| Primary information |
|---|
| ID | 1852 |
| ThPP ID | Th1239 |
| Therapeutic Peptide/Protein Name | Thrombomodulin Alfa |
| Sequence | NA view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 52124 |
| Chemical Formula | C2230-H3357-N633-O718-S50 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | 2–3 days after sc injection; 19.82 +/- 2.10 hours after IV injection |
| Description | Thrombomodulin Alfa is a novel, recombinant and soluble thrombomodulin (ART-123). It is a human protein with both thrombin inhibiting and protein C stimulating activities, for the potential treatment of thromboembolism and blood clotting disorders, such as disseminated intravascular thromboembolism. |
| Indication/Disease | Investigated for use/treatment in blood preservative, blood (blood forming organ disorders, unspecified), sepsis and septicemia, and thrombosis. |
| Pharmacodynamics | Thrombomodulin (TM) alfa, a recombinant human soluble TM, enhances activation of pro-carboxypeptidase B2 (pro-CPB2) by thrombin. Activated pro-CPB2 (CPB2) exerts anti-inflammatory and anti-fibrinolytic activities. |
| Mechanism of Action | Thrombomodulin alfa is a soluble form of recombinant human thrombomodulin comprising all extracellular domains of thrombomodulin. Bound to thrombin, Thrombomodulin alfa inhibits its procoagulant activity and promotes activation of protein C. Thrombomodulin alfa inhibits thrombin generation by the activation of protein C and the subsequent inactivation of factor Va in the presence of protein S. Thrombomodulin alfa attenuates the extension of the clot by inhibiting further thrombin generation on clots, while other anticoagulants inhibit the initiation of clot formation. A higher concentration of Thrombomodulin alfa is needed to affect clotting time and platelet aggregation than thrombin generation. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| Volume of Distribution | NA |
| Clearance | 7-10 days |
| Categories | Anticoagulant agent, Antiplatelet agent |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Prothrombin, Coagulation factor V |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Recomodulin (in Japan only) |
| Company | Asahi Kasei Pharma Corp |
| Brand Discription | It is a recombinant thrombomodulin and was approved in Japan on 25 Jan-2008. |
| Prescribed for | For the treatment of patients with disseminated intravascular cogulation (DIC) |
| Chemical Name | 1-498-thrombomodulin |
| Formulation | NA |
| Physcial Appearance | lyophilized powder for solution |
| Route of Administration | Intravenous |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link | https://www.drugs.com/international/thrombomodulin-alfa.html , http://www.genome.jp/dbget-bin/www_bget?dr:D06410 https://www.pharmacodia.com/web/drug/1_1433.html |
| PubMed ID | 17584906, 17059423, 15869592, 15456485, 12211414, 27693845 |
| 3-D Structure | N.A. |