Phase I Study Multi Dose of 7.5mg Tolvaptan in Health Male

NCT07166887 | Completed Phase 1 DMC

• 1 other identifier: 156-11-808-01
• Study Type: interventional
• Target: 12
• Locations: 0 countries
• Sites: N/A

Brief Summary

pharmacokinetics, pharmacological effects and safety of multi dose of 7.5mg Tolvaptan tablet in healthy male subjects

Conditions

Healthy Subjects

Outcome Measures

Primary Outcomes (6)

• Tolvaptan Pharmacokinetic

  peak concentration (Cmax)

  - On Day 1: 0.5 hour before the first dose - the Day 9th pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, day 24 (only on Day 2 and Day 10th morning), 36 ( on Day 2 and Day 10th everning) and 48 hours - Day 4th to 8th day pre-dose

• Tolvaptan Pharmacokinetic

  time to peak (Tmax)

  On Day 1: 0.5 hour before the first dose - the Day 9th pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, day 24 (only on Day 2 and Day 10th morning), 36 ( on Day 2 and Day 10th everning) and 48 hours - Day 4th to 8th day pre-dose

• Tolvaptan Pharmacokinetic

  area under the drug-time curve (AUC0-t and AUC0-∞)

  On Day 1: 0.5 hour before the first dose - the Day 9th pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, day 24 (only on Day 2 and Day 10th morning), 36 ( on Day 2 and Day 10th everning) and 48 hours - Day 4th to 8th day pre-dose

• Tolvaptan Pharmacokinetic

  elimination half-life (t1/2)

  On Day 1: 0.5 hour before the first dose - the Day 9th pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, day 24 (only on Day 2 and Day 10th morning), 36 ( on Day 2 and Day 10th everning) and 48 hours - Day 4th to 8th day pre-dose

• Tolvaptan Pharmacokinetic

  apparent clearance (CL/F)

  On Day 1: 0.5 hour before the first dose - the Day 9th pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, day 24 (only on Day 2 and Day 10th morning), 36 ( on Day 2 and Day 10th everning) and 48 hours - Day 4th to 8th day pre-dose

• Tolvaptan Pharmacokinetic

  apparent volume of distribution (Vd/F)

  On Day 1: 0.5 hour before the first dose - the Day 9th pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, day 24 (only on Day 2 and Day 10th morning), 36 ( on Day 2 and Day 10th everning) and 48 hours - Day 4th to 8th day pre-dose

Study Arms (1)

7.5mg Tolvaptan multi dosing group

EXPERIMENTAL

Drug: Tolvaptan

Interventions

Tolvaptan DRUG

One dose on the first day and one dose on days 3-9, for a total of eight doses.

7.5mg Tolvaptan multi dosing group

Eligibility Criteria

• Age: 18 Years - 40 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male, sign informed consent;
• When signing the informed consent, the age range is 18-40 years old (including the upper and lower limits);
• The body weight is not less than 50kg, and the body mass index is in the range of 19 \~ 24 (including the upper and lower limits);
• According to the results of medical history, serological examination (HIV antibody, HBsAg, HCV antibody and syphilis antibody), physical examination, vital signs (temperature, blood pressure, pulse), 12-lead electrocardiogram, laboratory examination (blood routine, blood biochemistry, coagulation function and urine routine), etc., the subjects are certified as healthy.

You may not qualify if:

• Patients with a history of heart, liver, kidney, digestive tract, metabolic, respiratory, blood, mental, nervous system and other disorders, and doctors judge that they are not suitable.
• Patients with a history of various types of arrhythmias judged by the researchers to have clinical significance, including a history of familial genetic disease (a history of arrhythmias with a genetic tendency in relatives), and a history of rapid and slow arrhythmias, such as atrioventricular transmission Conduction block, sinus arrest, supraventricular tachycardia and so on.
• Have a history, allergy or tendency to drugs and any other substances.
• Known intolerance to components of the test drug, including lactose. For example, people with rare genetic galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.
• Various voiding disorders (frequent urination, or difficulty urinating, etc.).
• People who smoke, drink or depend on other drugs.
• Blood donors had an equivalent amount of blood loss (\>350 ml) during the 12 weeks prior to enrollment.
• Participated in any drug trials within 12 weeks prior to enrollment.
• People who have taken preventive or therapeutic drugs in the last 2 weeks.
• Consumed grapefruit or foods containing grapefruit in the week prior to administration.
• In the investigator's judgment, the subject's diet deviates significantly from the normal intake of protein, carbohydrates, and fats (for example, vegetarian or vegan).
• Have a history of postural hypotension (refers to a blood pressure drop of ≥20/10mmHg when the blood pressure changes from the lying position to the standing position, accompanied by dizziness and other symptoms), standing vertigo, collapse, syncopation, and vertigo.
• Quiet for more than 3 minutes, sitting resting 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; Or diastolic depression of 60mmHg or more than 90mmHg.
• Clinically significant 12-lead electrocardiogram abnormalities.

Sponsors & Collaborators

• Otsuka Beijing Research Institute: lead

Related Publications (1)

• 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.

  PMID: 41357896 DERIVED

MeSH Terms

Interventions

Tolvaptan

Intervention Hierarchy (Ancestors)

Benzazepines; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 22, 2025
• First Posted: September 10, 2025
• Study Start: June 7, 2011
• Primary Completion: July 27, 2011
• Study Completion: July 27, 2011
• Last Updated: September 10, 2025

Record last verified: 2025-08

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL, SAP, ICF, CSR, ANALYTIC CODE