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Yong Chul Kim and Hajeong Lee

Tolvaptan, an oral selective vasopressin V2 receptor antagonist, was approved by the US Food and Drug Administration (FDA) for the treatment of clinically significant hypervolemic or euvolemic hyponatremia and rapidly progressing autosomal dominant polycystic kidney disease (ADPKD). It antagonizes the effect of an arginine vasopressin (antidiuretic hormone), which has a key role in water and circulatory homeostasis in the collecting duct of the kidney. Tolvaptan leads to an increase in urine water excretion (aquaresis) that results in enhanced free-water clearance in states of relative vasopressin excess, increasing serum sodium concentrations. Additionally, tolvaptan induces a reduction in cyclic adenosine monophosphate (cAMP),