Anisoylated Plasminogen-Streptokinase Activator Complex,

Anistreplase (anisoylated plasminogen streptokinase activator complex APSAC) consists of a complex of purified human plasminogen and bacterial streptokinase that has been acylated to protect the enzyme s active site. When administered, the acyl group spontaneously hydrolyzes, freeing the activated streptokinase-proactivator complex. This product (recently discontinued in the USA) allows for rapid intravenous injection, greater clot selectivity (ie, more activity on plasminogen associated with clots than on free plasminogen in the blood), and more thrombolytic activity. 

Chemical Name Anisoylated plasminogen streptokinase activator complex... 

Anistreplase (anisoylated plasminogen streptokinase activator complex, APSAC), is the plasminogen-streptokinase complex (above) in which the enzyme centre that converts plasminogen to plasmin is protected from deactivation, so prolonging its action. 

Been M, de Bono DP, Muir AL, Boulton FE, Fears R, Standring R, Ferres H. Clinical effects and kinetic properties of intravenous APSAC—anisoylated plasminogen-streptokinase activator complex (BRL 26921) in acute myocardial infarction. Int J Cardiol 1986 11(1) 53-61. 

J. L. Anderson, J. B. Boissel, and D. A. Chamberlain, eds. Symposium on anisoylated plasminogen streptokinase activator complex (APSAC). Drugs 3 33 (1987). 

Anistreplase This anisoylated plasminogen-streptokinase activator complex (APSAC) is a prodrug. As the anisoyl group is hydrolyzed in vivo (a slow, spontaneous process), the... 

Commonly used thrombolytics are streptokinase, urokinase, tissue plasminogen activator (t-PA, Alteplase), anisoylated plasminogen streptokinase activator complex (APSAC, Anistreplase), and reteplase (Retavase). 

Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells. Eminase is a lyophilized formulation of anistreplase, the p-anisoyl derivative of the primary Lys-plasminogen-streptokinase activator complex (a complex of Lys-plasminogen and streptokinase). A p-anisoyl group is chemically conjugated to a complex of bacterial-derived streptokinase and human plasma-derived Lys-plasminogen proteins. 

Anisoylatedplasminogen streptokinase activator complex (APSAC)(Table 11-4) is an anisoyl (p-methoxybenzoyl) derivative of the active (lysine) site of the plasminogen component of this complex. Acylation inactivates the enzyme but does not decrease the affinity of the complex for fibrin. The resultant slow deacylation (tU2 = 40 min) should achieve relative selectivity for the fibrin in the clot over circulating plasma fibrinogen. Hydrolysis of anisoyl amide following binding onto the thrombus (i.e., activation) leads to fibrinolysis. APSAC has been reported to produce a 60-80% reperfusion rate following IV administration. 

Unfortunately, the half-life of the activator complex is less than 30 minutes, which frequently is too short to completely lyse a thrombus. Anistreplase (APSAC Eminase) is a 1 1 streptokinase/lysine-plasminogen complex that has been acylated with an anisoyl group at the active-site serine within... 

O. Matsuo, D. Collen, and M. Verstrate. On the fibrinolytic and thrombolytic properties of active site p-anisoylated streptokinase-plasminogen-complex (BRL 26921). Thromb. Res. 24 347 (1981). 

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