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

NCT07166796 | Completed Phase 1 DMC

• 1 other identifier: 156-06-801-01
• Study Type: interventional
• Target: 64
• Locations: 0 countries
• Sites: N/A

Brief 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

Health Subjects

Outcome Measures

Primary Outcomes (12)

• single dose Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107

  peak concentration (Cmax)

  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)

  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)

  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-∞)

  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)

  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)

  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)

  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)

  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-∞)

  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)

  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)

  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)

  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 Arms (2)

single dose

EXPERIMENTAL

Drug: singe dose 15mg; Drug: single dose 30mg; Drug: single dose 60mg; Drug: single dose 120mg

multi dose

EXPERIMENTAL

Drug: multi dose 30mg; Drug: multi dose 60mg

Interventions

singe dose 15mg DRUG

succesfule screened subject, take single dose of 15mg Tolvaptan tablet with no feeding.

single dose

single dose 30mg DRUG

succesfule screened subject, take single dose of 30mg Tolvaptan tablet with no feeding.

single dose

single dose 60mg DRUG

succesfule screened subject, take single dose of 60mg Tolvaptan tablet with no feeding.

single dose

single dose 120mg DRUG

succesfule screened subject, take single dose of 120mg Tolvaptan tablet with no feeding.

single dose

multi dose 30mg DRUG

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.

multi dose

multi dose 60mg DRUG

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.

multi dose

Eligibility Criteria

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

You may qualify if:

• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Otsuka Beijing Research Institute: lead
• Chinese Academy of Medical Sciences, Fuwai Hospital: collaborator

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

Study Design

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

Study Record Dates

• First Submitted: August 25, 2025
• First Posted: September 10, 2025
• Study Start: October 1, 2006
• Primary Completion: January 31, 2007
• Study Completion: January 31, 2007
• Last Updated: September 10, 2025

Record last verified: 2025-08

Data Sharing

• IPD Sharing: Will share