Ticagrelor: The First Reversibly Binding Oral P2Y12 Receptor Antagonist

  title={Ticagrelor: The First Reversibly Binding Oral P2Y12 Receptor Antagonist},
  author={Steen Husted and J. J. J. van Giezen},
  booktitle={Cardiovascular therapeutics},
Ticagrelor (AZD6140) is the first reversibly binding oral P2Y(12) receptor antagonist that blocks ADP-induced platelet aggregation. Unlike thienopyridines, which irreversibly bind to the P2Y(12) receptor for the lifetime of the platelet, ticagrelor binds reversibly to the receptor and exhibits rapid onset and offset of effect, which closely follow drug exposure levels. Animal models indicate greater separation between antithrombotic effects and bleeding effects with ticagrelor than with… CONTINUE READING