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Article: Antithrombotische Wirkung - Vergleich des oralen, direkten Faktor-Xa-Inhibitors Rivaroxaban mit Enoxaparin

Perzborn, Elisabeth

2007 Volume 8, Issue 4, Page(s) 11

Language	German
Document type	Article
ZDB-ID	2041837-1
ISSN	1615-777X
Database	Current Contents Medicine

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Article ; Online: Effects of Rivaroxaban on Platelet Activation and Platelet-Coagulation Pathway Interaction: In Vitro and In Vivo Studies.

Perzborn, Elisabeth / Heitmeier, Stefan / Laux, Volker

Journal of cardiovascular pharmacology and therapeutics

2015 Volume 20, Issue 6, Page(s) 554–562

Abstract: Introduction: Activation of coagulation and platelets is closely linked, and arterial thrombosis involves coagulation activation as well as platelet activation and aggregation. In these studies, we investigated the possible synergistic effects of ... ...

Abstract	Introduction: Activation of coagulation and platelets is closely linked, and arterial thrombosis involves coagulation activation as well as platelet activation and aggregation. In these studies, we investigated the possible synergistic effects of rivaroxaban in combination with antiplatelet agents on thrombin generation and platelet aggregation in vitro and on arterial thrombosis and hemostasis in rat models. Materials and methods: Thrombin generation was measured by the Calibrated Automated Thrombogram method (0.5 pmol/L tissue factor) using human platelet-rich plasma (PRP) spiked with rivaroxaban (15, 30, or 60 ng/mL), ticagrelor (1.0 µg/mL), and acetylsalicylic acid (ASA; 100 µg/mL). Tissue factor-induced platelet aggregation was measured in PRP spiked with rivaroxaban (15 or 30 ng/mL), ticagrelor (1 or 3 µg/mL), or a combination of these. An arteriovenous (AV) shunt model in rats was used to determine the effects of rivaroxaban (0.01, 0.03, or 0.1 mg/kg), clopidogrel (1 mg/kg), ASA (3 mg/kg), and combinations on arterial thrombosis. Results: Rivaroxaban inhibited thrombin generation in a concentration-dependent manner and the effect was enhanced with ticagrelor and ticagrelor plus ASA. Rivaroxaban and ticagrelor also concentration-dependently inhibited tissue factor-induced platelet aggregation, and their combination increased the inhibition synergistically. In the AV shunt model, rivaroxaban dose-dependently reduced thrombus formation. Combining subefficacious or weakly efficacious doses of rivaroxaban with ASA or ASA plus clopidogrel increased the antithrombotic effect. Conclusion: These data indicate that the combination of rivaroxaban with single or dual antiplatelet agents works synergistically to reduce platelet activation, which may in turn lead to the delayed/reduced formation of coagulation complexes and vice versa, thereby enhancing antithrombotic potency.
MeSH term(s)	Adenosine/analogs & derivatives ; Adenosine/pharmacology ; Adult ; Animals ; Arteriovenous Shunt, Surgical ; Aspirin/pharmacology ; Blood Coagulation/drug effects ; Coronary Thrombosis/blood ; Dose-Response Relationship, Drug ; Female ; Humans ; Male ; Platelet Activation/drug effects ; Platelet Aggregation Inhibitors/pharmacology ; Rats ; Rats, Wistar ; Rivaroxaban/pharmacology ; Thrombin/metabolism ; Ticlopidine/analogs & derivatives ; Ticlopidine/pharmacology
Chemical Substances	Platelet Aggregation Inhibitors ; Rivaroxaban (9NDF7JZ4M3) ; clopidogrel (A74586SNO7) ; Thrombin (EC 3.4.21.5) ; Ticagrelor (GLH0314RVC) ; Adenosine (K72T3FS567) ; Ticlopidine (OM90ZUW7M1) ; Aspirin (R16CO5Y76E)
Language	English
Publishing date	2015-11
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1329372-2
ISSN	1940-4034 ; 1074-2484
ISSN (online)	1940-4034
ISSN	1074-2484
DOI	10.1177/1074248415578172
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Article ; Online: Reversal of rivaroxaban-induced anticoagulation with prothrombin complex concentrate, activated prothrombin complex concentrate and recombinant activated factor VII in vitro.

Perzborn, Elisabeth / Heitmeier, Stefan / Laux, Volker / Buchmüller, Anja

Thrombosis research

2014 Volume 133, Issue 4, Page(s) 671–681

Abstract: Introduction: Anticoagulation therapies carry a risk of bleeding; reversal agents may be beneficial in cases of severe bleeding even for anticoagulants with a relatively short half-life, such as the oral factor Xa inhibitor rivaroxaban.: Materials and ...

Abstract	Introduction: Anticoagulation therapies carry a risk of bleeding; reversal agents may be beneficial in cases of severe bleeding even for anticoagulants with a relatively short half-life, such as the oral factor Xa inhibitor rivaroxaban. Materials and methods: We investigated the in vitro reversal effect of prothrombin complex concentrate (PCC; 0.2-1.0U/mL), activated PCC (aPCC; 0.2-1.0U/mL) and recombinant activated factor VII (rFVIIa; 5-50μg/mL) on rivaroxaban-induced (200-1000ng/mL) changes in prothrombin time (PT) and thrombin generation (TG) in plasma, and in thromboelastometry (clotting time [CT]) in whole blood from healthy subjects. Results: All three agents were partially effective in reversing rivaroxaban-induced anticoagulation but showed different profiles. rFVIIa and aPCC were more effective than PCC in reversing prolongations of PT, CT and TG lag time; rFVIIa was more effective than aPCC. However, the reversal effect reached a plateau with a maximal effect of approximately 50%. Inhibition of maximum thrombin concentration was slightly reversed by these agents; aPCC was the most effective. In contrast, inhibition of endogenous thrombin potential (ETP) was strongly reversed by aPCC, with significant increases over baseline at low rivaroxaban concentrations. Compared with aPCC, PCC showed a similar but less effective reversal profile. rFVIIa reversed ETP inhibition by approximately 50%. Conclusions: The extent of reversal by aPCC, PCC and rFVIIa was dependent on the parameter measured in rivaroxaban-anticoagulated plasma or blood. ETP measurements may have predictive power for assessing the reversal potential of PCC or aPCC and may be used to indicate an increased prothrombotic risk.
MeSH term(s)	Anticoagulants/administration & dosage ; Blood Coagulation/drug effects ; Blood Coagulation Factors/pharmacology ; Blood Coagulation Tests/methods ; Drug Interactions ; Factor VIIa/metabolism ; Factor VIIa/pharmacology ; Humans ; Morpholines/antagonists & inhibitors ; Morpholines/pharmacology ; Recombinant Proteins/metabolism ; Recombinant Proteins/pharmacology ; Rivaroxaban ; Thiophenes/antagonists & inhibitors ; Thiophenes/pharmacology ; Thrombelastography ; Thrombin/pharmacology
Chemical Substances	Anticoagulants ; Blood Coagulation Factors ; Morpholines ; Recombinant Proteins ; Thiophenes ; prothrombin complex concentrates (37224-63-8) ; Rivaroxaban (9NDF7JZ4M3) ; recombinant FVIIa (AC71R787OV) ; Factor VIIa (EC 3.4.21.21) ; Thrombin (EC 3.4.21.5)
Language	English
Publishing date	2014-04
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	121852-9
ISSN	1879-2472 ; 0049-3848
ISSN (online)	1879-2472
ISSN	0049-3848
DOI	10.1016/j.thromres.2014.01.017
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Article: The discovery of rivaroxaban: translating preclinical assessments into clinical practice.

Kubitza, Dagmar / Perzborn, Elisabeth / Berkowitz, Scott D

Frontiers in pharmacology

2013 Volume 4, Page(s) 145

Abstract: Direct oral anticoagulants that target a single coagulation factor (such as factor Xa or thrombin) have been developed in recent years in an attempt to address some of the limitations of traditional anticoagulants. Rivaroxaban is an oral, direct factor ... ...

Abstract	Direct oral anticoagulants that target a single coagulation factor (such as factor Xa or thrombin) have been developed in recent years in an attempt to address some of the limitations of traditional anticoagulants. Rivaroxaban is an oral, direct factor Xa inhibitor that inhibits free and clot-bound factor Xa and factor Xa in the prothrombinase complex. Preclinical studies demonstrated a potent anticoagulant effect of rivaroxaban in plasma as well as the ability of this agent to prevent and treat venous and arterial thrombosis in animal models. These studies led to an extensive phase I clinical development program that investigated the pharmacological properties of rivaroxaban in humans. In these studies, rivaroxaban was shown to exhibit predictable pharmacokinetics and pharmacodynamics and to have no clinically relevant interactions with many commonly prescribed co-medications. The pharmacodynamic effects of rivaroxaban (for example, inhibition of factor Xa and prolongation of prothrombin time) were closely correlated with rivaroxaban concentrations in plasma. The encouraging findings from preclinical and early clinical studies were expanded upon in large, randomized phase III studies, which demonstrated the clinical efficacy and safety of rivaroxaban in a broad spectrum of patients. This article provides an overview of the discovery and development of rivaroxaban, describing the pharmacodynamic profile established in preclinical studies and the optimal translation to clinical studies in healthy subjects and patient populations.
Language	English
Publishing date	2013-11-25
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2587355-6
ISSN	1663-9812
ISSN	1663-9812
DOI	10.3389/fphar.2013.00145
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Article ; Online: Measurement and reversal of prophylactic and therapeutic peak levels of rivaroxaban: an in vitro study.

Körber, Mareike Kristina / Langer, Elisabeth / Ziemer, Sabine / Perzborn, Elisabeth / Gericke, Christine / Heymann, Christian von

Clinical and applied thrombosis/hemostasis : official journal of the International Academy of Clinical and Applied Thrombosis/Hemostasis

2014 Volume 20, Issue 7, Page(s) 735–740

Abstract: Background: Rivaroxaban (Xarelto, Bayer HealthCare, Leverkusen, Germany) is a new oral anticoagulant drug. Anticoagulants may cause bleeding, thereby requiring reliable monitoring and efficient therapy. We investigated thromboelastometry versus routine ... ...

Abstract	Background: Rivaroxaban (Xarelto, Bayer HealthCare, Leverkusen, Germany) is a new oral anticoagulant drug. Anticoagulants may cause bleeding, thereby requiring reliable monitoring and efficient therapy. We investigated thromboelastometry versus routine coagulation tests to measure prophylactic and therapeutic concentrations of rivaroxaban and their reversal with prothrombin complex concentrate (PCC) and activated recombinant factor VII (rFVIIa) in vitro. Methods: Rivaroxaban was solubilized, and PCC and rFVIIa were added in 2 concentrations to the rivaroxaban-spiked blood samples, and thromboelastometry and measurements were performed. Results: Rivaroxaban increased tissue factor-activated clotting time (CT(ExTEM)) dose dependently. Activated partial prothrombin time (aPTT), prothrombin time ratio (PTR), and prothrombin time (PT) were changed significantly in both concentrations. Reversal with PCC in both dosages caused no significant change in the measured parameters. For prophylactic rivaroxaban dosage, rFVIIa changed the PT significantly but not CT(ExTEM), aPTT, and PTR. For therapeutic rivaroxaban dosage, the CT(ExTEM) was significantly reduced. The other parameters remained unaffected. Conclusions: Thromboelastometry can detect rivaroxaban effects. In vitro rFVIIa seems highly effective for reversal in contrast to PCC.
MeSH term(s)	Adult ; Blood Coagulation Factors/metabolism ; Dose-Response Relationship, Drug ; Factor VIIa/metabolism ; Factor Xa Inhibitors/pharmacokinetics ; Factor Xa Inhibitors/pharmacology ; Female ; Humans ; Male ; Morpholines/pharmacokinetics ; Morpholines/pharmacology ; Rivaroxaban ; Thiophenes/pharmacokinetics ; Thiophenes/pharmacology ; Thrombelastography
Chemical Substances	Blood Coagulation Factors ; Factor Xa Inhibitors ; Morpholines ; Thiophenes ; prothrombin complex concentrates (37224-63-8) ; Rivaroxaban (9NDF7JZ4M3) ; Factor VIIa (EC 3.4.21.21)
Language	English
Publishing date	2014-10
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1237357-6
ISSN	1938-2723 ; 1076-0296
ISSN (online)	1938-2723
ISSN	1076-0296
DOI	10.1177/1076029613494468
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Article ; Online: The discovery and development of rivaroxaban.

Misselwitz, Frank / Berkowitz, Scott D / Perzborn, Elisabeth

Annals of the New York Academy of Sciences

2011 Volume 1222, Page(s) 64–75

Abstract: Thromboembolic conditions present a considerable challenge to healthcare services because they are associated with substantial morbidity and mortality. The mainstays of prevention and treatment are anticoagulants and antiplatelet agents. Established ... ...

Abstract	Thromboembolic conditions present a considerable challenge to healthcare services because they are associated with substantial morbidity and mortality. The mainstays of prevention and treatment are anticoagulants and antiplatelet agents. Established anticoagulants have drawbacks that make their use difficult to manage and sustain. This has stimulated the search for new oral anticoagulants that are more convenient and yet still effective. This paper describes the development and future potential of rivaroxaban (Xarelto; Bayer Schering Pharma AG, Berlin, Germany)-the first oral, direct Factor Xa inhibitor to be approved for clinical use in the prevention of venous thromboembolism in adult patients undergoing elective hip or knee replacement surgery.
MeSH term(s)	Adult ; Animals ; Clinical Trials as Topic/methods ; Clinical Trials as Topic/trends ; Drug Design ; Drug Discovery/methods ; Drug Discovery/trends ; Fibrinolytic Agents/chemical synthesis ; Fibrinolytic Agents/therapeutic use ; Humans ; Models, Biological ; Models, Molecular ; Molecular Targeted Therapy/methods ; Morpholines/chemical synthesis ; Morpholines/therapeutic use ; Rivaroxaban ; Thiophenes/chemical synthesis ; Thiophenes/therapeutic use ; Validation Studies as Topic ; Venous Thromboembolism/drug therapy
Chemical Substances	Fibrinolytic Agents ; Morpholines ; Thiophenes ; Rivaroxaban (9NDF7JZ4M3)
Language	English
Publishing date	2011-03
Publishing country	United States
Document type	Evaluation Studies ; Journal Article ; Review
ZDB-ID	211003-9
ISSN	1749-6632 ; 0077-8923
ISSN (online)	1749-6632
ISSN	0077-8923
DOI	10.1111/j.1749-6632.2011.05971.x
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Article ; Online: Expression of pro-inflammatory genes in human endothelial cells: Comparison of rivaroxaban and dabigatran.

Ellinghaus, Peter / Perzborn, Elisabeth / Hauenschild, Peter / Gerdes, Christoph / Heitmeier, Stefan / Visser, Mayken / Summer, Holger / Laux, Volker

Thrombosis research

2016 Volume 142, Page(s) 44–51

Abstract: Introduction: In addition to its central role in coagulation, thrombin is involved in non-hemostatic activities such as inflammation. Direct inhibition of thrombin activity (e.g. with dabigatran) or reducing its generation by inhibition of Factor Xa (e ... ...

Abstract	Introduction: In addition to its central role in coagulation, thrombin is involved in non-hemostatic activities such as inflammation. Direct inhibition of thrombin activity (e.g. with dabigatran) or reducing its generation by inhibition of Factor Xa (e.g. with rivaroxaban) may therefore have anti-inflammatory effects. Materials and methods: Microarray experiments were performed to identify transcriptome-wide changes in mRNA expression levels induced by thrombin in the presence and absence of the PAR-1 antagonist vorapaxar in primary human umbilical vein endothelial cells (HUVECs). On this basis, HUVECs were incubated with recalcified plasma, with or without rivaroxaban (0.3-3000nM), dabigatran (0.3-10,000nM), or vorapaxar (0.3-10nM). Expression levels of preselected pro-inflammatory genes were quantified by real-time PCR. Results: Vorapaxar abolished 67 of the 69 transcripts altered by more than twofold on addition of thrombin to HUVECs. ELAM-1, VCAM-1, ICAM-1, MCP-1, IL-8, CXCL1, and CXCL2 were among the genes most strongly induced by thrombin. Inflammatory gene expression after stimulation of thrombin generation was concentration-dependently suppressed by vorapaxar, dabigatran, and rivaroxaban. However, dabigatran at low concentrations (3-300nM) increased significantly the expression levels of CXCL1, CXCL2, IL-8, ELAM-1, MCP-1, and tissue factor. Conclusion: In HUVECs, plasma-induced transcriptional changes are mediated by thrombin-induced PAR-1 activation. Rivaroxaban downregulated the expression of pro-inflammatory markers and tissue factor to a similar extent to dabigatran.
MeSH term(s)	Antithrombins/pharmacology ; Dabigatran/pharmacology ; Endothelial Cells/drug effects ; Endothelial Cells/immunology ; Endothelial Cells/metabolism ; Factor Xa Inhibitors/pharmacology ; Human Umbilical Vein Endothelial Cells ; Humans ; Inflammation/chemically induced ; Inflammation/genetics ; Inflammation/immunology ; Lactones/pharmacology ; Pyridines/pharmacology ; Receptor, PAR-1/antagonists & inhibitors ; Receptor, PAR-1/immunology ; Rivaroxaban/pharmacology ; Thrombin/immunology ; Transcriptome/drug effects
Chemical Substances	Antithrombins ; Factor Xa Inhibitors ; Lactones ; Pyridines ; Receptor, PAR-1 ; Rivaroxaban (9NDF7JZ4M3) ; Thrombin (EC 3.4.21.5) ; Dabigatran (I0VM4M70GC) ; vorapaxar (ZCE93644N2)
Language	English
Publishing date	2016-06
Publishing country	United States
Document type	Comparative Study ; Journal Article
ZDB-ID	121852-9
ISSN	1879-2472 ; 0049-3848
ISSN (online)	1879-2472
ISSN	0049-3848
DOI	10.1016/j.thromres.2016.04.008
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Article ; Online: Hemostatic therapy in experimental intracerebral hemorrhage associated with rivaroxaban.

Zhou, Wei / Zorn, Markus / Nawroth, Peter / Bütehorn, Ulf / Perzborn, Elisabeth / Heitmeier, Stefan / Veltkamp, Roland

Stroke

2013 Volume 44, Issue 3, Page(s) 771–778

Abstract: Background and purpose: Rivaroxaban has recently been approved for stroke prevention in atrial fibrillation. However, lack of an effective antidote represents a major concern in the event of intracerebral hemorrhage (ICH). The aims of the present study ... ...

Abstract	Background and purpose: Rivaroxaban has recently been approved for stroke prevention in atrial fibrillation. However, lack of an effective antidote represents a major concern in the event of intracerebral hemorrhage (ICH). The aims of the present study were to establish a murine model of ICH associated with rivaroxaban, and to examine the effectiveness of different hemostatic factors in preventing excess hematoma expansion. Methods: In C57BL/6 mice receiving 10 or 30 mg/kg rivaroxaban by gastric gavage, plasma concentration, prothrombin time, and coagulation factor activities were measured repeatedly. Thirty minutes after inducing ICH by intrastriatal collagenase-injection, mice received an intravenous injection of either saline, prothrombin complex concentrate (100 U/kg), murine fresh frozen plasma (200 μL), or recombinant human Factor VIIa (1 mg/kg). ICH volume was quantified on brain cryosections and using hemoglobin spectrophotometry 24 hours later. Results: Rivaroxaban in 30 mg/kg dose substantially increased the hematoma volume in ICH induced by 0.060 U collagenase. Prothrombin complex concentrate, fresh frozen plasma, or Factor VIIa prevented excess hematoma expansion caused by anticoagulation. Prevention of hematoma expansion by prothrombin complex concentrate was dose-dependent. None of the 3 agents completely corrected the prolonged prothrombin time, although they restored the activities of deficient FII and X. Conclusions: Prothrombin complex concentrate, Factor VIIa, and fresh frozen plasma prevent excess intracerebral hematoma expansion in a murine ICH model associated with rivaroxaban. The efficacy and safety of this reversal strategy must be further evaluated in clinical studies.
MeSH term(s)	Animals ; Anticoagulants/adverse effects ; Blood Coagulation Factors/adverse effects ; Blood Coagulation Factors/therapeutic use ; Cerebral Hemorrhage/chemically induced ; Cerebral Hemorrhage/drug therapy ; Dose-Response Relationship, Drug ; Factor VIIa/adverse effects ; Factor VIIa/therapeutic use ; Hematoma/prevention & control ; Hemostatic Techniques ; Male ; Mice ; Mice, Inbred C57BL ; Models, Animal ; Morpholines/adverse effects ; Plasma ; Rivaroxaban ; Thiophenes/adverse effects ; Treatment Outcome
Chemical Substances	Anticoagulants ; Blood Coagulation Factors ; Morpholines ; Thiophenes ; prothrombin complex concentrates (37224-63-8) ; Rivaroxaban (9NDF7JZ4M3) ; Factor VIIa (EC 3.4.21.21)
Language	English
Publishing date	2013-03
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	80381-9
ISSN	1524-4628 ; 0039-2499 ; 0749-7954
ISSN (online)	1524-4628
ISSN	0039-2499 ; 0749-7954
DOI	10.1161/STROKEAHA.112.675231
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Article ; Online: The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor.

Perzborn, Elisabeth / Roehrig, Susanne / Straub, Alexander / Kubitza, Dagmar / Misselwitz, Frank

Nature reviews. Drug discovery

2010 Volume 10, Issue 1, Page(s) 61–75

Abstract: The activated serine protease factor Xa is a promising target for new anticoagulants. After studies on naturally occurring factor Xa inhibitors indicated that such agents could be effective and safe, research focused on small-molecule direct inhibitors ... ...

Abstract	The activated serine protease factor Xa is a promising target for new anticoagulants. After studies on naturally occurring factor Xa inhibitors indicated that such agents could be effective and safe, research focused on small-molecule direct inhibitors of factor Xa that might address the major clinical need for improved oral anticoagulants. In 2008, rivaroxaban (Xarelto; Bayer HealthCare) became the first such compound to be approved for clinical use. This article presents the history of rivaroxaban's development, from the structure-activity relationship studies that led to its discovery to the preclinical and clinical studies, and also provides a brief overview of other oral anticoagulants in advanced clinical development.
MeSH term(s)	Administration, Oral ; Animals ; Anticoagulants/administration & dosage ; Anticoagulants/adverse effects ; Anticoagulants/pharmacology ; Clinical Trials as Topic ; Drug Delivery Systems ; Drug Design ; Drug Evaluation, Preclinical ; Factor Xa Inhibitors ; Humans ; Morpholines/administration & dosage ; Morpholines/adverse effects ; Morpholines/pharmacology ; Rivaroxaban ; Structure-Activity Relationship ; Thiophenes/administration & dosage ; Thiophenes/adverse effects ; Thiophenes/pharmacology
Chemical Substances	Anticoagulants ; Factor Xa Inhibitors ; Morpholines ; Thiophenes ; Rivaroxaban (9NDF7JZ4M3)
Language	English
Publishing date	2010-12-17
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2062954-0
ISSN	1474-1784 ; 1474-1776
ISSN (online)	1474-1784
ISSN	1474-1776
DOI	10.1038/nrd3185
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Article: Preclinical and clinical characteristics of rivaroxaban: a novel, oral, direct factor Xa inhibitor.

Laux, Volker / Perzborn, Elisabeth / Kubitza, Dagmar / Misselwitz, Frank

Seminars in thrombosis and hemostasis

2007 Volume 33, Issue 5, Page(s) 515–523

Abstract: There are several novel anticoagulants in development that target factor Xa(FXa)-the pivotal point of the coagulation cascade. One promising agent is rivaroxaban (a highly selective, oral, direct FXa inhibitor), which is in advanced clinical development ... ...

Abstract	There are several novel anticoagulants in development that target factor Xa(FXa)-the pivotal point of the coagulation cascade. One promising agent is rivaroxaban (a highly selective, oral, direct FXa inhibitor), which is in advanced clinical development for the prevention and treatment of thromboembolic disorders. Oral rivaroxaban may be given in fixed once-daily doses, with the potential for no coagulation monitoring. These properties, along with results from preclinical and clinical studies, suggest that rivaroxaban may have advantages over current treatments. Studies in arterial and venous animal models demonstrated that rivaroxaban has potent antithrombotic effects, without prolonging bleeding times. In healthy subjects, rivaroxaban was well tolerated, with a predictable pharmacological profile and a low propensity for clinically relevant drug-drug interactions. Phase II studies of rivaroxaban for the prevention of venous thromboembolism (VTE) after major orthopedic surgery support these findings. The results also suggested that a total daily dose range of 5 to 20 mg rivaroxaban had similar efficacy and safety to enoxaparin, and that 10 mg rivaroxaban once daily was the optimal dose. This review assesses the preclinical and clinical characteristics of rivaroxaban, and discusses phase II findings with rivaroxaban for the prevention of VTE after major orthopedic surgery.
MeSH term(s)	Administration, Oral ; Animals ; Anticoagulants/administration & dosage ; Anticoagulants/adverse effects ; Anticoagulants/pharmacokinetics ; Bleeding Time ; Clinical Trials, Phase II as Topic ; Disease Models, Animal ; Drug Evaluation, Preclinical ; Enoxaparin/administration & dosage ; Enoxaparin/adverse effects ; Enoxaparin/pharmacokinetics ; Factor Xa Inhibitors ; Humans ; Morpholines/administration & dosage ; Morpholines/adverse effects ; Morpholines/pharmacokinetics ; Morpholines/pharmacology ; Orthopedics ; Rivaroxaban ; Thiophenes/administration & dosage ; Thiophenes/adverse effects ; Thiophenes/pharmacokinetics ; Thiophenes/pharmacology ; Thromboembolism/prevention & control
Chemical Substances	Anticoagulants ; Enoxaparin ; Factor Xa Inhibitors ; Morpholines ; Thiophenes ; Rivaroxaban (9NDF7JZ4M3)
Language	English
Publishing date	2007-07
Publishing country	United States
Document type	Comparative Study ; Journal Article ; Review
ZDB-ID	196901-8
ISSN	1098-9064 ; 0094-6176
ISSN (online)	1098-9064
ISSN	0094-6176
DOI	10.1055/s-2007-982083
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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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In stock of ZB MED Cologne/Königswinter

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