DB04932 - Defibrotide
| Identification | |
|---|---|
| Name | Defibrotide |
| Accession Number | DB04932 |
| Type | biotech |
| Description | 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 manufacturer is Gentium. |
| Structure |
|
| Categories (*) | |
| Molecular Weight | Not Available |
| Groups | approved |
| Monoisotopic Weight | Not Available |
| Pharmacology | |
| Indication | 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. |
| 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). |
| Absorption | Bioavailability is 58-70% following oral administration, compared to parenteral forms (i.v. and i.m. = 100%). |
| Protein binding | Not Available |
| Biotransformation | Not Available |
| Route of elimination | Not Available |
| Toxicity | Not Available |
| Affected organisms |
|
| Interactions | |
| Drug Interactions | Not Available |
| Food Interactions | Not Available |
Targets
| Adenosine A1 receptor | |
|---|---|
| Name | Adenosine A1 receptor |
| Gene Name | ADORA1 |
| Pharmacological action | unknown |
| Actions | Not Available |
| References |
|
| DTHybrid score | 0.5806 |
| Adenosine A2a receptor | |
| Name | Adenosine A2a receptor |
| Gene Name | ADORA2A |
| Pharmacological action | unknown |
| Actions | Not Available |
| References |
|
| DTHybrid score | 0.8311 |
| Adenosine A2b receptor | |
| Name | Adenosine A2b receptor |
| Gene Name | ADORA2B |
| Pharmacological action | unknown |
| Actions | Not Available |
| References |
|
| DTHybrid score | 0.5861 |