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Completed

NCT Number: NCT07166796

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

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.

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Key information

Conditions

Health Subjects

Age range

18 year–40 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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

  • 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.

Treatment and study plan

singe dose 15mg

Drug

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

single dose 30mg

Drug

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

single dose 60mg

Drug

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

single dose 120mg

Drug

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

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 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.

Primary outcomes

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

    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

    peak concentration (Cmax)

  2. multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103

    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.

    peak concentration (Cmax)

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

    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

    time to peak (Tmax)

  4. Tolvaptan plasma pharmacokinetics, and its motablics DM-4103 and DM-4107

    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

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

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

    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

    elimination half-life (t1/2)

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

    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

    apparent clearance (CL/F)

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

    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

    apparent volume of distribution (Vd/F)

  8. multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103

    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

    time to peak (Tmax)

  9. multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103

    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

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

  10. multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103

    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

    elimination half-life (t1/2)

  11. multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103

    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

    apparent clearance (CL/F)

  12. multi dose Tolvaptan plasma pharmacokinetics and it's motablics DM-4107 and DM-4103

    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

    apparent volume of distribution (Vd/F)

Sponsors and collaborators

Lead sponsor

Otsuka Beijing Research Institute

Industry

Collaborators

  • Chinese Academy of Medical Sciences, Fuwai Hospital

Registry information

Official study title

Tolvaptan Oral Administration Phase I Clinical Trial

Important dates

Study start
2006
Primary completion
2007
Study completion
2007
First posted
Sep 10, 2025
Registry last updated
Sep 10, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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