Adenosine-Mediated Effects of Ticagrelor Evidence and Potential Clinical Relevance

This review constitutes a critical evaluation of recent publications that have described an additional mode of action of the P2Y(12) receptor antagonist ticagrelor. The effect is mediated by inhibition of the adenosine transporter ENT1 (type 1 equilibrative nucleoside transporter), which provides protection for adenosine from intracellular metabolism, thus increasing its concentration and biological activity, particularly at sites of ischemia and tissue injury where it is formed. Understanding the mode of action of ticagrelor is of particular interest given that its clinical profile, both in terms of efficacy and adverse events, differs from that of thienopyridine P2Y(12) antagonists. (c) 2014 by the American College of Cardiology Foundation