Nesiritide
Explore a selection of our essential drug information below, or:
Identification
- Summary
Nesiritide is a recombinant natriuretic peptide used for the treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
- Generic Name
- Nesiritide
- DrugBank Accession Number
- DB04899
- Background
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.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Hormones - 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
Pharmacology
- Indication
For the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Acute decompensated heart failure •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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 AAtrial natriuretic peptide receptor 1 binderHumans AAtrial natriuretic peptide receptor 2 Not Available Humans AAtrial 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]
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- 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 Integrate drug-drug
interactions in your softwareAbaloparatide The risk or severity of adverse effects can be increased when Nesiritide is combined with Abaloparatide. Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Nesiritide. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Nesiritide. Aliskiren The risk or severity of adverse effects can be increased when Nesiritide is combined with Aliskiren. Ambrisentan Nesiritide may increase the hypotensive activities of Ambrisentan. - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Natrecor Powder, for solution 1.5 mg / vial 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 2020-06-15 US
Categories
- ATC Codes
- C01DX19 — Nesiritide
- Drug 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
- Chemical TaxonomyProvided by Classyfire
- 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
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- P7WI8UL647
- CAS number
- 124584-08-3
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. [Article]
- Maisel AS: Nesiritide: a new therapy for the treatment of heart failure. Cardiovasc Toxicol. 2003;3(1):37-42. [Article]
- Vichiendilokkul A, Tran A, Racine E: Nesiritide: a novel approach for acute heart failure. Ann Pharmacother. 2003 Feb;37(2):247-58. [Article]
- Cheng JW: Nesiritide: review of clinical pharmacology and role in heart failure management. Heart Dis. 2002 May-Jun;4(3):199-203. [Article]
- Bettencourt P: Brain natriuretic peptide (nesiritide) in the treatment of heart failure. Cardiovasc Drug Rev. 2002 Winter;20(1):27-36. [Article]
- External Links
- UniProt
- P16860
- PubChem Substance
- 46508506
- 19666
- ChEMBL
- CHEMBL1201668
- Therapeutic Targets Database
- DAP001320
- PharmGKB
- PA164781045
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Nesiritide
- FDA label
- Download (205 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Basic Science Cardiomyopathy / Diabetes Mellitus 1 somestatus stop reason just information to hide Not Available Completed Basic Science Hypertension 1 somestatus stop reason just information to hide Not Available Completed Health Services Research Congestive Heart Failure (CHF) 1 somestatus stop reason just information to hide Not Available Completed Treatment Dilated Cardiomyopathy (DCM) 1 somestatus stop reason just information to hide Not Available Completed Treatment Hypertension / Type 2 Diabetes Mellitus 1 somestatus stop reason just information to hide
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 / vial - 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) Region US5114923 No 1992-05-19 2014-05-19 US CA1339210 No 1997-08-05 2014-08-05 Canada
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General 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
- Specific Function
- adenylate cyclase activity
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General 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
- Specific Function
- adenylate cyclase activity
- Gene Name
- NPR2
- Uniprot ID
- P20594
- Uniprot Name
- Atrial natriuretic peptide receptor 2
- Molecular Weight
- 117020.97 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- General 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 cyclase activity
- Specific Function
- chloride ion binding
- Gene Name
- NPR3
- Uniprot ID
- P17342
- Uniprot Name
- Atrial natriuretic peptide receptor 3
- Molecular Weight
- 59807.34 Da
Drug created at October 21, 2007 22:23 / Updated at October 17, 2024 17:12