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血小板 P2Y₁₂ 受体抑制:临床药物研发的最新进展。

Platelet P2Y₁₂ receptor inhibition: an update on clinical drug development.

机构信息

Division of Cardiology, University of Florida College of Medicine, Jacksonville, Florida 32209, USA.

出版信息

Am J Cardiovasc Drugs. 2010;10(4):217-26. doi: 10.2165/11537670-000000000-00000.

DOI:10.2165/11537670-000000000-00000
PMID:20653328
Abstract

Antiplatelet therapy is the cornerstone of treatment for patients with coronary artery disease. Since adenosine diphosphate (ADP) represents one of the most important mediators of thrombosis, the inhibition of the platelet ADP receptor, in particular the P2Y₁₂ subtype, plays a pivotal role in secondary prevention of recurrent atherothrombotic events in high-risk settings. Numerous clinical trials have shown the efficacy of clopidogrel, an inhibitor of the ADP P2Y₁₂ receptor, in patients presenting with an acute coronary syndrome and undergoing percutaneous coronary intervention. However, laboratory and clinical experience with clopidogrel have led to understanding some of the limitations of this drug, the most important of which is its broad range in interindividual response variability, resulting in the development of novel ADP P2Y₁₂ receptor-inhibiting strategies. This article provides an overview of ADP P2Y₁₂ receptor-inhibiting strategies, including high clopidogrel dosing regimens and novel agents under advanced clinical development.

摘要

抗血小板治疗是冠心病患者治疗的基石。由于二磷酸腺苷(ADP)是血栓形成的最重要介质之一,因此抑制血小板 ADP 受体,特别是 P2Y₁₂ 亚型,在高危环境中对预防复发性动脉粥样血栓事件起着关键作用。许多临床试验表明,在急性冠状动脉综合征患者和经皮冠状动脉介入治疗患者中,ADP P2Y₁₂ 受体抑制剂氯吡格雷具有疗效。然而,氯吡格雷的实验室和临床经验使人们了解到该药物的一些局限性,其中最重要的是其在个体间反应变异性方面的广泛范围,导致了新型 ADP P2Y₁₂ 受体抑制策略的发展。本文概述了 ADP P2Y₁₂ 受体抑制策略,包括高剂量氯吡格雷方案和处于临床开发后期的新型药物。

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