DESMOTEPLASE

Desmoteplase in Stroke

Desmoteplase (INN) is the most specific plasminogen activator known to date. Based on promising efficacy and safety data from two randomised phase II trials, Desmoteplase is under investigation in phase III for treatment of ischemic stroke up to 9 hours after onset of symptoms.

Desmoteplase was originally discovered in the saliva of the vampire bat, Desmodus rotundus, whose only diet is mammalian blood. Optimized by evolution of nature, Desmoteplase specifically activates plasminogen that is bound to fibrin. Once activated, plasminogen is converted to plasmin, which in turn dissolves the clot by digesting the fibrin matrix.

In ischemic stroke patients, Desmoteplase has the potential to restore blood flow to the affected tissue and consequently to minimise ischemic damage.

Key advantages that characterize Desmoteplase include:

• High specificity and selectivity for fibrin-bound plasminogen¹
• No activation by beta-amyloid²
• No neurotoxicity in animals³
  
  ¹ Bringmann, 1995, J Biol Chem; Stewart, 1998, J Biol Chem
  ² Kruithof, 2004, Thromb Heamost
  ³ Liberatore, 2003, Stroke; Reddrop, 2005, Stroke

In two randomized Phase II trials (DIAS and DEDAS, respectively) Desmoteplase, given as a single IV dose, showed a higher rate of reperfusion and better clinical outcome compared with placebo in patients treated from 3 to 9 hours after onset of symptoms (Hacke, 2004, Stroke; Hacke, 2005, Cerebrovasc Dis, 19(suppl 2)).

The ongoing DIAS-2 study targeting over 60 participating centers worldwide was set up to further investigate Desmoteplase in stroke.