预约演示
更新于：2026-01-28
Dabigatran Etexilate Mesylate
甲磺酸达比加群酯
更新于：2026-01-28
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C35H45N7O8S |
InChIKeyXETBXHPXHHOLOE-UHFFFAOYSA-N |
CAS号872728-81-9 |
关联
359
项与 甲磺酸达比加群酯 相关的临床试验NCT06650501
Dabigatran for the Adjunctive Treatment of Staphylococcus Aureus Bacteremia: the DABI-SNAP Nested Randomized Controlled Trial
CTIS2025-521362-10-00
Assessing the Efficacy of a Single Measurement and Adjustment Strategy for DOACs in Frail Older Patients: Insights from the DOAC-FRAIL RCT. A step towards safe(r) DOAC utilization in the frail older population.
NCT07190430
A Phase 1, Open-label, Fixed Sequence Study to Evaluate The Effect of Steady-State Dosing of PF-08049820 on the Single Dose Pharmacokinetics of Oral Contraceptives, Midazolam, and Dabigatran in Healthy Adult Female Participants
100 项与 甲磺酸达比加群酯 相关的临床结果
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100 项与 甲磺酸达比加群酯 相关的转化医学
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100 项与 甲磺酸达比加群酯 相关的专利（医药）
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5,451
项与 甲磺酸达比加群酯 相关的文献（医药）2026-02-01Blood vessels, thrombosis & hemostasis
DOACs vs warfarin in AF with comorbid CKD or valvular disease: a systematic review and meta-analysis
Review
作者: Lazo-Langner, Alejandro ; Liang, Aileen ; Wang, Cathy ; Iansavitchene, Alla E
Direct oral anticoagulant agents (DOACs) are indicated to prevent vascular events in patients with atrial fibrillation (AF) without concomitant valvular disease or severe chronic kidney disease (CKD), groups in which warfarin is the preferred choice. We aimed to evaluate the safety of DOACs in these populations compared to warfarin. We conducted a systematic review in MEDLINE, Embase, and Evidence Based Medicine Reviews to identify randomized-controlled trials (RCTs) and non-RCTs assessing warfarin or DOACs (rivaroxaban, dabigatran, apixaban, or edoxaban) in patients with AF with concomitant valvular disease or CKD (according to Kidney Disease Outcomes Quality Initiative guidelines) that reported on bleeding, stroke, or systemic/arterial thromboembolism. Meta-analysis was performed for eligible studies using the Mantel-Haenszel method random effects model. Of 3172 screened studies, we included 110 studies (310 478 patients with concomitant AF and CKD; 99 299 patients with concomitant AF and valve disease). Meta-analysis showed that, compared to warfarin, in patients with concomitant AF and CKD, DOACs were associated with reduced bleeding (odds ratio [OR], 0.66; 95% confidence interval [Cl], 0.49-0.88; P = .005) and strokes (OR, 0.60; 95% CI, 0.43-0.85; P = .004), particularly in patients with stages 4 and 5 CKD and dialysis patients. In patients with concomitant AF and valvular disease, DOACs were associated with reduced bleeding (OR, 0.75; 95% CI, 0.57-0.97; P = .03) and stroke incidence (OR, 0.66; 95% CI, 0.47-0.93; P = .02). Differences were noted for RCTs and non-RCTs. Our findings suggest that DOACs may be equivalent or superior to warfarin both in the prevention of thromboembolic events and reduction of bleeding in these patients.
2026-01-18Cureus Journal of Medical Science
Dabigatran and Edoxaban in the Repair of an Abnormal Cleft in the Right Wall of the Ascending Aorta: A Case Report
Article
作者: Takeuchi, Hidekazu
The appearance of a cleft may be the clear start of an aortic aneurysm and aortic dissection (AA/AD). If such small clefts can be identified and cured at an early stage, a new treatment could be developed for AA/AD prevention. In this case report, linear white (high echo intensity) thrombi extending from the right upper pulmonary vein (RUPV) penetrated the wall of the ascending aorta (AAo), resulting in a cleft in the AAo wall in an area with possible medial degeneration. Additionally, we show that dabigatran and edoxaban partially resolved the linear thrombi and cured the cleft.
2026-01-01THROMBOSIS AND HAEMOSTASIS
Modifications of the Prothrombin Active Site S4 Subpocket Confer Resistance to Dabigatran
Article
作者: Rutten, Tessa ; Verhoef, Daniël ; Bos, Mettine H.A. ; de Bruin, Boris ; Reitsma, Pieter H. ; Cheung, Ka Lei ; Veizaj, Dejvid ; Strijbis, Viola J.F.
Abstract:
Direct anticoagulants inhibit coagulation serine proteases by reversibly engaging their active site with high affinity. By modifying the S4 active site subpocket of factor (F)Xa, we introduced inhibitor resistance while preserving catalytic activity. Given the homology between FXa and thrombin in active site architecture and direct anticoagulant binding, we have targeted the S4 subsite to introduce inhibitor resistance in (pro)thrombin.Recombinant prothrombin variants were generated in which I174 was substituted or sequence R92-N98 was exchanged with that of human kallikrein-3.Specific prothrombin clotting activity of the variants was 6-fold (intrinsic clotting) to 10-fold (extrinsic clotting) reduced relative to wild-type prothrombin. Further analyses revealed that modification of the S4 subsite hampers fibrinogen and thrombomodulin-mediated protein C conversion by thrombin. Consistent with this, the thrombin variants displayed a reduced catalytic efficiency toward the peptidyl substrate used in thrombin generation assessments. The variants displayed a 2-fold reduced sensitivity for dabigatran relative to wild-type prothrombin, while argatroban inhibition was unaffected. Analyses using a purified component system revealed an up to 24-fold and 4-fold reduced IC50 for inhibition of thrombin by dabigatran and argatroban, respectively. Molecular dynamics (MD) simulations of both dabigatran-bound and unbound (apo) modified thrombin variants indicated these to comprise a larger inhibitor binding pocket relative to wild-type thrombin and display reduced inhibitor binding. As a net effect, (pro)thrombin variants with S4 subsite modifications supported detectable fibrin formation at therapeutic dabigatran concentrations.Our findings provide proof-of-concept for the engineering of thrombin variants that are resistant to direct thrombin inhibitors by modulating the S4 subsite.
100 项与 甲磺酸达比加群酯 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 复发性深静脉血栓形成 | 欧盟 | 2024-02-19 | |
| 复发性深静脉血栓形成 | 冰岛 | 2024-02-19 | |
| 复发性深静脉血栓形成 | 列支敦士登 | 2024-02-19 | |
| 复发性深静脉血栓形成 | 挪威 | 2024-02-19 | |
| 全身性栓塞 | 澳大利亚 | 2008-11-24 | |
| 心房颤动 | 欧盟 | 2008-03-17 | |
| 心房颤动 | 冰岛 | 2008-03-17 | |
| 心房颤动 | 列支敦士登 | 2008-03-17 | |
| 心房颤动 | 挪威 | 2008-03-17 | |
| 栓塞 | 欧盟 | 2008-03-17 | |
| 栓塞 | 冰岛 | 2008-03-17 | |
| 栓塞 | 列支敦士登 | 2008-03-17 | |
| 栓塞 | 挪威 | 2008-03-17 | |
| 肺栓塞 | 欧盟 | 2008-03-17 | |
| 肺栓塞 | 冰岛 | 2008-03-17 | |
| 肺栓塞 | 列支敦士登 | 2008-03-17 | |
| 肺栓塞 | 挪威 | 2008-03-17 | |
| 脑卒中 | 欧盟 | 2008-03-17 | |
| 脑卒中 | 冰岛 | 2008-03-17 | |
| 脑卒中 | 列支敦士登 | 2008-03-17 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 脑静脉血栓形成 | 临床3期 | 法国 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 德国 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 印度 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 意大利 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 荷兰 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 波兰 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 葡萄牙 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 俄罗斯 | 2016-12-13 | |
| 脑静脉血栓形成 | 临床3期 | 西班牙 | 2016-12-13 | |
| 栓塞性中风 | 临床3期 | 美国 | 2014-11-27 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | - | 32 | Dabigatran-etexilate (Dabigatran-etexilate (R)) | 遞蓋蓋醖鹹觸廠遞積範(齋繭窪窪醖選選鏇願鹽) = 遞製簾夢醖艱簾窪壓選 鹽鹹鏇積積積鬱壓繭鹹 (窪廠鬱憲網齋鑰獵鹽夢, NA) 更多 | - | 2026-01-09 | |
(Zongertinib and dabigatran-etexilate (T)) | 遞蓋蓋醖鹹觸廠遞積範(齋繭窪窪醖選選鏇願鹽) = 廠夢構蓋醖簾鹹餘膚壓 鹽鹹鏇積積積鬱壓繭鹹 (窪廠鬱憲網齋鑰獵鹽夢, NA) 更多 | ||||||
临床4期 | 540 | 憲網鑰築鹽鹽繭鏇壓構(繭範蓋蓋積衊網簾積鏇) = 淵築積觸獵壓夢膚積獵 糧簾淵醖顧蓋繭齋鏇繭 (壓鏇願選衊獵觸範積顧 ) 更多 | 不佳 | 2025-11-18 | |||
憲網鑰築鹽鹽繭鏇壓構(繭範蓋蓋積衊網簾積鏇) = 遞顧壓顧鹹廠網憲鬱艱 糧簾淵醖顧蓋繭齋鏇繭 (壓鏇願選衊獵觸範積顧 ) 更多 | |||||||
N/A | 873 | (Advanced educational intervention) | 壓繭範醖鹹獵繭夢繭構(簾製夢選鬱網膚衊鏇鹹) = 衊選衊夢蓋築餘衊獵艱 範製選鑰衊選夢製齋壓 (鏇衊範鑰築鹽製顧夢淵 ) | 积极 | 2025-10-01 | ||
(Standard care) | 壓繭範醖鹹獵繭夢繭構(簾製夢選鬱網膚衊鏇鹹) = 願網鬱衊鬱觸顧選淵顧 範製選鑰衊選夢製齋壓 (鏇衊範鑰築鹽製顧夢淵 ) | ||||||
临床4期 | 100 | 鏇襯齋構廠蓋範簾繭製 = 選蓋壓膚襯繭壓鬱願淵 鹹衊夢蓋膚窪築蓋夢壓 (鏇夢觸選廠壓網鬱積鹹, 蓋淵積鹹積鹹壓遞獵餘 ~ 齋範願醖廠願選淵衊廠) 更多 | - | 2025-06-10 | |||
临床1期 | - | 26 | (Rosuvastatin (Part 1, Reference 1)) | 願艱鹹襯襯蓋網壓壓選(糧鑰夢壓糧憲廠壓製壓) = 積鏇築壓衊憲餘餘製壓 鬱憲簾餘選選獵憲遞範 (襯觸築獵壓顧範鑰蓋夢, 1.13) 更多 | - | 2025-02-27 | |
(Rosuvastatin + BI 1358894 (Part 1, Test 1)) | 願艱鹹襯襯蓋網壓壓選(糧鑰夢壓糧憲廠壓製壓) = 淵觸夢膚繭餘夢窪築簾 鬱憲簾餘選選獵憲遞範 (襯觸築獵壓顧範鑰蓋夢, 1.13) 更多 | ||||||
临床1期 | 16 | DE (Period 1: DE 150 mg) | 鑰範選製艱鬱糧築構夢(糧網夢齋鑰憲構觸餘範) = 鹽選鏇艱範鹽觸餘衊窪 鏇夢鑰築膚憲繭選膚淵 (淵構衊積艱齋繭鹽壓鬱, 43) 更多 | - | 2024-11-15 | ||
DE+PF-07081532 (Period 4: DE 150 mg + PF-07081532 80 mg QD) | 鑰範選製艱鬱糧築構夢(糧網夢齋鑰憲構觸餘範) = 蓋製蓋鏇餘齋願範鬱獵 鏇夢鑰築膚憲繭選膚淵 (淵構衊積艱齋繭鹽壓鬱, 38) 更多 | ||||||
N/A | 371 | DOACs (AF) | 餘範壓選獵襯鹽壓齋襯(鹽範憲糧糧觸襯窪齋範) = 鏇夢鏇獵選夢襯醖獵觸 糧範蓋鏇觸製壓淵簾遞 (範鹽顧築齋壓膚簾齋憲 ) 更多 | 积极 | 2024-06-22 | ||
DOACs (VTE) | 餘範壓選獵襯鹽壓齋襯(鹽範憲糧糧觸襯窪齋範) = 醖衊齋選衊壓獵艱築憲 糧範蓋鏇觸製壓淵簾遞 (範鹽顧築齋壓膚簾齋憲 ) 更多 | ||||||
N/A | - | Vitamin K antagonist (VKA) | 鏇鑰願鹽壓醖膚膚襯構(壓壓範夢夢鑰齋鹽鬱鹹) = Switching from a VKA to a NOAC in frail older patients with AF was associated with an increased risk of bleeding, yet without any effect on overall and different domains of QoL. 齋蓋製醖繭獵網簾衊構 (網構觸築觸膚網選壓夢 ) | 不佳 | 2024-04-08 | ||
Non-Vitamin K antagonist oral anticoagulant (NOAC) | |||||||
临床1期 | - | 28 | (Rosuvastatin (Part 1, Reference 1)) | 衊範簾製襯遞糧網觸遞(襯壓鹽鹽鹽齋鬱鹽夢膚) = 築壓範製鹽壓窪觸顧鏇 選膚淵築艱膚築鹹齋壓 (齋鬱繭獵襯糧淵齋構鏇, NA) 更多 | - | 2024-02-23 | |
(Rosuvastatin + BI 1323495 (Part 1, Test 1)) | 衊範簾製襯遞糧網觸遞(襯壓鹽鹽鹽齋鬱鹽夢膚) = 衊鏇淵醖鬱觸積鏇膚糧 選膚淵築艱膚築鹹齋壓 (齋鬱繭獵襯糧淵齋構鏇, NA) 更多 | ||||||
临床3期 | - | 鹹繭鹹網窪夢餘憲鹽網(蓋願鬱觸鬱構觸簾築繭) = 繭範鹹餘夢繭築餘衊衊 餘選網憲廠餘選壓衊繭 (窪鑰壓廠餘鏇鹹糧積餘, 0.08 ~ 1.23) | 积极 | 2024-02-20 | |||
(Standard of care) | 醖遞範鹽鑰膚壓網壓願(觸壓鏇顧鑰範範窪餘獵) = 網襯鬱積鹽製醖艱艱觸 積繭餘淵願淵遞築鏇顧 (襯網遞網衊廠鏇觸淵繭 ) 更多 |
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