By Stan Heptinstall B.Sc., Ph.D. (auth.), Albert Ferro, David A. Garcia (eds.)
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Extra info for Antiplatelet and Anticoagulation Therapy
Agents that act as antagonists at the EP3 receptor on platelets provide a potential new approach to antithrombotic therapy. Conflicts of Interest Stan Heptinstall on behalf of the University of Nottingham has received research grants for laboratory investigations on the P2Y12 antagonists clopidogrel, prasugrel, ticagrelor and cangrelor and the EP3 antagonist DG-041. He is also a shareholder and director of Platelet Solutions Ltd, a spinout company of the University of Nottingham that engages in platelet function testing.
Unlike clopidogrel and prasugrel the inhibition is reversible rather than irreversible, which means that the drug can come off the receptor when treatment is curtailed and platelet function can be restored. However, in actuality, this reversal of inhibition is quite slow (see below). Like clopidogrel and prasugrel, ticagrelor does have an active metabolite but this is present in lower quantities than the parent drug and it appears to act in an identical manner to the parent drug . There have been a number of studies in which the pharmacological effects of ticagrelor have been compared with those of clopidogrel.
Circulation. 2011;123:1891–9. 78. Firbas C, Siller-Matula JM, Jilma B. Targeting von willebrand factor and platelet glycoprotein Ib receptor. Expert Rev Cardiovasc Ther. 2010;8:1689–701. 79. Heptinstall S, Espinosa DI, Manolopoulos P, Glenn JR, White AE, Johnson A, Dovlatova N, Fox SC, May JA, Hermann D, Magnusson O, Stefansson K, Hartman D, Gurney M. DG-041 inhibits the EP3 prostanoid receptor--a new target for inhibition of platelet function in atherothrombotic disease. Platelets. 2008;19:605–13.