{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,4]],"date-time":"2026-10-04T02:44:11Z","timestamp":1791081851004,"version":"4.1.0"},"reference-count":33,"publisher":"Wiley","issue":"1","license":[{"start":{"date-parts":[[2013,4,12]],"date-time":"2013-04-12T00:00:00Z","timestamp":1365724800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["British J Pharmacology"],"published-print":{"date-parts":[[2013,5]]},"abstract":"<jats:sec><jats:title>Background and Purpose<\/jats:title><jats:p>Prasugrel is a third\u2010generation thienopyridine prodrug and ticagrelor is a non\u2010competitive <jats:styled-content style=\"fixed-case\">P2Y<jats:sub>12<\/jats:sub><\/jats:styled-content> receptor antagonist. In their phase 3 studies, both agents reduced rates of ischemic events relative to treatment with clopidogrel.<\/jats:p><\/jats:sec><jats:sec><jats:title>Experimental Approach<\/jats:title><jats:p>The pharmacodynamic profile of anti\u2010platelet effects of prasugrel was compared with that of ticagrelor in rats.<\/jats:p><\/jats:sec><jats:sec><jats:title>Key Results<\/jats:title><jats:p>The active metabolite of prasugrel was less potent than ticagrelor and its active metabolite on platelet aggregation <jats:italic>in vitro<\/jats:italic>. In contrast, prasugrel was a more potent antiplatelet agent than ticagrelor on <jats:italic>ex vivo<\/jats:italic> platelet aggregation: their <jats:styled-content style=\"fixed-case\">ED<\/jats:styled-content><jats:sub>50<\/jats:sub> values at peak for <jats:styled-content style=\"fixed-case\">ADP<\/jats:styled-content> 20\u2009\u03bcmol\u00b7L<jats:sup>\u22121<\/jats:sup> were 1.9 and 8.0\u2009mg\u00b7kg<jats:sup>\u22121<\/jats:sup>, respectively. Prasugrel's inhibition of platelet aggregation was maintained for up to 24\u2009h after administration, but ticagrelor's duration of action was substantially shorter. Prasugrel and ticagrelor significantly inhibited thrombus formation with <jats:styled-content style=\"fixed-case\">ED<\/jats:styled-content><jats:sub>50<\/jats:sub> values of 1.8 and 7.7\u2009mg\u00b7kg<jats:sup>\u22121<\/jats:sup>, respectively. Both agents also prolonged bleeding times (<jats:styled-content style=\"fixed-case\">ED<\/jats:styled-content><jats:sub>200<\/jats:sub> values of 3.0 and 13\u2009mg\u00b7kg<jats:sup>\u22121<\/jats:sup> respectively) suggesting that at equivalent levels of inhibition of platelet aggregation, the agents would show comparable antithrombotic activity with similar bleeding risk. Platelet transfusion significantly increased blood platelet numbers similarly in prasugrel\u2010 and ticagrelor\u2010treated rats. In the prasugrel\u2010treated group, platelet transfusion caused significant shortening of bleeding time, while in the ticagrelor\u2010treated group, platelet transfusion showed no influence on bleeding time under the experimental conditions employed.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusions and Implications<\/jats:title><jats:p>Prasugrel and ticagrelor showed several differences in their pharmacological profiles and these disparities may reflect their differing reversibility and\/or pharmacokinetic profiles.<\/jats:p><\/jats:sec>","DOI":"10.1111\/bph.12108","type":"journal-article","created":{"date-parts":[[2013,1,24]],"date-time":"2013-01-24T18:35:08Z","timestamp":1359052508000},"page":"82-89","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":32,"title":["A comparison of the pharmacological profiles of prasugrel and ticagrelor assessed by platelet aggregation, thrombus formation and haemostasis in rats"],"prefix":"10.1111","volume":"169","author":[{"given":"A","family":"Sugidachi","sequence":"first","affiliation":[{"name":"Biological Research Laboratories Daiichi Sankyo, Co., Ltd.  Tokyo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"K","family":"Ohno","sequence":"additional","affiliation":[{"name":"Biological Research Laboratories Daiichi Sankyo, Co., Ltd.  Tokyo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"T","family":"Ogawa","sequence":"additional","affiliation":[{"name":"Biological Research Laboratories Daiichi Sankyo, Co., Ltd.  Tokyo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"JA","family":"Jakubowski","sequence":"additional","affiliation":[{"name":"Lilly Research Laboratories Eli Lilly and Company  Indianapolis IN USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M","family":"Hashimoto","sequence":"additional","affiliation":[{"name":"Frontier Research Laboratories Daiichi Sankyo, Co., Ltd.  Tokyo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"A","family":"Tomizawa","sequence":"additional","affiliation":[{"name":"Biological Research Laboratories Daiichi Sankyo, Co., Ltd.  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