
Chinese General Practice ›› 2025, Vol. 28 ›› Issue (03): 379-384.DOI: 10.12114/j.issn.1007-9572.2024.0046
• Precision Medication • Previous Articles
Received:2024-01-10
Revised:2024-03-25
Published:2025-01-20
Online:2024-10-28
Contact:
ZHANG Fengjiang
通讯作者:
张冯江
作者简介:作者贡献:
陈越秀负责文章的构思与设计、研究资料的收集与整理、绘制表格、论文撰写;姚媛媛、孙大伟、唐志峰负责论文修订;王颖、吴超敏、赵麟茜负责研究资料的收集与整理;张冯江负责文章的构思与设计、论文修订、文章的质量控制及审校,对文章整体负责、监督管理。
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URL: https://www.chinagp.net/EN/10.12114/j.issn.1007-9572.2024.0046
| FⅪ抑制剂 | ASOs | mAb | 小分子 | 天然抑制物 | 核酸适配体 |
|---|---|---|---|---|---|
| 作用机制 | 结合/破坏mRNA,减少肝脏中FⅪ的生成 | 抑制FⅪa的生成/活性 | 阻断FⅪa的活性位点 | 阻断FⅪa活性位点 | 抑制FⅪa的活性 |
| 代表药物 | Fesomersen(IONIS-Ⅺ-LRX、FⅪ-LICA),INOIS FⅪ Rx(BAY2306001、ISIS-416858) | Osocimab(BAY 1213790),Abelacimab(MAA868),Gruticibart(Xisomab/AB203),MK-2060,BAY 1831865 | Milvexian(BMS-986177、JNJ-70033093),Asundexian(BAY 2433334),SHR2285 | Ir-CPI | FELIAP,12.7,11.16 |
| 给药途径 | 皮下注射 | 静脉/皮下注射 | 口服/静脉注射 | 静脉注射 | 静脉/皮下注射 |
| 起效时间 | 数周 | 数小时~数天 | 数分钟~数小时 | 数分钟 | 数分钟~数小时 |
| 作用时间 | 数周 | 数周~数月 | 数分钟~数小时 | 数小时 | 数分钟~数小时 |
| 用药频率 | 每周至每月 | 每月 | 每天 | 每天 | 每天 |
| 经肾清除 | 否 | 否 | 是 | 不确定 | 否 |
| 经肝代谢 | 否 | 否 | 是 | 否 | 否 |
Table 1 Pharmacological properties of FⅪ inhibitors
| FⅪ抑制剂 | ASOs | mAb | 小分子 | 天然抑制物 | 核酸适配体 |
|---|---|---|---|---|---|
| 作用机制 | 结合/破坏mRNA,减少肝脏中FⅪ的生成 | 抑制FⅪa的生成/活性 | 阻断FⅪa的活性位点 | 阻断FⅪa活性位点 | 抑制FⅪa的活性 |
| 代表药物 | Fesomersen(IONIS-Ⅺ-LRX、FⅪ-LICA),INOIS FⅪ Rx(BAY2306001、ISIS-416858) | Osocimab(BAY 1213790),Abelacimab(MAA868),Gruticibart(Xisomab/AB203),MK-2060,BAY 1831865 | Milvexian(BMS-986177、JNJ-70033093),Asundexian(BAY 2433334),SHR2285 | Ir-CPI | FELIAP,12.7,11.16 |
| 给药途径 | 皮下注射 | 静脉/皮下注射 | 口服/静脉注射 | 静脉注射 | 静脉/皮下注射 |
| 起效时间 | 数周 | 数小时~数天 | 数分钟~数小时 | 数分钟 | 数分钟~数小时 |
| 作用时间 | 数周 | 数周~数月 | 数分钟~数小时 | 数小时 | 数分钟~数小时 |
| 用药频率 | 每周至每月 | 每月 | 每天 | 每天 | 每天 |
| 经肾清除 | 否 | 否 | 是 | 不确定 | 否 |
| 经肝代谢 | 否 | 否 | 是 | 否 | 否 |
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