Dabigatran是可逆的高活性直接凝血酶抑制剂(DTI),Ki为4.5 nM。
Dabigatran (BIBR 953) is a potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay.
静脉注射给药
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Hauel NH, et al. J Med Chem. 2002, 45(9), 1757-1766.
分子式 C25H25N7O3 |
分子量 471.51 |
CAS号 211914-51-1 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO <1 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01590823 | Blood Coagulation Disorders | Drug: Dabigatran Etexilate 110 mg | Nova Scotia Health Authority|Capital Health, Canada|Dalhousie University|Universit de Montral | Phase 1 | 2012-07-01 | 2012-10-31 |
NCT02426229 | Scleroderma|Interstitial Lung Disease | Drug: dabigatran etexilate | Medical University of South Carolina|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS) | Phase 1 | 2016-02-01 | 2017-03-22 |
NCT01976507 | Atrial Fibrillation|Atrial Flutter | Drug: dabigatran etexilate mesylate | Vanderbilt University Medical Center|Boehringer Ingelheim | Phase 4 | 2013-10-01 | 2017-02-21 |
NCT02173717 | Healthy | Drug: Dabigatran etexilate|Drug: Rifampicin | Boehringer Ingelheim | Phase 1 | 2009-06-01 | 2014-06-24 |
NCT01385683 | Healthy | Drug: Dabigatran then dabigatran and clarithromycin|Drug: Clarithromycin and dabigatran then dabigatran | Centre Hospitalier Universitaire de Saint Etienne|Groupe de Recherche sur la Thrombose | Phase 1 | 2011-06-01 | 2012-03-21 |
NCT01546883 | Atrial Fibrillation | Drug: Dabigatran etexilate (Pradaxa) | University of Utah | Phase 4 | 2012-02-01 | 2015-09-10 |
NCT01769703 | Transient Ischemic Attack|Minor Ischemic Stroke | Drug: Dabigatran 110/150 mg BID | University of Alberta | Phase 2 | 2012-02-01 | 2014-10-29 |
NCT01852162 | Coronary Artery Disease | Drug: Dabigatran|Drug: Placebo | University of Florida | 2012-02-01 | 2015-03-10 | |
NCT02389582 | Coronary Disease | Drug: Dabigatran|Drug: Enoxaparin | University of Sao Paulo General Hospital|Fundao de Amparo Pesquisa do Estado de So Paulo | Phase 4 | 2014-05-01 | 2016-04-28 |
NCT02256683 | (Atrial Fibrillation) or (Atrial Flutter)|Thrombosis of Left Atrial Appendage | Drug: Dabigatran etexilate|Drug: Phenprocoumon | Johannes Gutenberg University Mainz|Boehringer Ingelheim|German Atrial Fibrillation Network | Phase 4 | 2014-07-01 | 2016-02-26 |
NCT01290757 | Healthy | Drug: Dabigatran etexilate|Drug: Dabigatran etexilate | Boehringer Ingelheim | Phase 1 | 2011-01-01 | 2014-05-08 |
NCT02596555 | Pulmonary Embolism | Drug: Dabigatran | Prof. Stavros Konstantinides, MD|European Georges Pompidou Hospital|Johannes Gutenberg University Mainz | Phase 4 | 2016-01-01 | 2016-04-26 |
NCT01711853 | Renal Insufficiency, Chronic | Drug: Dabigatran Etexilate | Boehringer Ingelheim | Phase 1 | 2012-10-01 | 2015-01-09 |
NCT02223260 | Venous Thromboembolism | Drug: dabigatran | Boehringer Ingelheim | Phase 2 | 2014-09-01 | 2016-07-28 |
NCT02331602 | Atrial Fibrillation | Drug: Rivaroxaban|Drug: Dabigatran | Yokohama City University Medical Center|Yokohama City University | Phase 4 | 2013-07-01 | 2015-08-04 |
NCT02102633 | Healthy | Drug: Dabigatran|Drug: Bosutinib|Drug: Dabigatran | Pfizer | Phase 1 | 2014-05-01 | 2014-06-23 |
NCT00808067 | Atrial Fibrillation | Drug: dabigatran dose 1|Drug: dabigatran dose 2 | Boehringer Ingelheim | Phase 3 | 2008-11-01 | 2014-06-03 |
NCT01868243 | Primary Disease | Drug: Dabigatran|Drug: Warfarin | Hospital Ana Nery | Phase 2|Phase 3 | 2013-08-01 | 2015-09-14 |
NCT02044367 | Healthy | Drug: Dabigatran etexilate|Drug: Dabigatran etexilate|Drug: Dabigatran etexilate | Boehringer Ingelheim | Phase 1 | 2014-01-01 | 2015-05-01 |
NCT00844415 | Venous Thromboembolism | Drug: dabigatran etexilate | Boehringer Ingelheim | Phase 2 | 2009-06-01 | 2014-06-03 |
NCT02170675 | Healthy | Drug: Dabigatran etexilate|Drug: Ketoconazole | Boehringer Ingelheim | Phase 1 | 2009-06-01 | 2014-06-20 |
NCT01083732 | Venous Thromboembolism | Drug: dabigatran etexilate | Boehringer Ingelheim | Phase 2 | 2010-03-01 | 2016-11-02 |
NCT01468155 | Atrial Fibrillation | Drug: dabigatran | Allan Skanes|Boehringer Ingelheim|Lawson Health Research Institute | Phase 4 | 2011-11-01 | 2012-10-16 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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