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Lixivaptan is an orally-active, non-peptide, selective vasopressin 2 receptor antagonist and a member of the vaptan class of drugs. It acts by inhibiting the binding of arginine vasopressin to vasopressin receptor 2 (V2R) in kidney tubular epithelial cells, resulting in aquaresis (electrolyte-free water excretion). This mechanism underlies its use for treating euvolemic and hypervolemic hyponatremia. Additionally, lixivaptan is being developed for autosomal dominant polycystic kidney disease (ADPKD), where it may reduce cyst growth by lowering intracellular cAMP levels. The drug has been granted orphan drug designation by the FDA for ADPKD and has reached Phase III clinical development. Lixivaptan is metabolized primarily via CYP3A4 with a half-life of approximately 11 hours[3][5][7].
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