- Design of an Ultralow Molecular Weight Heparin That Resists Heparanase Biodegradation. [Journal Article]J Med Chem. 2023 Jan 27 [Online ahead of print]JM
- Heparanase, an endo-β-d-glucuronidase produced by a variety of cells and tissues, cleaves the glycosidic linkage between glucuronic acid (GlcA) and a 3-O- or 6-O-sulfated glucosamine, typified by the disaccharide -[GlcA-GlcNS3S6S]-, which is found within the antithrombin-binding domain of heparan sulfate or heparin. As such, all current forms of heparin are susceptible to degradation by heparanas…
- Publisher Full Text (DOI)
- Modulation of ultralarge immune complexes in heparin-induced thrombocytopenia. [Journal Article]J Thromb Haemost. 2022 Dec 22 [Online ahead of print]JT
- CONCLUSIONS: HIT antigen and immune complexes are dynamic and amenable to modulation. Fondaparinux can be converted from an anticoagulant that acts at a downstream amplification step into a rationale, disease-specific intervention that blocks ULIC formation. Interventions that prevent ULIC formation and stability might increase the efficacy, permit use of lower doses, shorten the duration of antithrombotic therapy, and help prevent this serious thrombotic disorder.
- Publisher Full Text (DOI)
- An Enzymatic Activity Assay for Heparanase That Is Useful for Evaluating Clinically Relevant Inhibitors and Studying Kinetics. [Journal Article]Methods Mol Biol. 2023; 2619:227-238.MM
- The enzyme heparanase cleaves heparan sulfate and is involved in a range of human diseases including cancer, inflammation, diabetes, and viral infection. There is a need for a simple and reliable enzymatic assay to allow for the screening of compounds to find inhibitors of heparanase. We have developed an assay that uses the heparinoid fondaparinux as enzyme substrate and detects one of the produ…
- Publisher Full Text (DOI)
- Novel fondaparinux protocol for anticoagulation therapy in adults with renal failure and suspected heparin-induced thrombocytopenia: a retrospective review of institutional protocol. [Journal Article]
- CONCLUSIONS: Fondaparinux can be safely used in kidney failure using our protocol. However, despite its safety profile and relative success, this case series was small. More robust studies need to be conducted prior to drawing conclusions.
- PMC Free PDF
- Efficacy of 11 anticoagulants for the prevention of venous thromboembolism after total hip or knee arthroplasty: A systematic review and network meta-analysis. [Meta-Analysis]
- CONCLUSIONS: Apixaban, edoxaban, fondaparinux, rivaroxaban, and darexaban have the best efficacy for the prevention of VTE after total hip or knee arthroplasty.
- PMC Free PDF
- Impact of surface coating and systemic anticoagulants on hemostasis and inflammation in a human whole blood model. [Journal Article]
- CONCLUSIONS: The MPC-based protocols demonstrated better hemocompatibility compared to CHC, and ENOX and FPX proved useful for additional anticoagulation. Furthermore, this simple-to-use whole blood model may be useful for experimental analyses of the early coagulatory and immunological response without decalcification.
- PMC Free PDF
- Fondaparinux Sodium: Recent Advances in the Management of Thrombosis. [Review]J Cardiovasc Pharmacol Ther. 2023 Jan-Dec; 28:10742484221145010.JC
- Fondaparinux sodium is a chemically synthesized selective factor Xa inhibitor approved for the prevention and treatment of venous thromboembolic events, that is, deep vein thrombosis, pulmonary embolism, and superficial vein thrombosis, in acutely ill (including those affected by COVID-19 or cancer patients) and those undergoing surgeries. Since its approval in 2002, the efficacy and safety of fo…
- Publisher Full Text (DOI)
- Design and Synthesis of Neutralizable Fondaparinux. [Journal Article]
- Fondaparinux, a clinically approved anticoagulant pentasaccharide for the treatment of thrombotic diseases, displays better efficacy and biosafety than other heparin-based anticoagulant drugs. However, there is no suitable antidote available for fondaparinux to efficiently manage its potential bleeding risks, thereby precluding its widespread use. Herein, we describe a convergent and stereocontro…
- PMC Free PDF
- Heparin-Induced Thrombocytopenia at the Emergency Department Due to Intermittent Heparin Flush in a Patient Undergoing Stem Cell Transplant. [Case Reports]
- Heparin-induced thrombocytopenia (HIT) is an adverse reaction to heparin products, but not warfarin. HIT usually occurs 5‒10 days after exposure to heparin. Here, we report a case of HIT with multiple thrombotic events and severe thrombocytopenia resulting from intermittent intravenous heparin flushes for maintenance of a newly placed subclavian central venous catheter (CVC) for stem cell transpl…
- PMC Free PDF
- Time trends in antithrombotic therapy prescription patterns: Real-world monocentric study in hospitalized patients with atrial fibrillation. [Journal Article]World J Cardiol. 2022 Nov 26; 14(11):576-598.WJ
- CONCLUSIONS: Real-world patients with AF are elderly and affected by cardiovascular and non-cardiovascular diseases. The percentage of patients on OAT and DOACs increased. These data suggest a slow, gradual guidelines implementation process.
- PMC Free PDF
- Potential Application of Recombinant Snake Prothrombin Activator Ecarin in Blood Diagnostics. [Journal Article]
- We describe here the purification and cloning of a codon-optimized form of the snake prothrombin activator ecarin from the saw scaled viper (Echis carinatus) expressed in mammalian cells. Expression of recombinant ecarin (rEcarin) was carried out in human embryonic kidney cells (HEK) cells under conditions for the development and performance of a novel and scalable recombinant snake ecarin to ind…
- PMC Free PDF
- Promising Drug Fondaparinux for the Treatment of COVID-19: an In Silico Analysis of Low Molecular Weight Heparin, Direct Oral Anticoagulant, and Antiplatelet Drug Interactions with Host Protease Furin. [Journal Article]
- CONCLUSIONS: Our findings have shown that LMWHs and fondaparinux can be used for their possible antiviral effects in COVID-19 patients. Our results have shown that in accordance with heparin and LMWH, fondaparinux can also be a candidate for "drug repurposing" in COVID-19 therapy, not only because of their anticoagulant but also possible antiviral effects.
- PMC Free PDF
- Features of Parenteral Anticoagulant Therapy in Patients With Myocardial Infarction According to the Russian Register of Acute Myocardial Infarction - REGION-IM. [Multicenter Study]Kardiologiia. 2022 Oct 30; 62(10):3-15.K
- Aim To study specific features of the parenteral anticoagulant therapy for acute myocardial infarction (MI) in the Russian Federation and to evaluate the consistency of the prescribed parenteral anticoagulant therapy with the effective clinical guidelines.Material and methods REGION-MI, the Russian rEGIstry for acute myOcardial iNfarction, is a multicenter observational study. This registry inclu…
- Publisher Full Text (DOI)
- Clinical outcomes of cancer-associated isolated superficial vein thrombosis in daily practice. [Journal Article]Thromb Res. 2022 12; 220:145-152.TR
- Publisher Full Text (DOI)
- Low-Molecular-Weight Heparins (LMWH) and Synthetic Factor X Inhibitors Can Impair the Osseointegration Process of a Titanium Implant in an Interventional Animal Study. [Journal Article]
- Background and objectives: Cementless total hip arthroplasty is a common surgical procedure and perioperative thromboprophylaxis is used to prevent deep vein thrombosis or pulmonary embolism. Osseointegration is important for long-term implant survival, and there is no research on the effect of different thromboprophylaxis agents on the process of osseointegration. Materials and Methods: Seventy …
- PMC Free PDF
- Proline-Rich Region II (PRR2) Plays an Important Role in Tau-Glycan Interaction: An NMR Study. [Journal Article]
- (1) Background: Prion-like transcellular spreading of tau pathology in Alzheimer's disease (AD) is mediated by tau binding to the cell-surface glycan heparan sulfate (HS). However, the structural determinants for tau-HS interaction are not well understood. (2) Methods and Results: Binding-site mapping using NMR showed two major binding regions in full-length tau responsible for heparin interactio…
- PMC Free PDF
- Effectiveness of Fondaparinux in the Japanese Population with Acute Venous Thromboembolism -A Study Comparing Patients with and without Cancer. [Journal Article]Intern Med. 2022 Nov 02 [Online ahead of print]IM
- Objective Venous thromboembolism (VTE) is a common cancer complication. Patients with cancer have a high risk of recurrent VTE and bleeding. We analyzed the effectiveness of VTE treatment via subcutaneous fondaparinux injection for patients with and without cancer. Methods and Materials This study included 260 inpatients who had received fondaparinux therapy. Fondaparinux's therapeutic effect was…
- Publisher Full Text (DOI)
- Anticoagulants as Potential SARS-CoV-2 Mpro Inhibitors for COVID-19 Patients: In Vitro, Molecular Docking, Molecular Dynamics, DFT, and SAR Studies. [Journal Article]
- In this article, 34 anticoagulant drugs were screened in silico against the main protease (Mpro) of SARS-CoV-2 using molecular docking tools. Idraparinux, fondaparinux, eptifibatide, heparin, and ticagrelor demonstrated the highest binding affinities towards SARS-CoV-2 Mpro. A molecular dynamics study at 200 ns was also carried out for the most promising anticoagulants to provide insights into th…
- PMC Free PDF
- A case of aseptic bilateral cavernous sinus thrombosis following a recent inactivated SARS-CoV-2 vaccination. [Case Reports]
- This case report aims to describe the first report of bilateral aseptic cavernous sinus thrombosis (CST) with a recent history of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) vaccination. A 50-year-old woman presented with bilateral proptosis, decreased vision, and ophthalmoplegia 16 days following CoronaVac® vaccine. The visual acuity of the left eye was 20/150, while the right e…
- PMC Free PDF
- Facile chemoenzymatic synthesis of unmodified anticoagulant ultra-low molecular weight heparin. [Journal Article]Org Biomol Chem. 2022 Nov 02; 20(42):8323-8330.OB
- A chemoenzymatic approach, mimicking the biosynthetic pathway of heparin and heparan sulfate (HS), has been well developed to prepare a series of structurally well-defined heparin oligosaccharides with excellent anticoagulant activity in good overall yields. The current chemoenzymatic synthesis typically begins with an unnatural glycosyl acceptor, p-nitrophenyl glucuronide (GlcA-PNP), which is co…
- Publisher Full Text (DOI)
- Safety and effectiveness of fondaparinux as a postpartum thromboprophylaxis during puerperium among muslim women: A single centre prospective study. [Journal Article]
- Background: Venous thromboembolism (VTE) remains one of the leading causes of maternal morbidity and mortality, with postpartum period carrying the greatest risk. Perinatal thromboprophylaxis is often administered based on risk-factor assessment. Low molecular weight heparin has a proven safety profile in the obstetrics population, however, its porcine-derived content may lead to reduced uptake a…
- PMC Free PDF
- Current and emerging drug strategies for the prevention of venous thromboembolism in acutely ill medical inpatients. [Journal Article]Expert Opin Pharmacother. 2022 Oct; 23(14):1651-1665.EO
- Venous thromboembolism (VTE) is a common complication in patients hospitalized for acute medical illnesses. Therefore, medical inpatients require a careful VTE and bleeding risk assessment to drive optimal strategies for VTE prevention. Low molecular weight heparin and fondaparinux have long been used for inhospital prophylaxis for patients at increased risk of VTE. The selection of patients who …
- Publisher Full Text (DOI)
- The use of fondaparinux and rituximab for recurrent thrombotic events in antiphospholipid syndrome. [Journal Article]
- Limited evidence exists to guide the management of recurrent thrombosis occurring despite therapeutic anticoagulation in patients with thrombotic antiphospholipid syndrome (APS). In this case series, fondaparinux, with or without an antiplatelet agent, provided an effective and safe option in three patients with thrombotic APS, all two triple and one single positive for antiphospholipid antibodie…
- PMC Free PDF
- Native and activated antithrombin inhibits TMPRSS2 activity and SARS-CoV-2 infection. [Journal Article]
- Host cell proteases such as TMPRSS2 are critical determinants of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) tropism and pathogenesis. Here, we show that antithrombin (AT), an endogenous serine protease inhibitor regulating coagulation, is a broad-spectrum inhibitor of coronavirus infection. Molecular docking and enzyme activity assays demonstrate that AT binds and inhibits TMPRS…
- PMC Free PDF
- Treatment modalities in cancer-associated venous thromboembolism (VTE). [Review]Best Pract Res Clin Haematol. 2022 03; 35(1):101354.BP
- Anticoagulation is the cornerstone of cancer-associated VTE treatment, including vitamin K antagonists (VKA), unfractionated heparin (UFH), fondaparinux, low-molecular-weight heparins (LMWH) and direct oral anticoagulants (DOACs). The goals of anticoagulant therapy in cancer patients with cancer-associated thrombosis (CAT) are to improve symptoms, reduce risk of recurrent VTE or fatal pulmonary e…
- Publisher Full Text (DOI)
- The pharmacology of anticoagulant drug treatment options in COVID-19 patients: reviewing real-world evidence in clinical practice. [Journal Article]
- The optimal anticoagulation strategy for venous thromboembolism (VTE) prevention among COVID-19 patients, hospitalized or in the community setting, is still challenging and largely based on real-world evidence.
- Publisher Full Text (DOI)
- The role of antiaggregant agents and anticoagulants in the prevention of aortic valve endocarditis: A double-cohort retrospective study. [Journal Article]
- CONCLUSIONS: Ac were associated with IE in both cohorts, whereas Ag were not associated with PVE. This might reflect differences in the studied populations, with Ag and Ac being prescribed for conditions associated with long-term IE risk in the NVE cohort. Therefore, determining the potential protective effect of Ag and Ac will necessitate further well-controlled studies.
- PMC Free PDF
- Thromboprophylaxis for venous thromboembolism prevention in hospitalized patients with cirrhosis: Guidance from the SSC of the ISTH. [Journal Article]J Thromb Haemost. 2022 10; 20(10):2237-2245.JT
- Hospital-associated venous thromboembolism (HA-VTE) is a major cause of morbidity and mortality and is internationally recognized as a significant patient safety issue. While cirrhosis was traditionally considered to predispose to bleeding, these patients are also at an increased risk of VTE, with an associated increase in mortality. Hospitalization rates of patients with cirrhosis are increasing…
- Publisher Full Text (DOI)
- Recurrent thrombosis rescued by fondaparinux in high-risk patients: A case series. [Case Reports]
- CONCLUSIONS: With fondaparinux, no thrombosis progression was observed, and no bleeding complications occurred.
- PMC Free PDF
- Deep vein thrombosis after insertion of a central venous catheter: a case report. [Case Reports]
- A male patient aged 50 years, presented with a swelling in the right leg which had occurred five days before hospital admission. This was associated with pain in the swollen leg. The patient had a history of femoral double lumen catheter (DLC) insertion for hemodialysis. On physical examination, Wong Baker's scale was 3, Wells' score was 3, and the patient had edematous, red, and warm right lower…
- PMC Free PDF