Tenecteplase

Identification

Name
Tenecteplase
Accession Number
DB00031 / WGD229O42W
Groups
Metalyse
Description

Tissue plasminogen activator (tPA). Tenecteplase is a 527 amino acid glycoprotein developed with the aid of introducing the subsequent changes 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 inside the kringle 1 area, and a tetra-alanine substitution at amino acids 296-299 in the protease area.

Pharmacology

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.

Indication

For treatment of myocardial infarction and lysis of intracoronary emboli

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.