Drug intelligence / Profile preview

tolvaptan

Development stage
Approved
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral
01

Overview

Tolvaptan is a selective, competitive vasopressin V2 receptor antagonist used primarily for two indications. It is approved for the treatment of clinically significant hypervolemic and euvolemic hyponatremia (low blood sodium) in adults with conditions such as heart failure, cirrhosis, or syndrome of inappropriate antidiuretic hormone secretion (SIADH). Tolvaptan increases free water excretion by blocking vasopressin-mediated water reabsorption in the renal collecting ducts, leading to increased urine output and correction of serum sodium levels. Additionally, under the brand name Jynarque, it is indicated to slow kidney function decline in adults at risk of rapidly progressing autosomal dominant polycystic kidney disease (ADPKD), where it also reduces cyst growth by inhibiting vasopressin-driven cell proliferation and fluid secretion into renal cysts[1][2][3][4][5][6][7].

Brand names
SamscaJynarque
Other names
tolvaptan
02

Targets

AVPR1A (Arginine vasopressin receptor 1A)AVPR2 (Arginine vasopressin V2 receptor)

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