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tolvaptan sodium phosphate
- Development stage
- Approved
- Lead developer
- Otsuka Holdings
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
OPC-61815 is an intravenous, water-soluble phosphate ester prodrug of tolvaptan, developed by Otsuka. After administration, it is rapidly hydrolyzed in the body by alkaline phosphatase into active tolvaptan. Tolvaptan acts as a selective antagonist of the vasopressin V2 receptor in the renal collecting duct, inhibiting water reabsorption and promoting aquaresis (excretion of free water without electrolyte loss). OPC-61815 was designed for patients with cardiac edema or volume overload who cannot take oral medications. Clinical trials have shown that intravenous OPC-61815 is non-inferior in efficacy and safety compared to oral tolvaptan for treating cardiac edema associated with heart failure[1][2][3][4][5][6][7][8].
- Brand names
- Samtasu
- Other names
- tolvaptan sodium phosphate
02
Targets
AVPR2 (Arginine vasopressin V2 receptor)
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