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| Primary information |
|---|
| ID | 10210 |
| Therapeutic ID | Th1028 |
| Protein Name | Tenecteplase |
| Sequence | >Th1028_Tenecteplase
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGNWSTAESGAECTNWQSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAAAAASPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
|
| Molecular Weight | 58951.2 |
| Chemical Formula | C2561H3919N747O781S40 |
| Isoelectric Point | 7.61 |
| Hydrophobicity | -0.528 |
| Melting point | 60 |
| Half-life | 1.9 hours (mammalian reticulocytes, in vitro) |
| Description | Tenecteplase(527 amino acid) is a glycoprotein developed by introducing the following modifications to the complementary DNA for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain. |
| Indication/Disease | To treat myocardial infarction and lysis of intracoronary emboli. |
| Pharmacodynamics | Tenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and 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 | Tenecteplase 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 | NA |
| Metabolism | NA |
| Absorption | NA |
| NA |
| Clearance | 99 - 119 mL/min [acute myocardial infarction patients] |
| Categories | Agents causing angioedema, Amino Acids, Peptides, and Proteins, Anticoagulants, Biological Factors, Blood and Blood Forming Organs, Blood Proteins, Cardiovascular Agents, Endopeptidases, Enzymes, Enzymes and Coenzymes, Fibrin Modulating Agents, Fibrinolytic Agents, Hematologic Agents, Hydrolases, Peptide Hydrolases, Plasminogen Activators, Proteins, Serine Endopeptidases, Serine Proteases, Tissue Plasminogen Activator |
| Patents Number | CA2129660 |
| Date of Issue | 28-Jun-2005 |
| Date of Expiry | 28-May-2013 |
| Drug Interaction | Aprotonin may antagonize the effect of Tenecteplase. Monitor for decreased effects of Tenecteplase. |
| Target | Plasminogen,Fibrinogen alpha chain,Urokinase plasminogen activator surface receptor,Plasminogen activator inhibitor 1,Plasminogen activator inhibitor 2,Tetranectin,Keratin, type II cytoskeletal 8,Annexin A2,Calreticulin,Calnexin,Prolow-density lipoprotein |
| Brand Name | TNKase |
| Company | Genentech Inc, Hoffmann La Roche |
| Brand Description | Genentech Inc, Hoffmann La Roche |
| Prescribed For | To prevent death from a heart attack (acute myocardial infarction). |
| Chemical Name | NA |
| Formulation | Each vial of TNKase nominally contains 52.5 mg Tenecteplase, 0.55 g L-arginine, 0.17 g phosphoric acid, and 4.3 mg polysorbate 20, which includes a 5% overfill. Each vial will deliver 50 mg of Tenecteplase. |
| Physical Appearance | Sterile, white to off-white, lyophilized powder |
| Route of Administration | Intravenous Injection |
| Recommended Dosage | The recommended total dose should not exceed 50 mg and is based upon patient weight. For less than 60 kg of body weight recommended dose is 30 mg of TNKase. Similarly 35 mg for 60-70 kg, 40 mg for 70-80 kg, 45 mg for 80-90 kg and 50 mg for more than 90 kg. |
| Contraindication | Active internal bleeding, History of cerebrovascular accident |
| Side Effects | Nausea, vomiting; or fever. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |