The future of P2Y12 receptor antagonists

Platelet P2Y12 inhibitors have become a central component of the treatment strategy for patients with atherothrombosis due to the importance of platelet P2Y12 receptors in arterial thrombosis. P2Y12 inhibitors effectively reduce the risk of adverse cardiovascular events in patients with acute coronary syndromes (ACS) and patients undergoing percutaneous coronary intervention (PCI). However, despite this, patients with ACS continue to suffer from recurrent atherothrombosis and an increased risk of mortality. In addition, P2Y12 inhibitors increase the risk of bleeding, thereby limiting their clinical benefit. It is therefore clear that further optimizations are needed in the pharmacology and treatment strategies of P2Y12 inhibitors. The objective of these optimizations is to maximize cardiovascular benefit whilst minimizing adverse effects on haemostasis. This review article summarizes the most successful recent strategies in P2Y12 inhibition in order to identify the optimizations and developments that are most likely to be successful in the future.