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Identification
NameNesiritide
Accession NumberDB04899
TypeBiotech
GroupsApproved, Investigational
Description

Nesiritide is a medication used to treat acutely decompensated congestive heart failure with dyspnea at rest or with minimal exertion (such as talk, eating or bathing). Nesiritide is the recombinant form of the 32 amino acid human B-type natriuretic peptide, which is normally produced by the ventricular myocardium.

Protein structureDb04899
Related Articles
Protein chemical formulaNot Available
Protein average weight3464.0 Da
Sequences
>DB04899: Natriuretic peptides B
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Download FASTA Format
Synonyms
BNP
Brain natriuretic peptide 32
Natriuretic peptides B
Nesiritide recombinant
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Natrecorinjection, powder, lyophilized, for solution1.5 mg/5mLintravenousScios LLC2001-08-01Not applicableUs
Natrecorpowder for solution1.5 mgintravenousJanssen Inc2008-02-052012-08-01Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIP7WI8UL647
CAS number124584-08-3
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
PharmacodynamicsNesiritide works to facilitate cardiovascular fluid homeostasis through counterregulation of the renin-angiotensin-aldoesterone system, stimulating cyclic guanosine monophosphate, leading to smooth muscle cell relaxation. In simpler terms, it promotes vasodilation, natriuresis, and diuresis.
Mechanism of actionHuman BNP binds to the particulate guanylate cyclase receptor of vascular smooth muscle and endothelial cells, leading to increased intracellular concentrations of guanosine 3'5'-cyclic monophosphate (cGMP) and smooth muscle cell relaxation. Cyclic GMP serves as a second messenger to dilate veins and arteries. Nesiritide has been shown to relax isolated human arterial and venous tissue preparations that were precontracted with either endothelin-1 or the alpha-adrenergic agonist, phenylephrine. In human studies, nesiritide produced dose-dependent reductions in pulmonary capillary wedge pressure (PCWP) and systemic arterial pressure in patients with heart failure. In animals, nesiritide had no effects on cardiac contractility or on measures of cardiac electrophysiology such as atrial and ventricular effective refractory times or atrioventricular node conduction. Naturally occurring atrial natriuretic peptide (ANP), a related peptide, increases vascular permeability in animals and humans and may reduce intravascular volume. The effect of nesiritide on vascular permeability has not been studied.
Related Articles
AbsorptionAdministration of nesiritide exhibits biphasic disposition from the plasma.
Volume of distribution
  • 0.19 L/kg
Protein bindingNot Available
Metabolism

Nesiritide undergoes proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface.

Route of eliminationHuman BNP is cleared from the circulation via the following three independent mechanisms, in order of decreasing importance: 1) binding to cell surface clearance receptors with subsequent cellular internalization and lysosomal proteolysis; 2) proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface; and 3) renal filtration.
Half lifeApproximately 18 minutes
Clearance
  • 9.2 mL/min/k [patients with congestive heart failure receiving IV infusion]
ToxicityNo data are available with respect to overdosage in humans. The expected reaction would be excessive hypotension, which should be treated with drug discontinuation or reduction and appropriate measures.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintravenous1.5 mg/5mL
Powder for solutionintravenous1.5 mg
Prices
Unit descriptionCostUnit
Natrecor 1.5 mg vial716.36USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1339210 No1997-08-052014-08-05Canada
US5114923 No1994-05-192014-05-19Us
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. Jefferies JL, Price JF, Denfield SW, Chang AC, Dreyer WJ, McMahon CJ, Grenier MA, Clunie SK, Thomas A, Moffett BS, Wann TS, Smith EO, Towbin JA: Safety and efficacy of nesiritide in pediatric heart failure. J Card Fail. 2007 Sep;13(7):541-8. [PubMed:17826644 ]
  2. Maisel AS: Nesiritide: a new therapy for the treatment of heart failure. Cardiovasc Toxicol. 2003;3(1):37-42. [PubMed:12668889 ]
  3. Vichiendilokkul A, Tran A, Racine E: Nesiritide: a novel approach for acute heart failure. Ann Pharmacother. 2003 Feb;37(2):247-58. [PubMed:12549957 ]
  4. Cheng JW: Nesiritide: review of clinical pharmacology and role in heart failure management. Heart Dis. 2002 May-Jun;4(3):199-203. [PubMed:12028606 ]
  5. Bettencourt P: Brain natriuretic peptide (nesiritide) in the treatment of heart failure. Cardiovasc Drug Rev. 2002 Winter;20(1):27-36. [PubMed:12070532 ]
External Links
ATC CodesC01DX19
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (205 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Nesiritide.
ButabarbitalButabarbital may increase the hypotensive activities of Nesiritide.
ButethalButethal may increase the hypotensive activities of Nesiritide.
DuloxetineNesiritide may increase the orthostatic hypotensive activities of Duloxetine.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Nesiritide.
HexobarbitalHexobarbital may increase the hypotensive activities of Nesiritide.
LevodopaNesiritide may increase the orthostatic hypotensive activities of Levodopa.
MethohexitalMethohexital may increase the hypotensive activities of Nesiritide.
NicorandilNicorandil may increase the hypotensive activities of Nesiritide.
PentobarbitalPentobarbital may increase the hypotensive activities of Nesiritide.
PrimidonePrimidone may increase the hypotensive activities of Nesiritide.
RisperidoneNesiritide may increase the hypotensive activities of Risperidone.
SecobarbitalSecobarbital may increase the hypotensive activities of Nesiritide.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Nesiritide.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein kinase activity
Specific Function:
Receptor for the atrial natriuretic peptide NPPA/ANP and the brain natriuretic peptide NPPB/BNP which are potent vasoactive hormones playing a key role in cardiovascular homeostasis. Has guanylate cyclase activity upon binding of the ligand.
Gene Name:
NPR1
Uniprot ID:
P16066
Molecular Weight:
118918.11 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane signaling receptor activity
Specific Function:
Receptor for the C-type natriuretic peptide NPPC/CNP hormone. Has guanylate cyclase activity upon binding of its ligand. May play a role in the regulation of skeletal growth.
Gene Name:
NPR2
Uniprot ID:
P20594
Molecular Weight:
117020.97 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Peptide hormone binding
Specific Function:
Receptor for the natriuretic peptide hormones, binding with similar affinities atrial natriuretic peptide NPPA/ANP, brain natriuretic peptide NPPB/BNP, and C-type natriuretic peptide NPPC/CNP. May function as a clearance receptor for NPPA, NPPB and NPPC, regulating their local concentrations and effects. May regulate diuresis, blood pressure and skeletal development. Does not have guanylate cyc...
Gene Name:
NPR3
Uniprot ID:
P17342
Molecular Weight:
59807.34 Da
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Drug created on October 21, 2007 16:23 / Updated on August 17, 2016 12:24