Development of a Novel Oral Anticoagulant with Minimal Bleeding Risk

静脉或动脉中形成血栓是一种非常严重的疾病，仅在英国每年就导致22.5万人死亡。抗凝血剂是用来预防或治疗血栓的。心脏节律异常的患者[房颤(AF)]出现脑部血栓(中风)的可能性是后者的5倍。华法林是一种抗凝剂，可以将这种中风的高风险降低%。然而，华法林是一种难以管理的药物，因为它需要每月抽血进行监测，以确保体内药物的正确水平。此外，华法林有可能导致每100名服用该药物的患者中有3人大出血，其中1/8会死亡。最近，一种新药dabigatran已被批准长期用于治疗房颤患者。这种新药的好处是，患者不再需要用血样进行监测。然而，所有现有的抗凝药物和正在开发的新药物都有一个问题，那就是它们仍然具有非常高的出血风险。在这项提案中，我们第一次开发了一种新的抗凝药物，这种药物不需要监测，使用时不太可能导致出血。如果我们成功了，这将有可能改变抗凝治疗，提高患者的生活质量，并通过不必治疗出血并发症来节省患者医疗保健成本。

The generation of a blood clot in a vein or artery is a very serious condition, ultimately causing 225,000 deaths per year in the UK alone. Anticoagulants are prescribed to prevent or treat blood clots. Patients that have an abnormal heart rhythm [atrial fibrillation (AF)] are 5 times more likely to have a blood clot in the brain (stroke). Warfarin, an anticoagulant drug, can reduce this high risk of stroke by 64%. However, warfarin is a difficult drug to administer as it needs to be monitored with a blood sample every month to ensure the correct level of drug is in the body. Furthermore, warfarin carries a risk of causing major bleeding for up to 3 in 100 patients taking the drug of which 1 in 8 will die. Recently a new drug, dabigatran has been approved for long term use to treat patients with AF. The benefit of this new drug is that patients no longer need to be monitored with a blood sample. However, one problem that all existing anticoagulant drugs and the new ones that are being developed have is that they still carry a very high risk of bleeding. In this proposal, we are developing for the first time a new anticoagulant drug that will not need monitoring and is not likely to result in bleeding when used. If we are successful, this has the potential to transform anticoagulation treatment, improve patient quality of life and make large savings to the cost of patient healthcare through not having to treat bleeding complications.