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Th1109 details
Primary information
ID1530
ThPP IDTh1109
Therapeutic Peptide/Protein NameNesiritide
SequenceSPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH view full sequnce in fasta
Functional ClassificationIb
Molecular Weight3464
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeApprox. 18 mins
DescriptionRecombinant, 32 amino acid human B-type natriuretic peptide, which is normally produced by the ventricular myocardium. Nesiritide is a medication used to treat acutely decompensated congestive heart failure with dyspnea at rest or with minimal exertion.
Indication/DiseaseFor 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.
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.
MetabolismNesiritide undergoes proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface.
AbsorptionAdministration of nesiritide exhibits biphasic disposition from the plasma.
Volume of Distribution0.19 L/kg
Clearance9.2 mL/min/k [patients with congestive heart failure receiving IV infusion]
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameNATRECOR
CompanyScios unit of Johnson & Johnson,
Brand DiscriptionNATRECOR (nesiritide) is a sterile, purified preparation of human B-type natriuretic peptide (hBNP), and is manufactured from E. coli using recombinant DNA technology. Nesiritide has a molecular weight of 3464 g/mol and an empirical formula of C143H244N50O42S4. Nesiritide has the same 32 amino acid sequence as the endogenous peptide, which is produced by the ventricular myocardiu
Prescribed forNATRECOR (nesiritide) is indicated for the treatment of patients with acutely decompensated heart failure who have dyspnea at rest or with minimal activity. In this population, the use of NATRECOR reduced pulmonary capillary wedge pressure and improved short term (3 hours) symptoms of dyspnea.
Chemical NameN.A.
FormulationNATRECOR is formulated as the citrate salt of rhBNP, and is provided in a sterile, single-use vial. Each 1.5 mg vial contains a white- to off-white lyophilized powder for intravenous (IV) administration after reconstitution. The quantitative composition of the lyophilized drug per vial is: nesiritide 1.58 mg, citric acid monohydrate 2.1 mg, mannitol 20.0 mg, and sodium citrate dihydrate 2.94 mg
Physcial AppearanceWhite- to off-white lyophilized powde
Route of AdministrationIntravenous
Recommended DosageIV bolus of 2 mcg/kg followed by a continuous infusion of 0.01 mcg/kg/min
ContraindicationNATRECOR is contraindicated in patients with: Persistent systolic blood pressure < 100 mm Hg prior to therapy because of an increased risk of symptomatic hypotension Known hypersensitivity to any of its components.
Side EffectsHypotension
Useful Linkhttp://www.rxlist.com/natrecor-drug.htm https://en.wikipedia.org/wiki/Nesiritide http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=13531 http://www.fda.gov/Safety/MedWatch/SafetyInformation/ucm169897.htm
PubMed ID17826644, 12668889, 12549957, 12070532, 12028606
3-D StructureN.A.