V2 receptor antagonism with tolvaptan in heart failure

Lisa C. Costello-Boerrigter; Guido Boerrigter; John C. Burnett

doi:10.1517/13543784.16.10.1639

V₂ receptor antagonism with tolvaptan in heart failure

Lisa C. Costello-Boerrigter, Guido Boerrigter, John C. Burnett

Cardiovascular Medicine

Research output: Contribution to journal › Review article › peer-review

1 Scopus citations

Abstract

The prevalence and incidence of congestive heart failure continues to increase. The two hallmarks of this syndrome, sodium and water retention, are frequently a therapeutic challenge. Most conventional diuretics act primarily as saluretics by inhibiting renal tubular electrolyte reabsorption, which, due to osmotic pressure, promotes excretion of isotonic fluid. The peptide hormone arginine vasopressin vasoconstricts at the V_1A receptor and promotes water reabsorption via the V₂ receptor in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Tolvaptan, the first orally available non-pepticle V₂ receptor antagonist, acts as a potent aquaretic. In this paper, the authors review the pharmacology of tolvaptan and discuss the results of the initial clinical trials with this potent new drug.

Original language	English (US)
Pages (from-to)	1639-1647
Number of pages	9
Journal	Expert Opinion on Investigational Drugs
Volume	16
Issue number	10
DOIs	https://doi.org/10.1517/13543784.16.10.1639
State	Published - Oct 2007

Keywords

Aquaretic
Arginine vasopressin
Heart failure
Pharmacology
Tolvaptan
Vasopressin-2 receptor antagonist

ASJC Scopus subject areas

Pharmacology
Pharmacology (medical)

Access to Document

10.1517/13543784.16.10.1639

Cite this

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title = "V2 receptor antagonism with tolvaptan in heart failure",

abstract = "The prevalence and incidence of congestive heart failure continues to increase. The two hallmarks of this syndrome, sodium and water retention, are frequently a therapeutic challenge. Most conventional diuretics act primarily as saluretics by inhibiting renal tubular electrolyte reabsorption, which, due to osmotic pressure, promotes excretion of isotonic fluid. The peptide hormone arginine vasopressin vasoconstricts at the V1A receptor and promotes water reabsorption via the V2 receptor in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Tolvaptan, the first orally available non-pepticle V2 receptor antagonist, acts as a potent aquaretic. In this paper, the authors review the pharmacology of tolvaptan and discuss the results of the initial clinical trials with this potent new drug.",

keywords = "Aquaretic, Arginine vasopressin, Heart failure, Pharmacology, Tolvaptan, Vasopressin-2 receptor antagonist",

author = "Costello-Boerrigter, {Lisa C.} and Guido Boerrigter and Burnett, {John C.}",

note = "Funding Information: JC Burnett Jr was a consultant to Otsuka and a member of the steering committee of the EVEREST trial. This work was supported by grants HL POI76611, HL R0136634 (JCB), HL07111 (GB) and the Mayo Foundation, Rochester, MN, USA.",

year = "2007",

month = oct,

doi = "10.1517/13543784.16.10.1639",

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journal = "Expert Opinion on Investigational Drugs",

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T1 - V2 receptor antagonism with tolvaptan in heart failure

AU - Costello-Boerrigter, Lisa C.

AU - Boerrigter, Guido

AU - Burnett, John C.

N1 - Funding Information: JC Burnett Jr was a consultant to Otsuka and a member of the steering committee of the EVEREST trial. This work was supported by grants HL POI76611, HL R0136634 (JCB), HL07111 (GB) and the Mayo Foundation, Rochester, MN, USA.

PY - 2007/10

Y1 - 2007/10

N2 - The prevalence and incidence of congestive heart failure continues to increase. The two hallmarks of this syndrome, sodium and water retention, are frequently a therapeutic challenge. Most conventional diuretics act primarily as saluretics by inhibiting renal tubular electrolyte reabsorption, which, due to osmotic pressure, promotes excretion of isotonic fluid. The peptide hormone arginine vasopressin vasoconstricts at the V1A receptor and promotes water reabsorption via the V2 receptor in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Tolvaptan, the first orally available non-pepticle V2 receptor antagonist, acts as a potent aquaretic. In this paper, the authors review the pharmacology of tolvaptan and discuss the results of the initial clinical trials with this potent new drug.

AB - The prevalence and incidence of congestive heart failure continues to increase. The two hallmarks of this syndrome, sodium and water retention, are frequently a therapeutic challenge. Most conventional diuretics act primarily as saluretics by inhibiting renal tubular electrolyte reabsorption, which, due to osmotic pressure, promotes excretion of isotonic fluid. The peptide hormone arginine vasopressin vasoconstricts at the V1A receptor and promotes water reabsorption via the V2 receptor in the renal collecting duct by inserting aquaporin-2 water channels into the luminal membrane. Tolvaptan, the first orally available non-pepticle V2 receptor antagonist, acts as a potent aquaretic. In this paper, the authors review the pharmacology of tolvaptan and discuss the results of the initial clinical trials with this potent new drug.

KW - Aquaretic

KW - Arginine vasopressin

KW - Heart failure

KW - Pharmacology

KW - Tolvaptan

KW - Vasopressin-2 receptor antagonist

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