Primary information |
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ID | 10211 |
Therapeutic ID | Th1028 |
Protein Name | Tenecteplase |
Sequence | >Th1028_Tenecteplase
SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGNWSTAESGAECTNWQSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAAAAASPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
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Molecular Weight | 58951.2 |
Chemical Formula | C2561H3919N747O781S40 |
Isoelectric Point | 7.61 |
Hydrophobicity | -0.528 |
Melting point | 60 |
Half-life | 20 hours (yeast, in vivo) |
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 | CA1341432 |
Date of Issue | 17-Jun-2003 |
Date of Expiry | 17-Jun-2020 |
Drug Interaction | Drotrecogin alfa increases risk of bleeding. |
Target | NA |
Brand Name | Metalyse |
Company | Boehringer Ingelheim |
Brand Description | Boehringer Ingelheim |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | Intracranial neoplasm, Known bleeding diathesis |
Side Effects | Chest pain, slow or uneven heartbeats; pain, swelling, hot or cold feeling, skin changes, or discoloration anywhere on your body; sudden leg or foot pain, foot ulcer, purple toes or fingers; swelling or severe pain or signs of infection in your fingers. |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |