摘要
静脉血栓形成及栓塞是严重危害人类健康的疾病,是继急性冠脉综合征与脑卒中之后第三大心血管疾病。随着对凝血与血栓形成机制、静脉栓塞发病机制,及普通肝素、低相对分子质量肝素、华法林等传统用药研究与了解的进一步深入,以凝血因子靶点Ⅹa、Ⅱa、Ⅸa,以及Ⅲ(TF)/Ⅶa特异性抑制为基础的新抗凝药物研发取得了很大进展。同时,理想的抗凝药物标准为新型药物研发提出了更高的要求,靶点选择、获益与风险、效应与毒性评价等许多问题更值得关注。综述静脉血栓形成原因与机制,传统用药,以及新药研发靶点与研发进展、研发注意事项。
Venous thromboembolism （VTE） has been estimated to be the third most common vascular disorder after acute coronary syndromes and stroke, with a serious health hazard, resulting in high mortality, morbidity, and expenditures. With further understanding on the mechanism for blood coagulation, thrombosis, VTE, and application of classic anticoagulant drugs such as unfractionated heparin, low molecular heparin, and Warfarin, the novel anticoagulants based on coagulation factor-target e.g. Ⅹ a,Ⅱ a, Ⅸa, and TF/Ⅶa had markedly progressed in research and development. While, the ideal standard of anticoagulant drugs makes higher request for research and development of novel anticoagulants, the selection to target, benefit and risk, evaluation for effication and toxicity merit more attention. The aetiology and pathogenesis of VTE, classic anticoagulant drugs, and new trends and cautions of research and development in the novel anticoagulant drugs are reviewed in this paper.
出处
《现代药物与临床》
CAS
2011年第1期10-24,共15页
Drugs & Clinic
基金
系列化
国际化的国家生物医药国际创新园新药研发综合性大平台建设项目(2009ZⅩ09301-008)
关键词
血栓形成
静脉血栓栓塞
发病机制
抗凝药物
靶点
thrombosis
venous thromboembolism （VTE）
pathogenesis
anticoagulant drug
target
