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Journal articles on the topic 'Betrixaban'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Lee, Katie, Samantha Cham, and Sum Lam. "Betrixaban." Cardiology in Review 26, no. 6 (2018): 331–38. http://dx.doi.org/10.1097/crd.0000000000000227.

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2

Gras, J. A. "Betrixaban." Drugs of the Future 37, no. 11 (2012): 761. http://dx.doi.org/10.1358/dof.2012.037.011.1902385.

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Gras, J. A. "Betrixaban." Drugs of the Future 37, no. 11 (2012): 761. http://dx.doi.org/10.1358/dof.2012.37.11.1902385.

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4

Garland, Scott G., Christina E. DeRemer, Steven M. Smith, and John G. Gums. "Betrixaban: A New Oral Factor Xa Inhibitor for Extended Venous Thromboembolism Prophylaxis in High-Risk Hospitalized Patients." Annals of Pharmacotherapy 52, no. 6 (2018): 554–61. http://dx.doi.org/10.1177/1060028018754383.

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Objective: To review the pharmacology, pharmacokinetics, efficacy, and safety of the factor Xa (FXa) inhibitor betrixaban for extended-duration prophylaxis of acute medically ill patients with venous thromboembolism (VTE) risk factors. Data Sources: A MEDLINE/PubMed (January 1990 to October 2017) search was conducted using the following keywords: betrixaban, PRT054021, FXa inhibitor, novel oral anticoagulant, NOAC, direct oral anticoagulant, DOAC, and target specific oral anticoagulant, TSOAC. References of identified articles were searched by hand for additional relevant citations. Study Sele

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Hutchaleelaha, Athiwat, Christine Ye, Yonghong Song, Todd Lorenz, Daniel Gretler, and Joseph L. Lambing. "Metabolism and Disposition of Betrixaban and Its Lack of Interaction with Major CYP Enzymes." Blood 120, no. 21 (2012): 2266. http://dx.doi.org/10.1182/blood.v120.21.2266.2266.

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Abstract Abstract 2266 Betrixaban is a once daily oral Factor Xa inhibitor being investigated in a Phase 3 clinical trial to prevent venous thromboembolism in acute medically ill patients (APEX Study). Mass balance, metabolite profile and interaction with major CYP enzymes were evaluated in this study. Portola study 06–005 was an open-label, single-dose, mass-balance and metabolic profiling study using 14C-labeled betrixaban in 5 healthy male volunteers. Each subject received a single oral solution containing 40 mg of betrixaban labeled with 100 μCi of 14C. Blood samples were taken serially ov

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Murphy, Grazia, Yasmin Grace, Sadaf Chaudry, and Rita Chamoun. "Betrixaban: A Novel Oral Anticoagulant With a New Niche." Journal of Pharmacy Technology 34, no. 3 (2018): 123–33. http://dx.doi.org/10.1177/8755122518759765.

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Objective: To evaluate the efficacy, safety, and clinical implication of betrixaban for prophylaxis of venous thromboembolism (VTE) in patients with acute medical illness. Data Sources: A search for clinical trials was performed from January 2006 to January 2017 in English language using Clinicaltrials.gov and PubMed/MEDLINE. The following search terms were used: betrixaban, pharmacokinetics, pharmacology, and drug safety. Study Selection: The following limits were used to access the clinical trials: controlled clinical trial, randomized clinical trial, clinical trial, clinical trial phase II,

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Bauer, Kenneth, Bruce Davidson, William Fisher, et al. "A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT)." Thrombosis and Haemostasis 101, no. 01 (2009): 68–76. http://dx.doi.org/10.1160/th08-07-0460.

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SummaryBetrixaban is an oral direct inhibitor of factor Xa (FXa) being developed for the prevention of venous thromboembolism (VTE). Its antithrombotic effects had not been previously tested in patients. This exploratory clinical trial in the US and Canada randomized 215 patients undergoing elective total knee replacement (TKR) in a 2:2:1 ratio to receive post-operative betrixaban 15 mg or 40 mg p.o. bid or enoxaparin 30 mg s.c. q12h, respectively, for 10–14 days. The betrixaban dosage was blinded, but enoxaparin was not. Primary efficacy outcome was the incidence of VTE, consisting of deep-ve

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Siriez, Romain, Jonathan Evrard, Jean-Michel Dogné, et al. "Betrixaban: Impact on Routine and Specific Coagulation Assays—A Practical Laboratory Guide." Thrombosis and Haemostasis 118, no. 07 (2018): 1203–14. http://dx.doi.org/10.1055/s-0038-1657772.

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Introduction Betrixaban is a novel direct oral factor Xa inhibitor approved by the Food and Drug Administration for prophylaxis of venous thromboembolism in adult patients hospitalized for an acute illness at risk for thromboembolic complications. Assessment of the anti-coagulant effect of betrixaban may be useful in some situations. Also, clinicians need to know how routine coagulation assays are influenced. Objective The aim of this study is to determine which coagulation assay(s) should be used to assess the impact of betrixaban on haemostasis and provide laboratory guidance for their inter

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9

Rao Anna, Venkateswara, V. K. Rohini, K. Hemabala, Bhagya Kumar Tatavarti, and Vijaya N. "Evaluation of New Degradation Products Formed Under Stress Conditions of Betrixaban by LCMS/MS: Establishment of HPLC Method for Quantification of Genotoxic Impurities of Betrixaban." International Journal of Advancement in Life Sciences Research 07, no. 04 (2024): 64–78. http://dx.doi.org/10.31632/ijalsr.2024.v07i04.006.

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This study focused to optimize an accurate HPLC method for evaluation of genotoxic impurities of Betrixaban and further structural identification of forced degradation products (DPs) of betrixaban. The analytes were resolved on Zorbax SB C18 (4.6×250mm, 5μm, Agilent) column at 35°C temperature using 75 % aqueous ammonium formate (5 mM) and 50 % ammonium formate in acetonitrile in 60:40 (v/v) in isocratic elution at 1.0 mL/min and 245 nm as detection wavelength. In the optimized experimental conditions, the retention times of the analytes were precisely determined, resulting in retention times

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10

Gibson, C., Lisa Jennings, Gerald Chi, et al. "Association of D-dimer Levels with Clinical Event Rates and the Efficacy of Betrixaban versus Enoxaparin in the APEX Trial." TH Open 02, no. 01 (2018): e16-e24. http://dx.doi.org/10.1055/s-0037-1615288.

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Background Elevated D-dimer concentrations are associated with an increased risk of venous thromboembolism (VTE). However, they may also provide prognostic value. The present analysis sought to study the association of D-dimer levels with VTE event rates and the efficacy of betrixaban versus enoxaparin in the APEX trial. Methods Hospitalized acutely medically ill subjects (n = 7,513) were randomized in a double-dummy double-blind fashion to either extended-duration oral betrixaban (80 mg once daily for 35–42 days) or standard dose subcutaneous enoxaparin (40 mg once daily for 10 ± 4 days) for

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Crowther, Mark, Genmin Lu, Janet Leeds, et al. "314 Reversal of Betrixaban-Induced Anticoagulation in Healthy Volunteers by Andexanet Alfa." Neurosurgery 64, CN_suppl_1 (2017): 267. http://dx.doi.org/10.1093/neuros/nyx417.314.

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Abstract INTRODUCTION Andexanet alfa (andexanet) is a modified, recombinant human factor Xa (FXa) that acts as a decoy to bind and sequester FXa inhibitors, thus reversing their anticoagulation effects. Here, we report the efficacy of andexanet in reversing the anticoagulant activity of betrixaban, a direct FXa inhibitor which has recently completed a large Phase 3 clinical trial in acute medically ill patients (APEX). METHODS In this Phase 2, randomized, double-blind study, healthy subjects were dosed with 80 mg qd po betrixaban to steady state (7 days). In Cohort 1, subjects (n = 6) received

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Huisman, Menno V., and Frederikus A. Klok. "Pharmacological properties of betrixaban." European Heart Journal Supplements 20, suppl_E (2018): E12—E15. http://dx.doi.org/10.1093/eurheartj/suy016.

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Baker, Danial E. "Formulary Drug Review: Betrixaban." Hospital Pharmacy 53, no. 1 (2017): 29–37. http://dx.doi.org/10.1177/0018578717739397.

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Each month, subscribers to The Formulary Monograph Service receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing in-services. A comprehensive target drug utilization evaluation/medication use evaluation (DUE/MUE) is also provided each month. With a subscription, the monographs are available online to subscribers. Monographs can be customized to meet the nee

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Yee, Megan, C. Gibson, Tarek Nafee, et al. "Characterization of Major and Clinically Relevant Non-Major Bleeds in the APEX Trial." TH Open 03, no. 02 (2019): e103-e108. http://dx.doi.org/10.1055/s-0039-1685496.

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Background Among medically ill patients treated with thromboprophylaxis, betrixaban was not associated with an increase in major bleeding compared with enoxaparin, but an increase in clinically relevant non-major (CRNM) bleeding was observed. The aim of this analysis is to describe the severity and clinical consequences of major and CRNM bleeding in the APEX trial. Methods The APEX trial randomized 7,513 hospitalized acutely ill medical patients to receive either enoxaparin for 6 to 14 days or betrixaban for 35 to 42 days. Subjects receiving a concomitant strong p-glycoprotein inhibitor or wit

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Cohen, Alexander T., Rim Halaby, Serge Korjian, et al. "The Safety and Efficacy of Full Versus Reduced Dose Betrixaban in the Acute Medically Ill VTE (Venous Thromboembolism) Prevention with Extended Duration Betrixaban (APEX) Trial." Blood 128, no. 22 (2016): 3824. http://dx.doi.org/10.1182/blood.v128.22.3824.3824.

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Abstract Background: The exposure of all the currently licenced DOACs is increased in renal impairment and by certain drug interactions. The Acute Medically Ill VTE (Venous Thromboembolism) Prevention with Extended Duration Betrixaban (APEX) trial assessed the safety and efficacy of extended-duration thromboprophylaxis using betrixaban versus standard dosing of enoxaparin among acutely ill medical patients. The full 80 mg dose of betrixaban was halved to 40 mg among subjects with severe renal insufficiency (calculated creatinine clearance <30ml/min), or receiving a concomitant strong P-glyc

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Chi, Gerald, Samuel Goldhaber, Russell Hull, et al. "Thrombus Burden of Deep Vein Thrombosis and Its Association with Thromboprophylaxis and D-Dimer Measurement: Insights from the APEX Trial." Thrombosis and Haemostasis 117, no. 12 (2017): 2389–95. http://dx.doi.org/10.1160/th17-08-0538.

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Background The aim of this study was to evaluate the effect of betrixaban on the occurrence of deep vein thrombosis (DVT) and also the extent of thrombus and to assess the association of baseline D-dimer with subsequent thrombus burden. Methods In the APEX trial (ClinicalTrials.gov: NCT01583218), 7,513 acutely ill hospitalized medical patients were randomly assigned to extended-duration betrixaban (35–42 days) or enoxaparin (10 ± 4 days). D-dimer concentration was measured at baseline, and mandatory lower-extremity compression ultrasonography (CUS) was performed at 35 to 42 days. The thrombus

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Paravattil, Bridget, and Hazem Elewa. "Approaches to Direct Oral Anticoagulant Selection in Practice." Journal of Cardiovascular Pharmacology and Therapeutics 24, no. 2 (2018): 95–102. http://dx.doi.org/10.1177/1074248418793137.

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Direct oral anticoagulants (DOACs) carry many advantages over warfarin and are now considered first line or an alternative for mnay thromboembolic disorders. With the emergence of 5 DOAC agents to the market as well as the accumulating evidence gathered from head-to-head comparisons between the agents, we attempt to provide direction for clinicians when selecting the most appropriate DOAC agent. Important aspects such as efficacy, safety, cost effectiveness, approved indications, and other drug-related factors will be addressed to highlight the major similarities and diversities among the DOAC

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El-Masry, Amal A., Dalia R. El-Wasseef, Manal Eid, Ihsan A. Shehata, and Abdallah M. Zeid. "Optimization and Validation of a Facile RP-HPLC Method for Determination of Betrixaban and Lercanidipine in Pharmaceutical and Biological Matrices." Journal of Chromatographic Science 59, no. 8 (2021): 785–94. http://dx.doi.org/10.1093/chromsci/bmab088.

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Abstract A simple, accurate, rapid and sensitive reversed-phase high-performance liquid chromatography (RP-HPLC) method was established for determination of a novel non-vitamin K antagonist oral anticoagulant drug, betrixaban, and its co-administered calcium-channel blocker drug, lercanidipine, in pharmaceutical formulations and biological fluids. The proposed HPLC method was the first chromatographic method applied to estimate this mixture in a short chromatographic run (&lt;6 min), high resolution between betrixaban/lercanidipine (Rs = 7.12) and acceptable values of limit of detection (L

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Mehrotra, Siddharth, Debra Hoppensteadt, Walter Jeske, et al. "Differential Neutralization of Apixaban, Betrixaban, Edoxaban, and Rivaroxaban By Andexanet Alfa As Measured By Whole Blood Thromboelastographic Analysis." Blood 134, Supplement_1 (2019): 1155. http://dx.doi.org/10.1182/blood-2019-131907.

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Introduction/Background: Recombinant coagulation factor Xa (FXa), inactivated Zh-zo, also known as andexanet alfa (AA), is a modified version of human FXa that has been developed as an antidote to neutralize the bleeding effects of oral FXa inhibitors such as, Apixaban and Rivaroxaban. The relative biological effect of these drugs have been investigated using various clot based and amidolytic methods for FXa inhibition. This Factor Xa inhibitory activity acts as a surrogate marker for the circulating level of these agents. We have recently reported that the FXa activity of these Anti-Xa agents

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Siddiqui, Fakiha, Siddharth Mehrotra, Vishnu Venkitasubramony, et al. "Factor Xa Inhibitory Profile of Apixaban, Betrixaban, Edoxaban and Rivaroxaban Does Not Fully Reflect Their Biologic Spectrum." Blood 132, Supplement 1 (2018): 2520. http://dx.doi.org/10.1182/blood-2018-99-116993.

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Abstract Introduction: There are four oral anti-Xa drugs currently available for clinical use in various indications. These drugs are claimed to mediate their therapeutic effects by solely targeting factor Xa. While these agents are structurally similar, their biochemical properties and their effects on blood coagulation differ. Such differences may impact their safety and efficacy profile. The purpose of this study was to demonstrate the differences among factor Xa inhibitors in terms of their in vitro anticoagulant activity and other biochemical effects. Materials and Methods: Commercially o

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Traynor, Kate. "Betrixaban approved as oral VTE preventive." American Journal of Health-System Pharmacy 74, no. 15 (2017): 1118. http://dx.doi.org/10.2146/news170047.

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Schinzel, Helmut. "Verlängerte Thromboseprophylaxe: Betrixaban reduziert thromboembolische Ereignisse." DMW - Deutsche Medizinische Wochenschrift 141, no. 22 (2016): 1598. http://dx.doi.org/10.1055/s-0042-117367.

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Raji Reddy, Chada, and Sudam N. Sinare. "Expedient Approach to the Synthesis of Betrixaban." SynOpen 04, no. 03 (2020): 62–65. http://dx.doi.org/10.1055/s-0040-1707267.

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AbstractA new scalable route to synthesize the factor Xa (FXa) inhibitor betrixaban is disclosed. The product is obtained in a seven-step reaction sequence (in five stages using two one-pot reactions) starting from easily accessible 4-(N,N-dimethylcarbamimidoyl)benzoate. Effective isolation of intermediates, use of cost-effective amide formation and 2-methyltetrahydrofuran as an effective reaction solvent as well as for extraction in three of the stages, are key features. The strategy provides the desired product in 38% overall yield with high purity (>98%).

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Sinclair, H. Q., and M. D. Ezekowitz. "The Safety and Tolerability of Betrixaban Therapy." MD Conference Express 10, no. 2 (2010): 14–15. http://dx.doi.org/10.1177/155989771002007.

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Thoenes, Martin, Joan Minguet, Karin Bramlage, Peter Bramlage, and Carmen Ferrero. "Betrixaban – the next direct factor Xa inhibitor?" Expert Review of Hematology 9, no. 12 (2016): 1111–17. http://dx.doi.org/10.1080/17474086.2016.1256194.

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Hussar, Daniel A., and Bradley Inman. "Betrixaban, sofosbuvir/velpatasvir/voxilaprevir, and glecaprevir/pibrentasvir." Journal of the American Pharmacists Association 57, no. 6 (2017): 750–54. http://dx.doi.org/10.1016/j.japh.2017.10.002.

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Mehrotra, Siddharth, Debra Hoppensteadt, Walter Jeske, et al. "Differential Neutralization of Apixaban, Betrixaban, Edoxaban, and Rivaroxaban by Andexanet Alfa as Measured by Whole Blood Thromboelastographic Analysis." Clinical and Applied Thrombosis/Hemostasis 28 (January 2022): 107602962211382. http://dx.doi.org/10.1177/10760296221138297.

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Introduction The available oral anti-Xa agents are routinely used for the management of thrombotic disorders. A molecularly modified recombinant coagulation FXa, also known as Andexanet Alfa (AA), that has been developed as an antidote to neutralize the bleeding effects of oral FXa inhibitors, such as Apixaban and Rivaroxaban. Materials and Methods This study utilized thromboelastography (TEG 5000 Hemostasis System), to investigate the neutralizing effects of AA at different concentrations of oral FXa inhibitors measuring such parameters as R-Time, K-Time, Angle, and Max Amplitude (MA). Apixab

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Raymond, Johanna, Laurent Imbert, Thibault Cousin, et al. "Pharmacogenetics of Direct Oral Anticoagulants: A Systematic Review." Journal of Personalized Medicine 11, no. 1 (2021): 37. http://dx.doi.org/10.3390/jpm11010037.

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Dabigatran, rivaroxaban, apixaban, edoxaban, and betrixaban are direct oral anticoagulants (DOACs). Their inter-individual variability in pharmacodynamics and pharmacokinetics (transport and metabolism) is high, and could result from genetic polymorphisms. As recommended by the French Network of Pharmacogenetics (RNPGx), the management of some treatments in cardiovascular diseases (as antiplatelet agents, oral vitamin K antagonists, and statins) can rely on genetic testing in order to improve healthcare by reducing therapeutic resistance or toxicity. This paper is a review of association studi

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Raymond, Johanna, Laurent Imbert, Thibault Cousin, et al. "Pharmacogenetics of Direct Oral Anticoagulants: A Systematic Review." Journal of Personalized Medicine 11, no. 1 (2021): 37. http://dx.doi.org/10.3390/jpm11010037.

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Dabigatran, rivaroxaban, apixaban, edoxaban, and betrixaban are direct oral anticoagulants (DOACs). Their inter-individual variability in pharmacodynamics and pharmacokinetics (transport and metabolism) is high, and could result from genetic polymorphisms. As recommended by the French Network of Pharmacogenetics (RNPGx), the management of some treatments in cardiovascular diseases (as antiplatelet agents, oral vitamin K antagonists, and statins) can rely on genetic testing in order to improve healthcare by reducing therapeutic resistance or toxicity. This paper is a review of association studi

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Chan, Noel C., Jack Hirsh, Jeffrey S. Ginsberg, and John W. Eikelboom. "Betrixaban (PRT054021): pharmacology, dose selection and clinical studies." Future Cardiology 10, no. 1 (2014): 43–52. http://dx.doi.org/10.2217/fca.13.98.

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Li, Jianye, Ligong Chen, Xilong Yan, Yang Li, Daiyan Wei, and Donghua Wang. "A Facile Method for the Synthesis of Betrixaban." Journal of Chemical Research 39, no. 9 (2015): 524–26. http://dx.doi.org/10.3184/174751915x14400926401559.

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Lekura, Jona, and James S. Kalus. "Overview of betrixaban and its role in clinical practice." American Journal of Health-System Pharmacy 75, no. 15 (2018): 1095–102. http://dx.doi.org/10.2146/ajhp170785.

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Cohen, Alexander T., Robert A. Harrington, Samuel Z. Goldhaber, et al. "Extended Thromboprophylaxis with Betrixaban in Acutely Ill Medical Patients." New England Journal of Medicine 375, no. 6 (2016): 534–44. http://dx.doi.org/10.1056/nejmoa1601747.

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Palladino, Michael, Geno Merli, and Lynda Thomson. "Evaluation of the oral direct factor Xa inhibitor – betrixaban." Expert Opinion on Investigational Drugs 22, no. 11 (2013): 1465–72. http://dx.doi.org/10.1517/13543784.2013.825605.

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Dobesh, Paul P., and Brian J. Trevarrow. "Betrixaban: Safely Reducing Venous Thromboembolic Events with Extended Prophylaxis." American Journal of Medicine 132, no. 3 (2019): 307–11. http://dx.doi.org/10.1016/j.amjmed.2018.08.024.

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Gackowski, Marcin, Mateusz Jędrzejewski, Sri Satya Medicharla, et al. "Novel Thiourea and Oxime Ether Isosteviol-Based Anticoagulants: MD Simulation and ADMET Prediction." Pharmaceuticals 17, no. 2 (2024): 163. http://dx.doi.org/10.3390/ph17020163.

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Activated blood coagulation factor X (FXa) plays a critical initiation step of the blood-coagulation pathway and is considered a desirable target for anticoagulant drug development. It is reversibly inhibited by nonvitamin K antagonist oral anticoagulants (NOACs) such as apixaban, betrixaban, edoxaban, and rivaroxaban. Thrombosis is extremely common and is one of the leading causes of death in developed countries. In previous studies, novel thiourea and oxime ether isosteviol derivatives as FXa inhibitors were designed through a combination of QSAR studies and molecular docking. In the present

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Jasemizad, Tahereh, Lev Bromberg, T. Alan Hatton, and Lokesh P. Padhye. "Oxidation of betrixaban to yield N-nitrosodimethylamine by water disinfectants." Water Research 186 (November 2020): 116309. http://dx.doi.org/10.1016/j.watres.2020.116309.

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Gibson, C. Michael, Rim Halaby, Serge Korjian, et al. "The safety and efficacy of full- versus reduced-dose betrixaban in the Acute Medically Ill VTE (Venous Thromboembolism) Prevention With Extended-Duration Betrixaban (APEX) trial." American Heart Journal 185 (March 2017): 93–100. http://dx.doi.org/10.1016/j.ahj.2016.12.004.

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Lu, Genmin, Francis R. DeGuzman, Sanjay Lakhotia, Stanley J. Hollenbach, David R. Phillips, and Uma Sinha. "Recombinant Antidote for Reversal of Anticoagulation by Factor Xa Inhibitors." Blood 112, no. 11 (2008): 983. http://dx.doi.org/10.1182/blood.v112.11.983.983.

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Abstract Individuals anticoagulated with warfarin or heparin are typically treated with specific antidotes such as vitamin K or protamine, respectively, if they bleed or require surgery. In contrast, specific and effective antidotes are not available for the reversal of the anticoagulant effects of the low molecular weight heparins (LMWH) or the new oral anticoagulants targeting factor Xa (fXa) which are predictably only marginally affected by standard treatments using rfVIIa or fresh frozen plasma. The present study was designed to test the hypothesis that plasma-derived or recombinant fXa, m

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Sylvester, Katelyn W., and Jean M. Connors. "Betrixaban in the prevention of venous thromboembolism in medically ill patients." Future Cardiology 14, no. 6 (2018): 455–70. http://dx.doi.org/10.2217/fca-2018-0052.

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Beyer-Westendorf, Jan, Peter Verhamme, and Rupert Bauersachs. "Betrixaban for prevention of venous thromboembolism in acute medically ill patients." European Heart Journal Supplements 20, suppl_E (2018): E16—E22. http://dx.doi.org/10.1093/eurheartj/suy017.

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Crowther, Mark, Genmin Lu, Janet Leeds, et al. "202: ANDEXANET ALFA REVERSES ANTICOAGULATION INDUCED BY BETRIXABAN IN HEALTHY VOLUNTEERS." Critical Care Medicine 46, no. 1 (2018): 83. http://dx.doi.org/10.1097/01.ccm.0000528221.12371.1b.

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Crowther, Mark, Genmin Lu, Janet M. Leeds, et al. "Reversal of Betrixaban-Induced Anticoagulation in Healthy Volunteers By Andexanet Alfa." Blood 128, no. 22 (2016): 143. http://dx.doi.org/10.1182/blood.v128.22.143.143.

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Abstract Introduction: Andexanet alfa (andexanet) is a modified, recombinant human factor Xa (FXa) molecule that acts as a decoy to bind and sequester FXa inhibitors. We previously reported Phase 2 data with apixaban, rivaroxaban, edoxaban, and enoxaparin in healthy volunteers, and demonstrated that andexanet rapidly reversed pharmacodynamic (PD) markers of anticoagulation. Here, we report new clinical data demonstrating the efficacy of andexanet in reversing the anticoagulant activity of betrixaban, a direct FXa inhibitor which has recently completed a large Phase 3 clinical trial in acute me

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Liu, Lili, Xiujie Liu, Guangling Chen, and Kai Qiu. "Synthesis and Evaluation of in vitro Antiplatelet Aggregation Activities of 2-Methoxy-5-Aminobenzamides." Letters in Drug Design & Discovery 16, no. 9 (2019): 1040–50. http://dx.doi.org/10.2174/1570180816666181128105044.

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Objective: According to the principles of drug design, the structures of picotamide and betrixaban were combined to design novel series of 2-methoxy-5-aminobenzamides. A total of twenty new compounds 1a-1t have been synthesized and evaluated for their antiplatelet aggregation activities in vitro. Methods: In the structural design of target compounds 1a-1t, the betrixaban was retained group characteristics and the picotamide was retained its 1, 3, 4-substitution position. With 2-methoxybenzoic acid as starting material, compounds 1a-1t were synthesized after 5 steps of nitration, acylation, amm

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Siddiqui, Fakiha, Alfonso Tafur, Lorenzo Storino Ramacciotti, et al. "Reversal of Factor Xa Inhibitors by Andexanet Alfa May Increase Thrombogenesis Compared to Pretreatment Values." Clinical and Applied Thrombosis/Hemostasis 25 (January 1, 2019): 107602961986349. http://dx.doi.org/10.1177/1076029619863493.

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Recombinant coagulation factor Xa (FXa), inactivated Zh-zo, also known as andexanet alfa (AA), is a modified version of human FXa that has been developed to neutralize FXa inhibitors. We studied the reversal effect of AA for these inhibitors in various anticoagulant and thrombin generation (TG) assays. Individual aliquots of normal human plasma containing 1 µg/mL of apixaban, betrixaban, edoxaban, and rivaroxaban, were supplemented with saline or AA at a concentration of 100 µg/mL. Clotting profiles include prothrombinase-induced clotting time, activated partial thromboplastin time, and prothr

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Papaj, Katarzyna, Patrycja Spychalska, Patryk Kapica, et al. "Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease." PLOS ONE 17, no. 1 (2022): e0262482. http://dx.doi.org/10.1371/journal.pone.0262482.

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Based on previous large-scale in silico screening several factor Xa inhibitors were proposed to potentially inhibit SARS-CoV-2 Mpro. In addition to their known anticoagulants activity this potential inhibition could have an additional therapeutic effect on patients with COVID-19 disease. In this study we examined the binding of the Apixaban, Betrixaban and Rivaroxaban to the SARS-CoV-2 Mpro with the use of the MicroScale Thermophoresis technique. Our results indicate that the experimentally measured binding affinity is weak and the therapeutic effect due to the SARS-CoV-2 Mpro inhibition is ra

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Cohen, Alexander T. "Extended thromboprophylaxis with betrixaban: a new standard for acute medically ill patients." European Heart Journal Supplements 20, suppl_E (2018): E1—E2. http://dx.doi.org/10.1093/eurheartj/suy014.

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Huang, W., F. Anderson, I. Bucior, WR Neuman, and AT Cohen. "Extended Thromboprophylaxis With Betrixaban Is Cost-Effective In Acutely ILL Medical Patients." Value in Health 21 (May 2018): S61. http://dx.doi.org/10.1016/j.jval.2018.04.369.

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Kalayci, Arzu, C. Gibson, Gerald Chi, et al. "Asymptomatic Deep Vein Thrombosis is Associated with an Increased Risk of Death: Insights from the APEX Trial." Thrombosis and Haemostasis 118, no. 12 (2018): 2046–52. http://dx.doi.org/10.1055/s-0038-1675606.

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Aim Asymptomatic deep vein thrombosis (DVT) diagnosed with compression ultrasound (CUS) is a common endpoint in trials assessing the efficacy of anticoagulants to prevent venous thromboembolism (VTE), but the relationship of asymptomatic thrombus to mortality remains uncertain. Methods In the APEX trial (ClinicalTrials.gov: NCT01583218), 7,513 acutely ill hospitalized medical patients were randomly assigned to extended-duration betrixaban (35–42 days) or enoxaparin (10 ± 4 days). Asymptomatic DVT was assessed once with CUS between day 32 and 47, and mortality was assessed through 77 days. Resu

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Tomić, Maja. "The current place of direct oral anticoagulants in the prevention/treatment of venous thromboembolism." Arhiv za farmaciju 70, no. 5 (2020): 284–96. http://dx.doi.org/10.5937/arhfarm2005284t.

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Venous thromboembolism (VTE; includes deep venous thrombosis, DVT, and pulmonary embolism, PE) represents the third most common acute cardiovascular syndrome. Contemporary VTE management comprises primary prevention in high-risk patients, treatment of established VTE, and prevention of its recurrence (secondary prevention). Anticoagulants are the basis of VTE pharmacological prophylaxis and treatment. For several decades, parenteral (heparin and low-molecular-weight heparins, LMWHs) and oral anticoagulants (vitamin K antagonists, VKAs) have been the cornerstone of VTE prevention/treatment. The

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