OPC-61815 in Healthy Chinese Male Subjects

Study Overview
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Brief Summary
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To evaluate the pharmacokinetic (PK) characteristics and pharmacological effect of OPC-61815 in healthy Chinese Male subjects

Detailed Description
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To evaluate the pharmacokinetic (PK) characteristics of single and multiple intravenous administration of OPC-61815 in healthy Chinese subjects. To evaluate the safety of single and multiple intravenous administration of OPC-61815 in healthy Chinese subjects. To evaluate the pharmacological effect of single and multiple intravenous administration of OPC-61815 in healthy Chinese subjects.

Official Title
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A Phase I, Open-label, Single- and Multi-Dose Study to Evaluate the Safety, Pharmacokinetics, and Pharmacological Effect of OPC-61815 in Healthy Chinese Male Subjects

Conditions
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Healthy Adult Male

Intervention / Treatment
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* Drug: OPC-61815 injection


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Healthy male subjects aged 18-45 years (including the cutoff values, subject to the time of signing the Informed Consent Form (ICF)); Body mass index (BMI) of 19-26 kg/m2 (including the cutoff values), with a body weight of not less than 50 kg for male subjects; Exclusion Criteria: Those whose the sitting pulse is lower than 50 beats/min or higher than 100 beats/min after resting for over 3 minutes. Those whose sitting SBP is lower than 90 mmHg or higher than 140 mmHg, or DBP is lower than 50 mmHg or higher than 90 mmHg after resting for over 3 minutes. Various micturition disorders (pollakiuria or dysuria, etc.).

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 45 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Treatment
Intervention Model: Sequential Assignment
Interventional Model Description: 8 mg and 16 mg.
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: OPC-61815<br>Intravenous administration of OPC-61815 at 8 mg or 16 mg. 8mg group will be intravenously administered only on D1, once a day. 16mg group will be intravenously administered on D1，D3-D9, once a day | Drug: OPC-61815 injection<br>* Intravenous administration of OPC-61815 at 8 mg or 16 mg. 8mg group will be intravenously administered only on D1, once a day. 16mg group will be intravenously administered on D1，D3-D9, once a day.<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| To evaluate the pharmacokinetic (PK) characteristics：Tmax | Pharmacokinetic parameters of OPC-61815 free form and metabolites tolvaptan, DM4103 and DM4107 in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：Cmax | Pharmacokinetic parameters of OPC-61815 free form and metabolites tolvaptan, DM4103 and DM4107 in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：AUC0-t, AUC0-inf, AUC0-24h | Pharmacokinetic parameters of OPC-61815 free form and metabolites tolvaptan, DM4103 and DM4107 in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：t1/2 | Pharmacokinetic parameters of OPC-61815 free form and metabolites tolvaptan, DM4103 and DM4107 in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：λz | Pharmacokinetic parameters of OPC-61815 free form and metabolites tolvaptan, DM4103 and DM4107 in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：Rac(Cmax) | Pharmacokinetic parameters of OPC-61815 free form and metabolites tolvaptan, DM4103 and DM4107 in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：Rac(AUC0-24h) | Pharmacokinetic parameters of OPC-61815 free form and metabolites tolvaptan, DM4103 and DM4107 in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：CL (OPC-61815 free form only) | Pharmacokinetic parameters of OPC-61815 free form in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 
| To evaluate the pharmacokinetic (PK) characteristics：Vz (OPC-61815 free form only) | Pharmacokinetic parameters of OPC-61815 free form in plasma after intravenous administration of OPC-61815 | before dosing and after the start of dosing on Day1 and Day9(16mg group only); 16mg group also need collect on Day7 and Day8 | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| To evaluate the safety of single and multiple intravenous administration：laboratory tests | laboratory tests assessment variables include blood routine, blood biochemistry and urine routine. | from screening period to follow up period,assessed up to 16 Days. | 
| To evaluate the safety of single and multiple intravenous administration：adverse events | adverse events start date, end date , seriousness, severity, relationship to trial treatment (IMP causality), action taken with trial treatment, and outcome will be collect | from screening period to follow up period,assessed up to 16 Days. |