| Primary information |
|---|
| ThPP ID | Th1026 |
| Therapeutic Peptide/Protein Name | Anistreplase |
| Sequence | SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKS view full sequnce in fasta |
| Functional Classification | Ic |
| Molecular Weight | 59042.3 |
| Chemical Formula | C2569H3928N746O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.516 |
| Melting Point (℃) | 60 |
| Half Life | N.A. |
| Description | Human 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/Disease | For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction |
| Pharmacodynamics | Anistreplase 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 Action | Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Fibrinolytic Agents |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | The 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 |
| Target | Plasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1 |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Eminase |
| Company | Wulfing Pharma GmbH |
| Brand Discription | It 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 for | For 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 Name | N.A. |
| Formulation | Each 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 Appearnce | Dry powder |
| Route of Administration | Intravenous infusion |
| Recommended Dosage | 30 units of anistreplase administered only by i.v. injection over 2 to 5 minutes into an i.v. line or vein. |
| Contraindication | Allergic, 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 Effects | N.A. |
| Useful Link | http://www.drugs.com/mmx/eminase.html |
| PubMed ID | 27696935, 25574487, 18574277, 15383484, 12947366, 11232986, 10983734, 10235448, 9919745 |
| 3-D Structure | Th1026 (View) or (Download) |