Thrombin inhib 
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  • ||||||||||  bivalirudin / Generic mfg.
    Clinical, Review, Journal:  A Review of Bivalirudin for Pediatric and Adult Mechanical Circulatory Support. (Pubmed Central) -  Dec 16, 2021   
    A literature search identified ten studies in which bivalirudin was used in extracorporeal membrane oxygenation and five studies in which it was used in ventricular assist devices. The purpose of this review was to summarize the currently available literature for bivalirudin use for mechanical circulatory support in both adult and pediatric patients.
  • ||||||||||  Clinical, Review, Journal:  Direct oral anticoagulants for the treatment and prevention of venous thromboembolism in patients with cancer: current evidence. (Pubmed Central) -  Dec 16, 2021   
    Recent randomized clinical trials suggest a role for DOACs in the treatment of VTED in patients with cancer. This review will discuss the existing evidence and future perspectives on the role of DOACs in the treatment of VTE based on the current evidence about their overall efficacy and safety and the limited information in patients with cancer; in addition, we will briefly review their pharmacokinetic properties with special reference to potential interactions.
  • ||||||||||  dabigatran etexilate / Generic mfg.
    Clinical, Journal:  Pitfalls in the assessment of disseminated intravascular coagulation in patients on dabigatran. (Pubmed Central) -  Dec 16, 2021   
    Like the routine coagulation assays, there is a dabigatran concentration dependent effect on the accuracy of fibrinogen and D-dimer assays. Falsely low fibrinogen results due to dabigatran may confound the assessment of DIC and diagnostic laboratories need to evaluate the performance of their own reagents.
  • ||||||||||  paracetamol / Generic mfg.
    Journal:  Factor XIII cross-links fibrin(ogen) independent of fibrin polymerization in experimental acute liver injury. (Pubmed Central) -  Dec 16, 2021   
    The objective of this study was to determine the mechanisms of fibrin polymerization and cross-linking in acute liver injury induced by acetaminophen (APAP) overdose...In biochemical assays, peroxynitrite inhibited thrombin-mediated fibrin polymerization in a concentration-dependent manner without affecting fibrin(ogen) cross-linking over time. These studies depict a unique pathology wherein thrombin-catalyzed fibrin polymerization is circumvented to allow tissue deposition and FXIII-dependent fibrin(ogen) cross-linking.
  • ||||||||||  Journal:  Impaired Fibrinolysis in the Antiphospholipid Syndrome. (Pubmed Central) -  Dec 16, 2021   
    This review aims to summarize the present knowledge of the mechanisms involved in impaired fibrinolysis in APS patients. We also present a case from clinical practice as an illustration of fibrinolysis impairment in APS patients from a real-life setting.
  • ||||||||||  Journal:  Synthesis and evaluation of peptidic thrombin inhibitors bearing acid-stable sulfotyrosine analogues. (Pubmed Central) -  Dec 16, 2021   
    In order to overcome the inherent instability of the native modification, we report the synthesis of two sulfonate analogues and their incorporation into two thrombin-inhibiting sulfopeptides. The effective mimicry of these sulfonate analogues for native sulfotyrosine was validated in the context of their thrombin inhibitory activity and binding mode, as determined by X-ray crystallography.
  • ||||||||||  Clinical, Review, Journal:  Anticoagulation in patients with kidney failure on dialysis: factor XI as a therapeutic target. (Pubmed Central) -  Dec 16, 2021   
    However, FXI is emerging as a potential safer target for new anticoagulants because FXI plays a greater part in thrombosis than in hemostasis. In this paper, we (a) explain the rationale for considering anticoagulation therapy in patients with kidney failure to reduce atherothrombotic events, (b) highlight the limitations of current anticoagulants in this patient population, (c) explain the potential benefits of FXI inhibitors, and (d) summarize ongoing studies investigating FXI inhibition in patients with kidney failure on dialysis.
  • ||||||||||  Journal:  Identification of a substrate-like cleavage-resistant thrombin inhibitor from the saliva of the flea Xenopsylla cheopis. (Pubmed Central) -  Dec 16, 2021   
    The crystal structure of XC-43 in complex with thrombin shows that despite its substrate-like binding mode, XC-43 is not detectably cleaved by thrombin and that it interacts with the thrombin surface from the enzyme catalytic site through the fibrinogen-binding exosite I. The low rate of hydrolysis was verified in solution experiments with XC-43 which show the substrate to be largely intact after two hours of incubation with thrombin at 37° C. The low rate of XC-43 cleavage by thrombin may be attributable to specific changes in the catalytic triad observable in the crystal structure of the complex or to extensive interactions in the prime sites that may stabilize the binding of cleavage products. Based on the increased arterial occlusion time, tail bleeding time, and blood coagulation parameters in rat models of thrombosis XC-43 could be valuable as an anticoagulant.
  • ||||||||||  Clinical, Journal:  Factor Xa Inhibitors for Patients after Mechanical Heart Valve Replacement? (Pubmed Central) -  Dec 13, 2021   
    Finally, DOACs seem to represent a feasible treatment option in patients with mechanical heart valves, but further studies are needed to evaluate clinical safety. In addition to the ongoing PROACT Xa trial with apixaban in patients after aortic On-X valve implantation, studies in an all-comer collective with rivaroxaban could be promising.
  • ||||||||||  Review, Journal:  Anticoagulants for acute ischaemic stroke. (Pubmed Central) -  Nov 29, 2021   
    Treatment with anticoagulants reduced recurrent stroke, deep vein thrombosis, and pulmonary embolism but increased bleeding risk. Data do not support the routine use of any of the currently available anticoagulants for acute ischaemic stroke.
  • ||||||||||  cisplatin / Generic mfg., dabigatran etexilate / Generic mfg.
    Journal:  Dabigatran mitigates cisplatin-mediated nephrotoxicity through down regulation of thrombin pathway. (Pubmed Central) -  Nov 21, 2021   
    However, pretreatment of animals with either low or high doses of Dab significantly improved kidney function and decreased oxidative stress and apoptotic markers. We conclude that thrombin is an important factor in the pathogenesis of CDDP kidney toxicity via activation of ERK1/2, P53 and caspase-3 pathway, which can be effectively blocked by Dab.
  • ||||||||||  Review, Journal:  G-quadruplex-based aptamers targeting human thrombin: Discovery, chemical modifications and antithrombotic effects. (Pubmed Central) -  Nov 17, 2021   
    Considering the growing need of new efficient anticoagulant agents associated with the strong therapeutic potential of these thrombin inhibitors, the research on thrombin binding aptamers is still a very hot and intriguing field. Herein, we comprehensively described the state-of-the-art knowledge on the DNA-based aptamers targeting thrombin, especially focusing on the optimized analogues obtained by chemically modifying the oligonucleotide backbone, and their biological performances in therapeutic applications.
  • ||||||||||  Integrilin (eptifibatide) / Takeda, Activase (alteplase) / Roche, Boehringer Ingelheim, Kyowa Kirin, Mitsubishi Tanabe
    Clinical, P3 data, Journal:  The multiarm optimization of stroke thrombolysis phase 3 acute stroke randomized clinical trial: Rationale and methods. (Pubmed Central) -  Nov 16, 2021   
    These results suggest that the enzyme may have characteristics of a trypsin or serine-like enzyme with fibrinolytic and thrombolytic activities and may have potential as an antithrombotic agent for blood clotting disorders. Multiarm optimization of stroke thrombolysis is an innovative and collaborative project that is the culmination of many years of dedicated efforts to improve outcomes for stroke patients.
  • ||||||||||  argatroban / Generic mfg.
    Clinical, Journal:  Use of Argatroban in Donor Lung Procurement: A Case Report. (Pubmed Central) -  Nov 12, 2021   
    CONCLUSIONS The ultimate success of grafts without thromboembolic complications suggests the use of argatroban in multiorgan procurement in the setting of a HIT-positive recipient is safe and effective. This case report highlights an alternative to the traditional process of organ procurement with heparin, in which patients at risk of coagulopathies secondary to HIT are able to receive organs when traditional protocols would otherwise be prohibitive.
  • ||||||||||  bivalirudin / Generic mfg.
    [VIRTUAL] RETROSPECTIVE EVALUATION OF BIVALIRUDIN DOSING IN PATIENTS WITH RENAL IMPAIRMENT () -  Nov 9, 2021 - Abstract #ACFORUM2021ACFORUM_1;    
    Ideally, TG and thrombin dynamics simulation could in the future contribute to the management of patients undergoing AT targeting therapy. Based on the results of this study, bivalirudin starting doses should be based on renal function, and institutional guidelines should be optimized to achieve timely therapeutic DTI levels in patients with renal dysfunction.
  • ||||||||||  bivalirudin / Generic mfg.
    Use of Bivalirudin-Specific Monitoring Assays in Ventricular Assist Device Patients (GWCC - Hall B5, Level 1) -  Nov 5, 2021 - Abstract #ASH2021ASH_4907;    
    The two experimental assays had excellent correlation with each other and good correlation with the c-dTT; however, the fact that the c-dTT results shifted dramatically with a clinical laboratory platform change is illustrative of the need for a bivalirudin-specific monitoring assay as an essential tool for improving outcomes at our center and across centers. More research is needed to understand which type of monitoring assay (dTT or anti-FIIa) may be better suited to particular clinical circumstances.
  • ||||||||||  Chronically Elevated Interleukin-6 Disturbs the Coagulation Cascade in Mice (GWCC - Hall B5, Level 1) -  Nov 5, 2021 - Abstract #ASH2021ASH_3669;    
    These findings show the role of chronically elevated IL-6 in driving the accumulation of A2m on the surface of erythrocytes, thereby mediating a phenotype of increased bleeding complications. This work was supported by the DFG KA4035/1-1 and by the German Ministry for Education and Research (BMBF 01EO1503)
  • ||||||||||  dabigatran etexilate / Generic mfg., ibrutinib / Generic mfg.
    Investigating the Roles of Platelet PAR4 in Hemostasis, Thrombosis and Viral Infection Using a Newly Generated PAR4 Floxed Mouse (GWCC - Hall B5, Level 1) -  Nov 5, 2021 - Abstract #ASH2021ASH_2545;    
    Our results in mice demonstrate that 1) platelet PAR4 is not required for initial hemostatic plug formation but is necessary for maintaining hemostatic plug stability, 2) loss of platelet PAR4 protects from arterial thrombosis, and 3) platelet PAR4 does not alter the course of H1N1 IAV infection, at least at the virus dose used in this study. In summary, we generated a novel mouse line carrying a floxed PAR4 allele which can be used to investigate cell-specific roles of PAR4 in disease.
  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Review, Journal:  Protease-Activated Receptor Antagonist for Reducing Cardiovascular Events - A Review on Vorapaxar. (Pubmed Central) -  Nov 2, 2021   
    Based upon further subgroup analysis of both the TRA 2°P-TIMI 50 trial and TRACER trial, Vorapaxar was found to be potentially beneficial in patients with peripheral artery disease, coronary artery bypass grafting, and ischemic stroke. There are current trials in progress that are further evaluating the use of Vorapaxar in those conditions, and future research and trials are necessary to fully determine the utility of this drug.
  • ||||||||||  Savaysa (edoxaban) / Daiichi Sankyo, Fraxiparine (nadroparin) / Aspen
    Journal:  Performance Characteristics of DOAC Dipstick in Determining Direct Oral Anticoagulants in Urine. (Pubmed Central) -  Oct 28, 2021   
    The factor Xa and thrombin inhibitor pads did not interact with heparin, nadroparin, fondaparinux, or coumadin...In conclusion, we have demonstrated that interobserver variability when interpreting the DOAC Dipstick test strip is low and that factor Xa and thrombin inhibitor pads do not react to other anticoagulants such as heparins and coumadin. R-Hirudin and argatroban can be detected by the thrombin inhibitor pad and abnormal urine colors can be detected by the urine color pad to prevent false interpretation of the results in patient urine samples.
  • ||||||||||  dabigatran etexilate / Generic mfg.
    Clinical, Journal:  A comprehensive appraisal of dabigatran etexilate clinical evidence and applications: a 10-year-long story. (Pubmed Central) -  Oct 27, 2021   
    More recently, the availability of idarucizumab, a specific reversal agent, has increased the safety of dabigatran use in clinical practice, especially for those patients with severe and life-threatening bleeding. This review aims to summarize current evidence on dabigatran, starting from its pharmacological characteristics, and providing an updated overview of pivotal randomized controlled trials and real-world data on its efficacy and safety.