Lixivaptan is a nonpeptide antagonist of vasopressin V2 receptors (Ki = 2.3 nM).1 It is 100-fold selective for V2 over V1a.2 Formulations containing lixivaptan decrease urinary excretion of aquaporin-2 in patients with chronic heart failure and increase serum sodium levels in patients with hyponatremia due to congestive heart failure.3,4
1.Matthews, J.M., Hoekstra, W.J., Dyatkin, A.B., et al.Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templatesBioorg. Med. Chem. Lett.14(11)2747-2752(2004) 2.Izumi, Y., Miura, K., and Iwao, H.Therapeutic potential of vasopressin-receptor antagonists in heart failureJ. Pharmacol. Sci.124(1)1-6(2014) 3.Bowman, B.T., and Rosner, M.H.Lixivaptan - an evidence-based review of its clinical potential in the treatment of hyponatremiaCore Evid.847-56(2013) 4.Martin, P.-Y., Abraham, W.T., Lieming, X., et al.Selective V2-receptor vasopressin antagonism decreases urinary aquaporin-2 excretion in patients with chronic heart failureJ. Am. Soc. Nephrol.10(10)2165-2170(1999)