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https://www.readbyqxmd.com/read/29475063/characterization-of-a-novel-selective-factor-xa-inhibitor-djt06001-which-reduces-thrombus-formation-with-low-risk-of-bleeding
#1
Xuefeng Hu, Ying Xiao, Chuan Yu, Yinglin Zuo, Wen Yang, Xinan Wang, Baohua Gu, Jing Li
Factor Xa (FXa) is a serine protease that plays key roles in linking the intrinsic and extrinsic coagulation pathways to the final common pathway. DJT06001 is an oral, highly specific and direct FXa inhibitor for the prevention and treatment of thromboembolic diseases. We characterized the compound in vitro and studied its in vivo activity in rat thrombosis models, as well as bleeding risk and Pharmacokinetics and Pharmacodynamics (PK/PD) relationship. DJT06001 inhibited free FXa with an inhibitory constant (Ki) of 0...
February 20, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29474926/the-fibrogenic-actions-of-the-coagulant-and-plasminogen-activation-systems-in-pulmonary-fibrosis
#2
REVIEW
Michael Schuliga, Christopher Grainge, Glen Westall, Darryl Knight
Fibrosis causes irreversible damage to lung structure and function in restrictive lung diseases such as idiopathic pulmonary fibrosis (IPF). Extravascular coagulation involving fibrin formation in the intra-alveolar compartment is postulated to have a pivotal role in the development of pulmonary fibrosis, serving as a provisional matrix for migrating fibroblasts. Furthermore, proteases of the coagulation and plasminogen activation (plasminergic) systems that form and breakdown fibrin respectively directly contribute to pulmonary fibrosis...
February 20, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29468977/the-development-of-new-factor-xa-inhibitors-based-on-amide-synthesis
#3
Dmitry Tarasov, Dmitry Tovbin, Dmitry Malakhov, Arseniy Aybush, Natalia Tserkovnikova, Marina Savelyeva, Dmitry Sychev, Natalia Drozd, Alla Savchenko
BACKGROUND: Factor Xa (FXa) is known to play a central role in a blood coagulation cascade and considered to be one of the most attractive targets for oral anticoagulants of new generation. OBJECTIVE: Our approach for the development of directly acting oral anticoagulants (DOAC), FXa inhibitors was demonstrated in this work. METHOD: Chemical synthesis is the base of our approach for the development of potential inhibitors. In this work, the substances like R1-(CONH)-R2-(CONH)-R3 are being developed, using previously described docking and screening methods, where R1, R2, R3 are some chemical groups, (CONH) are amid bonds connecting R1, R2 and R3...
February 14, 2018: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29455567/apixaban-or-rivaroxaban-versus-warfarin-for-treatment-of-submassive-pulmonary-embolism-after-catheter-directed-thrombolysis
#4
Lara M Groetzinger, Taylor J Miller, Ryan M Rivosecchi, Roy E Smith, Mark T Gladwin, Belinda N Rivera-Lebron
BACKGROUND: Little data exist on the use of direct oral anticoagulant (DOAC) factor Xa inhibitors for submassive pulmonary embolism (PE) after catheter-directed thrombolysis (CDT). The objective of this evaluation was to determine whether the transition from parenteral anticoagulation to DOACs for submassive PE after CDT would decrease hospital length of stay (LOS) compared to warfarin. METHODS: A retrospective review of patients diagnosed with submassive PE who underwent CDT was conducted from January 1, 2012, to February 28, 2017...
January 1, 2018: Clinical and Applied Thrombosis/hemostasis
https://www.readbyqxmd.com/read/29452445/suppressive-role-of-tissue-factor-pathway-inhibitor-%C3%AE-in-platelet-dependent-fibrin-formation-under-flow-is-restricted-to-low-procoagulant-strength
#5
Stella Thomassen, Tom G Mastenbroek, Frauke Swieringa, Kristien Winckers, Marion A H Feijge, Roy Schrijver, Judith M E M Cosemans, Susan A Maroney, Alan E Mast, Tilman M Hackeng, Johan W M Heemskerk
Tissue factor pathway inhibitor-alpha (TFPI-α) is a Kunitz-type serine protease inhibitor, which suppresses coagulation by inhibiting the tissue factor (TF)/factor VIIa complex as well as factor Xa. In static plasma-phospholipid systems, TFPI-α thus suppresses both factor Xa and thrombin generation. In this article, we used a microfluidics approach to investigate how TFPI-α regulates fibrin clot formation in platelet thrombi at low wall shear rate. We therefore hypothesized that the anticoagulant effect of TFPI-α in plasma is a function of the local procoagulant strength-defined as the magnitude of thrombin generation under flow, due to local activities of TF/factor VIIa and factor Xa...
February 16, 2018: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/29451685/a-quantitative-lc-msms-method-for-determination-of-edoxaban-a-xa-inhibitor-and-its-pharmacokinetic-application-in-patients-after-total-knee-arthroplasty
#6
Kazuhiko Hanada, Shin-Ichi Matsumoto, Soichi Shibata, Hajime Matsubara, Yasunori Tsukimura, Harumi Takahashi
Edoxaban was extracted from human plasma by simple protein precipitation with acetonitrile, followed by quantitative determination using a liquid chromatography-mass spectrometry method. The recoveries of edoxaban and the internal standard (ticlopidine) from human plasma were higher than 85%, and the within- and between-day coefficients of variation were within 15%. The limit of quantification in human plasma was 1 ng/mL. The concentration of edoxaban in blood decreased at room temperature, but remained unchanged for 1 week at 4°C...
February 16, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29406387/in-silico-thrombin-and-factor-xa-generation-profiles-in-adult-patients-after-fontan-operation
#7
Matthew Gissel, Lidia Tomkiewicz-Pajak, Piotr Podolec, Piotr Hoffman, Olga Trojnarska, Magdalena Lipczyńska, Anetta Undas, Kathleen E Brummel-Ziedins
: Single-ventricle defects are associated with increased risk of thromboembolic events. To analyze the prothrombotic potential in a long-term follow-up on Fontan patients via plasma contribution to thrombin and factor (F)Xa generation profiles. Thrombin and FXa generation was simulated from plasma concentrations of FII, FV, FVII, FVIII, FIX, FX, antithrombin and tissue factor (TF) pathway inhibitor from Fontan patients (n = 48) and healthy controls (n = 34). TF and thrombin-antithrombin complex (TAT) were measured by ELISA...
February 5, 2018: Blood Coagulation & Fibrinolysis: An International Journal in Haemostasis and Thrombosis
https://www.readbyqxmd.com/read/29391805/role-of-rivaroxaban-in-the-management-of-atrial-fibrillation-insights-from-clinical-practice
#8
REVIEW
Kavitha Vimalesvaran, Seth J Dockrill, Diana A Gorog
Atrial fibrillation (AF) is the most common sustained cardiac arrhythmia, and it leads to significant morbidity and mortality, predominantly from ischemic stroke. Vitamin K antagonists, mainly warfarin, have been used for decades to prevent ischemic stroke in AF, but their use is limited due to interactions with food and other drugs, as well as the requirement for regular monitoring of the international normalized ratio. Rivaroxaban, a direct factor Xa inhibitor and the most commonly used non-vitamin K oral anticoagulant, avoids many of these challenges and is being prescribed with increasing frequency for stroke prevention in non-valvular AF...
2018: Vascular Health and Risk Management
https://www.readbyqxmd.com/read/29390574/a-case-report-of-parenchymal-hematoma-after-intravenous-thrombolysis-in-a-rivaroxaban-treated-patient-is-it-a-true-rivaroxaban-hemorrhagic-complication
#9
Eugenia Rota, Gianluca Bruzzone, Sergio Agosti, Roberto Pastorino, Nicola Morelli
RATIONALE: To date, the only treatment approved for acute ischemic strokes is thrombolysis. Whether intravenous thrombolysis may be safe in patients taking direct oral anticoagulants (DOACs) is currently a matter of debate. PATIENT CONCERNS: A 74-year-old woman, who was on rivaroxaban 20 mg/d for nonvalvular atrial fibrillation, was admitted to our stroke unit with left-sided hemiparesis and aphasia. The onset of neurologic deficits had occurred 5 hours after the last rivaroxaban dose...
December 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29389673/low-molecular-weight-heparin-versus-rivaroxaban-in-the-treatment-of-venous-thromboembolism-in-gastrointestinal-malignancies
#10
Hannah K Choe, Maria T De Sancho, Sunnie S Kim, Tong Dai, Manish A Shah
: Due to their ease of use, the direct oral anticoagulants (DOACs) are an attractive treatment option for cancer-associated venous thromboembolism (VTE) and have been readily adopted by many clinicians. A recent published study comparing a DOAC (edoxaban) to the current standard-of-care low molecular weight heparin dalteparin for the treatment of cancer-associated thrombosis showed that edoxaban was noninferior to dalteparin for recurrent VTE, but the risk of major bleeding was higher. We present three patients with high-risk gastrointestinal malignancies complicated by cancer-associated VTE with progression of thrombosis while treated with the oral direct Xa inhibitor rivaroxaban...
January 31, 2018: Blood Coagulation & Fibrinolysis: An International Journal in Haemostasis and Thrombosis
https://www.readbyqxmd.com/read/29386864/betrixaban-bevyxxa-a-direct-acting-oral-anticoagulant-factor-xa-inhibitor
#11
Jessica W Skelley, Angela R Thomason, Jeffery C Nolen, PharmD Candidate
Betrixaban (Bevyxxa): a direct-acting oral anti-coagulant factor Xa inhibitor.
February 2018: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/29376487/surfing-the-blood-coagulation-cascade-insight-into-the-vital-factor-xa
#12
Nicolas E Nunez-Navarro, Fabian M Santana, Loreto P Parra, Flavia C Zacconi
Factor Xa (FXa) plays a key role in haemostasis, it is a central part of the blood coagulation cascade which catalyzes the production of thrombin and leads to clot formation and wound closure. Therefore, FXa is an attractive target for the development of new anticoagulant agents. In this review, we will first describe the molecular features of this fundamental protein in order to understand its mechanism of action, an essential background for the design of novel inhibitors by means of synthetic organic chemistry or using peptides obtained from recombinant methodologies...
January 25, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29372400/andexanet-alfa-to-reverse-the-anticoagulant-activity-of-factor-xa-inhibitors-a-review-of-design-development-and-potential-place-in-therapy
#13
REVIEW
Michelangelo Sartori, Benilde Cosmi
Direct oral anticoagulants are associated with rates of major bleeding which are not negligible, albeit lower than those associated with vitamin K antagonists. No specific reversal agent for factor Xa (FXa) direct inhibitors is currently available for clinical use. A modified activated human FXa decoy protein, andexanet alfa, is being developed that binds FXa direct inhibitors in their active site, thus reversing their anticoagulant effect. The purpose of this article is to review the design, development and clinical trials of andexanet alfa...
January 25, 2018: Journal of Thrombosis and Thrombolysis
https://www.readbyqxmd.com/read/29360845/non-vitamin-k-antagonist-oral-anticoagulants-versus-warfarin-for-the-prevention-of-spontaneous-echo-contrast-and-thrombus-in-patients-with-atrial-fibrillation-or-flutter-undergoing-cardioversion-a-trans-esophageal-echocardiography-study
#14
Yun Gi Kim, Jong-Il Choi, Mi-Na Kim, Dong-Hyuk Cho, Suk-Kyu Oh, Hyungdon Kook, Hee-Soon Park, Kwang No Lee, Yong-Soo Baek, Seung-Young Roh, Jaemin Shim, Seong-Mi Park, Wan Joo Shim, Young-Hoon Kim
Spontaneous echo-contrast (SEC) and thrombus observed in trans-esophageal echocardiography (TEE) is known as a strong surrogate marker for future risk of ischemic stroke in patients with atrial fibrillation (AF) or atrial flutter (AFL). The efficacy of non-vitamin K antagonist oral anticoagulants (NOAC) compared to warfarin to prevent SEC or thrombus in patients with AF or AFL is currently unknown. AF or AFL patients who underwent direct current cardioversion (DCCV) and pre-DCCV TEE evaluation from January 2014 to October 2016 in a single center were analyzed...
2018: PloS One
https://www.readbyqxmd.com/read/29345686/reversal-agents-for-non-vitamin-k-antagonist-oral-anticoagulants
#15
REVIEW
Jerrold H Levy, James Douketis, Jeffrey I Weitz
The non-vitamin K antagonist oral anticoagulants (NOACs) include dabigatran, which inhibits thrombin, and apixaban, betrixaban, edoxaban, and rivaroxaban, which inhibit coagulation factor Xa. Although clinical studies of NOACs were conducted without antidotes, patient outcomes with major bleeding when receiving NOACs were no worse than those in patients treated with a vitamin K antagonist. Nonetheless, in patients with life-threatening bleeding or requiring urgent surgery, the capacity for rapid NOAC reversal is likely to increase patient safety...
January 18, 2018: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/29338293/betrixaban-a-new-oral-factor-xa-inhibitor-for-extended-venous-thromboembolism-prophylaxis-in-high-risk-hospitalized-patients
#16
Scott G Garland, Christina E DeRemer, Steven M Smith, John G Gums
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...
January 1, 2018: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29337837/accidental-rivaroxaban-intoxication-in-a-boy-some-lessons-in-managing-new-oral-anticoagulants-in-children
#17
Julieta Weirthein, Dennis Scolnik, Nili Yanai Milshtein, Tali Capua, Miguel Glatstein
Novel oral anticoagulants offer equivalent or improved therapeutic profiles compared with warfarin, with less risk of bleeding, no interactions with food, and no need for routine laboratory monitoring. Caution must be exercised in using these drugs in certain patient populations, for example, renal insufficiency, those receiving additional antithrombotic therapy, those with questionable compliance, children, and those with a high risk of gastrointestinal bleeding. One of the novel oral anticoagulants, rivaroxaban, is a direct Factor Xa inhibitor, used to reduce risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation, deep vein thrombosis, and pulmonary embolism...
January 15, 2018: Pediatric Emergency Care
https://www.readbyqxmd.com/read/29335786/anti-inflammatory-and-antiplatelet-effects-of-non-vitamin-k-antagonist-oral-anticoagulants-in-acute-phase-of-ischemic-stroke-patients
#18
Taizen Nakase, Junta Moroi, Tatsuya Ishikawa
BACKGROUND: Recently, non-vitamin K antagonist oral anticoagulants such as direct thrombin and direct factor Xa inhibitors have been prescribed for prevention of embolic stroke. While in Japan, argatroban, also a direct thrombin inhibitor, is available for the treatment of atherothrombotic stroke patients. This study aimed to explore whether there is any differences between direct thrombin and direct factor Xa inhibitors regarding the inhibiting effect against thrombogenesis in the clinical setting of acute ischemic stroke...
January 12, 2018: Clinical and Translational Medicine
https://www.readbyqxmd.com/read/29325495/management-of-cancer-associated-venous-thromboembolism-a-case-based-practical-approach
#19
Minna Voigtlaender, Florian Langer
In patients with solid tumours or haematological malignancies, venous thromboembolism (VTE) is a leading cause of death and significantly contributes to morbidity and healthcare resource utilization. Current practice guidelines recommend long-term anticoagulation with low-molecular-weight heparin (LMWH) as the treatment of choice for cancer-associated VTE, based on clinical trial data showing an overall improved safety and efficacy profile of LMWH compared to vitamin K antagonists. However, several open questions remain, e...
January 12, 2018: VASA. Zeitschrift Für Gefässkrankheiten
https://www.readbyqxmd.com/read/29321328/activities-of-thrombin-and-factor-xa-are-essential-for-replication-of-hepatitis-e-virus-and-are-possibly-implicated-in-the-orf1-polyprotein-processing
#20
Gayatri D Kanade, Kunal D Pingale, Yogesh A Karpe
Hepatitis E virus (HEV) is a clinically important positive-sense RNA virus. The ORF1 of HEV encodes a non-structural polyprotein of 1693 amino acids. It is not clear whether the ORF1 polyprotein is processed into distinct enzymatic domains. Many researchers have attempted to understand the mechanisms of pORF1 processing. However, these studies gave varied results and could never convincingly establish the mechanism of pORF1 processing. In this study, we demonstrated the possible role of thrombin and factor Xa in pORF1 processing...
January 10, 2018: Journal of Virology
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