Summary
BRL 26921 is the p-anisoyl derivative of the primary streptokinase-human plasminogen
complex in which the acyl group is specifically located at the catalytic centre of
the enzyme. Doses of BRL 26921 ranging from 5 mg to 25 mg were given intravenously
or into a coronary artery to 12 patients with acute myocardial infarction. The complex
was well tolerated and produced no serious bleeding. Coronary artery reperfusion was
demonstrated angiographically in three patients.
In most patients, fibrinogen, plasminogen, α2 antiplasmin and a2 macroglobulin levels
fell and the level of fibrinogen degradation products increased acutely post treatment
indicating systemic fibrinolytic activation. The degree of this activation was variable
but was profound in some. It appeared to be dose related and modified by the presence
of streptokinase antibodies. BRL 26921 appears less “selectively” thrombolytic in
patients than had been expected from animal models.
Keywords
Acylated streptokinase - plasminogen - Fibrinolytic activation - Acute myocardial
infarction