Abstract
Platelets participate centrally in atherothrombosis, resulting in vessel occlusion and ischaemia. Consequently, optimisation of antiplatelet regimens has the potential to further reduce the residual burden of morbidity and mortality associated with atherosclerosis. Ticagrelor is a potent oral platelet P2Y12 receptor antagonist that (1) inhibits a central amplification pathway of platelet activation directly as well as via an active metabolite, (2) has a rapid onset and offset of antiplatelet action that remains consistent in the circulation during twice-daily administration and is amenable to reversal, (3) has inverse agonist properties, and (4) demonstrates pleiotropic effects that contribute to anti-thrombotic, anti-inflammatory and vasodilatory properties. These advantageous characteristics of ticagrelor have translated to beneficial clinical outcomes in patients with acute coronary syndromes or ischaemic stroke, during prolonged maintenance therapy in specific high-risk populations, and following percutaneous coronary intervention but not definitively following coronary artery bypass graft surgery or in peripheral artery disease patients. Novel innovative strategies aim to reduce the risk of bleeding during dual antiplatelet therapy via shortening the duration of treatment and replacing the standard-of-care with ticagrelor monotherapy. In cases where aspirin is an essential component in secondary prevention, dose modification when combined with ticagrelor may hypothetically provide desirable clinical outcomes following appropriate clinical assessment as predicted by pharmacological studies. Overall, the future management of acute coronary syndromes could potentially involve the dichotomisation of antithrombotic therapies, whereby only those with high-risk of ischaemia, without a high-risk of bleeding, receive ticagrelor plus very-low-dose aspirin, while ticagrelor monotherapy is administered to the remaining majority.
Highlights
The formation of atherosclerotic plaques increases the risk of arterial thrombosis that can result in vascular occlusion and subsequently ischaemia or infarction of the distal tissue
In an exploratory analysis featuring a composite of irreversible and harmful outcomes, there was no significant difference between the ticagrelor and placebo treatment groups (10.1% vs. 10.8%; Hazard ratio (HR), 0.93; 95% confidence interval (CI) 0.86– 1.02), leading the authors to conclude that ticagrelor plus aspirin may not be an acceptable form of secondary prevention of ischaemic events in this population, due to the poor benefit-to-risk ratio
The results showed that the primary endpoint occurred significantly less frequently during ticagrelor monotherapy than dual antiplatelet therapy (DAPT) (4.0% [monotherapy] vs. 7.1% [DAPT]; HR, 0.56; 95% CI 0.45– 0.68; P < 0.001) without evidence for a difference in the key secondary endpoint (3.9% vs. 3.9%; HR, 0.99; 95% CI 0.78– 1.25; P < 0.001)
Summary
The formation of atherosclerotic plaques increases the risk of arterial thrombosis that can result in vascular occlusion and subsequently ischaemia or infarction of the distal tissue. Ticagrelor provides several hypothetical and pharmacological advantages over aspirin and other oral P2Y12 inhibitors that have the potential to optimise patient outcomes in novel antiplatelet strategies by reducing the risk of ischaemia in DAPT or reducing the risk of bleeding as a monotherapy [9, 10]. These strategies may be extended to benefit patients with other atherosclerotic conditions, such as ischaemic stroke and peripheral artery disease (PAD). This review aims to summarise pharmacological and clinical characteristics of ticagrelor and highlight the latest guidelines, developments and future potential in clinical practice
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