Single Dose of 7.5mg Tolvaptan Phase I Clinical Trial Protocol

NCT07166783 | Completed Phase 1 DMC

• 1 other identifier: 156-11-807-01
• Study Type: interventional
• Target: 10
• Locations: 0 countries
• Sites: N/A

Brief Summary

Pharmacokinetics, pharmacological effects and safety of single dose of 7.5mg Tolvaptan tablet in healthy male subjects

Conditions

Health Subjects

Outcome Measures

Primary Outcomes (6)

• Tolvaptan PK parameter

  peak concentration (Cmax)

  On Day 1 pre-dose and post-dose 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours.

• Tolvaptan PK parameter

  time to peak (Tmax)

  On Day 1 pre-dose and post-dose 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours

• Tolvaptan PK parameter

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

  On Day 1 pre-dose and post-dose 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours

• Tolvaptan PK parameter

  elimination half-life (t1/2)

  On Day 1 pre-dose and post-dose 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours

• Tolvaptan PK parameter

  apparent clearance (CL/F)

  On Day 1 pre-dose and post-dose 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours

• Tolvaptan PK parameter

  apparent volume of distribution (Vd/F)

  On Day 1 pre-dose and post-dose 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120 and 144 hours

Study Arms (1)

7.5mg Tolvaptan single dose

EXPERIMENTAL

Drug: Tolvaptan

Interventions

Tolvaptan DRUG

single dose oral administration of 7.5mg Tolvaptan

7.5mg Tolvaptan single dose

Eligibility Criteria

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

You may qualify if:

• Male, signing the informed consent form;
• At the time of signing the informed consent form, aged between 18 and 40 years old (inclusive);
• Body weight no less than 50kg, body mass index within the range of 19 to 24 (inclusive);
• Proven to be a healthy subject based on the results of medical history, serological tests (HIV antibody, HBsAg, HCV antibody and syphilis antibody), physical examination, vital signs (temperature, blood pressure, pulse), 12-lead electrocardiogram, and laboratory tests (blood routine, blood biochemistry, coagulation function and urine routine).

You may not qualify if:

• Those with a history of heart, liver, kidney, digestive tract, metabolic disorders, respiratory, blood, mental or nervous system diseases, or those judged by the physician as unsuitable.
• Those with a history of clinically significant arrhythmias of any type, including a family history of genetic diseases (relatives with a history of arrhythmias with genetic predisposition), such as rapid and slow types, including atrioventricular block, sinus arrest, supraventricular tachycardia, etc.
• Those with a history of drug or other substance allergies, allergic constitution or tendency.
• Those known to be intolerant to the components of the test drug (including lactose), such as those with rare hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
• Those with various urinary disorders (such as frequent urination or difficulty in urination, etc.).
• Those who smoke, are alcoholics or have other drug dependencies.
• Those who have donated blood or lost an equivalent amount of blood (\>350 ml) within 12 weeks before enrollment.
• Those who have participated in any drug trials within 12 weeks before enrollment.
• Those who have taken any preventive or therapeutic drugs within the past 2 weeks.
• Those who have consumed grapefruit or grapefruit-containing foods within one week before taking the drug.
• Those whose diet is significantly deviated from normal protein, carbohydrate and fat intake as judged by the investigator (such as vegetarians or absolute vegetarians).
• Those with a history of orthostatic hypotension (a drop in blood pressure of ≥20/10 mmHg when changing from a lying to a standing position, accompanied by symptoms such as dizziness), orthostatic dizziness, syncope, fainting or vertigo.
• Those whose resting pulse rate is less than 55 beats per minute or more than 90 beats per minute after sitting quietly for more than 3 minutes.
• Those whose sitting systolic blood pressure is less than 100 mmHg or more than 140 mmHg, or whose diastolic blood pressure is less than 60 mmHg or more than 90 mmHg after sitting quietly for more than 3 minutes.
• Those with clinically significant 12-lead electrocardiogram changes.

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 16, 2011
• Primary Completion: July 4, 2011
• Study Completion: July 4, 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