The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor.
Summary of "The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor."
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.
Global Therapeutic Research, Pharma R&D, Bayer HealthCare, Aprather Weg 18a, D-42096 Wuppertal, Germany.
This article was published in the following journal.
Name: Nature reviews. Drug discovery
Edoxaban, an oral direct factor Xa inhibitor, does not require routine monitoring. However, assessment of the anticoagulant effects may be required in certain situations.
Dabigatran, rivaroxaban, and apixaban are orally active anticoagulants that are approved in many countries. Dabigatran inhibits thrombin, whereas rivaroxaban and apixaban are factor Xa inhibitors. In ...
Rivaroxaban, a direct factor Xa inhibitor, affects laboratory clotting tests. We report here 10 venous thromboembolism patients with false-positive lupus anticoagulant during rivaroxaban therapy. Two ...
The clinical development of the non-vitamin K antagonists oral anticoagulants (NOACs), including the direct thrombin inhibitor dabigatran etexilate, and of the oral direct factor Xa inhibitors - rivar...
Rivaroxaban is a factor Xa inhibitor recently approved for use in the treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE). Older adults are at an increased risk for venous thromboembol...
This is a multicenter, cohort study evaluating an adapted rivaroxaban dose regimen in patients with acute, proximal deep-vein thrombosis (DVT) or acute pulmonary embolism (PE) who concomit...
The purpose of this study is to compare the safety and efficacy of BAY59-7939 with the safety and efficacy of the licensed drug enoxaparin and a licensed oral vitamin K-antagonist and to f...
Once - Daily Oral Direct Factor Xa Inhibitor Rivaroxaban In The Long-Term Prevention Of Recurrent Symptomatic Venous Thromboembolism In Patients With Symptomatic Deep-Vein Thrombosis Or Pulmonary Embolism. The Einstein-Extension Study
This is a multicenter, randomized, double-blind, placebo-controlled, event-driven, superiority study for efficacy. Patients with confirmed symptomatic DVT or PE who completed 6 or 12 month...
Rivaroxaban represent a new class of anticoagulation agents. As an oral direct factor Xa inhibitor it has been effective in preventing venous thromboembolism in patients undergoing electi...
The study drug, BAY59-7939, is a new drug currently being tested in the prevention of VTE. It directly inhibits factor Xa, a blood component in the pathway which leads to coagulation (clot...
Medical and Biotech [MESH] Definitions
A COUP transcription factor that was originally identified as a homodimer that binds to a direct repeat regulatory element in the chicken albumin promoter. It is a transcription factor that plays an important role in EMBRYONIC DEVELOPMENT of the CENTRAL NERVOUS SYSTEM.
The stages of development of the psychological aspects of sexuality from birth to adulthood; i.e., oral, anal, genital, and latent periods.
A specificity protein transcription factor that regulates expression of a variety of genes including VASCULAR ENDOTHELIAL GROWTH FACTOR and CYCLIN-DEPENDENT KINASE INHIBITOR P27.
A growth differentiation factor that plays a regulatory role as a paracrine factor for a diverse array of cell types during EMBRYONIC DEVELOPMENT and in the adult tissues. Growth differentiation factor 2 is also a potent regulator of CHONDROGENESIS and was previously referred to as bone morphogenetic protein 9.
A T-cell factor that plays an essential role in EMBRYONIC DEVELOPMENT.