Drug intelligence / Profile preview

tolvaptan + diuretics

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

Overview

Tolvaptan + diuretics refers to the combination therapy of tolvaptan, a selective vasopressin V2 receptor antagonist, with conventional diuretic agents (such as loop diuretics). Tolvaptan acts on the distal nephron by blocking the V2 receptor, thereby inhibiting water reabsorption and promoting aquaresis—excretion of free water without significant loss of electrolytes. This mechanism is distinct from traditional diuretics, which promote both fluid and electrolyte excretion. The combination is primarily used in patients with acute heart failure (AHF), especially those who are resistant to standard loop diuretic therapy or have hyponatremia. Clinical studies indicate that adding tolvaptan can improve symptoms of congestion, increase serum sodium levels in hyponatremic patients, reduce edema and body weight short-term, and may lower the risk of worsening renal function; however, it does not significantly impact long-term mortality or rehospitalization rates[1][5][6][7].

02

Targets

AVPR1B (Vasopressin V1b Receptor)AVPR2 (Arginine vasopressin V2 receptor)SLC12A3 (Thiazide-sensitive sodium-chloride cotransporter)NKCC2 (Sodium-potassium-chloride cotransporter 2)AVPR1A (Arginine vasopressin receptor 1A)ENaC

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