| Primary information |
|---|
| ThPP ID | Th1111 |
| Therapeutic Peptide/Protein Name | Defibrotide |
| Sequence | DNA (sodium Salt) view full sequnce in fasta |
| Functional Classification | N.A. |
| Molecular Weight | N.A. |
| Chemical Formula | N.A. |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | t1/2-alpha = minutes (10-20 minutes in rat); t1/2-beta = a few hours |
| Description | Sodium 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/Disease | Defibrotide 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 |
| Pharmacodynamics | Defibrotide 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 Action | 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). |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | Bioavailability is 58-70% following oral administration, compared to parenteral forms (i.v. and i.m. = 100%). |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Antithrombins |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | Adenosine receptor A1,Adenosine receptor A2a,Adenosine receptor A2b |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Noravid |
| Company | sanofi-aventis |
| Brand Discription | Defibrotide 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 for | Defibrotide 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 Name | Polydeoxyribonucleotides of bovine lung |
| Formulation | N. A. |
| Physcial Appearnce | N. A. |
| Route of Administration | N.A. |
| Recommended Dosage | 6.25mg/kg body weight every 6 hours (25mg/kg/day) |
| Contraindication | N.A. |
| Side Effects | N.A. |
| Useful Link | http://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 ID | 3754833, 17495522, 16584299, 8807733, 8511753, 7681375 |
| 3-D Structure | N.A. |