Thrombolytic agents.

Abstract

Thrombolytic agents are plasminogen activators that convert the zymogen plasminogen to the active enzyme plasmin, which degrades fibrin. Elucidation of the molecular mechanism of physiological fibrinolysis opened up a new era of fibrin-specific thrombolysis. Fibrin-specific plasminogen activators, including tissue-type plasminogen activator (t-PA), single-chain urokinase-type plasminogen activator (scu-PA) and staphylokinase (Sak), preferentially activate fibrin-associated plasminogen. Generated plasmin remains associated with fibrin, where it is protected from rapid inhibition and can efficiently degrade fibrin, avoiding systemic activation of the fibrinolytic system. Following a decade of clinical investigation t-PA and variants thereof are routinely used for treatment of patients with thromboembolic disease.