==== 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.====

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1852 details
Primary information
ThPP IDTh1239
Therapeutic Peptide/Protein NameThrombomodulin Alfa
SequenceNA view full sequnce in fasta
Functional ClassificationIb
Molecular Weight52124
Chemical FormulaC2230-H3357-N633-O718-S50
Isoelectric PointNA
HydrophobicityNA
Melting Point (℃)NA
Half Life2–3 days after sc injection; 19.82 +/- 2.10 hours after IV injection
DescriptionThrombomodulin 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/DiseaseInvestigated for use/treatment in blood preservative, blood (blood forming organ disorders, unspecified), sepsis and septicemia, and thrombosis.
PharmacodynamicsThrombomodulin (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 ActionThrombomodulin 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.
ToxicityNA
MetabolismNA
AbsorptionNA
Volume of DistributionNA
Clearance7-10 days
CategoriesAnticoagulant agent, Antiplatelet agent
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetProthrombin, Coagulation factor V
Information of corresponding available drug in the market
Brand NameRecomodulin (in Japan only)
CompanyAsahi Kasei Pharma Corp
Brand DiscriptionIt is a recombinant thrombomodulin and was approved in Japan on 25 Jan-2008.
Prescribed forFor the treatment of patients with disseminated intravascular cogulation (DIC)
Chemical Name1-498-thrombomodulin
FormulationNA
Physcial Appearncelyophilized powder for solution
Route of AdministrationIntravenous
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Linkhttps://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 ID17584906, 17059423, 15869592, 15456485, 12211414, 27693845
3-D StructureN.A.