Anistreplasa [INN-Spanish] Usage And Synthesis

Description

APSAC is an anisoylated human plasminogen-streptokinase complex useful in the treatment of myocardial infarct. Its reported advantages over other existing thrombolytics such as alteplase and streptokinase include a longer half life, ease of administration, and a more specific local antithrombotic effect.

Originator

Beecham (United Kingdom)

Uses

Fibrinolytic.

Manufacturing Process

Preparation of freeze dried p-anisoyl streptokinase/plasminogen complex without internal peptide bond cleavages:
Streptokinase (250,000 units, Kabi, Stockholm, Sweden) was dissolved in 0.1 M trishydroxymethylmethane hydrochloride pH 7.4 (2.5 ml) and a solution of 0.1 M p-amidinophenyl p'-anisate in dimethylsulphoxide (0.25 ml) added. A slight cloudiness resulted. To this mixture was added 0.5 ml of a solution of human lys-plasminogen (8.99 mg/ml in the above buffer) [Kabi, Stockholm] and the solution was thoroughly and rapidly mixed. After standing on ice for 15 minutes, the solution was stored on ice until use. After approximaely 2 hours 0.4 ml (40,000 units) of the material was diluted with 3.0 ml of a slurry of L-lysine-sepharose 4B (a 33% wet wt/volume suspension in the above buffer) and stood at 0°C for 1 hour. The gel was filtered on a glass sinter funnel at 4°C under suction and washed with the buffer (100 ml). The gel was eluted under gentle suction with the same buffer containing 0.1 M ε- aminocaproic acid (3 lots of 5 ml). The combined filtrates were dialysed for 2 hours at 4°C against ammonium bicarbonate buffer (50 mM pH 7.0) containing 2.5% w/v mannitol. The product was then freeze dried to 0.799 g of a white solid. Approximately 195 mg of this material was analysed by slab gel polyacrylamide gel electrophoresis using 10% w/v gels in the presence of sodium dodecyl sulphate. Two main polypeptide bands were observed corresponding to lys-plasminogen (m.w. 84,000) and streptokinase (m.w. 47,000). There was also a trace of contaminating human serum albumin derived from the commercial streptokinase preparation.

brand name

Eminase

Therapeutic Function

Thrombolytic

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