Single and Multiple Oral Dose Trial of OPC-131461 in Healthy Adult Male Subjects

JRCT ID: jRCT2071200061

Registered date:07/12/2020

Basic Information

• Recruitment status: Complete
• Health condition(s) or Problem(s) studied: Volume overload in heart failure
• Date of first enrollment: 22/12/2020
• Target sample size: 83
• Study type: Interventional

Intervention(s)

[Part A]
Suspension containing of OPC-131461 or placebo suspension will be orally administered as a single dose in a fasting state.
[Part B]
Suspension containing OPC-131461or placebo suspension will be orally administered once daily for 14 days.

Outcome(s)

Primary Outcome

[Pharmacokinetic endpoint]
Plasma concentration and plasma PK parameters of OPC-131461
[Pharmacodynamic endpoints]
Urine volume, urine excretion rate, urine osmolality, urinary sodium excretion, urinary potassium excretion, urinary albumin excretion, urinary protein excretion, urinary creatinine excretion, urinary aquaporin 2 excretion, and urinary urea nitrogen excretion
Fluid intake
Fluid balance
Free water clearance
Serum osmolality, serum sodium concentration, serum potassium concentration, serum uric acid concentration, serum cystatin C concentration, and serum creatinine concentration
Plasma arginine vasopressin (AVP) concentration, plasma renin activity, and plasma aldosterone concentration
Creatinine clearance and estimated glomerular filtration rate
Platelet aggregation
[Safety endpoints]
Clinical laboratory tests (hematology, biochemistry, urinalysis, and coagulation test)
Vital signs (blood pressure, pulse rate, and body temperature) and dizziness
Body weight
12-lead electrocardiogram (ECG) (safety evaluation)
12-lead ECG (QT evaluation)
Adverse events

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, with a decrease in blood pressure upon standing (supine systolic blood pressure-standing systolic blood pressure) of >=20 mmHg 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: Kim Seongryul