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 P2Y12 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 P2Y12 antagonists.
Unità di Medicina 3, Ospedale San Paolo, Dipartimento di Scienze della Salute, Università degli Studi di Milano, Milan, Italy. Electronic address: marco.cattaneo@unimi.it.
Marco
M
Cattaneo
Institute of Physiology, Justus-Liebig University Giessen, Giessen, Germany.
Rainer
R
Schulz
AstraZeneca Research and Development, Mölndal, Sweden.
Sven
S
Nylander
D054058:Acute Coronary Syndrome / Q000188:drug therapy* / Q000378:metabolism; D000241:Adenosine / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000627:therapeutic use; D006801:Humans; D058921:Purinergic P2Y Receptor Antagonists / Q000627:therapeutic use*; D000077486:Ticagrelor; D016896:Treatment Outcome
D058921:Purinergic P2Y Receptor Antagonists; D000077486:Ticagrelor; D000241:Adenosine
P2Y(12); acute coronary syndrome(s); adenosine; antiplatelet agents; ticagrelor