The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor.

05:24 EDT 31st July 2015 | BioPortfolio

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.

Affiliation

Global Therapeutic Research, Pharma R&D, Bayer HealthCare, Aprather Weg 18a, D-42096 Wuppertal, Germany.

Journal Details

This article was published in the following journal.

Name: Nature reviews. Drug discovery
ISSN: 1474-1784
Pages:

Links

PubMed Articles [28527 Associated PubMed Articles listed on BioPortfolio]

Laboratory measurements of the oral direct factor xa inhibitor edoxaban: comparison of prothrombin time, activated partial thromboplastin time, and thrombin generation assay.

Edoxaban, an oral direct factor Xa inhibitor, does not require routine monitoring. However, assessment of the anticoagulant effects may be required in certain situations.

Anti-coagulation assessment with prothrombin time and anti-Xa assays in real-world patients on treatment with rivaroxaban.

Monitoring of anti-coagulation with the direct factor Xa inhibitor rivaroxaban is considered unnecessary in a routine clinical setting. However, assessment of its anti-coagulant effect may be desirabl...

Intracranial bleedings in patients on long-term anticoagulant treatment: Benefits from oral thrombin and factor Xa inhibitors in clinical practice.

Dabigatran, a direct thrombin inhibitor and activated factor X inhibitors, rivaroxaban and apixaban, used in the prevention of stroke or systemic embolism in patients with nonvalvular atrial fibrillat...

Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.

The coagulation factor Xa (FXa) plays a central role in the blood coagulation cascade. Recent studies have shown that FXa is a particularly attractive target for the development of oral antithrombotic...

Reversing targeted oral anticoagulants.

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 ...

Clinical Trials [5638 Associated Clinical Trials listed on BioPortfolio]

Deep Vein Thrombosis Treatment With the Oral Direct Factor Xa Inhibitor Rivaroxaban in Patients Using a Strong CYP 3A4 Inducer

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...

Oral Direct Factor Xa Inhibitor BAY59-7939 in Patients With Acute Symptomatic Proximal Deep Vein Thrombosis(ODIXa-DVT)

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...

Effect of Rivaroxaban on Coagulation Parameters- an ex Vivo Study

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...

An Oral, Direct Factor Xa Inhibitor, BAY59-7939, for Prophylaxis Against Venous Thromboembolism After Total Knee Replacement: a Dose-Ranging Study

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.


Advertisement
 

Relevant Topics

Drug Discovery
Latest News Clinical Trials Research Drugs Reports Corporate
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...

The Top 100 Pharmaceutical Companies
Latest News Clinical Trials Research Drugs Reports Corporate
Top 10 biotech and pharmaceutical companies worldwide based on market value in 2014 Top 10 biotech and pharmaceutical companies worldwide based on market value in 2014 (in billion U.S. dollars) data Johnson & Johnson, U.S. 2...

Advertisement