Rivaroxaban是一种口服具有直接作用的Factor Xa抑制剂,Ki值为0.4 nM,IC50值为0.7 nM。
Rivaroxaban is a direct inhibitor of Factor Xa with Ki and IC50 of 0.4 nM and 0.7 nM in cell-free assays, respectively.
0 -100 μM
静脉注射≤0.3 mg/kg 口服 ≤3 mg/kg 静脉注射或口服
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] Perzborn E, et al. J Thromb Haemost, 2005, 3(3), 514–521.
[2] Eriksson, B.I., et al. 2005. J. Thromb. Haemost. 3: 103-111
[3] Ansell, J., et al. 2004. Drugs. 64: 1-5.
[4] Kubitza, D., et al. 2005. Clin. Pharmacol. Ther. 78: 412-421.
分子式 C19H18ClN3O5S |
分子量 88 |
CAS号 366789-02-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO >68 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 |
NCT02047006 | Chronic Renal Failure | Drug: Rivaroxaban 10 mg | AZ Sint-Jan AV|Onze Lieve Vrouw Hospital | Phase 4 | 2013-09-01 | 2015-01-13 |
NCT02486445 | Deep Venous Thrombosis | Drug: Rivaroxaban | Ostfold Hospital Trust | Phase 3 | 2015-02-01 | 2016-10-10 |
NCT02970773 | Spinal Cord Injuries|Thromboembolism | Drug: Rivaroxaban | Swiss Paraplegic Centre Nottwil | 2017-01-01 | 2016-11-18 | |
NCT01598168 | Heparin-induced Thrombocytopenia | Drug: Rivaroxaban | McMaster University | Phase 3 | 2013-01-01 | 2016-03-24 |
NCT02583191 | Venous Thromboembolism|Cancer | Drug: Rivaroxaban|Drug: low-molecular heparine | AIO-Studien-gGmbH|Charite University, Berlin, Germany|Bayer | Phase 3 | 2016-03-01 | 2016-03-18 |
NCT01989845 | Rivaroxaban|Cancer-associated Thrombosis|Recurrence|Bleeding | Drug: Rivaroxaban | Seoul National University Hospital|Korean Society of Hematology Thrombosis Working Party | Phase 4 | 2013-10-01 | 2017-01-06 |
NCT02438098 | Prophylaxis of Venous Thromboembolism | Drug: Rivaroxaban 10 mg | University Hospital Inselspital, Berne|Centre Hospitalier Universitaire Vaudois|Bayer | Phase 1 | 2015-06-01 | 2016-01-07 |
NCT02657512 | Healthy | Drug: rivaroxaban|Drug: rivaroxaban and activated charcoal | Centre Hospitalier Universitaire de Saint Etienne | Phase 1 | 2016-01-01 | 2016-05-24 |
NCT02116036 | Antiphospholipid Antibody Syndrome | Drug: Rivaroxaban | St. Joseph's Healthcare Hamilton|Heart and Stroke Foundation of Canada|Bayer|Hamilton Health Sciences Corporation|Jewish General Hospital|University of Alberta|The Ottawa Hospital|Queen Elizabeth II Health Sciences Centre | Phase 4 | 2014-09-01 | 2015-07-23 |
NCT02072668 | Sickle Cell Anemia|Sickle Cell-Beta0-Thalassemia | Drug: rivaroxaban|Drug: placebo | University of North Carolina, Chapel Hill|National Heart, Lung, and Blood Institute (NHLBI) | Phase 2 | 2014-02-01 | 2016-11-02 |
NCT02157272 | Antiphospholipid Syndrome | Drug: Experimental: Rivaroxaban | University of Padova | Phase 3 | 2014-12-01 | 2015-11-30 |
NCT02066662 | Atrial Fibrillation or Pulmonary Embolism|Need of Long Term Oral Anticoagulation Therapy (OAT)|Existent Coronary or Valvular Calcification, or Both and Agatston Score > 50 in at Least One Location | Drug: Rivaroxaban or Marcumar | RWTH Aachen University|Bayer | Phase 4 | 2013-07-01 | 2015-12-03 |
NCT02289703 | End-Stage Renal Disease | Drug: Rivaroxaban 15 mg | Janssen Research & Development, LLC|Bayer | Phase 1 | 2015-01-01 | 2017-01-23 |
NCT02333929 | Patients Receiving Rivaroxaban Treatment | Device: STA- Rivaroxaban Calibrator&Control | Diagnostica Stago | 2015-03-01 | 2017-02-13 | |
NCT01708850 | Neoplasm|Central Venous Catheter Thrombosis | Drug: Rivaroxaban | London Health Sciences Centre | Phase 4 | 2012-11-01 | 2016-09-06 |
NCT02042534 | Ischemic Stroke|Transient Ischemic Attack | Drug: Rivaroxaban|Drug: Warfarin | Asan Medical Center|Bayer | Phase 2 | 2014-01-01 | 2016-12-14 |
NCT01747746 | Atrial Fibrillation|Stroke|Thrombo-embolism|Bleeding | Drug: Rivaroxaban|Drug: Warfarin and Enoxaparin | John H. Stroger Hospital|Cook County Hospital | Phase 4 | 2012-10-01 | 2015-02-02 |
NCT02058199 | Gastric Bypass Status | Drug: rivaroxaban | State University of New York - Upstate Medical University | Phase 1 | 2014-12-01 | 2016-01-04 |
NCT02468102 | Acute Coronary Syndrome | Drug: Rivaroxaban (Xarelto, BAY59-7939)|Drug: Standard of care drugs | Bayer|Janssen Scientific Affairs, LLC | 2015-06-01 | 2017-03-13 | |
NCT02926170 | Antiphospholipid Syndrome | Drug: Rivaroxaban|Drug: acenocumarol | Hospital Universitari Vall d'Hebron Research Institute | Phase 3 | 2013-03-01 | 2016-10-05 |
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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