Tolvaptan

A selective vasopressin type 2 receptor antagonist in congestive heart failure

Umamahesh Rangasetty, Mihai Gheorghiade, Barry F. Uretsky, Cesare Orlandi, Alejandro Barbagelata

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

The neurohormone arginine vasopressin plays a significant role in the regulation of volume homeostasis, which is mediated via vasopressin type 2 (V2) receptors in the collecting tubules of the kidney. Diseases that are accompanied by abnormal volume homeostasis, including congestive heart failure and cirrhosis, are a frequent cause of hospital admissions and increasing health-care costs. Recently, several nonpepticle V2 receptor antagonists have emerged as promising agents in the management of these conditions with the advantage of having no electrolyte abnormalities, neurohormonal activation or worsening renal insufficiency. Tolvaptan, a highly selective non-pepticle V2 receptor antagonist, has demonstrated an improvement in the volume status, osmotic balance and haemodynamic profile in preclinical and Phase II trials in patients with congestive heart failure and is currently under-going testing in Phase III trials. This review discusses the evidence for the potential uses of tolvaptan, and its pharmacology and pharmacokinetics, particularly in congestive heart failure.

Original languageEnglish (US)
Pages (from-to)533-540
Number of pages8
JournalExpert Opinion on Investigational Drugs
Volume15
Issue number5
DOIs
StatePublished - May 2006

Fingerprint

Heart Failure
Homeostasis
Collecting Kidney Tubules
Vasopressin Receptors
Arginine Vasopressin
Health Care Costs
Electrolytes
Renal Insufficiency
Neurotransmitter Agents
Fibrosis
Pharmacokinetics
Hemodynamics
Pharmacology
tolvaptan
Antidiuretic Hormone Receptor Antagonists

Keywords

  • Heart failure
  • SIADH
  • Tolvaptan
  • Vasopressin receptor antagonist

ASJC Scopus subject areas

  • Pharmacology

Cite this

Tolvaptan : A selective vasopressin type 2 receptor antagonist in congestive heart failure. / Rangasetty, Umamahesh; Gheorghiade, Mihai; Uretsky, Barry F.; Orlandi, Cesare; Barbagelata, Alejandro.

In: Expert Opinion on Investigational Drugs, Vol. 15, No. 5, 05.2006, p. 533-540.

Research output: Contribution to journalArticle

Rangasetty, Umamahesh ; Gheorghiade, Mihai ; Uretsky, Barry F. ; Orlandi, Cesare ; Barbagelata, Alejandro. / Tolvaptan : A selective vasopressin type 2 receptor antagonist in congestive heart failure. In: Expert Opinion on Investigational Drugs. 2006 ; Vol. 15, No. 5. pp. 533-540.
@article{ba537aec9e054399aafdf9dcc413fe2d,
title = "Tolvaptan: A selective vasopressin type 2 receptor antagonist in congestive heart failure",
abstract = "The neurohormone arginine vasopressin plays a significant role in the regulation of volume homeostasis, which is mediated via vasopressin type 2 (V2) receptors in the collecting tubules of the kidney. Diseases that are accompanied by abnormal volume homeostasis, including congestive heart failure and cirrhosis, are a frequent cause of hospital admissions and increasing health-care costs. Recently, several nonpepticle V2 receptor antagonists have emerged as promising agents in the management of these conditions with the advantage of having no electrolyte abnormalities, neurohormonal activation or worsening renal insufficiency. Tolvaptan, a highly selective non-pepticle V2 receptor antagonist, has demonstrated an improvement in the volume status, osmotic balance and haemodynamic profile in preclinical and Phase II trials in patients with congestive heart failure and is currently under-going testing in Phase III trials. This review discusses the evidence for the potential uses of tolvaptan, and its pharmacology and pharmacokinetics, particularly in congestive heart failure.",
keywords = "Heart failure, SIADH, Tolvaptan, Vasopressin receptor antagonist",
author = "Umamahesh Rangasetty and Mihai Gheorghiade and Uretsky, {Barry F.} and Cesare Orlandi and Alejandro Barbagelata",
year = "2006",
month = "5",
doi = "10.1517/13543784.15.5.533",
language = "English (US)",
volume = "15",
pages = "533--540",
journal = "Expert Opinion on Investigational Drugs",
issn = "1354-3784",
publisher = "Taylor and Francis Ltd.",
number = "5",

}

TY - JOUR

T1 - Tolvaptan

T2 - A selective vasopressin type 2 receptor antagonist in congestive heart failure

AU - Rangasetty, Umamahesh

AU - Gheorghiade, Mihai

AU - Uretsky, Barry F.

AU - Orlandi, Cesare

AU - Barbagelata, Alejandro

PY - 2006/5

Y1 - 2006/5

N2 - The neurohormone arginine vasopressin plays a significant role in the regulation of volume homeostasis, which is mediated via vasopressin type 2 (V2) receptors in the collecting tubules of the kidney. Diseases that are accompanied by abnormal volume homeostasis, including congestive heart failure and cirrhosis, are a frequent cause of hospital admissions and increasing health-care costs. Recently, several nonpepticle V2 receptor antagonists have emerged as promising agents in the management of these conditions with the advantage of having no electrolyte abnormalities, neurohormonal activation or worsening renal insufficiency. Tolvaptan, a highly selective non-pepticle V2 receptor antagonist, has demonstrated an improvement in the volume status, osmotic balance and haemodynamic profile in preclinical and Phase II trials in patients with congestive heart failure and is currently under-going testing in Phase III trials. This review discusses the evidence for the potential uses of tolvaptan, and its pharmacology and pharmacokinetics, particularly in congestive heart failure.

AB - The neurohormone arginine vasopressin plays a significant role in the regulation of volume homeostasis, which is mediated via vasopressin type 2 (V2) receptors in the collecting tubules of the kidney. Diseases that are accompanied by abnormal volume homeostasis, including congestive heart failure and cirrhosis, are a frequent cause of hospital admissions and increasing health-care costs. Recently, several nonpepticle V2 receptor antagonists have emerged as promising agents in the management of these conditions with the advantage of having no electrolyte abnormalities, neurohormonal activation or worsening renal insufficiency. Tolvaptan, a highly selective non-pepticle V2 receptor antagonist, has demonstrated an improvement in the volume status, osmotic balance and haemodynamic profile in preclinical and Phase II trials in patients with congestive heart failure and is currently under-going testing in Phase III trials. This review discusses the evidence for the potential uses of tolvaptan, and its pharmacology and pharmacokinetics, particularly in congestive heart failure.

KW - Heart failure

KW - SIADH

KW - Tolvaptan

KW - Vasopressin receptor antagonist

UR - http://www.scopus.com/inward/record.url?scp=33646460418&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33646460418&partnerID=8YFLogxK

U2 - 10.1517/13543784.15.5.533

DO - 10.1517/13543784.15.5.533

M3 - Article

VL - 15

SP - 533

EP - 540

JO - Expert Opinion on Investigational Drugs

JF - Expert Opinion on Investigational Drugs

SN - 1354-3784

IS - 5

ER -