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Agent to Reverse Anticoagulant Effects of Direct Oral Anti-Coagulants

Scientists at Leiden University Medical Center (LUMC) have developed a Factor Xa variant that counteracts the effects of Factor Xa-inhibiting oral anticoagulants.

There is currently no approved method that specifically counteracts the anticoagulant effects of the oral direct Factor Xa (FXa)-inhibitors rivaroxaban (Xarelto), apixaban (Eliquis), and edoxaban (Lixiana). The most advance specific reversal strategy in development aims to neutralize the circulating inhibitors. The disadvantage of neutralizing strategies is that high doses of expensive biologicals are required to attain reversal and half-lives of agents are short. Scientists at LUMC have developed an FXa protein variant (LUMC-FXa) that is able to bypass and overcome the anticoagulant effect of direct FXa-inhibitors by functionally replacing endogenous FXa.

LUMC-FXa is resistant to inhibition by direct FXa-inhibitors that target human FXa. It is 100-fold less sensitive to inhibition by these anticoagulants in vitro as compared to human FXa and can still trigger normal blood clot formation in FX-depleted plasma.  Therefore, LUMC-FXa could be used as a rescue therapeutic agent to manage potential life-threatening bleeding events or emergency surgical interventions in patients receiving FXa-inhibiting oral anticoagulants.

We are seeking a collaboration partner and/or licensee.

Key benefits

  • The procoagulant effect of LUMC-Factor Xa is immediate
  • Much less protein needed as compared to other reversal strategies (e.q. prothrombin complex concentrate (PCC))

Applications

  • Antidote to the anticoagulant effect of direct Factor Xa-inhibitors in cases of severe bleeding
  • Restoring normal blood coagulation in patients using direct Factor Xa-inhibitors prior to emergency surgical interventions

Development stage

  • LUMC-Factor Xa has been tested in vitro
  • In vivo studies to assess both zymogen LUMC-Factor X and protease LUMC-Factor Xa are in preparation

Luris reference number

INV-088.034

Patent status

A patent application has been filed

Data available on request

Patent texts