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Tolvaptan Oral Tablet
Tolvaptan is a selective vasopressin V2-receptor antagonist that blocks water reabsorption in the kidney's collecting duct, promoting aquaresis (water excretion) without significant electrolyte loss.
Tolvaptan is a selective vasopressin V2-receptor antagonist that blocks water reabsorption in the kidney's collecting duct, promoting aquaresis (water excretion) without significant electrolyte loss. Used for Hyponatremia associated with syndrome of inappropriate antidiuretic hormone secretion (SIADH), Hyponatremia in heart failure, Autosomal dominant polycystic kidney disease (ADPKD).
At a glance
| Generic name | Tolvaptan Oral Tablet |
|---|---|
| Sponsor | Otsuka Pharmaceutical Co., Ltd. |
| Drug class | Vasopressin V2-receptor antagonist (vaptans) |
| Target | Vasopressin V2 receptor |
| Modality | Small molecule |
| Therapeutic area | Nephrology / Endocrinology |
| Phase | Phase 3 |
Mechanism of action
By antagonizing the V2 vasopressin receptor on the collecting duct principal cells, tolvaptan prevents aquaporin-2 water channel insertion and reduces water reabsorption. This leads to increased free water excretion and correction of hyponatremia (low serum sodium) in conditions characterized by inappropriate antidiuretic hormone (ADH) secretion or excessive vasopressin activity. The drug is selective for V2 receptors, minimizing off-target effects on V1a receptors.
Approved indications
- Hyponatremia associated with syndrome of inappropriate antidiuretic hormone secretion (SIADH)
- Hyponatremia in heart failure
- Autosomal dominant polycystic kidney disease (ADPKD)
Common side effects
- Thirst
- Dry mouth
- Polyuria (increased urination)
- Hypernatremia (elevated serum sodium)
- Fatigue
- Hepatotoxicity
Key clinical trials
- A Study to See Iftolvaptan is Safe in Infants and Children Who at Enrollment Are 28 Days to Less Than 18 Years Old withAutosomal Recessive Polycystic Kidney Disease (ARPKD) (PHASE3)
- Bempedoic Acid Therapy for Polycystic Kidney Disease (PHASE2)
- A Study of HRS-9057 in Patients With Heart Failure and Volume Overload (PHASE1)
- Single Dose of 7.5mg Tolvaptan Phase I Clinical Trial Protocol (PHASE1)
- a Phase I PK Study in Healthy Male Subjects. 2 Groups of Healthy Male Subjects (PHASE1)
- A Phase 2 Efficacy and Safety Study of the Tolvaptan Tablets in Patients With Non-hypovolemic Non-acute Hyponatremia (PHASE2)
- Safety, Pharmacokinetics, Tolerability and Efficacy of Tolvaptan in Children and Adolescents With ADPKD (Autosomal Dominant Polycystic Kidney Disease) (PHASE3)
- To Study Effect of the Combination of Midodrine and Tolvaptan Versus Tolvaptan Alone in Patients With Severe Hyponatremia in Cirrhosis(TOLMINA Trial) (NA)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Tolvaptan Oral Tablet CI brief — competitive landscape report
- Tolvaptan Oral Tablet updates RSS · CI watch RSS
- Otsuka Pharmaceutical Co., Ltd. portfolio CI