Vasopressin receptor antagonists, heart failure, and polycystic kidney disease

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53 Scopus citations


The synthesis of nonpeptide orally bioavailable vasopressin antagonists devoid of agonistic activity (vaptans) has made possible the selective blockade of vasopressin receptor subtypes for therapeutic purposes. Vaptans acting on the vasopressin V2 receptors (aquaretics) have attracted attention as a possible therapy for heart failure and polycystic kidney disease. Despite a solid rationale and encouraging preclinical testing, aquaretics have not improved clinical outcomes in randomized clinical trials for heart failure. Additional clinical trials with select population targets, more flexible dosing schedules, and possibly a different drug type or combination (balanced V1a/V2 receptor antagonism) may be warranted. Aquaretics are promising for the treatment of autosomal dominant polycystic kidney disease and have been approved in Japan for this indication. More studies are needed to better define their long-term safety and efficacy and optimize their utilization.

Original languageEnglish (US)
Pages (from-to)195-210
Number of pages16
JournalAnnual Review of Medicine
StatePublished - Jan 14 2015


  • aquaretics
  • baroreceptors
  • osmoreceptors
  • vaptans
  • vasopressin V1a receptor
  • vasopressin V2 receptor

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)


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