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Thrombolytics and fibrinolytics

8 articles

Ancrod

Ancrod (Arvin, Viprinex) is a thrombin-like enzyme from Malayan pit viper venom that defibrinogenates blood by cleaving fibrinopeptide A; tested for acute ischemic stroke in STAT and ESTAT trials, never US-approved, production discontinued in 2002.

Anistreplase

Anistreplase (APSAC, Eminase) is an acylated streptokinase-lys-plasminogen thrombolytic complex, given as a 30-unit IV bolus over 2-5 minutes, half-life about 90 minutes, FDA approved 1989 for acute myocardial infarction.

Desmoteplase

Desmoteplase (DSPAα1), a fibrin-selective plasminogen activator from vampire bat (Desmodus rotundus) saliva, was developed as a 3-9 hour window stroke thrombolytic; trials showed recanalization gains but no functional benefit.

Monteplase

Monteplase (Cleactor, E6010) is a recombinant mutant tissue-type plasminogen activator thrombolytic with a Cys84Ser mutation, approved in Japan in 2005 for acute pulmonary embolism and myocardial infarction, distinct from alteplase and tenecteplase.

Recombinant human prourokinase

Recombinant human prourokinase (rhPro-UK, 普佑克/Puyouke) is a CHO-cell-expressed fibrinolytic drug by Tasly, approved in China in 2011 for STEMI thrombolysis and the only marketed recombinant prourokinase product in China, with stroke and pulmonary embolism trials.

Reteplase

Reteplase (r-PA, Rapilysin) is a nonglycosylated recombinant tPA deletion mutant thrombolytic with kringle-2 and protease domains, given as two 10-unit boluses 30 minutes apart; FDA-approved 1996 for myocardial infarction, EU authorization withdrawn 2024.

Streptokinase (drug)

Streptokinase, a 47 kDa protein from beta-hemolytic streptococci (S. equisimilis H46A), is the first plasminogen-activator thrombolytic drug, discovered by Tillett in 1933, dosed at 1.5 million IU IV, and still the low-cost (~US$200) clot-buster of developing countries.

Tenecteplase

Tenecteplase (TNKase, Metalyse) is a modified recombinant tissue plasminogen activator thrombolytic, approved in 2000 for STEMI, given as a single bolus, with 14-fold higher fibrin specificity than alteplase.