Tolvaptan, a vasopressin V2 receptor antagonist, is the world’s first approved drug for treatment of autosomal dominant polycystic kidney disease (ADPKD)

Tolvaptan is a selective vasopressin V2 receptor antagonist that blocks binding of arginine vasopressin (AVP) to V2 receptors in collecting duct of kidney, thereby inducing water diuresis (aquaresis) without depletion of electrolytes. Tolvaptan was firstly approved as an aquaretic agent for treatment of hyponatremia including syndrome of inappropriate secretion of antidiuretic hormone and for treatment of fluid volume overload in heart failure and cirrhosis.