Nesiritide
Identification
- Name
- Nesiritide
- Accession Number
- DB04899
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Hormones - 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 a 32 amino acid recombinant human B-type natriuretic peptide.
- Protein structure
- Protein chemical formula
- Not Available
- Protein average weight
- 3464.0 Da
- Sequences
>DB04899: Natriuretic peptides B SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Download FASTA Format- Synonyms
- BNP
- BNP-32
- Brain natriuretic peptide 32
- Human brain natriuretic factor-32
- Nesiritide
- Nesiritide recombinant
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Unlock Additional DataNatrecor Powder, for solution 1.5 mg Intravenous Janssen Pharmaceuticals 2008-02-05 2012-08-01 Canada 
Natrecor Injection, powder, lyophilized, for solution 1.5 mg/5mL Intravenous Scios LLC 2001-08-01 Not applicable US 
Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Categories
- Amino Acids, Peptides, and Proteins
- Cardiac Therapy
- Cardiovascular Agents
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypotensive Agents
- Natriuretic Agents
- Natriuretic Peptide, Brain
- Natriuretic Peptides
- Nerve Tissue Proteins
- Peptide Hormones
- Peptides
- Proteins
- Vasodilators Used in Cardiac Diseases
- UNII
- P7WI8UL647
- CAS number
- 124584-08-3
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Pharmacology
- Indication
For the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
- Associated Conditions
- Pharmacodynamics
Nesiritide works by facilitating cardiovascular homeostasis through the negative regulation of the renin-angiotensin-aldosterone system. This regulation will in order stimulate cyclic guanosine monophosphate and smooth muscle cell relaxation. In simpler terms, it promotes vasodilation, natriuresis, and diuresis.
- Mechanism of action
Human 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.
Target Actions Organism UAtrial natriuretic peptide receptor 1 binderHumans UAtrial natriuretic peptide receptor 2 Not Available Humans UAtrial natriuretic peptide receptor 3 Not Available Humans - Absorption
Administration of nesiritide exhibits biphasic disposition from the plasma.
- Volume of distribution
- 0.19 L/kg
- Protein binding
- Not 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 elimination
Human 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 life
Approximately 18 minutes
- Clearance
- 9.2 mL/min/k [patients with congestive heart failure receiving IV infusion]
- Toxicity
No 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
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Learn moreStructured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Learn moreStructured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
Learn moreInteractions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional Data7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Nesiritide. Acebutolol The therapeutic efficacy of Acebutolol can be increased when used in combination with Nesiritide. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Nesiritide. Aliskiren The therapeutic efficacy of Aliskiren can be increased when used in combination with Nesiritide. Alprenolol The therapeutic efficacy of Alprenolol can be increased when used in combination with Nesiritide. Ambrisentan The therapeutic efficacy of Ambrisentan can be increased when used in combination with Nesiritide. Amifostine The risk or severity of adverse effects can be increased when Amifostine is combined with Nesiritide. Amiloride The risk or severity of adverse effects can be increased when Amiloride is combined with Nesiritide. Amiodarone The risk or severity of adverse effects can be increased when Amiodarone is combined with Nesiritide. Amlodipine The therapeutic efficacy of Amlodipine can be increased when used in combination with Nesiritide. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
References
- General References
- 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]
- Maisel AS: Nesiritide: a new therapy for the treatment of heart failure. Cardiovasc Toxicol. 2003;3(1):37-42. [PubMed:12668889]
- Vichiendilokkul A, Tran A, Racine E: Nesiritide: a novel approach for acute heart failure. Ann Pharmacother. 2003 Feb;37(2):247-58. [PubMed:12549957]
- Cheng JW: Nesiritide: review of clinical pharmacology and role in heart failure management. Heart Dis. 2002 May-Jun;4(3):199-203. [PubMed:12028606]
- 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
- UniProt
- P16860
- PubChem Substance
- 46508506
- RxNav
- 19666
- ChEMBL
- CHEMBL1201668
- Therapeutic Targets Database
- DAP001320
- PharmGKB
- PA164781045
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Nesiritide
- ATC Codes
- C01DX19 — Nesiritide
- FDA label
- Download (205 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Janssen-Ortho Inc.
- Scios Inc.
- Dosage forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 1.5 mg/5mL Powder, for solution Intravenous 1.5 mg - Prices
Unit description Cost Unit Natrecor 1.5 mg vial 716.36USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Unlock Additional DataUS5114923 No 1992-05-19 2014-05-19 US CA1339210 No 1997-08-05 2014-08-05 Canada Additional Data Available- Filed On
Properties
- State
- Solid
- Experimental Properties
- Not Available
Taxonomy
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- 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 ...
- Gene Name
- NPR1
- Uniprot ID
- P16066
- Uniprot Name
- Atrial natriuretic peptide receptor 1
- Molecular Weight
- 118918.11 Da
References
- 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
- Humans
- 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
- Uniprot Name
- Atrial natriuretic peptide receptor 2
- Molecular Weight
- 117020.97 Da
- Kind
- Protein
- Organism
- Humans
- 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 ...
- Gene Name
- NPR3
- Uniprot ID
- P17342
- Uniprot Name
- Atrial natriuretic peptide receptor 3
- Molecular Weight
- 59807.34 Da
Drug created on October 21, 2007 16:23 / Updated on February 06, 2020 12:07