摘要
抗凝血药是预防和治疗血栓栓塞性疾病的基石。现有的肠外和口服抗凝血药通过干扰凝血级联反应的关键环节,实现了对血栓的有效控制,但同时也伴随着出血风险的增加。以凝血因子Ⅺ(FⅪ)为靶点的抗凝血药--FⅪ抑制剂可通过抑制FⅪ来阻断凝血酶生成过程中的扩增阶段,减少血栓生成,且对正常止血作用的影响较小,已成为最有潜力的新型抗凝血药之一。目前尚无上市的FⅪ抑制剂类药物,而处于Ⅱ期或Ⅲ期临床试验阶段的FⅪ抑制剂包括3类--反义寡核苷酸、单克隆抗体和小分子抑制剂。另外,靶向FⅪ的天然抑制剂和核酸适配体大多正在进行临床前研发。作为抗凝治疗的新靶点药物,FⅪ抑制剂有望成为更安全、有效的治疗选择,弥补当前抗凝血药的局限性,在减少出血风险的同时为患者提供更有效的血栓预防和治疗方案。
Anticoagulants are the cornerstone of the prevention and treatment of thromboembolic diseases.Existing parenteral and oral anticoagulants achieve effective control of thrombosis by interfering with key aspects of the coagulation cascade reaction,but this is accompanied by an increased risk of bleeding.FⅪinhibitors,anticoagulants targeting coagulation factorⅪ(FⅪ),can block the amplification phase of the thrombin generation process by inhibiting FⅪ,reducing thrombogenesis with less impact on normal hemostatic effects,and have become one of the most promising new anticoagulants.There are currently no marketed FⅪinhibitor drugs,while FⅪinhibitors in phaseⅡor phaseⅢclinical trials include 3 classes:antisense oligonucleotide,monoclonal antibody and small molecule inhibitors.In addition,most of the natural inhibitors and nucleic acid aptamers targeting FⅪare under preclinical development.As new target drugs for anticoagulation therapy,FⅪinhibitors are expected to become a safer and more effective therapeutic option,compensating for the limitations of current anticoagulants and providing patients with more effective thromboprophylaxis and therapeutic options while reducing the risk of bleeding.
作者
苑新文
赵振宇
YUAN Xinwen;ZHAO Zhenyu(Dept.of Pharmacy,Tianjin Xiqing Hospital,Tianjin 300380,China;NHC Key Laboratory of Hormones and Development,Tianjin Medical University Chu Hsien-I Memorial Hospital,Tianjin Institute of Endocrinology/Tianjin Key Laboratory of Metabolic Diseases,Tianjin 300134,China)
出处
《中国药房》
CAS
北大核心
2024年第17期2165-2170,共6页
China Pharmacy
基金
天津市医学重点学科建设项目(No.TJYXZDXK032A)。
