==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1532 details
Primary information
ThPP IDTh1111
Therapeutic Peptide/Protein NameDefibrotide
SequenceDNA (sodium Salt) view full sequnce in fasta
Functional ClassificationN.A.
Molecular WeightN.A.
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Lifet1/2-alpha = minutes (10-20 minutes in rat); t1/2-beta = a few hours
DescriptionSodium salt of a mixture of single-stranded oligodeoxyribonucleotides, derived from porcine mucosal DNA. It has been shown to possess antithrombotic, anti-inflammatory and anti-ischemic properties and without the associated disadvantages of significant systemic anticoagulant effects. It is marketed under the brand names Dasovas (FM), Noravid, and Prociclide in a variety of countries, but is currently not approved in the USA. The manufacturer is Gentium.
Indication/DiseaseDefibrotide is used to treat or prevent a failure of normal blood flow (occlusive venous disease, OVD) in the liver of patients who have had bone marrow transplants or received certain drugs such as oral estrogens, mercaptopurine, and many others
PharmacodynamicsDefibrotide is a deoxyribonucleic acid derivative extracted from mammalian organs, which has been developed for the treatment of a number of vascular disorders. It appears to increase fibrinolysis and may possess antithrombotic, antiatherosclerotic and anti-ischaemic actions, probably due to its ability to selectively increase prostaglandin I2 and E2 levels and to increase tissue plasminogen activator and decrease plasminogen activator inhibitor function. Defibrotide is available as an intravenous and intramuscular preparation, and also as an oral formulation for long term use.
Mechanism of ActionThe drug appears to prevent the formation of blood clots and to help dissolve blood clots by increasing levels of prostaglandin I2, E2, and prostacyclin, altering platelet activity, increasing tissue plasminogen activator function, and decreasing activity of tissue plasminogen activator inhibitor. Prostaglandin I2 relaxes the smooth muscle of blood vessels and prevents platelets from adhering to each other. Prostaglandin E2 at certain concentrations also inhibits platelet aggregation. Moreover, the drug provides additional beneficial anti-inflammatory and antiischemic activities as recent sudies have shown. It is yet unclear, if the latter effects can be utilized clinically (e.g., treatment of ischemic stroke).
ToxicityN.A.
MetabolismN.A.
AbsorptionBioavailability is 58-70% following oral administration, compared to parenteral forms (i.v. and i.m. = 100%).
Volume of DistributionN.A.
ClearanceN.A.
CategoriesAntithrombins
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetAdenosine receptor A1,Adenosine receptor A2a,Adenosine receptor A2b
Information of corresponding available drug in the market
Brand NameNoravid
Companysanofi-aventis
Brand DiscriptionDefibrotide is the sodium salt of a mixture of single-stranded oligodeoxyribonucleotides derived from porcine mucosal DNA. It has been shown to have antithrombotic, anti-inflammatory and anti-ischemic properties (but without associated significant systemic anticoagulant effects). It is marketed under the brand names Dasovas (FM), Noravid, and Prociclide in a variety of countries, but is currently not approved in the USA. The drug appears to prevent the formation of blood clots and to help dissolve blood clots by increasing levels of prostaglandin I2, E2, and prostacyclin, altering platelet activity, increasing tissue plasminogen activator function, and decreasing activity of tissue plasminogen activator inhibitor. Prostaglandin I2 relaxes the smooth muscle of blood vessels and prevents platelets from adhering to each other. Prostaglandin E2 at certain concentrations also inhibits platelet aggregation. Moreover, the drug provides additional beneficial anti-inflammatory and antiischemic activities as recent sudies have shown. It is yet unclear, if the latter effects can be utilized clinically (e.g., treatment of ischemic stroke).
Prescribed forDefibrotide is used to treat or prevent a failure of normal blood flow (occlusive venous disease, OVD) in the liver of patients who have had bone marrow transplants or received certain drugs such as oral estrogens, mercaptopurine, and many others.
Chemical NamePolydeoxyribonucleotides of bovine lung
FormulationN. A.
Physcial AppearnceN. A.
Route of AdministrationN.A.
Recommended Dosage6.25mg/kg body weight every 6 hours (25mg/kg/day)
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttp://drug-info.in/noravid-defibrotide-sanofi-aventis/ http://www.pharmgkb.org/drug/PA164749105#tabview=tab1&subtab=31 https://duckduckgo.com/l/?kh=-1&uddg=http%3A%2F%2Fwww.fda.gov%2Fohrms%2Fdockets%2Fac%2F07%2Fslides%2F2007-4316s1-01-FDA-Shashaty.ppt
PubMed ID3754833, 17495522, 16584299, 8807733, 8511753, 7681375
3-D StructureN.A.