生物活性

• 描述The activated serine protease Factor Xa (FXa), activated by both the intrinsic and the extrinsic pathways, plays a central role in the blood coagulation cascade. FXa catalyzes the conversion of prothrombin tothrombin through the prothrombinase complex^[3]. Rivaroxaban, also called BAY 59-7939, is an inhibitor of FXa with IC₅₀ of 0.7 nM and Ki of 0.4 nM which is under clinical development for the treatment of thrombotic disease^[3]. Rivaroxaban (15, 30, or 60 ng/mL) inhibited thrombin generation in a concentration-dependent manner and the effect was enhanced with ticagrelor (1.0 µg/mL) and ticagrelor plus acetylsalicylic acid (100 µg/mL). Rivaroxaban (0.01, 0.03, or 0.1 mg/kg) also dose-dependently reduced thrombus formation in arteriovenous shunt model in rats^[4]. Oral rivaroxaban (2.5 mg twice-daily [bid] and 5 mg bid) reduced mortality and morbidity in patients with acute coronary syndrome, when combined with antiplatelets^[5].
• 作用机制Rivaroxaban forms two hydrogen bonds to Gly219 of Factor Xa.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02248610	-	-	Recruiting	November 2019	United Kingdom ... more >> Basingstoke Hospital Not yet recruiting Basingstoke, United Kingdom Bournemouth Hospital Not yet recruiting Bournemouth, United Kingdom Kings College Hospital NHS Foundation Trust Recruiting London, United Kingdom, SE5 9RS Contact: Kathryn Lang, MBBS, MRCP(UK)    02032999000 ext 31421    kathryn.lang@nhs.net    Contact: Rosalind Wilmott    02032993000    rosalind.wilmott@nhs.net    Salisbury Hospital Not yet recruiting Salisbury, United Kingdom Collapse <<
  NCT02549963	Atrial Fibrillation ... more >> Stroke Collapse <<	Phase 4	Unknown	-	China, Beijing ... more >> Beijing Anzhen Hospital Not yet recruiting Beijing, Beijing, China, 100029 Contact: Changsheng Ma, M.D. Ph.D.          China, Guangdong Nanfang Hospital Not yet recruiting Guangzhou, Guangdong, China, 510000 Contact: Xiaobo Huang, M.D. Ph.D.          The first Affiliated Hospital of Guangzhou medical University Not yet recruiting Guangzhou, Guangdong, China, 510000 Contact: Wei Wang, M.D.          The first affiliated hospital of Jinan university Not yet recruiting Guangzhou, Guangdong, China, 510000 Contact: Aidong Zhang, M.D. Ph.D.          The First Affiliated Hospital of Sun Yat-sen University Not yet recruiting Guangzhou, Guangdong, China, 510000 Contact: Yugang Dong, M.D. Ph.D.          The second Affiliated Hospital of Guangzhou medical University Not yet recruiting Guangzhou, Guangdong, China, 510000 Contact: Shiming Liu, M.D. Ph.D.          Guangdong Cardiovascular Institute, Guangdong General Hospital Guangzhou, Guangdong, China, 510080 The Affiliated Hospital of Guangdong Medical College Not yet recruiting Zhanjiang, Guangdong, China, 524000 Contact: Chan Chen, M.D. Ph.D.          China, Hubei Wuhan Asia Heart Hospital Not yet recruiting Wuhan, Hubei, China, 430000 Contact: Su Xi, M.D. Ph.D. Collapse <<
  NCT02123524	Symptomatic Superficial Vein T... more >>hrombosis Collapse <<	Phase 3	Completed	-	Canada, Alberta ... more >> University of Alberta Hospital Edmonton, Alberta, Canada, T6G 2B7 Canada, Ontario Hamilton General Hospital Hamilton, Ontario, Canada, L8L2X2 St Josephs Healthcare Hamilton, Ontario, Canada, L8N4A6 Juravinski Hospital Hamilton, Ontario, Canada, L8V1C3 McMaster Hospital Hamilton, Ontario, Canada The Ottawa Hospital Ottawa, Ontario, Canada, K1H8L6 Canada, Quebec Hopital Maisonneuve - Rosemount Montreal, Quebec, Canada, H1T 2M4 Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 Hopital Sacre Coeur Montreal, Quebec, Canada, H4J1C5 Montreal General Hospital Montreal, Quebec, Canada St Mary's Hospital Montreal, Quebec, Canada Collapse <<

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• 参考文献

• [1] Gnoth MJ, Buetehorn U, Muenster U, Schwarz T, Sandmann S. In vitro and in vivo P-glycoprotein transport characteristics of rivaroxaban. J Pharmacol Exp Ther. 2011 Jul;338(1):372-80.

  [2] Perzborn E, Strassburger J, et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor. J Thromb Haemost. 2005 Mar;3(3):514-21.

  [3] Roehrig S, Straub A, Pohlmann J, Lampe T, Pernerstorfer J, Schlemmer KH, Reinemer P, Perzborn E. Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor. J Med Chem. 2005 Sep 22;48(19):5900-8. doi: 10.1021/jm050101d. PMID: 16161994.

  [4] Effects of Rivaroxaban on Platelet Activation and Platelet–Coagulation Pathway Interaction: In Vitro and In Vivo Studies

  [5] Bauersachs R, Zannad F. Rivaroxaban: A New Treatment Paradigm in the Setting of Vascular Protection? Thromb Haemost. 2018 May;118(S 01):S12-S22. doi: 10.1055/s-0038-1636530. Epub 2018 Mar 22. PMID: 29566413.

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