Drug intelligence / Profile preview

tolvaptan + torasemide

Development stage
Phase 4
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Tolvaptan + torasemide is a combination of two diuretic agents used primarily in the management of acute heart failure and conditions associated with fluid overload. Tolvaptan is a selective vasopressin V2-receptor antagonist that promotes aquaresis (excretion of free water) by inhibiting the action of antidiuretic hormone on renal collecting ducts, leading to increased urine output without significant loss of electrolytes[2][6][8]. Torasemide (also known as torsemide) is a loop diuretic that inhibits sodium-potassium-chloride cotransporters in the thick ascending limb of Henle’s loop, resulting in increased excretion of sodium, chloride, and water[9]. The combination may be considered for patients with resistance to conventional loop diuretics or when enhanced decongestion is required. Clinical studies have shown that adding tolvaptan to standard loop diuretic therapy can improve symptoms such as dyspnea and edema, increase serum sodium levels, and reduce body weight more effectively than monotherapy[2][4]. However, long-term benefits on mortality or rehospitalization remain unproven.

02

Targets

NKCC2 (Sodium-potassium-chloride cotransporter 2)AVPR2 (Arginine vasopressin V2 receptor)

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