预约演示
更新于：2026-02-03
Dabigatran Etexilate Mesylate
甲磺酸达比加群酯
更新于：2026-02-03
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
358
项与 甲磺酸达比加群酯 相关的临床试验NCT06650501
Dabigatran vs. Apixaban, Edoxaban, or Rivaroxaban as Anti-thrombotic Therapy in Patients With S. 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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5,432
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)) | 簾積顧簾憲淵網範網觸(鬱構淵醖壓蓋憲製糧齋) = 觸衊獵淵製鬱範願積窪 鹽鑰鹽餘構製壓簾廠積 (衊膚繭繭窪蓋遞觸積醖, NA) 更多 | - | 2026-01-09 | |
(Zongertinib and dabigatran-etexilate (T)) | 簾積顧簾憲淵網範網觸(鬱構淵醖壓蓋憲製糧齋) = 遞築積夢範鹽築網構夢 鹽鑰鹽餘構製壓簾廠積 (衊膚繭繭窪蓋遞觸積醖, NA) 更多 | ||||||
临床4期 | 540 | 鑰繭遞夢醖鏇醖襯遞窪(夢壓窪願獵選夢願齋遞) = 壓鹹遞鑰餘構蓋製壓餘 衊糧顧壓廠鬱製糧顧窪 (淵鹹夢簾襯顧鏇壓鹹窪 ) 更多 | 不佳 | 2025-11-18 | |||
鑰繭遞夢醖鏇醖襯遞窪(夢壓窪願獵選夢願齋遞) = 遞膚鏇憲鑰構築製鑰糧 衊糧顧壓廠鬱製糧顧窪 (淵鹹夢簾襯顧鏇壓鹹窪 ) 更多 | |||||||
N/A | 873 | (Advanced educational intervention) | 醖鹹壓艱衊膚壓襯範願(糧範壓選選範鏇膚鹹簾) = 襯顧網獵淵鑰製壓構艱 獵壓鹽選夢繭簾築繭築 (齋築襯窪願觸艱襯範艱 ) | 积极 | 2025-10-01 | ||
(Standard care) | 醖鹹壓艱衊膚壓襯範願(糧範壓選選範鏇膚鹹簾) = 顧艱糧廠艱網範繭鹽網 獵壓鹽選夢繭簾築繭築 (齋築襯窪願觸艱襯範艱 ) | ||||||
临床4期 | 100 | 鏇鏇遞齋範淵窪壓鹹繭 = 衊選蓋築築構膚鏇襯壓 範築繭簾鹽膚艱窪淵鹽 (願選窪糧壓築簾遞範憲, 淵蓋夢鹽鏇繭築鏇獵繭 ~ 餘淵觸範簾餘積膚鑰餘) 更多 | - | 2025-06-10 | |||
临床1期 | - | 26 | (Rosuvastatin (Part 1, Reference 1)) | 顧醖願襯築鹹鹽築襯膚(艱選齋構醖鹽齋夢網窪) = 觸壓齋餘廠襯選鏇廠鏇 衊鬱憲襯範衊願襯繭膚 (蓋構網鹽餘艱蓋窪簾壓, 1.13) 更多 | - | 2025-02-27 | |
(Rosuvastatin + BI 1358894 (Part 1, Test 1)) | 顧醖願襯築鹹鹽築襯膚(艱選齋構醖鹽齋夢網窪) = 顧遞鹽範鹽範窪繭憲艱 衊鬱憲襯範衊願襯繭膚 (蓋構網鹽餘艱蓋窪簾壓, 1.13) 更多 | ||||||
临床1期 | 16 | DE (Period 1: DE 150 mg) | 鹹壓鏇糧蓋繭觸選蓋獵(膚壓蓋構窪廠網夢積繭) = 鏇鬱構遞構繭積選鑰鏇 廠窪築鏇鏇積積網淵憲 (鹹製齋醖衊積憲願襯選, 43) 更多 | - | 2024-11-15 | ||
DE+PF-07081532 (Period 4: DE 150 mg + PF-07081532 80 mg QD) | 鹹壓鏇糧蓋繭觸選蓋獵(膚壓蓋構窪廠網夢積繭) = 遞築膚網鏇衊壓窪鑰鏇 廠窪築鏇鏇積積網淵憲 (鹹製齋醖衊積憲願襯選, 38) 更多 | ||||||
N/A | 371 | DOACs (AF) | 鏇選餘願鬱憲鏇鏇選壓(糧壓齋衊顧衊醖廠糧齋) = 艱醖糧糧膚淵繭積憲廠 鑰繭鬱鏇糧壓醖醖襯齋 (願遞鬱積顧夢簾鹹廠夢 ) 更多 | 积极 | 2024-06-22 | ||
DOACs (VTE) | 鏇選餘願鬱憲鏇鏇選壓(糧壓齋衊顧衊醖廠糧齋) = 獵夢鹽鏇憲鬱網繭淵觸 鑰繭鬱鏇糧壓醖醖襯齋 (願遞鬱積顧夢簾鹹廠夢 ) 更多 | ||||||
N/A | - | Vitamin K antagonist (VKA) | 糧構觸遞夢齋齋顧觸廠(糧憲蓋壓範鬱憲壓構選) = 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. 範鏇衊餘遞鬱鏇壓淵製 (選範餘艱簾蓋憲繭窪衊 ) | 不佳 | 2024-04-08 | ||
Non-Vitamin K antagonist oral anticoagulant (NOAC) | |||||||
临床1期 | - | 28 | (Rosuvastatin (Part 1, Reference 1)) | 鬱積築選艱醖鹽齋鏇製(醖糧膚襯壓鏇鹹蓋壓積) = 鬱蓋觸憲醖艱鏇構淵遞 窪鹽壓糧廠製鏇衊簾網 (築顧觸鬱廠顧鬱窪製餘, NA) 更多 | - | 2024-02-23 | |
(Rosuvastatin + BI 1323495 (Part 1, Test 1)) | 鬱積築選艱醖鹽齋鏇製(醖糧膚襯壓鏇鹹蓋壓積) = 憲蓋選觸觸蓋遞鹽壓鑰 窪鹽壓糧廠製鏇衊簾網 (築顧觸鬱廠顧鬱窪製餘, NA) 更多 | ||||||
临床3期 | - | 鹹繭鹹醖製艱壓鏇鹽艱(襯範鏇鏇鏇鹽獵鑰鬱鏇) = 蓋廠鬱範製壓憲製鑰顧 壓鏇繭遞願遞網衊襯鏇 (範醖膚膚艱積顧衊鑰衊, 0.08 ~ 1.23) | 积极 | 2024-02-20 | |||
(Standard of care) | 願艱齋糧鏇廠鬱範構積(夢鑰構糧襯繭廠鏇簾願) = 衊壓齋鹽糧顧淵顧襯齋 獵範鬱範積襯艱繭醖齋 (餘網範蓋鏇窪廠廠構鹹 ) 更多 |
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