Clinical profile of prasugrel, a novel thienopyridine

被引：41

作者：

Angiolillo, Dominick J. ^{[1
]}

Bates, Eric R. ^{[2
]}

Bass, Theodore A. ^{[1
]}

机构：

[1] Univ Florida, Coll Med, Div Cardiol, Jacksonville, FL USA

[2] Univ Michigan, Div Cardiol, Ann Arbor, MI 48109 USA

来源：

AMERICAN HEART JOURNAL | 2008年 / 156卷 / 02期

关键词：

D O I：

10.1016/j.ahj.2008.06.005

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Prasugrel (CS-747; LY-640315) is a novel, third-generation oral thienopyridine that is a specific, irreversible antagonist of the platelet adenosine 5'-diphosphate P2Y(12) receptor. Laboratory results with prasugrel support more potent antiplatelet effects, a lower incidence of interpatient variability in antiplatelet response, and a reduced time to onset of antiplatelet activity compared with clopidogrel. Phase II results indicate that prasugrel produces a greater antiplatelet effect than clopidogrel administered even at doses higher than the currently approved 300-mg loading dose and 75-mg/d maintenance dose. Recent phase III data show that prasugrel is superior to clopidogrel in preventing ischemic events in patients with acute coronary syndrome undergoing percutaneous coronary intervention, although this was associated with a greater risk of bleeding.

引用

页码：S16 / S22

页数：7

共 15 条

[1] Randomized comparison of a high clopidogrel maintenance dose in patients with diabetes mellitus and coronary artery disease - Results of the Optimizing antiPlatelet Therapy In diabetes MellitUS (OPTIMUS) study [J].

Angiolillo, Dominick J. ;

Shoemaker, Steven B. ;

Desai, Bhaloo ;

Yuan, Hang ;

Charlton, Ronald K. ;

Bernardo, Esther ;

Zenni, Martin M. ;

Guzman, Luis A. ;

Bass, Theodore A. ;

Costa, Marco A. .

CIRCULATION, 2007, 115 (06) :708-716

[2] A comparison of prasugrel and clopidogrel loading doses on platelet function: magnitude of platelet inhibition is related to active metabolite formation [J].

Brandt, John T. ;

Payne, Christopher D. ;

Wiviott, Stephen D. ;

Weerakkody, Govinda ;

Farid, Nagy A. ;

Small, David S. ;

Jaknbowski, Joseph A. ;

Naganuma, Hideo ;

Winters, Kenneth J. .

AMERICAN HEART JOURNAL, 2007, 153 (01) :66.e9-66.e16

[3] A comparison of the antiplatelet effects of prasugrel and high-dose clopidogrel as assessed by VASP-phosphorylation and light transmission aggregometry [J].

Jakubowski, Joseph A. ;

Payne, Christopher D. ;

Li, Ying G. ;

Farid, Nagy A. ;

Brandt, John T. ;

Small, David S. ;

Salazar, Daniel E. ;

Winters, Kenneth J. .

THROMBOSIS AND HAEMOSTASIS, 2008, 99 (01) :215-222

[4] A multiple dose study of prasugrel (CS-747), a novel thienopyridine P2Y12 inhibitor, compared with clopidogrel in healthy humans [J].

Jakubowski, Joseph A. ;

Matsushima, Nobuko ;

Asai, Fumitoshi ;

Naganuma, Hideo ;

Brandt, John T. ;

Hirota, Takashi ;

Freestone, Stephen ;

Winters, Kenneth J. .

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 2007, 63 (04) :421-430

[5] Prasugrel achieves greater inhibition of platelet aggregation and a lower rate of non-responders compared with clopidogrel in aspirin-treated patients with stable coronary artery disease [J].

Jernberg, T ;

Payne, CD ;

Winters, KJ ;

Darstein, C ;

Brandt, JT ;

Jakubowski, JA ;

Naganuma, H ;

Siegbahn, A ;

Wallentin, L .

EUROPEAN HEART JOURNAL, 2006, 27 (10) :1166-1173

[6] The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrel's active metabolite [J].

Sugidachi, A. ;

Ogawa, T. ;

Kurihara, A. ;

Hagihara, K. ;

Jakubowski, J. A. ;

Hashimoto, M. ;

Niitsu, Y. ;

Asai, F. .

JOURNAL OF THROMBOSIS AND HAEMOSTASIS, 2007, 5 (07) :1545-1551

[7]

Varenhorst C, 2007, EUR HEART J, V28, P189

[8] A double-blind, randomized study on platelet aggregation in patients treated with a daily dose of 150 or 75 mg of clopidogrel for 30 days [J].

Von Beckerath, Nicolas ;

Kastrati, Adnan ;

Wieczorek, Anna ;

Pogatsa-Murray, Gisela ;

Sibbing, Dirk ;

Graf, Isolde ;

Schoemig, Albert .

EUROPEAN HEART JOURNAL, 2007, 28 (15) :1814-1819

[9] Prasugrel achieves greater and faster P2Y12 receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite in aspirin-treated patients with coronary artery disease [J].

Wallentin, Lars ;

Varenhorst, Christoph ;

James, Stefan ;

Erlinge, David ;

Braun, Oscar Oe ;

Jakubowski, Joseph A. ;

Sugidachi, Atsuhiro ;

Winters, Kenneth J. ;

Siegbahn, Agneta .

EUROPEAN HEART JOURNAL, 2008, 29 (01) :21-30

[10]

Winters KJ, 2007, EUR HEART J, V28, P218

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