摘 要：靜脈血栓形成及栓塞是嚴(yán)重危害人類健康的疾病，是繼急性冠脈綜合征與腦卒中之后第三大心血管疾病。隨著對(duì)凝血與血栓形成機(jī)制、靜脈栓塞發(fā)病機(jī)制，及普通肝素、低相對(duì)分子質(zhì)量肝素、華法林等傳統(tǒng)用藥研究與了解的進(jìn)一步深入，以凝血因子靶點(diǎn)Ⅹa、Ⅱa、Ⅸa，以及Ⅲ（TF）/Ⅶa特異性抑制為基礎(chǔ)的新抗凝藥物研發(fā)取得了很大進(jìn)展。同時(shí)，理想的抗凝藥物標(biāo)準(zhǔn)為新型藥物研發(fā)提出了更高的要求，靶點(diǎn)選擇、獲益與風(fēng)險(xiǎn)、效應(yīng)與毒性評(píng)價(jià)等許多問(wèn)題更值得關(guān)注。綜述靜脈血栓形成原因與機(jī)制，傳統(tǒng)用藥，以及新藥研發(fā)靶點(diǎn)與研發(fā)進(jìn)展、研發(fā)注意事項(xiàng)。

Abstract：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. Ⅹa, Ⅱa, 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.

系列化、國(guó)際化的國(guó)家生物醫(yī)藥國(guó)際創(chuàng)新園新藥研發(fā)綜合性大平臺(tái)建設(shè)項(xiàng)目（2009ZⅩ09301-008）