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Th1239 details
Primary information
ID10880
Therapeutic IDTh1239
Protein NameThrombomodulin Alfa
SequenceNA
Molecular Weight52124
Chemical FormulaC2230-H3357-N633-O718-S50
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
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
NA
Clearance7-10 days
CategoriesAmino Acids, Peptides, and Proteins,Carbohydrates,Glycoconjugates,Glycoproteins,Membrane Glycoproteins,Membrane Proteins,Platelet Membrane Glycoproteins,Proteins,Receptors, G-Protein-Coupled,Receptors, Peptide,Receptors, Proteinase-Activated,Receptors, Thrombin
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetProthrombin,Coagulation factor V
Brand NameRecomodulin (in Japan only)
CompanyAsahi Kasei Pharma Corp
Brand DescriptionAsahi Kasei Pharma Corp
Prescribed ForFor the treatment of patients with disseminated intravascular cogulation (DIC)
Chemical Name1-498-thrombomodulin
FormulationNA
Physical Appearance lyophilized powder for solution
Route of AdministrationIntravenous
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA