Alteplase

Use

Alteplase (Activase) is a tissue plasminogenactivator (t-PA) produced by rDNA technology. It is a single-chain glycoprotein protease consisting of 527 aminoacid residues. Native t-PA is isolated from a melanoma cellline. The single-chain molecule is susceptible to enzymaticdigestion to a two-chain molecule, in which the two chainsremain linked with a disulfide bond. Both forms of the nativet-PA are equipotent in fibrinolytic (and plasminogenactivating)properties. It is an extrinsic plasminogen activatorassociated with vascular endothelial tissue, whichpreferentially activates plasminogen bound to fibrin. Thefibrinolytic action of alteplase (t-PA) is confined to thrombi,with minimal systemic activation of plasminogen. It is producedcommercially by rDNA methods by inserting the alteplasegene (acquired from human melanoma cells) intoovarian cells of the Chinese hamster, serving as host cells.The melanoma-derived alteplase is immunologically andchemically identical with the uterine form. Alteplase is indicatedfor the intravenous management of acute myocardialinfarction.