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Home / Drugs / Starting with T / Tenecteplase
 
Tenecteplase
 

Tissue plasminogen activator (tPA). Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) 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.
BrandsTNKase (Genentech Inc)
CategoriesThrombolytic Agents
PackagersF Hoffmann-La Roche Ltd.
Genentech Inc.
Synonymst- PA
t-plasminogen activator
Tissue-type plasminogen activator precursor
tPA

indication

For treatment of myocardial infarction and lysis of intracoronary emboli

pharmacology

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.

half life

1.9 hours (mammalian reticulocytes, in vitro) >20 hours (yeast, in vivo) >10 hours (Escherichia coli, in vivo)

drug interactions

Aprotinin: Aprotonin may antagonize the effect of Tenecteplase. Monitor for decreased effects of Tenecteplase.

Drotrecogin alfa: Increased risk of bleeding.

Ginkgo biloba: Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.

Ginseng: Increased risk of bleeding.

Ticlopidine: Increased bleeding risk. Monitor for signs of bleeding.