) for the plasma Cmax, AUC(infinity), and AUCt of OPC-131461 between the 2 formulations following administration of OPC-131461 suspension or OPC-131461 tablet in a fasting state
2) Food effect arm:
Differences in the mean natural-log-transformed values and two-sided 90% CIs for the plasma Cmax, AUC(infinity), and AUCt of OPC-131461 between administration of OPC-131461in a fasting state and administration of OPC-131461 tablet in a fed states

Secondary Pharmacokinetic Endpoints:
Plasma OPC-131461 concentration and plasma pharmacokinetic parameters of plasma OPC-131461

Safety:
Clinical laboratory tests (hematology, blood chemistry, and urinalysis), vital signs (blood pressure, pulse rate, and temperature), body weight, 12-lead electrocardiography (ECG), and adverse events (AEs)

Key inclusion & exclusion criteria

• Age minimum: >= 20age old
• Age maximum: < 40age old
• Gender: Male

Include criteria

1) Healthy Japanese men at least 20 years and less than 40 years of age at the time of informed consent.
2) Body mass index (BMI = body weight [kg]/[height {m}]2) of >=18.5 kg/m2 to <25.0 kg/m2 (at screening).
3) Individuals who provide written consent prior to the commencement of any trial-related procedure and who are able to comply with the trial procedures in the opinion of the investigator or subinvestigator.

Exclude criteria

1) Clinically significant abnormalities are found on screening examinations (eg, a marked deviation from the normal range) or in the subject's medical history that, in the opinion of the investigator, subinvestigator, or sponsor, may pose a risk to the subject or affect the absorption, distribution, metabolism, or elimination of the investigational medicinal product.
Such abnormalities include but are not limited to current or a history of cardiac, hepatic, renal, neurological, gastrointestinal, respiratory, hematological, and immunological conditions.
2) Systolic blood pressure of >140 mmHg or <100 mmHg or diastolic blood pressure of >90 mmHg or <50 mmHg at rest for at least 3 minutes in the supine position at screening.
3) Pulse rate outside the range of 50 to 90 bpm at rest for at least 3 minutes in the supine position at screening.
4) Clinically significant 12-lead ECG findings at screening, such as atrioventricular block, QRS interval of >120 msec, and QTcF interval of >=450 msec.
5) Any of the following hepatitis criteria is met:
-Prior or current hepatitis B, or current hepatitis C. A positive test for hepatitis B surface antigen or hepatitis C virus antibody at screening.
-Prior or current alcoholic hepatitis or non-alcoholic steatohepatitis.
6) Prior or current acquired immunodeficiency syndrome. A positive test for human immunodeficiency virus or syphilis or a positive polymerase chain reaction (PCR) test for SARS CoV 2 at screening.
7) History of serious mental disorders.

Related Information

• Primary Sponsor: Matsumaru Takehisa