A specific antidote for dabigatran: functional and structural characterization.

摘要: Dabigatran etexilate is a direct thrombin inhibitor and used widely as an anticoagulant for the prevention of stroke in patients with atrial fibrillation. However, anticoagulation therapy can be associated increased risk bleeding. Here, we present data on identification, humanization, vitro pharmacology antidote dabigatran (aDabi-Fab). The X-ray crystal structure complex reveals many structural similarities recognition compared thrombin. By tighter network interactions, achieves affinity that ~350 times stronger than its Despite mode binding, does not bind known substrates has no activity coagulation tests or platelet aggregation. In addition demonstrate rapidly reversed vivo rat model anticoagulation. This first report specific next-generation may become valuable tool who require emergency procedures.