| Primary information |
|---|
| ThPP ID | Th1012 |
| Therapeutic Peptide/Protein Name | Reteplase |
| Sequence | SYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQ view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 39589.6 |
| Chemical Formula | C1736H2671N499O522S22 |
| Isoelectric Point | 6.86 |
| Hydrophobicity | -0.435 |
| Melting Point (℃) | 60 |
| Half Life | N.A. |
| Description | Human tissue plasminogen activator which is glycosylated and purified (355 residues) from CHO cells. Retavase is considered a third-generation thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase – kringle-1, finger, and epidermal growth factor (EGF). |
| Indication/Disease | For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction. |
| Pharmacodynamics | Reteplase cleaves Arg/Val bonds 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 further cause myocardial infarction. |
| Mechanism of Action | Reteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then 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. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Fibrinolytic Agents |
| Patents Number | CA2107476 |
| Date of Issue | 18/12/07 |
| Date of Expiry | 15/04/12 |
| Drug Interaction | Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided with Ginkgo biloba |
| Target | Plasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1 |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Retavase |
| Company | Centocor |
| Brand Discription | Retavase(39,571 daltons) is a non-glycosylated deletion mutein of tissue plasminogen activator containing the kringle 2 and the protease domains of human tPA. Retavase contains 355 of the 527 amino acids of native tPA (amino acids 1-3 and 176-527). Retava |
| Prescribed for | Improves heart function and reduces long-term effects of a heart attack. |
| Chemical Name | N.A. |
| Formulation | Each single-use vial contains:Reteplase 18.1 mg, Tranexamic Acid 8.32 mg, Dipotassium Hydrogen Phosphate 136.24 mg, Phosphoric Acid 51.27 mg, Sucrose 364.0 mg, Polysorbate 805.20 mg |
| Physcial Appearnce | Sterile, white, lyophilized powder |
| Route of Administration | Intravenous Injection |
| Recommended Dosage | Retavase is administered as a 10 + 10 unit double-bolus injection. Two 10 unit bolus injections are required for a complete treatment. Each bolus is administered as an Intravenous infusion over 2 minutes. The second bolus is given 30 minutes after initial one. |
| Contraindication | Allergic, or you have an aneurysm, heart or blood vessel defects, bleeding disorders |
| Side Effects | Rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue. |
| Useful Link | http://www.drugs.com/cdi/retavase.html |
| PubMed ID | 15650539 |
| 3-D Structure | Th1012 (View) or (Download) |