==== 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.====

Detailed description page of THPdb

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1201 details
Primary information
ThPP IDTh1026
Therapeutic Peptide/Protein NameAnistreplase
SequenceSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta
Functional ClassificationIc
Molecular Weight59042.3
Chemical FormulaC2569H3928N746O781S40
Isoelectric Point7.61
Hydrophobicity-0.516
Melting Point (℃)60
Half LifeN.A.
DescriptionHuman tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells. Eminase is a lyophilized (freeze-dried) formulation of anistreplase, the p-anisoyl derivative of the primary Lys-plasminogen-streptokinase activator complex (a complex of Lys-plasminogen and streptokinase). A p-anisoyl group is chemically conjugated to a complex of bacterial-derived streptokinase and human Plasma-derived Lys-plasminogen proteins.
Indication/DiseaseFor lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction
PharmacodynamicsAnistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of ActionAnistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesFibrinolytic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionThe use of anistreplase with other cardioactive drugs has not been studied. In addition to bleeding associated with heparin and vitamin K antagonists, drugs that alter platelet function (such as ASA and dipyridamole) may increase the risk of bleeding
TargetPlasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1
Information of corresponding available drug in the market
Brand NameEminase
CompanyWulfing Pharma GmbH
Brand DiscriptionIt is an inactive derivative of a fibrinolytic (thrombolytic) enzyme composed of streptokinase and lys-plasminogen in which the catalytic center of the enzymatic complex is temporarily blocked by a p-anisoyl group.
Prescribed forFor use in the management of ( acute myocardial infarction) AMI in adults for the lysis of thrombi obstructing coronary arteries, the reduction of infarct size, the improvement of ventricular function following AMI, and the reduction of mortality associat
Chemical NameN.A.
FormulationEach unit-dose vial of sterile lyophilized, white to off-white powder contains: anistreplase 30 units, dimethylsulfoxide <3 mg, sodium hydroxide <0.2 mg and the following buffers or stabilizers: p-amidinophenyl-p'-anisate (acylating agent) 150 µg, mannito
Physcial AppearnceDry powder
Route of AdministrationIntravenous infusion
Recommended Dosage30 units of anistreplase administered only by i.v. injection over 2 to 5 minutes into an i.v. line or vein.
ContraindicationAllergic, active internal bleeding; history of cerebrovascular accident (CVA); patients receiving other i.v. thrombolytic agents; recent (within 2 months) intracranial or intraspinal surgery or trauma, intracranial neoplasm, arteriovenous malformation, or
Side EffectsN.A.
Useful Linkhttp://www.drugs.com/mmx/eminase.html
PubMed ID27696935, 25574487, 18574277, 15383484, 12947366, 11232986, 10983734, 10235448, 9919745
3-D StructureTh1026 (View) or (Download)