Reteplase Drugbank ID : DB00015 Protein chemical formula : C1736H2671N499O522S22 Protein average weight : 39589.6000

Description : Indication : Pharmacodynamics : Human tissue plasminogen activator, purified, glycosylated, 355 residues purified 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 : For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction Pharmacodynamics : Reteplase 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 : 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.

Drug Interaction: Targets : Affected organisms : Ginkgo biloba : Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided. Ticlopidinen : Increased bleeding risk. Monitor for signs of bleeding. Targets : Plasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1 Affected organisms : Humans and other mammals

Categories : Patents : Sequence : Fibrinolytic Agents and Thrombolytic Agents Patents : Country Patent Number Approved Expires Canada 2107476 2007-12-18 2012-04-15 Sequence : SYQGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP

Brands : Retavase Company : Centocor Description : Retavase® (Reteplase) is a non-glycosylated deletion mutein of tissue plasminogen activator (tPA), containing the kringle 2 and the protease domains of human tPA. Retavase® (reteplase) contains 355 of the 527 amino acids of native tPA (amino acids 1-3 and 176-527). Retavase® (reteplase) is produced by recombinant DNA technology in E.coli. The protein is isolated as inactive inclusion bodies from E.coli, converted into its active form by an in vitro folding process and purified by chromatographic separation. The molecular weight of Reteplase is 39,571 daltons. Used for/Prescribed for : Improving heart function and reducing long-term effects of a heart attack. 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 Form : sterile, white, lyophilized powder Route of administration : intravenous injection

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 injection over 2 minutes. The second bolus is given 30 minutes after initiation of the first bolus injection Contraindication : allergic, or you have an aneurysm, heart or blood vessel defects, bleeding disorders, severe uncontrolled high blood pressure, a history of stroke, or internal bleeding; you have had brain or spinal surgery; or you have suffered recent trauma Side effects : SEVERE side effects : Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); black, tarry stools; bleeding at the injection site; chest pain; severe bleeding; sudden, severe headache; trouble breathing; vomiting blood or material that looks like coffee grounds. Drug interaction : A total of 183 drugs (709 brand and generic names) are known to interact with Retavase (reteplase).

References : http://www. drugs. com/cdi/retavase. html http://www