USE OF A FACTOR XA INHIBITOR FOR TREATING AND PREVENTING BLEEDING EVENTS AND RELATED DISORDERS IN PATIENTS HAVING SENSITIVITY TO VITAMIN K ANTAGONISTS USED AS ANTICOAGULANTS
WALKER, JOSEPH RAY, JR.,沃克 乔瑟夫 雷 二世,沃克 喬瑟夫 雷 二世,VANDELL, ALEXANDER GENE,范德 亚利山大 琴,范德 亞利山大 琴
申请号：
TW104110558
公开号：
TW201620516A
申请日:
2015.03.31
申请国别(地区):
TW
年份:
2016
代理人:
摘要：
The invention provides methods of treating or preventing bleeding events or over- anticoagulation in a subject in need thereof who is identified as having sensitivity to a vitamin K antagonist such as warfarin by administering to the subject a therapeutically effective amount of an FXa inhibitor, which can be a direct or indirect FXa inhibitor, or a warfarin or VKA alternative drug or compound. The direct FXa inhibitor can be the small molecule edoxaban p-toluenesulfonate monohydrate, edoxaban, or a pharmaceutically acceptable salt and/or hydrate thereof. In aspects, the subject is identified as having one or more genetic polymorphisms in genes CYP2C9 and/or VKORC1 resulting in loss of function, reduction in function, or aberrant function of these genes and/or their protein products, and sensitivity to warfarin. The invention provides methods of administering an FXa inhibitor or warfarin alternative to safely and effectively reduce, prevent, reduce the risk of, prevent the recurrence of, or prevent the risk of recurrence of, conditions such as embolism, thrombosis, thromboembolism, etc. in a subject who is in need of anticoagulant therapy and who is identified as having one or more genetic polymorphisms resulting in warfarin sensitivity.本發明提供藉由向有需要之個體投與治療有效量之FXa抑制劑或殺鼠靈(warfarin)或VKA替代藥物或化合物來治療或預防該個體之出血現象或過度抗凝血的方法,該個體鑑別為對維生素K拮抗劑(例如殺鼠靈)具有感受性,該FXa抑制劑可為直接或間接FXa抑制劑。該直接FXa抑制劑可為小分子依杜沙班(edoxaban)對甲苯磺酸鹽單水合物、依杜沙班或其醫藥上可接受之鹽及/或水合物。在態樣中,該個體鑑別為具有基因CYP2C9及/或VKORC1中之一或多種遺傳多型性,其引起該等基因及/或其蛋白產物之功能損失、功能降低或異常功能及對殺鼠靈之感受性。本發明提供投與FXa抑制劑或殺鼠靈替代物以安全且有效地減輕、預防個體諸如栓塞、血栓形成、血栓栓塞等病況、降低該等病況之風險、預防其復發或預防其復發之風險的方法,該個體需要抗凝血療法且鑑別為具有一或多種引起殺鼠靈感受性之遺傳多型性。
