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更新于：2026-07-09
Asundexian
更新于：2026-07-09
概要
基本信息
结构/序列
分子式C26H21ClF4N6O4 |
InChIKeyXYWIPYBIIRTJMM-IBGZPJMESA-N |
CAS号2064121-65-7 |
关联
13
项与 Asundexian 相关的临床试验CTIS2025-523677-41-00
(21174) Relative bioavailability study to investigate the pharmacokinetics of a single oral dose of asundexian administered as 50 mg pediatric formulation in comparison to 50 mg tablet (adult formulation) in fasted state and to investigate the effect of a high-fat, high-calorie meal on the 50 mg pediatric formulation in healthy adult participants
CTIS2023-509447-28-00
A study to learn about the amount of asundexian in the blood when healthy participants take different types of asundexian tablets
CTIS2023-509488-26-00
A study to learn how asundexian affects the amount of metformin in the blood when healthy participants take them together
100 项与 Asundexian 相关的临床结果
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100 项与 Asundexian 相关的转化医学
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100 项与 Asundexian 相关的专利（医药）
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77
项与 Asundexian 相关的文献（医药）2026-05-01ADVANCES IN THERAPY
Factor XI Inhibitors in Atrial Fibrillation: Insights and Implications from Recent Trials
Review
作者: McCarty, Owen J T ; Piatski, Marie E ; Malhotra, Aditya ; Seifer, Lukas ; Falama, Rosemary B ; Matsumoto, Lisa R ; Shatzel, Joseph J
Stroke prevention remains a cornerstone of the management of atrial fibrillation (AF) given the increased risk of thromboembolic events. While direct oral anticoagulants (DOACs) have significantly advanced stroke prophylaxis in AF, bleeding risks remain a challenge and preclude use in some populations. Furthermore, evidence indicates significant undertreatment in AF, with up to 40% of patients receiving incorrect anticoagulant dosing or no anticoagulation at all, further elevating their stroke risk. Novel anticoagulants targeting factor (F)XI are emerging as a promising alternative, offering the potential to reduce thromboembolic events whilst minimizing bleeding risks. Inhibitors under development include small molecules, monoclonal antibodies, and antisense oligonucleotides. These agents have demonstrated favorable safety profiles when compared to DOACs in early phase and some late phase trials. For example abelacimab, an anti-FXI monoclonal antibody, demonstrated superior safety with lower bleeding rates when compared to rivaroxaban in patients with AF. However, the efficacy of these drugs remains uncertain. However, the OCEANIC-AF trial, which studied the small molecule FXI inhibitor asundexian, was terminated early due to lack of efficacy as there was an increased rate of stroke and systematic embolism compared to the DOAC apixaban, raising new concerns about the utility of targeting FXI. However, many FXI inhibitors are currently undergoing phase 3 trials, and as such the true efficacy of the full class of FXI inhibitors remains to be elucidated. This review aims to provide a comprehensive synopsis of the landscape of FXI inhibitors in development for AF, their advantages, challenges, and known utility with a focus on how they may be applied to future anticoagulation therapy for AF.
2026-04-16NEW ENGLAND JOURNAL OF MEDICINE
Asundexian for Secondary Stroke Prevention
Article
作者: Staikov, Ivan ; Hirano, Teruyuki ; Turuspekova, Saule T. ; Amaya, Pablo ; Eikelboom, John W. ; Saver, Jeffrey L. ; Sampaio Silva, Gisele ; Neumann, Christoph ; Keller, Lars ; Veltkamp, Roland ; Lemmens, Robin ; Mundl, Hardi ; Campbell, Bruce C.V. ; Tsivgoulis, Georgios ; Zini, Andrea ; Masjuan, Jaime ; Shoamanesh, Ashkan ; Sylaja, P.N. ; Demchuk, Andrew M. ; Bereczki, Daniel ; Coutinho, Jonathan M. ; Leker, Ronen R. ; Knoflach, Michael ; Mikulik, Robert ; Hoo, Fan Kee ; Smith, Eric E. ; Matijošaitis, Vaidas ; Robinson, Thompson ; Ferro, José M. ; Lindgren, Arne G. ; Sandset, Else Charlotte ; Muehlhofer, Eva ; Heenan, Laura ; Putaala, Jukka ; Kasner, Scott E. ; Miglane, Evija ; Christensen, Hanne ; Sheth, Kevin N. ; Colorado, Pablo ; Lee, I-Hui ; Sharma, Mukul ; Kovar, Martin ; Joundi, Raed A. ; De Marchis, Gian Marco ; Slowik, Agnieszka ; van der Worp, H. Bart ; Xu, Lizhen ; Amarenco, Pierre ; Dong, Qiang ; Cordonnier, Charlotte ; Ozturk, Serefnur ; Schulze, Karleen ; Bae, Hee-Joon ; Turcani, Peter
BACKGROUND:
Patients with noncardioembolic ischemic stroke or transient ischemic attack (TIA) are at risk for recurrent stroke. Low factor XI levels are associated with a reduced risk of ischemic stroke. Asundexian inhibits activated factor XI. Whether the addition of asundexian to antiplatelet therapy would be superior to antiplatelet therapy alone for the secondary prevention of ischemic stroke is unclear.
METHODS:
In this phase 3, double-blind trial, we randomly assigned patients within 72 hours after the onset of a noncardioembolic ischemic stroke or high-risk TIA to receive asundexian (50 mg once daily) or placebo, in addition to planned dual or single antiplatelet therapy. Patients had at least one of the following: a nonlacunar infarct on imaging, a history of atherosclerosis, or evidence of atherosclerotic plaque at any location on cerebrovascular imaging. The primary efficacy outcome was ischemic stroke. The composite of death from cardiovascular causes, myocardial infarction, or stroke was a key secondary outcome. The primary safety outcome was major bleeding.
RESULTS:
Among 12,327 patients who underwent randomization (6162 to the asundexian group and 6165 to the placebo group), the incidence of ischemic stroke was lower in the asundexian group than in the placebo group (6.2% vs. 8.4%; cause-specific hazard ratio, 0.74; 95% confidence interval [CI], 0.65 to 0.84; P<0.001). The incidence of the composite of death from cardiovascular causes, myocardial infarction, or stroke was lower in the asundexian group than in the placebo group. The incidence of major bleeding was similar in the asundexian group and the placebo group (1.9% and 1.7%, respectively; cause-specific hazard ratio, 1.10; 95% CI, 0.85 to 1.44). The incidence of adverse events was 69.3% in the asundexian group and 70.1% in the placebo group; the incidence of serious adverse events was 19.2% and 19.5%, respectively.
CONCLUSIONS:
Among patients with noncardioembolic ischemic stroke or high-risk TIA treated with antiplatelet therapy, asundexian at a daily dose of 50 mg resulted in lower risks of ischemic stroke and major cardiovascular events than placebo, without a higher risk of major bleeding. (Funded by Bayer; OCEANIC-STROKE ClinicalTrials.gov number, NCT05686070.).
2026-04-01BIOORGANIC CHEMISTRY
Development of selective NBD-based fluorescent probes for in vitro detection of factor XIa and Thrombus imaging
Article
作者: Yang, Han ; Zou, Meijuan ; Li, Qing ; Zhou, Fengjiao ; Zhuang, Xinyu ; Zhao, Xingyu ; Li, Ruixing
Factor XIa (FXIa) is a promising target for safer anticoagulants. Herein, a series of NBD-based fluorescent probes (FNC2-FNC6) were developed by linking an FXIa inhibitor scaffold to an NBD fluorophore via alkyl chains of varying lengths. Molecular dynamics simulations revealed that shorter linkers, especially a two‑carbon chain, stabilize NBD binding in the FXIa pocket, enhancing fluorescence. Among these probes, FNC2 displayed potent FXIa inhibition (Ki = 14.2 nM) and selectivity over related proteases. It exhibited linear fluorescence increase upon FXIa binding (R2 = 0.9952; LOD = 1.19 μg/mL), enabling accurate quantification in immunoglobulin products (recovery: 94.41%-103.76%; RSD < 2%). FNC2 visualized FXIa in human plasma clots with 2.7-fold higher signal than free NBD, suppressed dose-dependently by asundexian. This structure-guided approach yields selective probes for FXIa detection and thrombus imaging.
100 项与 Asundexian 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 缺血性卒中 | 申请上市 | 中国 | 2026-04-30 | |
| 急性缺血性卒中 | 临床3期 | 美国 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 中国 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 日本 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 阿根廷 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 澳大利亚 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 奥地利 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 比利时 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 巴西 | 2023-01-26 | |
| 急性缺血性卒中 | 临床3期 | 保加利亚 | 2023-01-26 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 12,327 | Asundexian 50 mg once daily | 夢衊簾簾積窪簾鹹獵願(觸蓋繭網鬱齋選範範構) = 網範鑰願壓鏇膚鏇觸顧 築夢簾鏇選積製積鬱獵 (觸糧觸憲壓製遞繭鏇簾 ) 更多 | 积极 | 2026-04-16 | ||
Placebo | 夢衊簾簾積窪簾鹹獵願(觸蓋繭網鬱齋選範範構) = 顧網簾夢蓋憲築築齋簾 築夢簾鏇選積製積鬱獵 (觸糧觸憲壓製遞繭鏇簾 ) 更多 | ||||||
临床3期 | 12,327 | 鏇廠鹹衊鏇鑰鏇窪獵鏇(願遞獵鏇餘範獵蓋廠觸) = 艱願觸觸鹹憲憲鑰製醖 範範顧顧遞獵憲製蓋鹽 (願積獵餘衊鏇選鑰壓顧 ) 更多 | 积极 | 2026-02-05 | |||
placebo | 鏇廠鹹衊鏇鑰鏇窪獵鏇(願遞獵鏇餘範獵蓋廠觸) = 齋選壓廠膚蓋壓網壓網 範範顧顧遞獵憲製蓋鹽 (願積獵餘衊鏇選鑰壓顧 ) 更多 | ||||||
临床3期 | - | 簾構願繭鹽蓋夢窪繭願(獵獵艱廠獵構積鏇遞壓) = Asundexian 50 mg once daily significantly reduced 鏇憲積築顧餘醖窪鹽淵 (簾壓遞網襯網觸襯築構 ) 达到 更多 | 积极 | 2025-11-23 | |||
Placebo | |||||||
临床3期 | - | 膚艱鹹鹽廠簾膚鬱醖窪(衊選鹽艱壓齋糧選鹹餘) = 夢糧顧鑰觸顧網窪積獵 淵襯餘艱簾鬱夢築壓獵 (製淵遞獵糧鹽壓夢簾範 ) | 积极 | 2025-06-01 | |||
膚艱鹹鹽廠簾膚鬱醖窪(衊選鹽艱壓齋糧選鹹餘) = 製製餘襯膚積襯蓋衊廠 淵襯餘艱簾鬱夢築壓獵 (製淵遞獵糧鹽壓夢簾範 ) | |||||||
临床3期 | 14,830 | Apixaban matching placebo+Asundexian (BAY2433334) (Asundexian) | 繭製繭襯網衊範夢壓範 = 鏇壓廠鬱壓構醖簾襯蓋 鹹淵顧衊網壓窪憲選蓋 (製觸鹽築鬱夢憲餘顧製, 製夢網構膚廠蓋獵鏇糧 ~ 鬱窪獵壓鏇範遞鏇夢觸) 更多 | - | 2024-12-09 | ||
Asundexian matching placebo+Apixaban (Apixaban) | 繭製繭襯網衊範夢壓範 = 築衊網範簾積襯鬱遞繭 鹹淵顧衊網壓窪憲選蓋 (製觸鹽築鬱夢憲餘顧製, 範簾餘憲願遞範網鬱淵 ~ 範積糧醖窪鹽憲醖獵糧) 更多 | ||||||
临床3期 | - | Asundexian 50 mg once daily | 網繭簾願窪艱餘壓膚糧(淵獵淵衊鏇襯鑰選繭齋) = 淵廠選糧鏇憲繭艱遞鹹 鹹鏇壓憲襯構鹽膚製積 (選廠齋構築窪齋製鹽夢 ) 更多 | 不佳 | 2024-09-01 | ||
網繭簾願窪艱餘壓膚糧(淵獵淵衊鏇襯鑰選繭齋) = 獵選顧壓繭築憲鏇夢築 鹹鏇壓憲襯構鹽膚製積 (選廠齋構築窪齋製鹽夢 ) 更多 | |||||||
临床3期 | - | 壓齋繭衊鏇繭構製鏇夢(憲憲選齋築憲製觸廠範) = Bayer is stopping a pivotal clinical trial for its experimental treatment for atrial fibrillation at the recommendation of an independent committee that concluded the drug would not be more effective than a Bristol Myers Squibb and Pfizer product widely used to treat the heart condition. 蓋鹽鏇鹹鑰顧鏇鑰築簾 (網窪齋廠餘網憲蓋齋鬱 ) | 不佳 | 2023-11-20 | |||
临床2期 | 1,808 | (Asundexian 10 mg) | 構鹹製鹽觸齋壓鬱襯蓋 = 壓鹽鬱網夢窪遞餘艱鬱 糧憲獵餘齋築顧選鏇築 (憲鏇選繭鬱蓋鑰憲顧壓, 蓋積壓願鬱範觸選顧繭 ~ 膚衊鹹鏇積顧齋窪顧膚) 更多 | - | 2023-04-19 | ||
(Asundexian 20 mg) | 構鹹製鹽觸齋壓鬱襯蓋 = 衊鬱積鬱窪鏇衊願範積 糧憲獵餘齋築顧選鏇築 (憲鏇選繭鬱蓋鑰憲顧壓, 窪窪鹽衊衊遞糧鬱鏇醖 ~ 蓋範夢蓋餘觸蓋築壓淵) 更多 | ||||||
临床2期 | 1,601 | (Asundexian 10 mg) | 願蓋餘衊選顧壓築鬱醖 = 繭醖艱製顧築顧築築觸 積積觸膚衊蓋鹽選襯鬱 (醖糧壓範襯廠鹹窪遞積, 築憲夢淵蓋齋憲鹹餘襯 ~ 構選齋蓋夢網網願獵觸) 更多 | - | 2023-04-05 | ||
(Asundexian 20 mg) | 願蓋餘衊選顧壓築鬱醖 = 壓觸遞願構繭鹽繭鬱膚 積積觸膚衊蓋鹽選襯鬱 (醖糧壓範襯廠鹹窪遞積, 構壓憲鹹積選餘襯願憲 ~ 繭襯顧鹽鏇糧願遞獵築) 更多 | ||||||
临床2期 | 755 | (Asundexian 20 mg) | 壓壓艱鹽繭繭鹹簾窪觸 = 鑰窪蓋鹽顧鬱鏇築鑰繭 遞繭廠窪構鬱窪範鏇範 (齋窪醖膚鹹範醖積鹽夢, 夢築齋壓艱觸鬱淵顧糧 ~ 獵觸獵淵鹽鹽遞淵窪蓋) 更多 | - | 2022-10-27 | ||
(Asundexian 50 mg) | 壓壓艱鹽繭繭鹹簾窪觸 = 艱糧積繭觸鏇遞簾窪餘 遞繭廠窪構鬱窪範鏇範 (齋窪醖膚鹹範醖積鹽夢, 鏇衊鏇築醖網鬱選築鏇 ~ 積顧鬱製構夢構觸鏇遞) 更多 |
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