CompletedNCT07166796Updated Sep 10, 2025

a Phase I PK Study in Healthy Male Subjects. 2 Groups of Healthy Male Subjects

A Phase 1 interventional study of singe dose 15mg and single dose 30mg in Health Subjects, sponsored by Otsuka Beijing Research Institute. Completed. Open to male participants aged 18 Years to 40 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2025-09-10.

Sponsored by Otsuka Beijing Research Institute · Phase 1, Interventional, and Treatment

Phase: Phase 1
Study type: Interventional
Enrollment: 64
Allocation: Non-randomized
Ages: 18 Years to 40 Years
Sex: Male

Study summary

Tolvaptan oral administraction phase I PK clinical trial. Two groups of healthy male subjects. One group receives single dose of Tolvaptan. The other group receives multi dose of Tolvaptan.

Conditions studied

Health Subjects

Who can participate

Ages eligible: 18 Years to 40 Years
Sexes eligible: Male
Accepts healthy volunteers: Yes

Inclusion criteria

Healthy male volunteers.
Aged 18 to 40 years old.
Weight no less than 50kg and within the range of standard weight (body mass index between 19 and 24).
Auxiliary examinations: blood routine and coagulation, urine routine, blood biochemistry (total protein, albumin, blood glucose, total bilirubin, AST (GOT), ALT (GPT), ALP, γ-GTP, LDH, CK (CPK), total cholesterol, triglycerides, urea nitrogen, creatinine, uric acid, Na, K, Cl, Mg, Ca, P), hepatitis B surface antigen, hepatitis C antibody, HIV antibody, syphilis antibody, 12-lead electrocardiogram, 24-hour ambulatory electrocardiogram (Holter) examination, all items are normal.
Signed the informed consent form.

Exclusion criteria

Exclusion Criteria:

The patient has a history of heart, liver, kidney, digestive tract, metabolic, respiratory, blood, mental, nervous system and other disorders, and the doctor's judgment is not suitable.
Hepatitis B virus, syphilis, hepatitis C virus, HIV infection.
Patients with a history of clinically significant arrhythmias of various types, including rapid and slow types, such as atrioventricular block, sinus arrest, and supraventricular tachycardia, were assessed by the investigators.
He has a history of postural hypotension (blood pressure drop ≥20/10mmHg when he changes from lying position to standing position, accompanied by dizziness and other symptoms), standing dizziness, collapse, fainting, and vertigo.
Quiet for more than 3 minutes, sitting pulse below 55 beats/min or more than 90 beats/min.
Quiet for more than 3 minutes, sitting systolic blood pressure is lower than 100mmHg or higher than 140mmHg; Diastolic depression of 60mmHg or higher than 90mmHg.
Various voiding disorders (frequent urination, or difficulty urinating, etc.).
Have a family history of genetic diseases (including a history of genetically predisposed arrhythmias in relatives).
A history, allergy or propensity to be allergic to drugs or any other substance.
Smokers, alcoholics, or other drug addicts.
Physical examination had clinically significant positive findings.
People who have donated blood or been sampled as a subject within the last 3 months.
People who have taken prophylactic or therapeutic drugs in the last 2 weeks.
Otherwise, the clinical trial physician or the clinical trial physician determines that the safety of the trial is affected.

Study design

Phase: Phase 1
Primary purpose: Treatment
Allocation: Non-randomized
Intervention model: Single group
Masking: None (open label)
Enrollment: 64 participants (actual)

Study arms

Experimental
single dose
Drug: singe dose 15mg · Drug: single dose 30mg · Drug: single dose 60mg · Drug: single dose 120mg
Experimental
multi dose
Drug: multi dose 30mg · Drug: multi dose 60mg

Interventions

Drugsinge dose 15mg
succesfule screened subject, take single dose of 15mg Tolvaptan tablet with no feeding.
Drugsingle dose 30mg
succesfule screened subject, take single dose of 30mg Tolvaptan tablet with no feeding.
Drugsingle dose 60mg
succesfule screened subject, take single dose of 60mg Tolvaptan tablet with no feeding.
Drugsingle dose 120mg
succesfule screened subject, take single dose of 120mg Tolvaptan tablet with no feeding.
Drugmulti dose 30mg
radomize 24 healthy adult male to 2 groups, 12 subjects each. One group take 30mg Tolvaptan. First day, with no feeding, take single 30mg dose, then start from day 3rd, take medication for 7 days. 8 days treatment in total.
Drugmulti dose 60mg
radomize 24 healthy adult male to 2 groups, 12 subjects each. One group take 60mg Tolvaptan. First day, with no feeding, take single 60mg dose, then start from day 3rd, take medication for 7 days. 8 days treatment in total.

What researchers measure

Primary outcomes

single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
peak concentration (Cmax)
Time frame: Day 1 pre-dose and post-dose 0.5hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
peak concentration (Cmax)
Time frame: Day 1 & Day 9 at pre-dose, post-dose 0.5hr, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 (2nd and 10th day) and 48 (day 3rd and 11th). For other dosing day ( day 4 to 8) to collect at pre-dose( 24hr after last dose) point.
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
time to peak (Tmax)
Time frame: Day 1 pre-dose and post-dose 0.5 hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours
Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
area under the drug-time curve (AUC0-t and AUC0-∞)
Time frame: Day 1 pre-dose and post-dose 0.5 hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
elimination half-life (t1/2)
Time frame: Day 1 pre-dose and post-dose 0.5 hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
apparent clearance (CL/F)
Time frame: Day 1 pre-dose and post-dose 0.5 hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours
single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107
apparent volume of distribution (Vd/F)
Time frame: Day 1 pre-dose and post-dose 0.5 hour, 1 ,2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
time to peak (Tmax)
Time frame: Day 1 & Day 9 at pre-dose, post-dose 0.5hr, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 (2nd and 10th day) and 48 (day 3rd and 11th). For other dosing day ( day 4 to 8) to collect at pre-dose( 24hr after last dose) point
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
area under the drug-time curve (AUC0-t and AUC0-∞)
Time frame: Day 1 & Day 9 at pre-dose, post-dose 0.5hr, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 (2nd and 10th day) and 48 (day 3rd and 11th). For other dosing day ( day 4 to 8) to collect at pre-dose( 24hr after last dose) point
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
elimination half-life (t1/2)
Time frame: Day 1 & Day 9 at pre-dose, post-dose 0.5hr, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 (2nd and 10th day) and 48 (day 3rd and 11th). For other dosing day ( day 4 to 8) to collect at pre-dose( 24hr after last dose) point
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
apparent clearance (CL/F)
Time frame: Day 1 & Day 9 at pre-dose, post-dose 0.5hr, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 (2nd and 10th day) and 48 (day 3rd and 11th). For other dosing day ( day 4 to 8) to collect at pre-dose( 24hr after last dose) point
multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103
apparent volume of distribution (Vd/F)
Time frame: Day 1 & Day 9 at pre-dose, post-dose 0.5hr, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 (2nd and 10th day) and 48 (day 3rd and 11th). For other dosing day ( day 4 to 8) to collect at pre-dose( 24hr after last dose) point

Study locations

No study locations are listed for this record.

References and documents

Publications

Liu H, Liu T, Liu M, Zheng X, Zhong W, Zhao Q, Jiang J, Hu P, Li Y. Clinical trial on the pharmacokinetics, pharmacodynamics and safety of tolvaptan in healthy Chinese males: an open-label, single and multiple dosage, parallel group study. Front Pharmacol. 2025 Nov 21;16:1713702. doi: 10.3389/fphar.2025.1713702. eCollection 2025. PubMed 41357896 ↗

Individual participant data

Plan to share: Yes

Registry details

Key details

Study ID: NCT07166796
Lead sponsor: Otsuka Beijing Research Institute
Collaborators: Chinese Academy of Medical Sciences, Fuwai Hospital
Responsible party: Sponsor
First posted: Sep 10, 2025
Start date: Oct 1, 2006
Primary completion: Jan 31, 2007
Completion: Jan 31, 2007
Last update: Sep 10, 2025

Oversight

Data monitoring committee: Yes
FDA-regulated drug: No
FDA-regulated device: No

View the source record on ClinicalTrials.gov ↗

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