Ticagrelor: A Novel Player in the field of Anti-Platelet Therapy

Abstract

Anti-platelet therapy has long been proven to be of clinical benefit for both the treatment and prevention of acute coronary syndromes (ACS). Although clopidogrel has continued to dominate the field as a potent anti-platelet agent, several new oral and intravenous P2Y12 inhibitors are under development to overcome the current limitations of clopidogrel therapy (slow onset, low level of inhibition, interindividual variability). Ticagrelor (Brilinta) is a novel, selective, orally active, reversible P2Y12 purinoceptor antagonist that belongs to a novel class of compounds called cyclopentyltriazolopyrimidine inhibitors. Unlike thienopyridines, ticagrelor does not require conversion to an active metabolite. Compared with clopidogrel, ticagrelor produces a greater and more consistent inhibition of ADP-induced platelet aggregation. Its rapid onset of action has the potential to improve outcomes for patients with acute coronary syndromes, and its reversibility may offer advantages to patients needing surgery after initiating anti-platelet therapy. Preliminary investigations in early-phase clinical trials have demonstrated ticagrelor to be characterized by a rapid, greater and consistent anti-platelet effect with a favorable safety profile. Recently concluded pivotal phase III (PLATO) trial have shown ticagrelor to be more effective in preventing ischemic events in acute coronary syndrome patients without an increased risk of protocol-defined major bleeding, but with an increase in the rate of non procedure-related bleeding, compared with currently recommended treatment regimens. This contribution provides a comprehensive review of ticagrelor, as a valuable option for the prevention of ischemic events, with the results from large-scale, randomized trials as its vivid backdrop.