Testa L, Biondi Zoccai G G L, Valgimigli M, Latini R A, Pizzocri S, Lanotte S, Laudisa M L, Brambilla N, Ward M R, Figtree G A, Bedogni F, Bhindi R
Interventional Cardiology Department, St. Ambrogio Clinical Institute, 20149, Milan, Italy.
Adv Hematol. 2010;2010:595934. doi: 10.1155/2010/595934. Epub 2010 Dec 5.
Thienopyridines are a class of drug targeting the platelet adenosine diphosphate (ADP) 2 receptor. They significantly reduce platelet activity and are therefore clinically beneficial in settings where platelet activation is a key pathophysiological feature, particularly myocardial infarction. Ticlopidine, the first of the class introduced to clinical practice, was soon challenged and almost completely replaced by clopidogrel for its better tolerability. More recently, prasugrel and ticagrelor have been shown to provide a more powerful antiplatelet action compared to clopidogrel but at a cost of higher risk of bleeding complications. Cangrelor, a molecule very similar to ticagrelor, is currently being evaluated against clopidogrel. Considering the key balance of ischemic protection and bleeding risk, this paper discusses the background to the development of prasugrel, ticagrelor, and cangrelor and aims to characterise their risk-benefit profile and possible implementation in daily practice.
噻吩并吡啶类是一类作用于血小板二磷酸腺苷（ADP）2受体的药物。它们能显著降低血小板活性，因此在血小板活化是关键病理生理特征的情况下，尤其是心肌梗死，具有临床益处。噻氯匹定是该类药物中首个应用于临床实践的药物，但因其耐受性较差，很快受到挑战并几乎完全被氯吡格雷取代。最近，与氯吡格雷相比，普拉格雷和替格瑞洛已显示出更强的抗血小板作用，但代价是出血并发症风险更高。坎格雷洛是一种与替格瑞洛非常相似的分子，目前正在与氯吡格雷进行对比评估。考虑到缺血性保护与出血风险之间的关键平衡，本文讨论了普拉格雷、替格瑞洛和坎格雷洛的研发背景，旨在描述它们的风险效益概况以及在日常实践中的可能应用。
